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Topical palmitoyl pentapep-tide provides improvement in photoaged human facial skin
Abstract
The palmitoyl pentapeptide palmitoyl-lysine-threonine-threonine-lysine-serine (pal-KTTKS) is a synthetic material that was designed as a topical agent to stimulate collagen production and thus provide a skin anti-wrinkle benefit. To determine if pal-KTTKS is effective, the clinical study reported here was conducted. Caucasian female subjects (n = 93, aged 35–55) participated in a 12-week, double-blind, placebo-controlled, split-face, left–right randomized clinical study assessing two topical products: moisturizer control product vs. the same moisturizer product containing 3 ppm pal-KTTKS. Pal-KTTKS was well tolerated by the skin and provided significant improvement vs. placebo control for reduction in wrinkles/fine lines by both quantitative technical and expert grader image analysis. In self-assessments, subjects also reported significant fine line/wrinkle improvements and noted directional effects for other facial improvement parameters.
Le pentapeptide palmitoyl-lysine-thréonine-lysine-sérine (pal-KTTKS) est un composé synthétique décrit comme agent topique stimulant la production de collagène et possédant donc des propriétés anti-rides. L'efficacité du pal-KTTKL a étéévaluée dans l’étude clinique faisant l'objet de cet article. Des femmes de type caucasien (n = 93, de 35 à 55 ans) ont participé pendant 12 semaines à un test en double aveugle avec placébo, en apparié par demie face comparant deux produits topiques: un produit témoin hydratant et le même produit contenant 3 ppm de pal-KTTKS. Bien toléré par la peau, le pal-KTTKS a montré par rapport au témoin, une amélioration significative dans la réduction des rides et ridules que se soit par des techniques quantitatives et par l'analyse d'image quantifiée par un expert. Dans le cadre d'auto-évaluations, les sujets ont fait état d'améliorations significatives et attiré l'attention sur des effets pouvant servir de pistes pour d'autres paramètres d'amélioration faciale.
... Robinson et al. hav conducted a double-blind, placebo, randomized study on ninety-three Caucasian femal subjects presenting facial wrinkles and fine lines. After the 12-week trial period o applying oil in water cream containing Palmitoyl Pentapeptide-4, expert grader identified an improvement in fine lines and overall skin appearance [49]. ...
... Robinson et al. have conducted a double-blind, placebo, randomized study on ninety-three Caucasian female subjects presenting facial wrinkles and fine lines. After the 12-week trial period of applying oil in water cream containing Palmitoyl Pentapeptide-4, expert graders identified an improvement in fine lines and overall skin appearance [49]. ...
... Palmitoyl Pentapeptide-4 o/w cream 0.0003% [49] Tripeptide-10 Citrulline w/w cream 5% [50] Palmitoyl hexapeptide-12 w/w cream 0.0004% [34] Copper Tripeptide-1 serum 1% [57] Acetyl Hexapeptide-3 o/w or w/w cream 10% [50,65] Pentapeptide-18 o/w cream 2% [25] Acetyl Octapeptide-3 solution 0.05% [78] Tripeptide-3 o/w cream 4% [69] w/w-water in water; o/w-oil in water. ...
One class of cosmetic compounds that have raised interest of many experts is peptides. The search for ingredients with good biocompatibility and bioactivity has led to the use of peptides in cosmetic products. Peptides are novel active ingredients that improve collagen synthesis, enhance skin cell proliferation, or decrease inflammation. Based on their mechanism of action, they can be classified into signal peptides, carrier peptides, neurotransmitter inhibitor peptides, and enzyme inhibitor peptides. This review focuses on the main types of peptides and their application in the cosmetic field, underlining their main limitations. One of the most significant drawbacks of cosmetic peptides is their poor permeability through membranes, which limits their delivery and effectiveness. As a result, this review follows the methods used for improving permeability through the stratum corneum. Increasing peptide bioavailability and stability for enhanced delivery to the desired site of action and visible effects have become central points for the latest research due to their promising features. For this purpose, several methods have been identified and described. Physical techniques include thermal ablation (radiofrequency and laser), electrical methods (electroporation, iontophoresis), mechanical approach (microneedles), and ultrasounds. As an alternative, innovative formulations have been developed in nano-systems such as liposomes, niosomes, ethosomes, nanoemulsions, and other nanomaterials to reduce skin irritation and improve product effectiveness. The purpose of this review is to provide the latest information regarding these noteworthy molecules and the reasoning behind their use in cosmetic formulations.
... 33 Peptides upregulate in vitro collagen production and topical formulations have shown clinical improvement when applied to photodamaged skin. 12 A topical pentapeptide, containing the sequence lysinethreonine-threonine-lysine-serine (KTTKS) is a fragment of procollagen I. 34 This synthetic peptide stimulates collagen production, which provides structure and support to the skin. 34 A 12-week double-blind, placebo-controlled, split-face study with moisturizer containing 3 parts/million palmitoyl-KTTKS showed a significant reduction in fine lines and wrinkles. ...
