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Efficacy of a piroctone olamine/climbazol shampoo in comparison with a zinc pyrithione shampoo in subjects with moderate to severe dandruff
Abstract
Synopsis
Dandruff is a chronic scalp disorder characterized by scaling and itching. A successful anti‐dandruff shampoo not only has to provide superior anti‐dandruff relief to ensure patient compliance. It also needs to offer excellent cosmetic and hair conditioning benefits at the same time. In this study, the efficacy of a shampoo containing 0.5% piroctone olamine and 0.45% climbazole (shampoo 1) was compared with a widely available commercial shampoo containing 1% zinc pyrithione (shampoo 2). In vitro studies investigating the anti‐mycotic efficacy of a combination of 0.5% piroctone olamine and 0.45% climbazole as well as 1% zinc pyrithione were performed. To study substantivity, pig skin punches were used as a model system and a test of wet combability was performed to characterize combing ease. In vivo home‐in‐use studies were carried out to determine the efficacy of both shampoos to improve scalp condition and reduce itching in subjects suffering from moderate to severe dandruff. Results demonstrated a comparable anti‐fungal effectiveness for 0.5% piroctone olamine plus 0.45% climbazole and 1% zinc pyrithione, respectively. Shampoo 1 showed a significantly higher anti‐mycotics substantivity compared to shampoo 2. After treatment with shampoo 1, the wet combing force was significantly reduced compared with shampoo 2, suggesting a better combability following the use of shampoo 1. In an in vivo split head design study, shampoo 1 was shown to be equally effective in reducing the amount of dandruff on the scalp compared with shampoo 2. The approval rate of volunteers regarding the question ‘The use of this shampoo decreases the itching of my scalp?’ after a 4‐week treatment with shampoo 1 equaled 90%. Overall, the shampoo formulation with 0.5% piroctone olamine and 0.45% climbazole effectively reduces the amount of dandruff and, at the same time, provides hair conditioning advantages.
... The evaluated shampoo was 1 % zinc pyrithione (ZPT) 1.6 % zinc carbonate shampoo (H and S, Procter, and Gamble), and 0.5 % piroctone olamine (PO) shampoo (H and S, Procter, and Gamble). The active components of these shampoo formulations are ZPT (fungistatic) and PO (fungicidal), which are two of the most employed antifungal actives for commercial shampoo formulations [21]. To achieve this goal, G. mellonella larvae were abraded to emulate the loss of the epidermal barrier integrity proposed as an essential factor for dandruff and SD [22]. ...
... In this study, for the first time, G. mellonella has been implemented as a superficial infection model for M. globosa to evaluate the infection and commercial antifungal shampoo effectiveness. Many studies have implemented diverse in vitro protocols to assess the efficacy of different commercial shampoo formulations against M. furfur, M. restricta, and M. globosa [21,28,29]. Zinc pyrithione and piroctone olamine have been tested in distinct combinations. ...
... Zinc pyrithione and piroctone olamine have been tested in distinct combinations. Since testing cosmetics on animals has been prohibited in many regions of the globe, in vivo evaluation of the effectiveness of anti-dandruff shampoos has relied on human studies to assess dandruff symptom relief [21]. However, assessment of the effect of the interaction of shampoos and Malassezia have not been tested in vivo, requiring in vivo models to evaluate the efficacy of products like anti-dandruff shampoos. ...
Introduction. Malassezia globosa is a yeast species that belongs to the mycobiota of humans and animals, associated with dermatological disorders, such as dandruff. This is a chronic scalp skin disorder characterized by flaking and itching. Treatments include commercial shampoo with different formulations that contain antifungal activities like zinc pyrithione (ZPT) or piroctone olamine (PO). The effectiveness of these formulations has been evaluated for decades for dandruff symptom relief of volunteers. To date, non-mammalian, in vivo methods exist to test formulations of these actives.
Aim. To evaluate in vivo in Galleria mellonella larva, two commercial antifungal shampoos (shampoo with 1 % ZPT and 1.6 % zinc Carbonate and shampoo with 0.5 % PO) against this species.
Methodology. G. mellonella larvae were inoculated with M. globosa on abraded cuticular surface. Then, integument cell viability, histological changes, and fungal burden were evaluated.
Results. Larvae inoculated with M. globosa showed higher lesion melanization and tissue damage. In addition, M. globosa population showed to increase over time. Concerning the shampoo’s effectiveness, both formulations significantly reduced M. globosa burden and tissue damage.
Conclusion. G. mellonella larvae were allowed to evaluate M. globosa superficial infection and antifungal effectiveness. Shampoos with ZPT and PO showed a positive effect on inoculated larvae.
... It is used as a cream or shampoo at a 0.5-1% concentration. Piroctone olamine alone or in combination with other agents has been demonstrated to reduce erythema, scaling, burning/stinging sensation, and pruritus in patients with FSD, with excellent cosmetic results [17][18][19][20]. ...
... Skin cleansing-removal of liposoluble, hydrosoluble, and insoluble dirt-is essential in the care of both disease-affected and disease-free skin [18,22]. The numerous cleansing products available have various different mechanisms of action, and include surfactants, makeup removers, astringents, and abrasive cleansers [2,18]. ...
... Skin cleansing-removal of liposoluble, hydrosoluble, and insoluble dirt-is essential in the care of both disease-affected and disease-free skin [18,22]. The numerous cleansing products available have various different mechanisms of action, and include surfactants, makeup removers, astringents, and abrasive cleansers [2,18]. It is important to take into account the quantity of sebum and degree of irritation when choosing the most suitable cleanser. ...
Facial seborrheic dermatitis (FSD) is a chronic and relapsing inflammatory skin disorder occurring in areas of the face rich in sebaceous glands. It clinically manifests as erythematous scaly macules or plaques, often associated with pruritus. Although the pathogenesis of seborrheic dermatitis is not yet fully understood, Malassezia yeast, hormones, sebum levels, and immune response are known to play important roles. Additional factors including drugs, cold temperatures, and stress may exacerbate the condition. Currently, the available treatments do not cure the disease but relieve symptoms. Various pharmacological treatments are available, including antifungal agents, keratolytics, topical low-potency steroids, and calcineurin inhibitors. All of them provide several benefits, but they also have potential side effects. Seborrheic dermatitis tends to have a chronic, recurrent course. To avoid the long-term use of drugs, topical non-pharmacological products such as cosmetics or medical devices may improve clinical outcomes. Products with antimicrobial and anti-inflammatory ingredients such as zinc, piroctone olamine, dihydroavenanthramide, biosaccharide gum-2, and stearyl glycyrrhetinate may speed FSD recovery and avoid flare-ups. Finally, the use of specific cleansers, moisturizers, and sunscreens formulated as light creams or gel/creams should be strongly recommended to all FSD patients. We provide a brief review of the most used non-pharmacological cleansers, topical gel/creams, and specific sunscreens in the management of FSD.
... From the physicochemical point of view, shampoos are usually aqueous solutions of surface active agents and various additives including conditioning agents, medicinal compounds (e.g. anti-dandruff additives), pH regulators, preservatives, fragrances, colorants, substances giving formulations a pearly appearance, etc. [1][2][3][4][5][6][7] The key determinants of the quality of modern hair shampoos are surfactants forming the shampoo base. They are most commonly anionic surface active agents which, however, can cause epidermal dryness and irritation. ...
... The formulations differed in the zwitterionic compound used. [1][2][3][4][5][6][7][14][15][16][17][18][19][20][21][22][23][24][25][26][27][28][29][30][31][32][33] With the exception of the reference formulation (A), all the formulations contained new amphoteric surfactants at a concentration of 2% (Table 1). ...
... Sikora et al. evaluated the effect of adding a supercritical CO 2 extract from strawberry seeds on a range of parameters including the volume and stability of foam. [31] The studies showed that an increase in the concentration of the supercritical CO 2 extract from strawberry seeds induced a drop in the measured parameter from 320 to 300 cm 3 . ...
The purpose of the study was to applicate new synthesized zwitterionic surfactants as hair shampoo components. Hair shampoos formulated for the study contained newly synthesized sulfobetaines at a concentration of 2%. The above additives were evaluated to determine their effect on shampoo dynamic viscosity, texture, yield stress, foaming properties and surface tension of aqueous shampoo solutions. The viscosity of the sulfobetaine-enriched hair shampoos ranged between 6,000 and 21,000 mPa·s, which ensures the required application properties of the formulated products. The yield stress in three prototypical shampoos was equal to approximately 10 Pa, which represents the minimum value that should characterize cosmetics of this type. The sulfobetaines added to the formulations were not found to significantly affect the parameters of hardness and adhesive force. All the formulations under study, except for the shampoo containing N-dodecyl-N-piperidinium-1-propanesulfonate, exhibited good foaming properties. The incorporation of sulfobetaines into hair shampoos contributes to an effective decrease in the surface tension of their aqueous solutions, which may indicate beneficial washing properties. The use of the proposed sulfobetaines in hair shampoos favorably modifies their physicochemical and functional properties. The findings of the study can provide useful insights for the formulation of hair shampoos containing zwitterionic surfactants.
https://www.tandfonline.com/doi/full/10.1080/01932691.2018.1503545
... However, only few studies have evaluated the effectiveness of shampoos against Malassezia yeasts in dogs. The efficacy of shampoos containing from 2% to 4% chlorhexidine was demonstrated in vitro [13][14][15][16][17][18][19][20][21][22][23][24][25][26][27][28][29] as well as in vivo in association with miconazole [5][6][7][8][9][10][11][12][13][14][15][16][17] or alone [11][12][13][14][15][16][17]. Climbazole is a member of the azole chemical group and is incorporated in some veterinary products (shampoos or wipes). ...
... Climbazole is a member of the azole chemical group and is incorporated in some veterinary products (shampoos or wipes). It has been found effective in vitro against Malassezia yeasts [25][26][27]. In dogs, a 3% chlorhexidine and 0.5% climbazole shampoo was effective to reduce Malassezia yeasts in naturally infected dogs [6]. ...
... In dogs, a 3% chlorhexidine and 0.5% climbazole shampoo was effective to reduce Malassezia yeasts in naturally infected dogs [6]. In humans, climbazole is often an ingredient in shampoos used to reduce seborrheic dermatitis associated with Malassezia proliferation [27,28]. ...
Objective of the study:
Shampoo therapy is often recommended for the control of Malassezia overgrowth in dogs. The aim of this study was to evaluate the in vivo activity of a 2% climbazole shampoo against Malassezia pachydermatis yeasts in naturally infected dogs.
Animals:
Eleven research colony Beagles were used.
Materials and methods:
The dogs were distributed randomly into two groups: group A (n=6) and group B (n=5). Group A dogs were washed with a 2% climbazole shampoo, while group B dogs were treated with a physiological shampoo base. The shampoos were applied once weekly for two weeks. The population size of Malassezia yeasts on skin was determined by fungal culture through modified Dixon's medium contact plates pressed on left concave pinna, axillae, groins, perianal area before and after shampoo application. Samples collected were compared by Wilcoxon rank sum test.
Results:
Samples collected after 2% climbazole shampoo application showed a significant and rapid reduction of Malassezia population sizes. One hour after the first climbazole shampoo application, Malassezia reduction was already statistically significant and 15days after the second climbazole shampoo, Malassezia population sizes were still significantly decreased. No significant reduction of Malassezia population sizes was observed in group B dogs.
Conclusion:
The application of a 2% climbazole shampoo significantly reduced Malassezia population sizes on the skin of naturally infected dogs. Application of 2% climbazole shampoo may be useful for the control of Malassezia overgrowth and it may be also proposed as prevention when recurrences are frequent.