... 12 A topical pentapeptide, containing the sequence lysinethreonine-threonine-lysine-serine (KTTKS) is a fragment of procollagen I. 34 This synthetic peptide stimulates collagen production, which provides structure and support to the skin. 34 A 12-week double-blind, placebo-controlled, split-face study with moisturizer containing 3 parts/million palmitoyl-KTTKS showed a significant reduction in fine lines and wrinkles. 34 Another study utilizing 3 peptide derivatives, in a mixed form, resulted in increases in dermal collagen and epidermal protein expression, leading to significant improvement in crow's feet and other wrinkles. ...
... 34 A 12-week double-blind, placebo-controlled, split-face study with moisturizer containing 3 parts/million palmitoyl-KTTKS showed a significant reduction in fine lines and wrinkles. 34 Another study utilizing 3 peptide derivatives, in a mixed form, resulted in increases in dermal collagen and epidermal protein expression, leading to significant improvement in crow's feet and other wrinkles. 31 Cosmetic manufacturers also offer topical cell culture extracts with natural enzymes and growth factor proteins that have shown improvement in periorbital wrinkles, roughness, and pigmentation when tested. ...
Background
Due to the periorbital region’s high susceptibility to damage from external factors, along with its tendency to demonstrate early signs of aging, periorbital skin is a common target for antiaging therapy.
Objective
This review aims to evaluate the efficacy of active ingredients commonly found in eye creams, particularly focusing on their impact on periorbital skin concerns.
Methods
A comprehensive review of the literature on active ingredients in eye creams, including retinoids, vitamins C and E, peptides, ceramides, hyaluronic acid, caffeine, and niacinamide, was conducted. Clinical studies assessing the efficacy of these ingredients in addressing periorbital concerns were examined.
Results
Studies demonstrate the potential of these ingredients to improve various aspects of periorbital skin, including hydration, elasticity, collagen synthesis, and reduction of inflammatory mediators. Ingredients such as retinoids, vitamin C, and caffeine show promise in addressing wrinkles and hyperpigmentation, while peptides and hyaluronic acid aid in collagen production and hydration. Niacinamide and ceramides offer benefits in reducing wrinkles and enhancing the skin barrier function.
Limitations
The lack of clinical trials specifically targeting eye cream formulations and periorbital skin is a notable limitation. Furthermore, the variability in study designs, sample sizes, and concentrations of active ingredients across studies complicates direct comparisons.
Conclusion
The reviewed studies highlight the potential of active ingredients in eye creams to address various periorbital concerns. Further research, particularly large-scale clinical trials focusing on eye cream formulations and their efficacy on periorbital skin, is warranted to establish their significance and comparability with other dermatologic products.
... Briefly, 1-bromohexadecane and 1-bromotetradecane were first reacted with imidazole, following a procedure previously described by Colonna et al. (step i, Fig. 1A) (26), to afford 1-tetradecyl-imidazole (C 14 Im) and 1-hexadecylimidazole (C 16 Im), respectively. After confirming the structures of both C 14 Im and C 16 Im by Nuclear Magnetic Resonance ( 1 H-and 13 C-NMR), these imidazoles were reacted with propargyl bromide according to Hu et al. (step ii, Fig. 1A) (27), to afford the three target imidazolium ILs, propargyl-MeIm (Pr-MeIm), propargyl-C 14 Im (Pr-C 14 Im) and propargyl-C 16 Im (Pr-C 16 Im). The structures of these ILs were confirmed by 1 H-NMR, 13 C-NMR, and electrospray ionization-ion trap mass spectrometry (ESI-IT MS). ...
... Notably, the reference peptides C 16 -KTTKS-NH 2 and C 16 -KTTKS-OH were respectively soluble in water and dimethyl sulfoxide (DMSO), but both precipitated when diluted in cation-adjusted Mueller-Hinton broth (MHB2), the culture medium recommended by the CLSI guidelines, which hampered the determination of the MIC values for these reference peptides. Data in Table 1 show, as expected, that the peptide KTTKS alone is devoid of significant antibacterial activity, and that MIC values for the reference 1-hexadecyl-3-methylimidazolium bromide ([C 16 M1Im] [Br]) IL are in agreement with those previously reported (29). Interestingly, all conjugates bearing methyl imidazolium (MeIm) units were inactive against the tested bacterial species, even at the highest concentrations used, regardless the number or position of the MeIm moieties in the overall structure. ...
... In turn, replacing the methyl substituent in the imidazolium ring by either a tetradecyl (C 14 ) or a hexadecyl (C 16 ) group, led to an improvement in the antibacterial activity, delivering MIC values from 6.45 to 52.6 mg/mL, hence adding antimicrobial activity to the parent KTTKS peptide. Given that KTTK(C 16 Im)S and C 16 Im-KTTKS showed the strongest antibacterial activities, and reflect two different conjugation FIG 1 Route to the target IL-KTTKS conjugates. (A) Synthesis of the alkyne derivatives of the IL: (i) 1 molar equivalent (eq) of imidazole, 1.5 eq of potassium hydroxide, 1-bromotetradecane or 1-bromohexadecane in dimethyl sulfoxide (DMSO), 70°C, 5 h; (ii) 1.1 eq of C 16 Im, C 14 Im or MeIm and 1.0 eq of propargyl bromide (80% in toluene), 40°C, 24 h. ...
As life expectancy increases, diseases causing chronic wound infections become more prevalent. Diabetes, peripheral vascular diseases, and bedridden patients are often associated with non-healing wounds that become infected, resulting in high morbidity and mortality.
... Several clinical published studies have shown that topical formulations containing palmitoyl-KTTS have the capacity to reduce fine lines, wrinkles, and improve skin texture significantly [58,59]. However, most of reported clinical benefits were obtained by using a formulation containing palmitoyl-KTTKS and other active ingredients (e.g., niacinamide and vitamin E), or at least in the presence of a basic moisturizer, suggesting that the observed benefits may not be solely produced by the conjugated peptide. ...
... However, most of reported clinical benefits were obtained by using a formulation containing palmitoyl-KTTKS and other active ingredients (e.g., niacinamide and vitamin E), or at least in the presence of a basic moisturizer, suggesting that the observed benefits may not be solely produced by the conjugated peptide. Furthermore, study design and data evaluation are not described in detail in all studies, except for the studies by Robinson et al. [58] and Fu et al. [60]. ...
... Furthermore, some peptides are relatively well investigated. Several scientific studies indicate that palmitoyl-KTTS has a capacity to significantly reduce signs of skin aging on the face [58][59][60]. In vivo synergistic activity of cell regulators and antioxidants, as observed in some studies [60,73], makes the combination of differently acting active substances promising for cosmetic and dermatological applications. ...
Over-the-counter antiaging formulations aim to prevent or minimize the signs of aging skin, and to maintain the benefits obtained from different cosmetic procedures. Even though a huge selection of such products is available on the market, evidence and good clinical practice of the data supporting their use are oftentimes lacking. In this systematic review, the authors reviewed scientific data available in the published literature on the most common ingredients used in antiaging cosmetics, with a particular focus on in vivo studies.
... Although these strategies are considered promising, the paucity of literature regarding the transdermal permeation and retention of KTTKS raises questions about the clinical benefits of its intended use. Indeed, the clinical benefits of the new and modified KTTKSrelated molecules were marginal in several human trials [8][9][10][11] . Furthermore, the molecular weights of palmitoyl and ascorbyl KTTKS are 802.05 and 811.74 g/mol, respectively, which are too large for the prodrug type molecules to permeate the stratum corneum layer without the aid of transdermal delivery system technology. ...
... It belongs to a signaling peptide which is capable of regulating cell proliferation and extracellular matrix regeneration by interacting with specific receptor. By regulating the extracellular matrix regeneration, pal-KTTKS has been claimed to be a useful bioactive peptide molecule for skin anti-aging [8,18,19] . ...
... 13 For instance, the Palmitoyl pentapeptide-4 (pal-KTTKS), derived from collagen type αI, has shown in vitro elevated expression of fibronectin, hyaluronic acid (HA), and collagen type I and III, 14 while as a topical agent, it has shown to reduce wrinkles and age spots, and restored skin elasticity. 15 Similarly, Palmitoyl hexapeptide-12 (pal-VGVAPG), derived from elastin, 16 has been shown to be a chemoattractant for skin fibroblasts in vitro 17 and successfully improved skin elasticity and tone when applied topically in vivo. 18 Both peptides have been shown to cross the skin barrier while acting as moisturizers. ...
Self-assembling peptides (SAPs) represent a rich source of building blocks that interact with biological structures. For instance, cosmetic SAPs like Palmitoyl hexapeptide-12 have gained increasing interest for their anti-aging properties. However, their short-term impact on the skin composition and mechanics remains unclear. In this study, a battery of label-free techniques is exploited to objectively monitor the effects of Palmitoyl hexapeptide-12 on human skin. Orbital trapping secondary ion mass spectrometry (OrbiSIMS) is used to discern between Palmitoyl hexapeptide-12 sol and gel forms, tracking its self-assembly and penetration within full-thickness human skin. Palmitoyl hexapeptide-12 is shown to permeate both stratum corneum and epidermal layers, initiating gel formation by harnessing endogenous ions. Hence, the ability of the peptide to strengthen and repair the skin barrier after delipidation is also demonstrated through a high-throughput mechanical characterization and stimulated Raman scattering (SRS). Finally, the co-assembling properties of Palmitoyl hexapeptide-12 with native skin molecules are shown via in vitro tests and ex vivo histology. This study establishes a methodological benchmark for measuring the effects of cosmetic peptides on skin mechanics and hydration, introducing a platform to design SAPs capable of harnessing native skin molecules to create "biocooperative" structures with cosmetic benefits.