... KTZ, CLZ, and PRT are common agents that are active againstTA B L E 1 Studied formulations and their properties.Malassezia sp.; however, the outcomes of their application are mostly based on clinical interpretations since standard antifungal testing is not possible due to the lipophilic nature of Malassezia sp.4,31,33,34,37 ...
... The combination forms had a remarkable inhibitory effect on all three Malassezia sp.Previously, it has been shown that 2% climbazole shampoo lowered the number of Malassezia sp. on the dogs.42 Clinical efficacy was reported with combination formulas, as well.31,34 KTZ is an old antifungal agent of the azole group; it has long been sold in the market worldwide as a commercial medical shampoo. ...
Objectives
Malassezia species are common, clinically relevant, and lipid‐dependent yeasts of humans. They are also the leading causes of the dandruff problem of humans, and the azoles are used primarily in their topical and systemic treatment. Resistance to azoles is an emerging problem among Malassezia sp., which indicates the need of new drug assessments that will be effective against dandruff and limit the use of azoles and other agents in treatment. Among them, the efficacy of various combinations of piroctone olamine and climbazole against Malassezia sp. is highly important. Here, we assessed the efficacies of various piroctone olamine and climbazole formulations against Malassezia sp. in comparison with ketoconazole.
Methods
A total of nine formulations were included in the study, where each formulation was prepared from different concentrations of piroctone olamine and climbazole and both. All formulations contained the same ingredients as water, surfactants, hair conditioning agents, and preservatives. Malassezia furfur CBS1878, Malassezia globosa CBS7874, and Malassezia sympodialis CBS9570 were tested for antifungal susceptibility of each formulation by agar diffusion method. Sizes of the inhibition zones were compared with standard medical shampoo containing 2% ketoconazole, and the data were analyzed by Dunnett's multiple‐comparison test.
Results
For all Malassezia sp. strains, climbazole 0.5% and piroctone olamine/climbazole (0.1%/0.1% and 0.1%/0.5%) combinations were found to have the same effect as the medical shampoo containing 2% ketoconazole. Piroctone olamine/climbazole 1.0%/0.1% formulation showed the same efficacy as 2% ketoconazole on M. furfur and M. sympodialis, while 0.1%/0.5% formulation to only M. furfur. For M. globosa, none of the formulations tested were as effective as ketoconazole.
Conclusion
The species distribution of Malassezia sp. varies depending on the anatomical location on the host. According to the results of this study, climbazole and piroctone olamine combinations seem to be promising options against the dandruff problem with their high antifungal/anti dandruff efficacy.
... Dandruff is a generally known scalp disorder, also defined as the mildest version of seborrheic dermatitis. 1 It is characterized by the formation of small flakes and sebum that occur in localized areas on the scalp, such as the forehead and the back of the ears beyond the hairline. 2 Other symptoms derived from dandruff may be the feeling of a tight or dry scalp, producing irritation and itching. 3 Therefore, it is stated as an abnormal condition that affects more than 50% of adults. ...
... Among those agents, molecules such as azoles or hydroxypyridones and agents such as piroctone olamine, salicylic acid, selenium sulfide, ketoconazole, and zinc pyrithione can be found. 2,6,7 Among these compounds, there is no big difference in efficacy. 8,9 However, Zn pyrithione is preferred in terms of the overall performance, improving the appearance and feel of the hair. ...
The cosmetic industry provides a wide variety of shampoos to treat dandruff, containing insoluble ingredients such as Zn pyrithione. However, the solubility of this active ingredient is quite limited in both water and oil media; thus, antidandruff formulations must include a large amount of chemically synthesized stabilizing ingredients to avoid their precipitation. In this work, the stabilization of Zn pyrithione in O/W emulsions using a biosurfactant (BS) extract and Tween 80 is studied. The study includes an incomplete factorial design based on the tea tree oil/water ratio and both surfactant and biosurfactant concentrations. The formulations are characterized in terms of particle size, stability after 30 days, and solubility of Zn pyrithione. The formulation that provided the most favorable results contains Tween 80 (5%) and BS extract (2.5%), with an O/W ratio of 0.01. This provides the smallest particle size (40.5 μm), good stability after 30 days (91.0%), and the highest solubility of Zn pyrithione (59%). The results obtained enable the use of the combination of BS extract and Tween 80 as bio/surfactants of antidandruff shampoo formulations, along with another antiseptic agent such as tea tree oil. Furthermore, this is the first work where a biosurfactant is considered to be a stabilizing agent in antidandruff formulations.
... On the other hand, piroctone olamine appears to be the most interesting molecule as it has been proven superior in terms of effectiveness and user safety [89][90][91]. Ichthyol, cade oil, and various plant extracts were also found in the shampoos studied that were sold in pharmacies. ...
... Ichthyol, cade oil, and various plant extracts were also found in the shampoos studied that were sold in pharmacies. In the past, tars were used to treat squamous conditions, but coal tars were banned by Directive 2004/93/EC as their use in shampoos was found to be carcinogenic [90][91][92][93][94][95][96][97]. However, tars obtained from bituminous rock such as ichthyol and vegetable tars such as cade oil (that we rarely found in shampoos; see table 8) can still be used. ...
Shampoo is a hair care product designed to clean the skin and hair of the scalp. Among the ingredients that go into the making of a shampoo are detergents, conditioners, thickeners, sequestering agents, pH adjusters, preservatives, and active ingredients such as anti-dandruff agents. The purpose of this study was to identify the composition of 140 shampoos available in pharmacies, in stores of a mass-market chain, or from mail-order retailers. Forty-one shampoos were advertised as "gentle", 12 as specially formulated for infants, 35 as anti-dandruff, and 52 without any particular claim. We analysed the cleansing base, preservatives, and anti-dandruff agents when relevant and identified the allergens regardless of whether or not they are listed under Regulation (EC) No. 1223/2009 as one of the 26 regulated substances. We discovered that unlike shampoos sold in stores of a mass-market chain and those available from mail-order retailers, those sold in pharmacies expose users to some of the 26 substances listed under Regulation (EC) No. 1223/2009. We also determined that baby shampoos sold in pharmacies are allergen-free. Regarding anti-dandruff formulations, the largest variety of active ingredients was found in shampoos sold in pharmacies. Overall, the most common active ingredients were olamines, zinc pyrithione, azoles, selenium disulphide, and plant extracts. Shampoos sold in pharmacies appear to contain fewer allergens listed under Regulation (EC) No. 1223/2009 compared to those sold elsewhere.
... The overall efficacy of antifungal shampoos in clinical trials has been compared in patients suffering from dandruff and seborrhoeic dermatitis [12][13][14][15][16][17]. Comprehensive scalp microbiome comparisons have also been performed between cohorts of healthy individuals and dandruff/seborrhoeic dermatitis patients [18]. ...
... Numerous clinical trials have been conducted to access the efficacy of antifungal treatments on different cohorts of patients with dandruff and seborrhoeic dermatitis [12][13][14][15][16][17][18]. Ketoconazole is welldocumented to be an efficacious anti-dandruff treatment [14,16]. ...
Objective
Dandruff is a complex skin condition characterized by unpleasant itching and flaking of the scalp. It is primarily attributed to the over colonization of Malassezia yeasts such as M. globosa and M. restricta. Some studies also suggest the involvement of Staphylococci bacteria in dandruff disease pathogenesis. We aimed to access the effectiveness of anti‐dandruff treatments by determining the efficacy of the active antifungal agents alone or in commercial shampoo formulations against Malassezia and Staphylococcus.
Methods
The minimum inhibitory concentrations of three anti‐dandruff shampoo antifungals (zinc pyrithione, ketoconazole and ciclopirox) and the witch hazel extract, hamamelitannin were tested against commensal Malassezia and Staphylococcus species using broth microdilution methods. In experiments simulating shampoo exposure and washing conditions on the scalp, we also tested the ability of the above agents in shampoo formulation (Head and Shoulders®, Ketomed®, Sebiprox®, Erol Healthcare Hair Shampoo®, respectively) along with a generic over‐the‐shelf shampoo to inhibit microbial growth.
Results
Ketomed® and Head and Shoulders® shampoo were the most effective treatments against Malassezia in in vitro assays and washing simulation. experiments. Erol Healthcare Hair Shampoo® was less effective against Malassezia as it required a longer contact time to achieve growth inhibition for some species. Sebiprox® showed variable efficacy in washing and contact time experiments while the generic over‐the‐shelf shampoo was the least effective in inhibiting Malassezia and Staphylococcus growth.
Conclusion
From these findings, it is reasonable that patients with dandruff may benefit from applying specific antifungal shampoo although results may vary with microbial species, time of contact and shampoo formulation components.
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... This article summarizes current interventions and treatments, with a particular focus on medium-chain fatty acid esters as a novel option for dandruff control. It is worth noting that many commercially available anti-dandruff products combine multiple active ingredients to address the multifaceted nature of the condition, often targeting both fungal activity and scalp inflammation [4][5][6][7][8][9][10][11]. ...
Recent data suggest that dandruff might be associated with dysbiosis of the scalp microbiome. This mini review summarizes the microbiome changes seen with the dandruff condition, as well as different solutions for dandruff control and their effects on the scalp microbiome in relation to in vivo efficacy. Since zinc pyrithione has been banned from cosmetics in the EU, the medium-chain fatty acid ester propanediol caprylate is a new option, in addition to the remaining conventional ingredients: piroctone olamine, climbazole, and salicylic acid. The ester is rapidly cleaved by Malassezia hydrolases in the external milieu, thereby releasing active caprylic acid. In addition to its auto-regulatory effects on Malassezia, propanediol caprylate is also able to influence the bacterial microbiota towards a healthier scalp microbiome. In vivo data have shown an efficacy comparable to climbazole and piroctone olamine. In vivo additive and synergistic effects in different combinations allow reductions in the concentration of conventional agents. Surprisingly, a new effect of a lasting healthier scalp has been identified in connection with ester use, in contrast to the usual return of dandruff experienced upon the discontinuation of anti-dandruff shampoo with conventional actives. We also report on new data from an unpublished comparative study on two propanediol monoesters confirming the long-lasting effect.
... Доказали эффективность лекарственные средства, в состав которых входят такие компоненты, как климбазол, пироктон оламин [14], цинка пиритион [15], полидоканол; кроме того, шампунь с 2 %-ным содержанием полидоканола обладает выраженным противозудным эффектом [16]. Стоит отметить, что данные препараты обладают выраженной антимикотической и противовоспалительной активностью, а также самым высоким профилем безопасности, но зачастую монотерапия не всегда эффективна, поэтому современные производители фармацевтической продукции для борьбы с СД предлагают готовые шампуни, имеющие в составе комбинации активных компонентов, что позволяет улучшить качество проводимой терапии [17]. ...
The article is of the overview nature and contains up-to-date information about the current methods of treatment of various forms of seborrheic dermatitis (SD). The data on modern methods of management of patients with severe forms of SD, allowing for a long time to achieve regression of skin rashes and significantly improve the quality of life of the patient, are presented.
... a) Климбазол представляет собой имидазольное гетероциклическое органическое соединение, обладающее противогрибковой активностью. Механизм действия основан на влиянии на липидный состав мембраны белка и замедлении процессов синтеза эргостерола по аналогии с производными имидазола препаратами [8]. b) Пироктоноламин -этаноламиновая соль гидроксамовой кислоты, производная пироктона, которая служит гидроксипиридоновым антимикотическим агентом. ...