... Nonapeptide-1 is a synthetic nonapeptide derived from arginine, lysine, methionine, phenylalanine, proline, tryptophan, and valine including reducing wrinkles or fine lines [83]. To identify peptides with better anti-aging effects, a series of oligopeptides were synthesized and screened in vitro for evaluating their capacity in the 2000s. ...
Peptides are molecules that consist of at least two amino acids linked by peptide bonds. The difference between peptides and proteins is primarily based on size and structure. Typically, oligopeptides consist of fewer than about 10–20 amino acids, and polypeptides consist of more than 20 amino acids, whereas proteins usually are made up more than 50 amino acids and often contain multiple peptide subunits as stated in the International Union of Pure and Applied Chemistry rules. Beyond the nutritional properties, peptides are also structural components of hormones, enzymes, toxins, and antibiotics and play several fundamental physiological roles in the body. Since the introduction of the first commercial peptide drug, insulin, peptide‐based drugs have gained increased interest. So far, more than 80 peptide‐based drugs have reached the market for a wide range of conditions, such as diabetes, cardiovascular diseases, and urological disorders. Meanwhile, peptides have also gained significant attention in the cosmetic industry because of their potential in boosting skin health. In this review, peptides were comprehensively summarized in the aspects of sources, function, the use of peptides in cosmetics and skin care, and indications for the delivery of cosmetic peptides.
... Enhancing collagen and glycosaminoglycan production boosts skin cell activity, counteracts aging effects, improves elasticity, and increases skin thickness. Notably, it possesses impressive skin-healing capabilities, addressing damage from UV exposure and external factors [88,89]. Including capric acid & myristic acid (MA) in the TES enhanced flexibility compared to ethosomes and conventional liposomes. ...
In the dynamic landscape of pharmaceutical advancements, the strategic application of active pharmaceutical ingredients to the skin through topical and transdermal routes has emerged as a compelling avenue for therapeutic interventions. This non-invasive approach has garnered considerable attention in recent decades, with numerous attempts yielding approaches and demonstrating substantial clinical potential. However, the formidable barrier function of the skin, mainly the confinement of drugs on the upper layers of the stratum corneum, poses a substantial hurdle, impeding successful drug delivery via this route. Ultradeformable vesicles/carriers (UDVs), positioned within the expansive realm of nanomedicine, have emerged as a promising tool for developing advanced dermal and transdermal therapies. The current review focuses on improving the passive dermal and transdermal targeting capacity by integrating functionalization groups by strategic surface modification of drug-loaded UDV nanocarriers. The present review discusses the details of case studies of different surface-modified UDVs with their bonding strategies and covers the recent patents and clinical trials. The design of surface modifications holds promise for overcoming existing challenges in drug delivery by marking a significant leap forward in the field of pharmaceutical sciences.
... One of the primary roles of bioactive peptides in skin regeneration involves the stimulation of collagen synthesis. Peptides such as copper tripeptide-1 and palmitoyl pentapeptide-4 are known to upregulate collagen production in fibroblasts, the principal cells responsible for extracellular matrix synthesis [42]. This not only aids in reducing the appearance of wrinkles but also enhances skin firmness and integrity, counteracting the effects of aging. ...
The relentless pursuit of effective strategies against skin aging has led to significant interest in the role of bioactive factors, particularly secondary metabolites from natural sources. The purpose of this study is to meticulously explore and summarize the recent advancements in understanding and utilization of bioactive factors against skin aging, with a focus on their sources, mechanisms of action, and therapeutic potential. Skin, the largest organ of the body, directly interacts with the external environment, making it susceptible to aging influenced by factors such as UV radiation, pollution, and oxidative stress. Among various interventions, bioactive factors, including peptides, amino acids, and secondary metabolites, have shown promising anti-aging effects by modulating the biological pathways associated with skin integrity and youthfulness. This article provides a comprehensive overview of these bioactive compounds, emphasizing collagen peptides, antioxidants, and herbal extracts, and discusses their effectiveness in promoting collagen synthesis, enhancing skin barrier function, and mitigating the visible signs of aging. By presenting a synthesis of the current research, this study aims to highlight the therapeutic potential of these bioactive factors in developing innovative anti-aging skin care solutions, thereby contributing to the broader field of dermatological research and offering new perspectives for future studies. Our findings underscore the importance of the continued exploration of bioactive compounds for their potential to revolutionize anti-aging skin care and improve skin health and aesthetics.
... 25 Previous studies reported that topical use of carbohydrates viz stachyose (present in mustard seeds, 35 chickpea, 27 and faba bean 37 ), mannose (present in gum kateera 38 ) and amino acids viz arginine (present in chickpea 27 ), threonineand leucine (present in milk 39,40 ), proline (present in mustard seeds 41 ), and aspartic acid (present in faba bean 37 ) have stimulatory effects on fibroblast proliferation and collagen fibers. [42][43][44][45][46][47][48] Vitamin C (present in barley, 31 chickpea, 30 turmeric, 33 and lentil 32 promotes collagen formation. 34 Polyphenols viz anthocyanins (present in barley, 49 mustard 35 ), epicatechin (present in faba bean 50 ) catechin, epicatechin gallate, andisoflavones (present in lentil 32 ) have antiaging activity and stimulate collagen synthesis. ...