Seborrheic dermatitis (SD) is a chronic recurrent inflammatory skin disease caused by changes of quantitative and qualitative sebum characteristics. SD comes out by appearing of erythematous plaques with sense of itch and peeling skin in areas with high concentration of sebaceous glands: on the scalp, face, upper part of the body and in the folds of skin. Due to the fact that the development of the SD is promoted by the colonization of the skin with a lipophilic yeast fungus Malassezia spp., in the treatment of uncomplicated simple forms of the disease can be applied external antifungal medicines, topical glucocorticosteroids and anti-inflammatory drugs of non-steroidal origin. Systemic therapy is also used in severe course of seborrheic dermatitis and in the treatment of forms, resistant to external therapy. In the treatment of persistent and long-term forms of SD, systemic antifungal agents and systemic retinoids are used, which allow for a long time to achieve regression of skin rashes and significantly improve the quality of life of the patient.
... The aetiology of dandruff is multifactorial, but includes sebaceous lipids, Malassezia yeast and individual susceptibility [4]. Currently, the most common treatment for dandruff is regular use of antidandruff (AD) shampoos that contain fungistatic agents, such as zinc pyrithione (ZnPT) and climbazole, or a potentiated ZnPT, which have shown significant efficacy on the resolution of dandruff [5][6][7][8]. The efficacy of AD shampoos is always assessed by measuring scalp flaking, the most important dandruff symptom, within a doubleblind, randomized controlled clinical trial. ...
Objective
Dandruff is a common scalp condition that can be improved by regular use of shampoos containing anti-fungal actives. The efficacy of anti-dandruff shampoos can be assessed by measuring scalp flaking, one of the important dandruff symptoms. A randomized, double-blind trial is often used with one of two clinical designs: whole-head parallel design and split-head paired design. We aimed to explore the difference in product differentiation between these two designs using the same two test shampoos and the same scalp flaking assessment method (Total Weighted Head Score Adhered Flakes – TWHS AF).
Methods
A clinical study was conducted with a 2-3 weeks wash-out phase and a 4-week test phase, consisting of 2 cells: 120 subjects with whole-head parallel design, divided into 2 subgroups (1:1) using on-site controlled washing method (either wash their own hair at a study site, under the instruction of a study supervisor or wash their own hair at home, as per instructions, but without supervision) and 35 subjects with split-head paired design using salon-staff washing method. Both cells employed hair washing at frequency of three times a week, and TWHS AF measurement once a week from the baseline assessment.
Results
Both designs gave similar differences in TWHS AF between products: 5.6 units (95% CI: 4.1 to 7.0 units) in whole-head design and 5.9 units (95% CI: 4.9 to 6.9 units) in split-head Design.
Conclusion
Split-head paired design shows a similar ability of detecting product difference as whole-head parallel design, whereas it is a choice of more efficient and more cost-effective, as only a quarter of the subjects are required to demonstrate the efficacy between anti-dandruff shampoos.
... Major side effect of Climbazole may cause localized irritation of the skin with symptoms including redness, rashes and itching [9] . ...
... These and other microbial species were found to be associated with dandruff and other human skin conditions [20,21]. A causative link was made due to the observed reduction in Malassezia numbers, and subsequent reduction in scalp skin flaking, following the application of a shampoo containing antifungal compounds such as zinc pyrithione, ketoconazole, piroctone olamine and climbazole [22][23][24]. In addition, the cessation of treatment in some individuals results in an increased level of skin flaking [25]. ...
Dandruff is a skin condition that affects the scalp of up to half the world’s population, it is characterised by an itchy, flaky scalp and is associated with colonisation of the skin by Malassezia spp. Management of this condition is typically via antifungal therapies, however the precise role of microbes in the aggravation of the condition are incompletely characterised. Here, a combination of 454 sequencing and qPCR techniques were used to compare the scalp microbiota of dandruff and non-dandruff affected Chinese subjects. Based on 454 sequencing of the scalp microbiome, the two most abundant bacterial genera found on the scalp surface were Cutibacterium (formerly Propionibacterium) and Staphylococcus, while Malassezia was the main fungal inhabitant. Quantitative PCR (qPCR) analysis of four scalp taxa (M. restricta, M. globosa, C. acnes and Staphylococcus spp.) believed to represent the bulk of the overall population was additionally carried out. Metataxonomic and qPCR analyses were performed on healthy and lesional buffer scrub samples to facilitate assessment of whether the scalp condition is associated with differential microbial communities on the sampled skin. Dandruff was associated with greater frequencies of M. restricta and Staphylococcus spp. compared with the healthy population (p<0.05). Analysis also revealed the presence of an unclassified fungal taxon that could represent a novel Malassezia species.
... To date, it is available a novel nonsteroidal cream (NSC) containing different ingredients, which have been reported to exert effects in SD treatment [14]. In particular, this cosmeceutical is composed of: (1) piroctone olamine, that has an anti-fungal property [15][16][17]; (2) zinc salt of L-pyrrolidone carboxylate (PCA), that has anti-fungal and anti-inflammatory properties [18][19][20]; ...
Introduction
The pathogenesis of seborrheic dermatitis (SD) is multifactorial and traditional treatments may not target all aspects of it. The aim of this study was to evaluate short-term anti-fungal, anti-microbial, anti-inflammatory and anti-pruritus properties of a novel non-steroidal cream (NSC) containing piroctone olamine, zinc salt of l-pyrrolidone carboxylate (PCA), hydroxyphenyl propamidobenzoic acid, biosaccharide gum-2 and stearyl glycyrrhetinate in patients with face and chest SD.
Methods
Twelve male subjects affected by SD, presenting face and chest manifestations, were enrolled. Patients were instructed to apply NSC twice a day, performing regular visits at baseline (W0), after 7 (W1) and 14 (W2) days of treatment. A limitation of the study was that no control group treated with the vehicle without active ingredients was enrolled. To evaluate the efficacy of the NSC, investigator’s assessments were represented by scoring index (SI) and investigator’s global assessment score (IGA). In order to assess NSC anti-fungal and anti-microbial effects, skin scale scrapings were collected and used for Malassezia furfur (MF) and Staphylococcus epidermidis (SE) cultures. In parallel, in order to assess NSC anti-inflammatory effects, gene expression of IL-1α, IL-1β, IL-6, IL-8, and TNF-α was assessed. In addition, anti-pruritus effects were also evaluated through gene expression of cathepsin S and l-histidine decarboxylase.
Results
SI mean scores significantly decreased at W1 and, to a greater extent, at W2 compared with W0. The IGA score registered an important improvement efficacy both for face and chest, from W1 to W2. MF and SE growth was already inhibited at W1, with a more pronounced decrease at W2. Gene expression of all analyzed mediators was significantly reduced at W1 compared to W0.
Conclusion
In conclusion, our assessment is that NSC is an effective and well tolerated treatment option for SD with anti-fungal, anti-microbial and anti-inflammatory properties.
Trial Registration
ISRCTN registry, ISRCTN77871064 (retrospectively registered October 17, 2019). EudraCT number, 2019-003813-32.
Funding
ISDIN.
... Studi tersebut menyimpulkan bahwa sampo yang mengandung kombinasi piroctone olamine/climbazole efektif dan menyebabkan penurunan jumlah ketombe yang bermakna dari baseline hingga minggu ke-4 (p<0,01). 14 Pada studi ini, 78,6% pasien kelompok uji dan 28,6% pasien kelompok plasebo pada subjek ketombe mengalami kesembuhan (perbaikan ≥70%). Hal ini serupa dengan studi oleh Rastegar dkk. ...
Dermatitis seboroik (DS) merupakan kelainan inflamasi kulit di area seboroik berupa lesi eritematosa dan skuama, bersifat kronik-residif, sedangkan ketombe adalah DS derajat ringan berupa skuama pada skalp. Etiopatogenesis DS bersifat multifaktor, salah satunya berupa kolonisasi Malassezia. Studi pendahuluan ini menguji efikasi dan keamanan sampo dengan formulasi khusus yang mengandung climbazole 1% dan piroctone olamine 0,75%. Sebanyak 28 pasien ketombe dan 18 pasien DS ringan di skalp dibagi menjadi dua kelompok secara paralel, acak, dan tersamar ganda, yaitu kelompok uji dan kontrol. Kedua kelompok dilakukan pemeriksaan setiap 1 minggu selama 4 minggu. Efikasi dinilai menggunakan skor modifikasi Seborrheic Dermatitis Area and Severity Index (SDASI) dan penilaian pruritus menggunakan visual analogue scale (VAS). Analisis efikasi dilakukan secara intention-to-treat dan per-protokol. Pada kelompok pasien ketombe, didapatkan penurunan skor modifikasi SDASI, luas lesi, derajat skuama yang berbeda bermakna antara kelompok uji dan plasebo (p<0,05). Pada kelompok pasien DS ringan pada skalp, tidak didapatkan perbedaan yang bermakna pada penurunan skor modifikasi SDASI, luas lesi, derajat skuama, lesi eritematosa, dan skor lesi papul antara kelompok uji dan plasebo (p>0,05). Sampo uji terbukti efektif mengobati ketombe, namun pada DS ringan di skalp sampo hanya efektif mengurangi jumlah skuama tetapi tidak mengurangi lesi inflamasi.Kata kunci: climbazole, dermatitis seboroik, ketombe, piroctone olamine, sampo
... This interest has been determined primarily because inorganic compounds are efficiently delivered in the body, in part because they are small molecules/ions, or they exploit oxidation and ligand substitution reactions [1,2]. Some of the well-known inorganic drugs incorporate metal ions, which are used in a variety of human disease treatments, such as silver sulphadiazine (antibacterial); auranofin (antiarthritic); sodium bromide (sedative); mercurochrome (antiseptic); lithium carbonate (anti-depressive); bismuth derivatives (anti-acid); cisplatin and carboplatin (anticancer); and zinc pyrithione and selenium sulfide (anti-dandruff agents) [3][4][5][6]. They are used in modern medicine to control cancer, infections, diabetes, neurological and cardiovascular problems, ulcers, and anti-inflammatory processes [3]. ...
Carbonic anhydrases (CAs, EC 4.2.1.1) are ubiquitous metalloenzymes, which catalyze the crucial physiological CO2 hydration/dehydration reaction (CO2 + H2O ⇌ HCO3− + H+) balancing the equilibrium between CO2, H2CO3, HCO3− and CO32−. It has been demonstrated that their selective inhibition alters the equilibrium of the metabolites above affecting the biosynthesis and energy metabolism of the organism. In this context, our interest has been focalized on the fungus Malassezia restricta, which may trigger dandruff and seborrheic dermatitis altering the complex bacterial and fungal equilibrium of the human scalp. We investigated a rather large number of inorganic metal-complexing anions (a well-known class of CA inhibitors) for their interaction with the β-CA (MreCA) encoded by the M. restricta genome. The results were compared with those obtained for the two human ?-CA isoforms (hCAI and hCAII) and the β-CA from Malassezia globosa. The most effective MreCA inhibitors were diethyldithiocarbamate, sulfamide, phenyl arsenic acid, stannate, tellurate, tetraborate, selenocyanate, trithiocarbonate, and bicarbonate. The different KI values obtained for the four proteins investigated might be attributed to the architectural features of their catalytic site. The anion inhibition profile is essential for better understanding the inhibition/catalytic mechanisms of these enzymes and for designing novel types of inhibitors, which may have clinical applications for the management of dandruff and seborrheic dermatitis.
... Accordingly, shampoos have evolved into high-tech products consisting of ten to thirty ingredients that are combined in precise formulations to meet consumer demands. [78] Ultimately, shampoo treatments are the most commonly used means of managing hair and scalp conditions and have proven to be effective for the treatment of dandruff and seborrheic dermatitis, [79][80][81][82][83] psoriasis, [84] and atopic dermatitis of the head-and-neck type. [85,86] Today, it is understood that scalp care products for dandruff and seborrheic dermatitis, psoriasis, and atopic dermatitis exert their benefits by controlling scalp Malassezia levels. ...
Conventionally, the medical focus has been either on hair loss or the condition of the scalp in terms of specific dermatological diseases. Indeed, the proximate structural arrangement of the scalp and hair leads to an interdependent relationship between the two. While protective benefits of the hair to the scalp are obvious, the role of the scalp as an incubatory environment for the preemergent hair fiber has largely been ignored. In fact, there is a wealth of observational data on specific dermatological conditions of the scalp providing evidence for the role of the scalp condition in supporting the production of healthy hair. Oxidative stress, the inability of the body to sufficiently counteract the sources of oxidation, is prevalent in many skin conditions, including normal skin aging. On the scalp, the hair appears to be impacted prior to emergence, and oxidative stress appears to play a role in premature hair loss. The scalp commensal organism, Malassezia, has been recognized to be a source of oxidative damage. Therefore, hair care products, specifically shampoos, with active Malassezia inhibitory agents, such as zinc pyrithione, tend to reduce premature hair loss, besides the known benefits in treating specific dermatologic scalp pathologies, and therefore should represent an integral part of every treatment regimen for hair loss, even in individuals not showing symptoms of scalp pathologies. © 2019 International Journal of Trichology | Published by Wolters Kluwer - Medknow.
... For example, a double-blind, placebo-controlled study with 30 patients treated with 1% zinc pyrithione shampoo resulted in reduced extension and severity of symptoms and significant reduction of scalp sebum production, whereas only mild and tolerable side effects were observed in a small group of patients [221]. In another randomized, double-blind split head design clinical study with 98 subjects, both 1% zinc pyrithione shampoo and shampoo containing 0.5% piroctone olamine, 0.45% climbazole and 2% polydocanol were equally effective showing significant dandruff reduction when compared to baseline and vehicle control [222]. In a multicenter, single-blind, controlled clinical study with 189 patients, the efficacy of a shampoo containing the 1.5% ciclopirox olamine and 1% zinc pyrithione was compared to a vehicle shampoo and to 2% ketoconazole foaming gel in the treatment of seborrheic dermatitis. ...
A number of papers reporting antimicrobial properties of extracts, essential oils, resins and various classes of compounds isolated from higher plants has been published in recent years; however, a comprehensive analysis of plant-derived antimicrobial agents currently applied in practice for improvement of human health is still lacking. This review summarizes data on clinical efficacy, antimicrobial effects and the chemistry of commercially available antibacterial and antifungal agents of plant origin currently used in the prevention and treatment of gastrointestinal, oral, respiratory, skin, and urinary infections. As a result of an analysis of the literature, more than 40 plant-derived over-the-counter pharmaceuticals, dietary supplements, cosmetics, herbal medicines, and functional foods containing complex mixtures (e.g. Glycyrrhiza glabra extract, Melaleuca alternifolia essential oil, and Pistacia lentiscus resin), pure compounds (e.g. benzoic acid, berberine, eucalyptol, salicylic acid and thymol) as well as their derivatives and complexes (e.g. bismuth subsalicylate and zinc pyrithione) have been identified. The effectiveness of many of these products is illustrated by results of clinical trials and supported by data on their in vitro antimicrobial activity. A broad spectrum of various commercial products currently available on the market and their well-documented clinical efficacy suggests that plants are prospective sources for the identification of new types of antimicrobial agents in future. Innovative approaches and methodologies for effective proof-of-concept research and the development of new types of plant-derived products effective against recently emerging problems related to human microbial diseases (e.g. antimicrobial resistance) are also proposed in this review.
... Lower MICs have been reported by Youn et al. (2016), in the order of 1-2 µg ml -1 , showing a higher antifungal efficacy of CBZ compared with piroctone olamine, another antifungal agent used for the treatment of dandruff. Various authors have reported the in vitro activity and associated clinical outcomes of CBZ in the literature (Chen et al., 2015;Schmidt-Rose et al., 2011;Youn et al., 2016). Garrett et al. (2017) also investigated the deposition of CBZ and zinc pyrithione in porcine skin with stimulated Raman scattering microscopy. ...
Dandruff is a common condition, affecting up to half the global population of immunocompetent adults at some time during their lives and it has been highly correlated with the over-expression of the fungus Malassezia spp. Climbazole (CBZ) is used as an antifungal and preservative agent in many marketed formulations for the treatment of dandruff. While the efficacy of CBZ in vitro and in vivo has previously been reported, limited information has been published about the uptake and deposition of CBZ in the skin. Hence, our aim was to investigate the skin permeation of CBZ as well as the influence of various solvents on CBZ skin delivery. Four solvents were selected for the permeability studies of CBZ, namely propylene glycol (PG), octyl salicylate (OSal), Transcutol® P (TC) and polyethylene glycol 200 (PEG). The criteria for selection were based on their wide use as excipients in commercial formulations, their potential to act as skin penetration enhancers and their favourable safety profiles. 1% (w/v) solutions of CBZ were applied under infinite and finite dose conditions using Franz type diffusion cells to human and porcine skin. In line with the topical use of CBZ as an antidandruff agent, comparatively low amounts of CBZ penetrated across the skin barrier (< 1% of the applied dose of CBZ). Finite dose studies resulted in a higher extraction of CBZ from human skin compared with infinite dose studies (p<0.05). CBZ was also taken up to a higher extent in porcine skin (> 7-fold) compared with human skin (p<0.05). Nevertheless, no statistical differences were observed in the amounts that permeated across the different membranes. These preliminary results confirm the potential of simple formulations of CBZ to target the outer layers of the epidermis. The PG and OSal formulations appear to be promising vehicles for CBZ in terms of overall skin extraction and penetration. Future work will expand the range of vehicles studied and explore the reasons underlying the retention of CBZ in the outer layers of the skin.
... Wash off products such as anti-dandruff shampoos containing ZnPT i.e. the market leading product manufactured by Proctor and Gamble, Head & Shoulders shampoo, are designed to act topically. These consumer products remove the superficial scales from the scalp in conjunction with inhibiting the growth of Malassezia species that causes dandruff (Schmidt-Rose et al., 2011). Leave-on products such as creams, however, are available on the market to treat psoriasis, eczema and seborrheic dermatitis due to ZnPT also possessing non-selective kerolytic properties i.e. thins the skin. ...
Zinc pyrithione is an active component incorporated in an extensive range of topically applied commercial products that are used worldwide. Despite its prevalence, no published study has investigated the penetration of zinc from the zinc pyrithione complex into human skin. Zinc is crucial for healthy skin function however an elevated concentration of labile zinc is toxic outside a narrow concentration range. Synchrotron X-ray fluorescence microscopy in conjunction with X-ray absorption near edge structure spectroscopy was used to map the deposition of zinc, quantitate the amount of zinc within the skin and to identify a change in the chemical form of zinc after application. This study has demonstrated a ~3.8 fold increase in zinc concentration within the viable epidermis (VE) after 24 h topical application of zinc pyrithione that increased significantly by ~250 fold after 48 h when compared to control skin. Confocal microscopy using a labile zinc specific dye, ZinPyr-1, showed that zinc pyrithione disrupted the skin cells zinc homeostasis and significantly increased the intracellular zinc concentration leading to cell toxicity. Overall, this study demonstrates that topical application of zinc pyrithione formulations leads to an increase in zinc penetration in human skin, consequently, raising concerns for potential localised toxicity to occur.
... 2) Schmidt-Rose T et al., reported in their study that a combination of Piroctone Olamine (0.5%) and Climbazole (0.45%) proved to be equally effective on comparison with Zinc Pyrithione (1%) alone 28 . ...
This review gives an insight of the scalp condition- dandruff which affects more than 50% of the human population. Malassezia furfur is reported as the main cause of dandruff. This article aims at investigating other causes of dandruff which include microbial and non - microbial factors. These factors have been explained in this article. It also highlights the various treatment options and newer formulations. Various active agents like anti- fungal agents, keratolytic agents and anti - proliferative agents that are used against dandruff, along with their mechanisms of action are covered in this article. Conventional formulations like Shampoos, creams and lotions have their own set of advantages and limitations. To overcome the disadvantages and prolong the release of actives, novel formulations like Liposomes, Niosomes, Solid lipid nanoparticles, Nanolipid carriers and Silver nanoparticles are being developed. Novel delivery systems have been successfully used for pharmaceutical formulations and they can prove to be a promising delivery system for scalp treatment too.
... Shampoos with different active ingredients (e.g. zinc pyrithione, ketoconazole, selenium sulphide, tar, salicylic acid) have been used with success [20,21]. In this regard, zinc pyrithione-based shampoos are effective, affordable, and have excellent cosmetic and hair conditioning effects; all of which will encourage long-term compliance. ...
... Fungal skin conditions such as dandruff are caused by numerous host factors in conjunction with the skin flora yeast Malassezia. 1 Clinical studies have shown that topical administration of antifungal agents leads to an improvement in the condition, 2 and most commercially available antidandruff shampoo formulations include antifungal agents as the main active ingredients. ...
Treatment of dandruff condition usually involves use of antidandruff shampoos containing antifungal agents. Different antifungal agents show variable clinical efficacy based on their cutaneous distribution and bioavailability. Using stimulated Raman scattering (SRS), we mapped the distribution of unlabeled low-molecular weight antifungal compounds zinc pyrithione (ZnPT) and climbazole (CBZ) on the surface of intact porcine skin with cellular precision. SRS has sufficient chemical selectivity and sensitivity to detect the agents on the skin surface based on their unique chemical motifs that do not occur naturally in biological tissues. Moreover, SRS is able to correlate the distribution of the agents with the morphological features of the skin using the CH2 stretch mode, which is abundant in skin lipids. This is a significant strength of the technique since it allows the microscopic accumulation of the agents to be correlated with physiological features and their chemical environment without the use of counter stains. Our findings show that due to its lower solubility, ZnPT coats the surface of the skin with a sparse layer of crystals in the size range of 1 to 4 μm. This is consistent with the current understanding of the mode of action of ZnPT. In contrast, CBZ being more soluble and hydrophobic resulted in diffuse homogeneous distribution. It predominantly resided in microscopic lipid-rich crevasses and penetrated up to 60 μm into the infundibular spaces surrounding the hair shaft. The ability of the SRS to selectively map the distribution of agents on the skin's surface has the potential to provide insight into the mechanisms underpinning the topical application of antifungal or skin-active agents that could lead to the rational engineering of enhanced formulations. © 2017 Society of Photo-Optical Instrumentation Engineers (SPIE).
... Poor consumer/patient adherence to treatment is recognized in several skin conditions. For example, the lack of persistence and compliance with antidandruff products is recognized as a confounding factor that may limit the benefits of treatment [8,[43][44][45]51]. Market research in this area has revealed that only 25 % of people who use antidandruff shampoos use them for every wash, with the majority of female users tending to switch regularly between antidandruff shampoos and non-antidandruff ''beauty'' shampoos (Unilever, data on file). ...
The use of a post-treatment period of observation or "regression phase" is common in pharmaceutical and cosmetic clinical dermatology studies. Regression phases can be incorporated into a variety of study designs, ranging from simple post-treatment observation for a defined period, as has been used for moisturizers, antidandruff formulations, and treatments for acne, to more complex randomized intermittent-treatment designs, as used in studies of psoriasis pharmacotherapies. Extensive information can be derived from a regression phase. Notably, it can provide useful data on the persistence of effect and time to relapse after treatment cessation, which are particularly relevant to skin conditions in which consumer or patient adherence to treatment is suboptimal. By incorporating a regression phase, a clinical study can more closely reflect "real-world" behavior, e.g., the switching by consumers from antidandruff to beauty shampoos. The regression phase can also help to differentiate between products that show similar effectiveness during the treatment phase, and monitoring post-treatment physiological end points can provide valuable evidence on the safety and mechanism of action of the therapy.