Introduction:
Ageing is a natural process of life. With increasing age, the skin suffers progressive morphological and physiological decrement. Hyperpigmentation, Wrinkles, and roughness of skin are some of the symptoms of aged skin. Exposure to sunlight, pollution, stress, nicotine, etc aggravates Skin aging. This study aimed to determine the efficacy and safety of polyherbal formulation and compare its efficacy with the standard drug tretinoin in subjects of moderate to advanced Photoaged facial skin. Ingredients of polyherbal formulation are Aarade baqla (Vicia faba), Jau (Hordeum vulgare), Nakhud (Cicer arietinum),Masoor (Lens esculenta), Tukhm e turb (Raphanus sativus), Khardal (Brassica nigra), Haldi (Curcuma longa), Kateera (Cochlospermum religiosum).
Methods:
This was a randomized open-label standard controlled study. 82 eligible subjects were allocated equally into test and control groups by computer-generated random numbers. In the test group, a paste of 15 gm polyherbal formulation in milk, and the control group, 0.025% Tretinoin 1 gram was used topically on the face once a day for two months. The response was assessed by theclinician using following different scales for different parameters.
Assessment of skin hyperpigmentation:
It was assessed by the Skin Hyperpigmentation Index online calculator (SHI). It describes the ratio of two scores, namely the hyperpigmented skin of the affected area and normal sun-protected skin from the same patient. The image was recorded with a Digital microscope-Win7 from a hyperpigmented area and normal sun-protected area. Both the images were uploaded on https://shi.skinimageanalysis.com/ and calculated the mean value of hyperpigmentation. SHI ranges from 1 (no hyperpigmentation) to 4 (maximum hyperpigmentation) where scores between 1 and 2 showed as light hyperpigmentation, 2-3 as medium hyperpigmentation, and scores between 3 and 4 as severe hyperpigmentation.
Assessment of fine wrinkles:
Fine wrinkles number was determined by digital photography. The photographs were taken through Canon EOS 1500D DSLR Camera with an 18-55 mm Lens. Three images were taken of each subject's face (right, left, and center full face) on Baseline and Day 15th, 30th, 45th, and 60th to assess visible changes/improvement in their fine wrinkles score.
Assessment of nasolabial fold:
Modified Fitzpatrick Wrinkle Scale (MFWS) was used to assess Nasolabial folds. The scale comprised four main classes of Nasolabial wrinkling: 0, 1, 2, and 3 representing absent, fine, moderate, and deep wrinkles, respectively, and three inter classes i.e., 0.5, 1.5, and 2.5 to estimate wrinkle depth. The definitions of the entire classes of the scale are as follows: Class 0 = No wrinkle. No visible wrinkle; continuous skin line; Class 0.5 = Very shallow yet visible wrinkle; Class 1= Fine wrinkle. Visible wrinkle and slight indentation; Class 1.5= Visible wrinkle and clear indentation. <1-mm wrinkle depth; Class 2= Moderate wrinkle. Visible wrinkle, 1- to 2-mm wrinkle depth; Class 2.5= Prominent and visible wrinkle. More than 2-mm and less than 3-mm wrinkle depth; Class 3=Deep wrinkle. Deep and furrow wrinkle; more than 3-mm wrinkle depth.
Assessment of forehead lines score:
Forehead lines were assessed (number and depth) by a Validated Grading Scale for Forehead Lines. The Forehead Lines Grading Scale is a 5- point photonumeric rating scale that was developed to objectively quantify resting (static) and hyperkinetic (dynamic) forehead lines. The scale ratings are 0 for no wrinkles, 1 for no wrinkles present at rest but fine lines with facial expression, 2 for fine wrinkles present at rest and deep lines with facial expression, 3 for fine wrinkles present at rest and deeper lines with facial expression, and 4 for deeper wrinkles at rest and deeper furrows with facial expression.
Assessment of lateral canthal lines:
The number of lateral canthal lines was determined by a Validated Grading Scale for Crow's Feet. The Crow's Feet Grading Scale is a 5- point photonumeric rating scale developed to objectively quantify the severity of crow's feet. This scale was applied to two separate evaluations of crow's feet: at rest (static) and with expression (dynamic). The scale ratings are 0 for no wrinkles, 1 for very fine wrinkles, 2 for fine wrinkles, 3 for moderate wrinkles, and 4 for severe wrinkles.
Assessment of facial skin roughness:
The Allergan Skin Roughness Scale was used for facial skin roughness assessment. The area of assessment for the Allergan Skin roughness Scale is the area between the nasolabial fold to the preauricular cheek and from the inferior orbital rim to the mandible. The Allergan Skin Roughness Scale assigns a grade from none (0) to extreme (4) that describes the severity of skin coarseness, crosshatching, and elastosis in the midface area. The scale grading are 0 (None) Smooth visual skin texture, 1 (Minimal) Slightly coarse and uneven visual skin texture, 2 (Moderate) Moderately coarse and uneven visual skin texture; may have early elastosis, 3 (Severe) Severely coarse visual skin texture, cross-hatched fine lines; may have some elastosis, and 4 (Extreme) Extremely coarse visual skin texture, cross Hatched deep creases; extreme elastosis.