... Variances in the total composition and the 10-fold difference of concentration of the active ingredients of the formulations we tested are items that help to explain this result. In contrast to this study, a study carried out by Schmidt-Rose et al. (2011) compared the in vitro efficacy of a shampoo containing 0.5% piroctone olamine and 0.45% climbazole with a shampoo containing 1% zinc pyrithione against M. furfur CBS 1878. The inhibition zone assay experiments performed indicated that both shampoos exhibited comparable antifungal activity in contrast to the free vehicle. ...
This study aimed to investigate the in vitro antifungal effectiveness of five different formulations against dandruff and ringworm dermatophytes. Candida albicans was also included in our assays. Fungal susceptibility tests were performed with planktonic cells and biofilms of reference strains. Microbiological and physicochemical quality parameters were assessed for all formulations. Our data indicated that the formulations were effective against the dermatophytes strains, and to our knowledge, the effectiveness of cosmetic formulations against fungal biofilms is shown for the first time. The formulations were considered effective against the explored dermatophytes and were considered safe given the adequate microbiological and physicochemical characteristics shown in the proposed assays.
... A shampoo comprising of 0.5% piroctone olamine and 0.45% climbazole showed an anti-fungal effectiveness comparable to shampoos containing particulate zinc pyrithione. After 4 weeks treatment, a sustained reduction of flaking and scalp itching was documented for this shampoo, as well as hair conditioning advantages [20]. Based on these results, we chose a shampoo containing piroctone olamine and climbazole for our in vivo study and also incorporated piroctone olamine into the tonic. ...
... Dandruff can be treated with many ingredients, most commonly with antifungals such as zinc pyrithione [13], selenium sulphide [14], and imidazoles such as climbazole or hydroxypyridones, for example piroctone olamine [15,16]. Although antifungal activity is a key driver of the efficacy of these ingredients in the treatment of dandruff, it has been recognized that many anti-dandruff agents have other effects which may be contributing to the clinical benefit [17]. ...
Objective:
Dandruff is a troubling consumer problem characterized by flaking and pruritus of the scalp and is considered a multifactorial condition with sebum, individual susceptibility and the fungus Malassezia all thought to play a part. The condition is commonly treated with shampoo products containing antifungal ingredients such as zinc pyrithione and climbazole. It is hypothesized that these ingredients may be delivering additional scalp skin benefits besides their antifungal activity helping to relieve dandruff effectively. The objective of this study was to evaluate the anti-dandruff ingredient climbazole for potential skin benefits using genomics and in vitro assays.
Methods:
Microarray analysis was performed to profile gene expression changes in climbazole-treated primary human keratinocyte cells. Results were independently validated using qPCR and analysis of protein expression using ELISA and immunocytochemistry.
Results:
Microarray analysis of climbazole-treated keratinocytes showed statistically significant expression changes in genes associated with the gene ontology groups encompassing epidermal differentiation, keratinization, cholesterol biosynthesis and immune response. Upregulated genes included a number encoding cornified envelope proteins such as group 3 late-cornified envelope proteins, LCE3 and group 2 small-proline-rich proteins, SPRR2. Protein analysis studies of climbazole-treated primary keratinocytes using ELISA and immunocytochemistry were able to demonstrate that the increase in gene transcripts translated into increased protein expression of these cornified envelope markers.
Conclusion:
Climbazole treatment of primary keratinocytes results in an upregulation in expression of a number of genes including those encoding proteins involved in cornified envelope formation with further studies demonstrating this did translate into increased protein expression. A climbazole-driven increase in cornified envelope proteins may improve the scalp skin barrier, which is known to be weaker in dandruff. These studies suggest climbazole, besides its antifungal activity, is delivering positive skin benefits helping to relive dandruff symptoms effectively.
... Interestingly, we found that Trichogen â could not only inhibit trypsin activity. Climbazole is an imidazole anti-fungal agent commonly used to treat dandruff, but has no known protease inhibition activity [37]. However, we sought to combine a protease inhibition agent with an anti-dandruff agent and surprisingly found that trypsin activity was further reduced with the addition of climbazole compared with Trichogen â alone. ...
In humans the process of hair shedding, referred to as exogen, is believed to occur independently of the other hair cycle phases [1]. Although the actual mechanisms involved in hair shedding are not fully known it has been hypothesised that the processes leading to the final step of hair shedding may be driven by proteases and/or protease inhibitor activity [2, 3]. In this study we investigated the presence of proteases and protease activity in naturally shed human hairs and assessed enzyme inhibition activity of test materials.
We measured enzyme activity using a fluorescence based assay and protein localisation by indirect immunohistochemistry (IHC). We also developed an ex vivo skin model for measuring the force required to pull hair fibres from skin.
Our data demonstrates the presence of protease activity in the tissue material surrounding club roots. We also demonstrated the localisation of specific serine protease protein expression in human hair follicle by IHC. These data provide evidence demonstrating the presence of proteases around the hair club roots which may play a role during exogen. We further tested the hypothesis that a novel protease inhibitor system (combination of Trichogen(®) and climbazole) could inhibit protease activity in hair fibre club root extracts collected from a range of ethnic groups (UK, Brazil, China, 1(st) generation Mexicans in the US, Thailand and Turkey) in both males and females. Furthermore, we demonstrated that this combination is capable of increasing the force required to remove hair in an ex vivo skin model system.
These studies indicate the presence of proteolytic activity in the tissue surrounding the human hair club root and show that it is possible to inhibit this activity with a combination of Trichogen(®) and climbazole. This technology may have potential to reduce excessive hair shedding. This article is protected by copyright. All rights reserved.
One of the sensitive skin types is the “burning scalp” syndrome. It is the most expressed subjective symptom complex of tactile sensations in the projection of the skin of the scalp. The most common manifestations of this syndrome, which significantly reduces the quality of patient’s life, are burning, itching, pain, trichodynia, redness like flushing and persistent erythema, mild exfoliation and hair loss sometimes. The “burning scalp” formation is heterogeneous and can be associated with comorbid dermatoses (seborrheic dermatitis, eczema, atopic dermatitis, psoriasis, rosacea, fungal and bacterial contamination, alopecia, etc.), organ and visceral pathology (diabetes mellitus, multiple sclerosis, tumors of the central nervous system, paraneoplastic conditions, immunodeficiencies, etc.), psychosomatic abnormalities (conversion disorders, sensory hypochondria, somatoform pruritus) and environmental influences (aquagenic pruritus, ultraviolet radiation). Now, there are no general recommendations for the “burning scalp” treatment. For long-term accompanying treatment and prevention, therapeutic cosmetics that normalize the microbiome and have antipruritic and anti-inflammatory effects are promising.
Introduction. Malassezia globosa is a yeast species that belongs to the mycobiota of humans and animals, associated with dermatological disorders such as dandruff. This is a chronic scalp skin disorder characterized by flaking and itching. Treatments include commercial shampoo with different formulations that contain antifungal activities like Zinc pyrithione or Piroctone Olamine. The effectiveness of these formulations have been evaluated for decades for dandruff symptom relief of volunteers. To date, non-mammalian, in-vivo methods exist to test formulations of these actives. Aim. To evaluate in vivo in Galleria mellonella larva, two commercial antifungal shampoos (Shampoo with 1% ZPT & 1.6% Zinc Carbonate and shampoo with 0.5% PO) against this species. Methodology. G. mellonella larvae were inoculated with M. globosa on abraded cuticular surface. Then, integument cell viability, histological changes, and fungal burden were evaluated. Results. Larvae inoculated with M. globosa showed higher lesion melanization and tissue damage. In addition, M. globosa population showed to increase over time. Concerning the shampoo’s effectiveness, both formulations significantly reduced M. globosa burden and tissue damage. Conclusion. G. mellonella larvae were allowed to evaluate M. globosa superficial infection and antifungal effectiveness. Shampoos with ZPT and PO showed a positive effect on inoculated larvae.
The research into new pharmaceutical substances based on essential oils, individual biologically active phytochemicals, and plant extracts is a priority in field of pharmaceutical sciences. A novel multicomponent substance based on Melaleuca alternifolia (M. alternifolia) leaf oil (TTO), 1,8-cineole (eucalyptol), and (-)-α-bisabolol with potent synergetic antimicrobial activity was investigated and suggested for the treatment of seborrheic dermatitis (SD) and dandruff. The objective of this research was to establish and validate a specific, accurate, and precise gas chromatography–mass spectrometry (GC–MS) method for further quantitative and qualitative analysis in order to ensure quality control. The main parameters of validation were suitability, specificity, linearity, accuracy, and intermediate precision according to the European Pharmacopoeia (XI edition), Russian Pharmacopoeia (XIV edition), and some parameters of ICH requirements. The peaks of fifteen chemical phytoconstituents were identified in the test sample solution with the prevalence of (−)-α-bisabolol (27.67%), 1,8-cineole (25.63%), and terpinen-4-ol (16.98%). These phytochemicals in the novel substance were chosen for standardization and validation of the GC–MS method. The chosen chromatographic conditions were confirmed for testing of the plant-based substance in a suitability test. It was established that the GC–MS method provides a significant separation, symmetry of peaks and resolution between phytochemicals. The calibration curves of each phytochemical had good linearity (R2 > 0.999) in five concentrations. In the same concertation range, the accuracy of terpinen-4-ol, 1,8-cineol, and (−)-α-bisabolol determination using the method of additives was 98.3–101.60%; the relative standard deviation (RSD) ranged from 0.89% to 1.51% and corresponded to requirements. The intraday and interday precision was ≤2.56%. Thus, the GC–MS method was validated to be specific, sensitive, linear, accurate, and precise. This GC–MS method could be recommended as a routine analytic technique for multicomponent plant-based substances-enriched terpenes.
The Coronavirus-2 (SARS-CoV-2) outbreak resulted in a surge in prices of soaps, disinfectants, and hand sanitizers. The majority of these products contain chemical surfactants in their formulations that have proved to cause damaging effects such as skin burns and irritations along with allergic reactions. On the contrary, biosurfactants are surface-active amphipathic biomolecules that demonstrate effective health-care and medicinal properties such as low toxicity, biocompatibility, protection of skin, surface moisturizing effects, good anti-microbial ability, high swelling properties and rapid wound healing properties. This review will discuss different biosurfactants that are being used in healthcare industry and will focus on their mechanism of action along with their applications and formulations.
Seborrheic dermatitis (SD) is a common chronic inflammatory skin disorder that mostly affects young adults in areas rich in sebaceous glands (scalp, face, and trunk). In adolescents and adults, SD clinical presentation may range from mild patches to diffuse scalp scaling. In infants, it mainly occurs on the scalp as yellowish, scaly patches (“cradle cap”). In adults, several environmental triggers are likely to promote SD development, along with fungal colonization by Malassezia spp., sebaceous gland activity, as well as immunosuppression, endocrine, neurogenic and iatrogenic factors. In children, early occurrence in the first trimester suggests the role of excessive sebaceous gland activity from maternal hormones, along with cutaneous microbiome alterations. The diagnosis of SD is usually clinical, and specific laboratory and/or instrumental investigations are seldom required. Treatment is aimed at modulating sebum production, reducing skin colonization by Malassezia spp., and controlling inflammation. In adults, mild-to-moderate scalp SD forms can be managed with topical antifungals (ketoconazole, ciclopirox, miconazole) or antiinflammatory (mild-to-moderate potency corticosteroids) or keratolytic/humectant (propylene glycol) agents. Recommended topical therapeutic options for mild-to-moderate facial or body areas SD include topical ketoconazole, ciclopirox, clotrimazole, mild-to-moderate potency corticosteroids, lithium succinate/gluconate, and topical calcineurin inihibitors (off-label use). In severe and/or resistant cases, the use of systemic antifungal drugs (terbinafine, itraconazole), as well as UVB phototherapy, may be considered. In children, scant scientific evidence supports the effectiveness and safety of topical drugs, and “cradle cap” is usually successfully managed with baby shampoos enriched with emollient agents and vegetable oils. Alternatively, similarly to adult scalp SD, medical device shampoos with antiinflammatory and antifungal properties, containing piroctone olamine, bisabolol, alyglicera, telmesteine, may be used. Beyond pharmacological treatments, an appropriate cosmetic approach, if correctly prescribed, may improve therapeutic outcomes.