Assessment of facial dullness:
Dullness was assessed on a clinical basis with an arbitrary scoring ranging from 0 to 9 where 0-3=mild, 3.5-6=moderate, and 6.5-9=severe facial skin dullness.
Assessment of quality of life:
Subjects' life quality was assessed by the Dermatology Life Quality Index questionnaire. It consists of 10 questions. Each question is scored on a four-point Likert scale: Very much = 3, A lot = 2, A little = 1, Not at all = 0, Not relevant = 0 and Question unanswered = 0. The DLQI is calculated by adding the score of each question, resulting in a maximum of 30 and a minimum of 0. Where, 0-1= no effect at all on patient's life, 2-5 = small effect on patient's life, 6-10 = moderate effect on patient's life, 11-20 = very large effect on patient's life, 21-30 = extremely large effect on patient's life.
Results:
Both groups showed a significant improvement in Fine Wrinkles, Forehead Lines, Crow's Feet, Roughness, Dullness, Nasolabial Fold, Hyperpigmentation, and Quality of Life parameters. (P < .001) A large number of subjects in the control group reported mild to moderate redness, itching, dryness, and blackening of the skin, while in the test group, absolutely no side effects were reported during treatment.
Conclusion:
The effects in both groups were substantial, but the polyherbal formulation is safe and effective for use in photoaged facial skin. It may be a more feasible easily accessible cheap and safe formulation to prevent skin aging and restore skin elasticity and make skin brighter. Further studies to evaluate the efficacy of formulation on objective parameters using standard instruments should be done for appropriate measurements of parameters.
... 76 Matrixyl is well tolerated by the skin and was found in a double-blind placebo-controlled split-face trial to cause a visible improvement to fine lines and wrinkles by both quantitative technical and expert grader analysis. 77 It is also customary to find proprietary formulations containing combinations of matrikines with additional cosmeceutical products. 78 For example, Matrixyl and palmitoyl tetrapeptide-7, in combination with natural extracts of white lupin, ginseng and mulberry, was found in a double-blind randomized clinical trial to provide significant clinical improvement to facial wrinkles, which was associated with significant histological deposition of fibrillin-rich microfibrils within the papillary dermis. ...
Skin ageing is a complex process involving the additive effects of skin’s interaction with its external environment, predominantly chronic sun exposure, upon a background of time-dependent intrinsic ageing. Skin health and beauty is considered one of the principal factors perceived to represent overall ‘health and wellbeing’; thus, the demand for skin rejuvenation strategies has rapidly increased, with a worldwide annual expenditure expected to grow from US44.5 billion by 2030 (https://www.databridgemarketresearch.com/reports/global-facial-rejuvenation-market). Skin rejuvenation can be achieved in several ways, ranging from laser and device-based treatments to chemical peels and injectables; however, topical skin care regimes are a mainstay treatment for ageing skin and all patients seeking skin rejuvenation can benefit from this relatively low-risk intervention. While the most efficacious topical rejuvenation treatment is application of tretinoin (all-trans retinoic acid) – a prescription-only medicine considered to be the clinical ‘gold standard’ – a hybrid category of ‘cosmeceutical’ products at the midpoint of the spectrum of cosmetics and pharmaceutical has emerged. This article reviews the clinical manifestations of skin ageing and the available topical treatments for skin rejuvenation, including retinoids, peptides and antioxidants.
... Lipopeptides have important applications in biomedicine and can be used as antimicrobial agents to treat MRSA infections [7,8], and as therapeutics for cancer and immune diseases [9,10]. They have also founds applications in cosmetics [11,12], and as fungicides in crop development [13]. Some lipopeptides are able to penetrate through the cell membrane and are found in different cell components [14][15][16]17]. ...
... These peptides have beneficial growth factor-like activities, but are much smaller and simpler to utilize for formulation purposes [76]. Minor modifications to the peptide structures, such as by adding palmitoyl to KTTKS or octanoyl to carnosine, have led to significant improvements in skin permeation, and thus, to efficacy [75,77]. ...
Successful aging" counters the traditional idea of aging as a disease and is increasingly equated with minimizing age signs on the skin, face, and body. From this stems the interest in preventative aesthetic dermatology that might help with the healthy aging of skin, help treat or prevent certain cutaneous disorders, such as skin cancer, and help delay skin aging by combining local and systemic methods of therapy, instrumental devices, and invasive procedures. This review will discuss the main mechanisms of skin aging and the potential mechanisms of action for commercial products already on the market, highlighting the issues related to the permeation of the skin from different classes of compounds, the site of action, and the techniques employed to overcome aging. The purpose is to give an overall perspective on the main challenges in formulation development, especially nanoparticle formulations, which aims to defeat or slow down skin aging, and to highlight new market segments, such as matrikines and matrikine-like peptides. In conclusion, by applying enabling technologies such as those delivery systems outlined here, existing agents can be repurposed or fine-tuned, and traditional but unproven treatments can be optimized for efficacious dosing and safety.