Background
Dandruff is a scalp malady affecting predominantly the male populace. Topical agents and synthetic drugs used for dandruff treatment have specific side effects including burning at the application site, depression, dizziness, headache, itching or skin rash, nausea, stomach pain, vision change, vomiting, discoloration of hair, dryness or oiliness of the scalp and increased loss of hair. Thus, essential oils and extracts from plants could be valuable in the treatment and prevention of dandruff.
Aim & Objective
This review aims to highlight current findings in dandruff occurrence, its etiology, promising plant essential oils/extracts, and novel treatment strategies. The main emphasis has been given on the anti-dandruff effect of essential oils and plant extracts to disrupt microbial growth. The proposed mechanism (s) of action, novel approaches used to perk up its biopharmaceutical properties, and topical application have been discussed.
Results
The literature survey was done, bibliographic sources and research papers were retrieved from different search engines and databases, including SciFinder, PubMed, NCBI, Scopus, and Google Scholar. The selection of papers was accomplished based on exclusion and inclusion criteria. The scalp of diverse populations revealed an association of dandruff with microbial symbiosis, including Staphylococcus, Propionibacterium, Malassezia, and Candida as the pathogens responsible for the cause of dandruff. Topical antifungals are considered as the first line of treatment for dandruff including azoles, with clotrimazole (1%), ketoconazole (2%), and miconazole (2%). Other commonly used therapies integrate benzoyl peroxide, coal tar, glycerin, zinc pyrithione, lithium succinate/gluconate, salicylic acid, selenium disulfide/sulfide, sodium sulfacetamide, etc. However, these medicaments and chemicals are known to cause specific side effects. Alternative therapies, including tea tree oil, thyme, Aloe vera, Mentha have been reported to demonstrate anti-dandruff activity by disrupting the microbial growth associated with dandruff formation.
Conclusion
Overall, this review explains the occurrence of dandruff, its etiology, and the potential applicability of promising plant essential oils/extracts, and their novel treatment strategies. Further studies based on pre-clinical and clinical research are essential before making any conclusion about its efficacy in humans.
Therapeutic shampoos are used around the world in both over-the-counter and prescription formulations because of their safety, efficacy, and ease of use for a variety of inflammatory scalp dermatoses including seborrheic dermatitis, psoriasis, and eczematous dermatoses, and as adjunctive treatment for tinea capitis. The majority of these products contain antifungal, anti-inflammatory, or keratolytic actions. Irritant and allergic contact dermatitis are the most common adverse effects of treatment.
Autophobicity or pseudo partial wetting, a phenomenon of a liquid not spreading on its own monolayer, is characterized by an energy barrier that prevents the growth of a wetting film beyond the monolayer thickness. Applying a molecularly detailed self-consistent field theory we illustrate how autophobic wetting can be overcome by wetting additives. More specifically we use an emulsifier which keeps the interfacial tension between the wetting component and the majority solvent low, and a co-solvent additive which partitions inside the film and then destroys the molecular order in it so that the barrier for film growth is cleared. An application wherein it is believed that autophobic wetting is counteracted by such a set of wetting additives is found in an antidandruff shampoo formulation. We have experimental results that show thick deposits onto hydrophobic hair surfaces by administration of the antidandruff shampoo. The complementary modeling of such a system suggests that the active ingredient plays the role of the co-solvent additive. As significant amounts of the co-solvent additives are needed to approach the completely wet state, the formulation naturally brings large amounts of active ingredient to the root of the hair where its presence is required.
Seborrheic dermatitis (SD) is a chronic relapsing erythematous scaly disease with a prevalence of 1–3% in the general population. The exact etiology is unknown and multifactorial; the most accepted theory suggests that yeast of Malassezia spp. causes skin irritation and inflammation on the seborrheic areas in susceptible individuals. The clinical diagnosis is based on the location and appearance of the lesions. Treatment objective is to clear the signs of the disease, ameliorate the symptoms, and maintain remission with long-term therapy. Topical antifungal and anti-inflammatory agents are the first-line therapy. Systemic therapy is reserved only for severe or refractory cases, and alternative therapies have also been reported.
Seborrheic Dermatitis (SD) is a chronic, recurring inflammatory skin disorder that manifests as erythematous macules or plaques with varying levels of scaling associated with pruritus. The condition typically occurs as an inflammatory response to Malassezia species and tends to occur on seborrheic areas, such as the scalp, face, chest, back, axilla, and groin areas. SD treatment focuses on clearing signs of the disease; ameliorating associated symptoms, such as pruritus; and maintaining remission with long-term therapy. Since the primary underlying pathogenic mechanisms comprise Malassezia proliferation and inflammation, the most commonly used treatment is topical antifungal and anti-inflammatory agents. Other broadly used therapies include lithium gluconate/succinate, coal tar, salicylic acid, selenium sulfide, sodium sulfacetamide, glycerin, benzoyl peroxide, aloe vera, mud treatment, phototherapy, among others. Alternative therapies have also been reported, such as tea tree oil, Guassia amara, and Solanum chrysotrichum. Systemic therapy is reserved only for widespread lesions or in cases that are refractory to topical treatment. Thus, in this comprehensive review, we summarize the current knowledge on SD treatment and attempt to provide appropriate directions for future cases that dermatologists may face.
Background
Seborrheic dermatitis (SD) is a multifactorial disease; Malassezia species play an important role in its pathogenesis.
Objective
We aimed to determine whether a cream containing climbazole/piroctone olamine (C/P cream), antifungal agents with expected efficacy against Malassezia species, could improve SD symptoms.
Methods
We instructed 24 patients with mild-to-moderate SD to apply the C/P cream and emollient cream on the right and left sides of the face, respectively, every morning and evening for 4 weeks. The casual sebum level (measured with Sebumeter®; Courage & Khazaka Electronic GmbH, Germany) and the extent of erythema (measured with Mexameter®; Courage & Khazaka Electronic GmbH) on the face were measured at baseline and after 4 weeks. The minimal inhibitory concentration (MIC) was determined to demonstrate the antifungal activity of the C/P cream.
Results
The casual sebum level and erythema were measured at week 4, and the median values demonstrated a quantitative improvement on the C/P cream-treated right side of the face compared to the emollient cream-treated left side. For the C/P cream, the MICs were 0.625, 5, 0.625, and 2.5 mg/ml for Malassezia restricta, M. globosa, M. sympodialis, and M. slooffiae, respectively.
Conclusion
Based on the reduced casual sebum level and extent of erythema, the antifungal activity of C/P cream against Malassezia species seems useful for the treatment of mild to moderate SD.
Las micosis superficiales son infecciones fúngicas que comprometen el estrato córneo, las estructuras anexiales o ambos, sin invadir más profundamente. Incluyen la pitiriasis versicolor, la dermatitis seborreica, la tinea nigra, la piedra blanca y la piedra negra. Producen lesiones clínicas variadas según el sitio afectado y el agente causal. Generalmente, producen poca o ninguna reacción inmunitaria; por lo tanto, su tratamiento usualmente incluye medidas y medicamentos tópicos, y solo en casos muy graves o resistentes, requieren fármacos sistémicos.
Flaking of the scalp is a symptom of seborrhoeic dermatitis, also called dandruff. It frequently occurs around the folds of the nose and eyebrows in addition to the scalp. The epidermal layers of the scalp are continually replaced and the cells are pushed outwards and they flake off giving white or grayish patches on the scalp, skin and clothes. Oily scalp, hormones or a fungus Malassezia seems to be the cause of dandruff. Dandruff can be treated with over the counter products, which are shampoos containing antifungal and antibacterial ingredients like zinc-pyrithione and selenium sulfide, salicylic acid etc. These can only slow down the flaking. Herbal extracts have proved to be good alternatives for the chemical preparations. A number of herbal shampoos and polyherbal hair oils have excellent results due to their synergistic, antifungal, anti-inflammatory and immunostimulatory action.
Background:
Seborrhoeic dermatitis is a chronic inflammatory skin condition that is distributed worldwide. It commonly affects the scalp, face and flexures of the body. Treatment options include antifungal drugs, steroids, calcineurin inhibitors, keratolytic agents and phototherapy.
Objectives:
To assess the effects of antifungal agents for seborrhoeic dermatitis of the face and scalp in adolescents and adults.A secondary objective is to assess whether the same interventions are effective in the management of seborrhoeic dermatitis in patients with HIV/AIDS.
Search methods:
We searched the following databases up to December 2014: the Cochrane Skin Group Specialised Register, the Cochrane Central Register of Controlled Trials (CENTRAL) (2014, Issue 11), MEDLINE (from 1946), EMBASE (from 1974) and Latin American Caribbean Health Sciences Literature (LILACS) (from 1982). We also searched trials registries and checked the bibliographies of published studies for further trials.
Selection criteria:
Randomised controlled trials of topical antifungals used for treatment of seborrhoeic dermatitis in adolescents and adults, with primary outcome measures of complete clearance of symptoms and improved quality of life.
Data collection and analysis:
Review author pairs independently assessed eligibility for inclusion, extracted study data and assessed risk of bias of included studies. We performed fixed-effect meta-analysis for studies with low statistical heterogeneity and used a random-effects model when heterogeneity was high.
Main results:
We included 51 studies with 9052 participants. Of these, 45 trials assessed treatment outcomes at five weeks or less after commencement of treatment, and six trials assessed outcomes over a longer time frame. We believe that 24 trials had some form of conflict of interest, such as funding by pharmaceutical companies.Among the included studies were 12 ketoconazole trials (N = 3253), 11 ciclopirox trials (N = 3029), two lithium trials (N = 141), two bifonazole trials (N = 136) and one clotrimazole trial (N = 126) that compared the effectiveness of these treatments versus placebo or vehicle. Nine ketoconazole trials (N = 632) and one miconazole trial (N = 47) compared these treatments versus steroids. Fourteen studies (N = 1541) compared one antifungal versus another or compared different doses or schedules of administration of the same agent versus one another. KetoconazoleTopical ketoconazole 2% treatment showed a 31% lower risk of failed clearance of rashes compared with placebo (risk ratio (RR) 0.69, 95% confidence interval (CI) 0.59 to 0.81, eight studies, low-quality evidence) at four weeks of follow-up, but the effect on side effects was uncertain because evidence was of very low quality (RR 0.97, 95% CI 0.58 to 1.64, six studies); heterogeneity between studies was substantial (I² = 74%). The median proportion of those who did not have clearance in the placebo groups was 69%.Ketoconazole treatment resulted in a remission rate similar to that of steroids (RR 1.17, 95% CI 0.95 to 1.44, six studies, low-quality evidence), but occurrence of side effects was 44% lower in the ketoconazole group than in the steroid group (RR 0.56, 95% CI 0.32 to 0.96, eight studies, moderate-quality evidence).Ketoconozale yielded a similar remission failure rate as ciclopirox (RR 1.09, 95% CI 0.95 to 1.26, three studies, low-quality evidence). Most comparisons between ketoconazole and other antifungals were based on single studies that showed comparability of treatment effects. CiclopiroxCiclopirox 1% led to a lower failed remission rate than placebo at four weeks of follow-up (RR 0.79, 95% CI 0.67 to 0.94, eight studies, moderate-quality evidence) with similar rates of side effects (RR 0.9, 95% CI 0.72 to 1.11, four studies, moderate-quality evidence). Other antifungalsClotrimazole and miconazole efficacies were comparable with those of steroids on short-term assessment in single studies.Treatment effects on individual symptoms were less clear and were inconsistent, possibly because of difficulties encountered in measuring these symptoms.Evidence was insufficient to conclude that dose or mode of delivery influenced treatment outcome. Only one study reported on treatment compliance. No study assessed quality of life. One study assessed the maximum rash-free period but provided insufficient data for analysis. One small study in patients with HIV compared the effect of lithium versus placebo on seborrhoeic dermatitis of the face, but treatment outcomes were similar.