... It has been previously shown that peptide fragments result from damage to the ECM and thus are a "sensing" medium of extracellular matrix damage (17,54). Cosmetically, peptides have been utilized in skin repair regimens to exploit this sensing mechanism of repair (55). However, ...
Objective:
To explore synergistic effects related to skin regeneration, peptides with distinct biological mechanisms of action were evaluated in combination in different skin cell lines in the presence or absence of niacinamide (Nam). Furthermore, the synergistic responses of peptide combinations on global gene expression were compared to the changes that occur with fractional laser resurfacing treatment, a gold standard approach for skin rejuvenation, to further define optimal peptide combinations.
Methods:
Microarray profiling was used to characterize the biological responses of peptide combinations (+/- Nam) relative to the individual components in epidermal keratinocyte and dermal fibroblast cell lines. Cellular functional assays were utilized to confirm the synergistic effects of peptide combinations. Bioinformatics approaches were used to link the synergistic effects of peptide combinations on gene expression to the transcriptomics of the skin rejuvenation response from fractional laser treatment.
Results:
Microarray analysis of skin cells treated with peptide combinations revealed synergistic changes in gene expression compared to individual peptide controls. Bioinformatic analysis of synergy genes in keratinocytes revealed activation of NRF2-mediated oxidative stress responses by a combination of Ac-PPYL, Pal-KTTKS, and Nam. Additional analysis revealed direct downstream transcriptional targets of NRF2/ARE exhibiting synergistic regulation by this combination of materials, which was corroborated by a cellular reporter assay. NRF2-mediated oxidative stress response pathways were also found to be activated in the transcriptomics of the early skin rejuvenation response to fractional laser treatment, suggesting the importance of this biology in the early stages of tissue repair. Additionally, a second combination of peptides (pal-KT and Ac-PPYL) was found to synergistically restore cellular ATP levels that had been depleted due to the presence of ROS, indicating an additional mechanism whereby peptide synergies may accelerate skin repair.
Conclusion:
Through combinatorial synergy studies, we have identified additional in vitro skin repair mechanisms beyond the previously described functions of individual peptides and correlated these to the transcriptomics of the skin rejuvenation response of fractional laser treatment. These findings suggest that specific peptides can act together, via complementary and synergistic mechanisms, to holistically enhance the regenerative capacity of in vitro skin cells.
... It has been previously shown that peptide fragments result from damage to the ECM and thus are a "sensing" medium of extracellular matrix damage (17,54). Cosmetically, peptides have been utilized in skin repair regimens to exploit this sensing mechanism of repair (55). However, the synergistic potential of peptides with diverse repair functions across the epidermis and dermis is not well understood. ...
OBJECTIVE: To explore synergistic effects related to skin regeneration, peptides with distinct biological mechanisms of action were evaluated in combination in different skin cell lines in the presence or absence of niacinamide (Nam). Furthermore, the synergistic responses of peptide combinations on global gene expression were compared to the changes that occur with fractional laser resurfacing treatment, a gold standard approach for skin rejuvenation, to further define optimal peptide combinations.
METHODS: Microarray profiling was used to characterize the biological responses of peptide combinations (+/- Nam) relative to the individual components in epidermal keratinocyte and dermal fibroblast cell lines. Cellular functional assays were utilized to confirm the synergistic effects of peptide combinations. Bioinformatics approaches were used to link the synergistic effects of peptide combinations on gene expression to the transcriptomics of the skin rejuvenation response from fractional laser treatment.
RESULTS: Microarray analysis of skin cells treated with peptide combinations revealed synergistic changes in gene expression compared to individual peptide controls. Bioinformatic analysis of synergy genes in keratinocytes revealed activation of NRF2-mediated oxidative stress responses by a combination of Ac-PPYL, Pal-KTTKS, and Nam. Additional analysis revealed direct downstream transcriptional targets of NRF2/ARE exhibiting synergistic regulation by this combination of materials, which was corroborated by a cellular reporter assay. NRF2-mediated oxidative stress response pathways were also found to be activated in the transcriptomics of the early skin rejuvenation response to fractional laser treatment, suggesting the importance of this biology in the early stages of tissue repair. Additionally, a second combination of peptides (pal-KT and Ac-PPYL) was found to synergistically restore cellular ATP levels that had been depleted due to the presence of ROS, indicating an additional mechanism whereby peptide synergies may accelerate skin repair.
CONCLUSION: Through combinatorial synergy studies, we have identified additional in vitro skin repair mechanisms beyond the previously described functions of individual peptides and correlated these to the transcriptomics of the skin rejuvenation response of fractional laser treatment. These findings suggest that specific peptides can act together, via complementary and synergistic mechanisms, to holistically enhance the regenerative capacity of in vitro skin cells.