Authors' conclusions:
Ketoconazole and ciclopirox are more effective than placebo, but limited evidence suggests that either of these agents is more effective than any other agent within the same class. Very few studies have assessed symptom clearance for longer periods than four weeks. Ketoconazole produced findings similar to those of steroids, but side effects were fewer. Treatment effect on overall quality of life remains unknown. Better outcome measures, studies of better quality and better reporting are all needed to improve the evidence base for antifungals for seborrhoeic dermatitis.
Dandruff and seborrheic dermatitis are common afflictions of the human scalp caused by commensal scalp fungi belonging to the genus Malassezia. Malassezia globosa and Malassezia restricta are the predominant species found on the scalp. The intergenic spacer regions of these species' rRNA genes contain short sequence repeats (SSR): (GT)n and (CT)n in M. globosa and (CT)n and (AT)n in M. restricta. In the present study, we compared the genotypes (SSR) of M. globosa and M. restricta colonizing the scalps of patients with dandruff and healthy individuals. For M. globosa, the genotype (GT)10:(CT)8 (40.3 %, 25/62) was predominant followed by (GT)9:(CT)8 (14.5 %, 9/62) and (GT)11:(CT)8 (14.5 %, 9/62) in patients with dandruff, whereas the genotypes in healthy subjects were diverse. For M. restricta, the genotype (CT)6:(AT)6 (59.7 %, 37/62) was predominant followed by (CT)6:(AT)8 (24.2 %, 15/62) in patients with dandruff, while four genotypes, (CT)6:(AT)6 (10.5 %, 6/57), (CT)6:(AT)7 (22.8 %, 13/57), (CT)6:(AT)8 (17.5 %, 10/57), and (CT)6:(AT)10 (21.1 %, 12/57), accounted for 71.9 % of all combinations in healthy subjects. The results of this study suggest that the M. globosa genotype (GT)10:(CT)8 and the M. restricta genotype (CT)6:(AT)6 may be involved in the development of dandruff.
In the present study, Fe3 O4 magnetic nanoparticles was synthesized by co-precipitation of Fe(2+) and Fe(3+) ions and used as a nano carrier for production of piroctone olamine loaded Fe3 O4 nanoparticles (Fe3 O4 @PO NPs). The nanocrystalline structure of the prepared iron oxide species was confirmed by X-ray diffraction spectroscopy method. Particle size distribution analysis showed that the size of Fe3 O4 @PO NPs was in the range of 5-55 nm. The magnetization curve of Fe3 O4 @PO NPs (with saturation magnetization of 28.2 emu/g) confirmed its ferromagnetic property. Loading of PO on the surface of Fe3 O4 NPs qualitatively verified by FTIR spectrum obtained from Fe3 O4 @PO NPs. Cytotoxicity studies on the fibrosarcoma cell line (HT-1080) revealed higher inhibitory effect of Fe3 O4 @PO NPs (IC50 of 8.1 μg/mL) compare to Fe3 O4 NPs (IC50 of 117.1 μg/mL) and PO (IC50 of 71.2 μg/mL) alone. In the case of human normal fibroblast (Hs68), the viability percent was found to be 75% in presence of Fe3 O4 @PO NPs (120 μg/mL). Gelatin zymography showed 17.2% and 34.6% inhibition of matrix metalloproteinase-2 (MMP-2) in presence of Fe3 O4 @PO and PO, respectively at the same concentration of 40 μg/mL while Fe3 O4 NPs did not inhibit MMP-2 at any concentration. This article is protected by copyright. All rights reserved.
Seborrheic dermatitis (SD) is a common, chronic inflammatory skin disease that mainly affects the scalp. The objective of this study was to evaluate the activities of superoxide dismutase (SOD) and catalase (CAT) and the levels of malondialdehyde (MDA) in scraping samples of patients with scalp SD. Thirty consecutive patients with a diagnosis of scalp SD and thirty-one healthy volunteers were enrolled. The samples were obtained by scraping the skin surface of the scalp. SOD and CAT activities and MDA levels were measured in scraping samples by spectrophotometric method. SOD and CAT activities and MDA levels were significantly higher in patients than in controls (p<0.001 all). There was a positive correlation between the severity of the disease and itching scores (contingency coefficient = 0.671, p<0.001). Except for this correlation, there was no significant correlation among age, sex, duration and severity of the disease, itching scores, antioxidant enzymes and MDA levels in the patient group (p>0.05). Cutaneous oxidative stress in patients with SD may play an important role in the pathogenesis of the disease. Further clinical and laboratory evaluation of the oxidant/antioxidant system in patients with SD is warranted.
A sensitive and specific ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed and validated for the measurement of climbazole deposition from hair care products onto artificial skin and human scalp. Deuterated climbazole was used as the internal standard. Atmospheric pressure chemical ionization (APCI) in positive mode was applied for the detection of climbazole. For quantification, multiple reaction monitoring (MRM) transition 293.0>69.0 was monitored for climbazole, and MRM transition 296.0>225.1 for the deuterated climbazole. The linear range ran from 4 to 2000ngmL(-1). The limit of detection (LOD) and the limit of quantification (LOQ) were 1ngmL(-1) and 4ngmL(-1), respectively, which enabled quantification of climbazole on artificial skin and human scalp at ppb level (corresponding to 16ngcm(-2)). For the sampling of climbazole from human scalp the buffer scrub method using a surfactant-modified phosphate buffered saline (PBS) solution was selected based on a performance comparison of tape stripping, the buffer scrub method and solvent extraction in in vitro studies. Using this method, climbazole deposition in in vitro and in vivo studies was successfully quantified.
Seborrheic dermatitis and its minimal variant, dandruff (pityriasis simplex capillitii), are among the most frequent diseases caused by Malassezia (M.) yeasts. Treatment studies have shown that antimycotics achieve clinical improvement, while recolonization leads to recurrent symptoms. Among the antimycotics used are azoles, hydroxypyridones, and various agents such as zinc pyrithione, tar, and selenium disulfide. However, comparative efficacy studies in vitro should not only consider the minimal inhibitory concentrations against Malassezia yeasts but also the bioavailability of the individual substances with regard to hair and scalp. By means of a new method, the hair strand test, hairs from ten volunteers were subjected to standardized 5-min incubation with different shampoo formulations. Thereafter they were rinsed with running water for 1 min and dried. Two hundred each of these hairs (length 1 cm) were given into a medium (olive oil on selective agar for pathogenic fungi) inoculated with M. sympodialis or M. globosa (5 x 10(3) CFU/microl), and the influence on growth was semiquantitatively determined over a period of up to 18 days. According to preliminary results, 1% climbazole proved to be particularly effective. The hair strand test, which can also be performed ex vivo, is a new method to find out whether antimycotic agents bind differently to the hair substance and, via a depot effect, may influence the growth of Malassezia yeasts and thus affect dandruff. This allows conclusions about the efficacy of antidandruff formulations.
Forty-six strains of Malassezia spp. with atypical biochemical features were isolated from 366 fresh clinical isolates from human subjects and dogs. Isolates
obtained in this study included 2 (4.7%) lipid-dependent M. pachydermatis isolates; 1 (2.4%) precipitate-producing and 6 (14.6%) non-polyethoxylated castor oil (Cremophor EL)-assimilating M. furfur isolates; and 37 (34.3%) M. slooffiae isolates that were esculin hydrolyzing, 17 (15.7%) that were non-tolerant of growth at 40°C, and 2 (1.9%) that assimilated
polyethoxylated castor oil. Although their colony morphologies and sizes were characteristic on CHROMagar Malassezia medium (CHROM), all strains of M. furfur developed large pale pink and wrinkled colonies, and all strains of M. slooffiae developed small (<1 mm) pale pink colonies on CHROM. These atypical strains were distinguishable by the appearance of their
colonies grown on CHROM. Three clinically important Malassezia species, M. globosa, M. restricta, and M. furfur, were correctly identified by their biochemical characteristics and colony morphologies. The results presented here indicate
that our proposed identification system will be useful as a routine tool for the identification of clinically important Malassezia species in clinical laboratories.
Seborrhoeic dermatitis was first described by P. G. Unna more than 100 years ago. Its localization on the scalp has often been referred to synonymously with dandruff, and there is little evidence to refuse the concept that it corresponds clinically to severe dandruff. Nevertheless, the lower incidence of seborrhoeic scalp dermatitis, the presence of erythema as a sign of inflammation, considerably more scaling, and the frequent correlation with eczematous lesions of scalp skin or else where on the body are, however, features of seborrhoeic dermatitis which distinguish it from dandruff. Of course, none of these features alone is clearly diagnostic, and seborrhoeic dermatitis as an entity has remained controversial. Whatever the cause, transient alopecia may occur in seborrhoeic scalp dermatitis, particularly in infants (Agache 1986).
Synopsis The "half-head" technique can be used as a suitable and reliable method for comparative evaluation of the efficacy of antidandruff agents. Two modes of experimental design which differ in schedule and scoring system are described. Data are given for shampoos and cream rinses containing the new antidandruff agent PIROCTONE OLAMINE (1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)-2(1H)-pyridone ethanolamine salt) in comparison to the corresponding nonmedicated formulations as well as to the same shampoo bases containing ZINC PYRITHIONE as a known efficacious antidandruff agent. Piroctone olamine has been demonstrated to be highly effective in the treatment of dandruff and more effective than zinc pyrithione at the same concentration (p < 0.05). An appreciable effect on skin lipid regeneration rate could not be measured. A tentative explanation for the often perceived increase in scalp and hair oiliness after the use of antidandruff products is advanced.
As early as can be traced, written documents testify endeavors shown by humanity to please by means of the hair. Hair care, color and style play an important role in people's physical appearance and self-perception. Dermatologists should be knowledgeable about the procedures people follow to look their best and should have the competence to provide patients with information on the benefits and hazards of hair cosmetics and pharmaceuticals. Shampooing is the most common form of cosmetic hair treatment. The diversity of qualities expected from a shampoo by today's consumer surpass the primary function of cleansing. Current shampoo formulations are adapted to the variations associated with hair quality, hair care habit and specific problems related to the superficial condition of the scalp. Hand in hand, test methods are developed to evaluate the efficacy of hair care products so that consumers are offered products that perform as claimed. Through the development of cosmetics with pharmaceutically active compounds, products are evolving that are becoming more similar to topical therapeutic agents (cosmeceuticals). The efficacy of cosmeceuticals that claim to act as hair growth stimulants should be measured by the standards set by the drugs minoxidil and, more recently, oral finasteride. Finally, health hazards associated with the use of hair care products, especially rinse-off products, have been overemphasized by the media and need careful correction by opinion leaders. Copyright (C) 2001 S. Karger AG, Basel.
Introduction. Methods for One-Sided Equivalence Problems. General Approaches to the Construction of Tests for Equivalence in the Strict Sense. Equivalence Tests for Selected One-Parameter Problems. Equivalence Tests for Designs with Paired Observation. Equivalence Tests for Two Unrelated Samples. Multi-sample Tests for Equivalence. Tests for Establishing Goodness of Fit. The Assessment of Bio-Equivalence. Appendix. References. Index
Climbazole is an imidazole antifungal agent that can provide anti-dandruff benefits when incorporated into a shampoo matrix. A series of genotoxicity studies were performed to support the human safety of this azole antifungal drug. Climbazole was not mutagenic in the Salmonella typhimurium or Escherichia coli Ames assay and did not induce micronuclei in human lymphocytes. In the mouse lymphoma assay (MLA), climbazole was negative (non-mutagenic) with and without metabolic (S9) activation after a 4 h exposure; an increase in small colony mutants was observed without metabolic activation after a 24 h exposure at concentrations of 15 and 17.5 μg/mL. An in vivo mouse micronucleus test was negative up to a maximum tolerated dose (MTD) of 150 mg/kg climbazole administered orally. In the in vivo/in vitro unscheduled DNA synthesis assay, climbazole showed no evidence of DNA damage in the livers of rats at doses up to the MTD of 200 mg/kg orally. A toxicokinetic study was performed in mice with oral administration of [14C]-climbazole (150 mg/kg). Radioactivity (20.42 μg-equiv./g plasma) was detected 15 min after oral administration of [14C]-climbazole, and the peak concentration was 62.96 μg-equiv./g plasma at 8 h after dosing. The measured amounts of radioactivity in plasma, at all sample times from 15 min up to 24 h, exceeded the concentrations that induced increases in mutation frequency after 24 h exposure of mouse lymphoma cells in vitro (15 and 17.5 μg/mL). These observations lend support to the conclusion that climbazole does not present a genotoxic risk in vivo. Furthermore, these data are consistent with the published data for other azole antifungals that work by preventing the synthesis of ergosterol and, as a class, are generally non-genotoxic, except some isolated positive results of questionable significance. Collectively, these data are supportive of the view that climbazole does not present a genotoxic or carcinogenic risk to humans.
A simple and rapid method for the determination of zinc pyrithione (ZPT) in antidandruff preparations by high-performance liquid chromatography (HPLC) has been developed. ZPT in samples was converted into a stable copper(II) complex by mixing with cupric sulphate solution followed by extraction with chloroform. HPLC was carried out on a Nucleosil 5 C18 column (15 cm X 4.6 mm I.D.) using methanol-water (3:2) as the mobile phase with UV detection at 320 nm. The calibration graph was linear from 0.1-0.5 micrograms for ZPT. The recoveries from four shampoos were 98.0-100.6% with high accuracy.
As early as can be traced, written documents testify endeavors shown by humanity to please by means of the hair. Hair care, color and style play an important role in people's physical appearance and self-perception. Dermatologists should be knowledgeable about the procedures people follow to look their best and should have the competence to provide patients with information on the benefits and hazards of hair cosmetics and pharmaceuticals. Shampooing is the most common form of cosmetic hair treatment. The diversity of qualities expected from a shampoo by today's consumer surpass the primary function of cleansing. Current shampoo formulations are adapted to the variations associated with hair quality, hair care habit and specific problems related to the superficial condition of the scalp. Hand in hand, test methods are developed to evaluate the efficacy of hair care products so that consumers are offered products that perform as claimed. Through the development of cosmetics with pharmaceutically active compounds, products are evolving that are becoming more similar to topical therapeutic agents (cosmeceuticals). The efficacy of cosmeceuticals that claim to act as hair growth stimulants should be measured by the standards set by the drugs minoxidil and, more recently, oral finasteride. Finally, health hazards associated with the use of hair care products, especially rinse-off products, have been overemphasized by the media and need careful correction by opinion leaders.
Pityrosporum ovale appears to play an important role in the pathogenesis of dandruff as a symptom of seborrheic dermatitis. Climbazole is an antimycotic agent with a high in vitro and in vivo efficacy against P. ovale. In the presented work we investigated the efficacy and safety of a climbazole 0.65% shampoo on seborrheic dermatitis of 30 volunteers. Subjects were diagnosed as having moderate to severe seborrheic dermatitis of the scalp. After a 1-week washout and a 4-week treatment the clinical evaluation showed a successful reduction of dandruff, skin redness and itching in 80% of the volunteers and a mild improvement in 20% of the volunteers. The cosmetic acceptability was very good by the majority. It is concluded that the formulation tested is effective in the treatment of moderate to severe dandruff.
The yeasts of the genus Malassezia have been associated with a number of diseases affecting the human skin, such as pityriasis versicolor, Malassezia (Pityrosporum) folliculitis, seborrheic dermatitis and dandruff, atopic dermatitis, psoriasis, and--less commonly--with other dermatologic disorders such as confluent and reticulated papillomatosis, onychomycosis, and transient acantholytic dermatosis. Although Malassezia yeasts are a part of the normal microflora, under certain conditions they can cause superficial skin infection. The study of the clinical role of Malassezia species has been surrounded by controversy because of their fastidious nature in vitro, and relative difficulty in isolation, cultivation, and identification. Many studies have been published in the past few years after the taxonomic revision carried out in 1996 in which 7 species were recognized. Two new species have been recently described, one of which has been isolated from patients with atopic dermatitis. This review focuses on the clinical, mycologic, and immunologic aspects of the various skin diseases associated with Malassezia. It also highlights the importance of individual Malassezia species in the different dermatologic disorders related to these yeasts.
Hair cosmetic agents are preparations intended for placing in contact with the hair and scalp, with the purpose of cleansing, promoting attractiveness, altering appearance, and/or protecting them in order to maintain them in good condition. Current shampoo formulations and styling products are tailored to the variations associated with age, gender, hair quality, hair care habit, and specific problems relating to the superficial condition of the scalp. The great amount of variables to be accounted for, some of them contradictory and hard to bring into accord, makes adequate product formulation a challenge and requires continuous research. Recent hair cosmetic developments include topical hair growth stimulants, photoprotectors, and anti-aging compounds. The advances in molecular technology have opened the avenue to the study of the molecular basis of hair growth and its deviations, as well as of the aging process. The discovery of potential pharmacological targets and the development of selective and effective delivery systems following topical application indicate further strategies for maintenance of healthy hair and scalp in the young and old.
Dandruff is a chronic condition of the scalp requiring vigilant treatment to ameliorate the symptoms of scaling and itching. Frequent shampooing is key to controlling these symptoms while contributing to the cosmetic appearance of the hair. The success of the treatment depends not only on the ability of the shampoo to control the dandruff but also on patient compliance engendered by the cosmetic attributes of the shampoo. This double-blind cross-over study enrolled 40 women with mild to moderate dandruff. Following a 1-wk washout with an unmedicated basic cleansing shampoo, all subjects used each of the two study shampoos for 1 wk. Subjects preferred the 1% pyrithione zinc conditioning shampoo over the 2% ketoconazole shampoo by 75% in terms of overall performance. The dermatologist investigator confirmed the subject preference by noting that hair-combing ease, hair smoothness, and hair frizz/flyaway were statistically significantly better in subjects who used the 1% pyrithione zinc conditioning shampoo for 1 wk. This study suggests that hair condition is an important consideration in the treatment of dandruff due to compliance.
The zinc-enhanced PTZ activity observed in vitro and understood in terms of increased bio-availability results in increased performance in vivo in complex matrices as well. Quantitation of in vivo Malassezia reduction from shampoo matrices demonstrates PTZ formulation with zinc to be more effective than PTZ formulations alone. This benefit also translates to significantly improved clinical flake reduction from shampoos containing added zinc as an excipient.
Scalp skin is unique on the body due to the density of hair follicles and high rate of sebum production. These features make it susceptible to superficial mycotic conditions (dandruff, seborrheic dermatitis, and tinea capitis), parasitic infestation (pediculosis capitis), and inflammatory conditions (psoriasis). Because these scalp conditions share similar clinical manifestations of scaling, inflammation, hair loss, and pruritus, differential diagnosis is critically important. Diagnostic techniques and effective treatment strategies for each of the above conditions will be discussed.
Synopsis
Dandruff is a common problem in approximately 30% of the world's population. Reports in the literature regarding treatment of this condition with various antidandruff shampoos usually report the level of active ingredient within the formulation. However, we propose that a more important parameter relating to antidandruff efficacy is the amount of active ingredient delivered to the scalp from the shampoo. This report describes the results from two studies designed to investigate the relationship between the level of zinc pyrithione (ZnPTO) deposited onto the scalp and the resultant scalp condition. A double‐blind randomized vehicle‐controlled clinical study comparing three shampoos – a vehicle, a low‐depositing ZnPTO shampoo and a high‐depositing ZnPTO shampoo – was carried out in the U.K. with 53 panelists with dandruff or mild‐to‐moderate seborrheic dermatitis of the scalp. Both shampoos containing ZnPTO were significantly superior in antidandruff efficacy to the vehicle. Furthermore, the high‐depositing ZnPTO shampoo was significantly superior compared with the low‐depositing ZnPTO shampoo in terms of both antidandruff efficacy and antimycotic activity. Antidandruff performance and antimycotic activity of ZnPTO‐containing shampoos is highly dependent on the amount of active ingredient delivered to the scalp. Furthermore, careful manipulation of the formulation parameters of an antidandruff shampoo can result in enhanced levels of delivery of the active ingredient without having to increase the level of active ingredient within the formulation.
Synopsis
Dandruff (pityriasis capitis) is a chronic scalp condition characterized by scaling and sometimes itching and redness. Shampoos containing antifungal agents are used to control the scaling condition. In the present study, two shampoos with different actives are compared in a double-blind, randomised and bilateral study on 19 subjects. One shampoo contained piroctone olamine (0.75%) combined with salicylic acid (2%) and the other contained zinc pyrithione (1%) as active ingredient. The subjects were treated twice weekly with the shampoos for almost 4 weeks. Before each treatment the degree of dandruff was evaluated.
Both shampoos were highly effective in reducing the dandruff. The combination of piroctone olamine and salicylic acid appeared to be slightly more effective than zinc pyrithione in reducing the severity and area affected by the scaling.
Résumé
L’état pelliculaire pityraisis capitis est une maladie chronique du cuir chevelu, caractérisée par des desquamations et dans certain cas des démangeaisons et des rougeurs. Les shampooings contenant des agents antifongiques sont utilisés pour contrôler l’état du cuir chevelu. Dans cette étude, deux shampooings aux actifs differents sont comparés dans un test bilatéral en double aveugle et au hasard sur 19 sujets. Un des shampooings contient de la piroctone olamine (0,75%) combinée avec de l’acide salicylique (2%). L’autre shampooing contient de la pyrithione zinc (1%) comme actif. Les sujets sont traités avec les shampooings deux fois par semaine pendant quatres semaines. Avant chaque traîtement, le degré de l’état pelliculaire a étéévalué.
Les shampooings ont réduit de façon significative l’état pelliculaire dans les deux cas. Toutefois la combinasion piroctone olamine/acide salicylique semble être plus efficace que la pyrithione zinc tant au niveau de la severité de la maladie et de la surface affectée par la desquamation.
Evaluation of the genotoxi
- A A Pé-Rivera
- T Hu
- M J Aardema
- J F Nash
Pé-Rivera, A.A., Hu, T., Aardema, M.J. and Nash, J.F. Evaluation of the genotoxi-10(3), 198–200 (2005).