... The literature describes two major KTTKS derivatives which display enhanced delivery across the skin: palmitoyl-KTTKS and ascorbyl conjugated KTTKS. [4,5] Carrier peptides are involved in copper or manganese transport into skin cells. The most important and wellexamined peptide of this class is Cu-GHK complex. ...
Front Cover. Creams and other cosmetics are often applied to reduce the visible ageing effects, such as facial wrinkles. Argireline, an acetyl hexapeptide Ac‐Glu‐Glu‐Met‐Gln‐Arg‐Arg‐NH2, sometimes described as ‘needle‐free Botox' is often added to higher‐end anti‐wrinkle cosmetic products. However, detection and quantification of argireline content in commercially available cosmetics is complicated due to the low concentration and very complex matrix. The application of such sensitive method as LC‐MS may not be enough to detect argireline in some products, moreover, the experiments revealed that the methionine residue is often oxidized, which may affect its biological properties in unexpected and as of yet uninvestigated ways, as reported by Kluczyk et al. in their full paper at 10.1002/cbdv.202000992.
... For example, a synthetic hexapeptide marketed under the name Argireline acts similarly to botulinum neurotoxins to reduce wrinkles 223 . Palmitoyl pentapeptide 4 (Matrixyl), launched in 2000, is a fragment of procollagen I and is thought to reduce wrinkles by stimulating extracellular matrix renewal in fibroblasts 224 ; the palmitoyl chain improves delivery across skin. Copper peptide GHK-Cu is a naturally occurring tripeptide with high affinity for copper ions that has anti-inflammatory properties and stimulates collagen and glycosaminoglycan synthesis in skin fibroblasts 225 . ...
Since the introduction of insulin almost a century ago, more than 80 peptide drugs have reached the market for a wide range of diseases, including diabetes, cancer, osteoporosis, multiple sclerosis, HIV infection and chronic pain. In this Perspective, we summarize key trends in peptide drug discovery and development, covering the early efforts focused on human hormones, elegant medicinal chemistry and rational design strategies, peptide drugs derived from nature, and major breakthroughs in molecular biology and peptide chemistry that continue to advance the field. We emphasize lessons from earlier approaches that are still relevant today as well as emerging strategies such as integrated venomics and peptide-display libraries that create new avenues for peptide drug discovery. We also discuss the pharmaceutical landscape in which peptide drugs could be particularly valuable and analyse the challenges that need to be addressed for them to reach their full potential.
... Conjugation is a new and popular concept in order to minimize long sequence and enhance the properties of peptide drug candidates [16]. This type of therapeutic agent extensively demonstrates efficacy in wound healing since the fatty acid as a chemical penetration enhancer which improve topical delivery across the epidermis [17,18]. There are some fatty acid conjugated drugs have been approved by U.S. Food and Drug Administration (FDA) for clinical applica-tions such as liraglutide and insulin detemir (myristic acid conjugated to lysine side-chain) [19]. ...
The standard treatment of open wounds via the direct usage of therapeutic agents is not without limitations with respect to healing. Small peptides can create a favorable milieu for accelerating the healing of wounds. This study presents the potential of a novel fatty acid conjugated tetrapeptide (palmitic acid-glycine-aspartic acid-proline-histidine; Palmitoyl-GDPH) in alleviating wound healing. Tetracycline was employed as a standard control drug following its significance in wound healing including biologically active and antimicrobial effects. The peptide in liquid form was applied on to a 4 cm2 full thickness wound surgically induced at the dorsum of Sprague Dawley (SD) rats. The in vivo wound treatment with Palmitoyl-GDPH for eighteen days, histologically demonstrated an almost perfect healing exhibited by increased re-epithelialization, enhanced collagen deposition, and diminished scar formation compared to the controls. In addition, the well-developed epidermal-dermal junction and ultimate stimulation of hair follicle-growth in the Palmitoyl-GDPH treated group indicated the wound to have healed as functionally viable tissues. In general, the much lower hemogram values in the Palmitoyl-GDPH group indicated that the ongoing healing is en route to an earlier recovery. Additionally, the liver, kidney, and pancreas function biomarkers being within normal limits indicated the relatively non-toxic nature of Palmitoyl-GDPH at the used dosage. These results indisputably supported the great potential of this newly synthesized Palmitoyl-GDPH to be used as an effective therapeutic agent for wound healing (this actually means creating a new wound).
... The literature describes two major KTTKS derivatives which display enhanced delivery across the skin: palmitoyl-KTTKS and ascorbyl conjugated KTTKS. [4,5] Carrier peptides are involved in copper or manganese transport into skin cells. The most important and wellexamined peptide of this class is Cu-GHK complex. ...
Argireline‐containing cosmetics attract public interest due to their confirmed reduction of facial wrinkles. Argireline is a peptide that works by inhibiting the release of neurotransmitters in the neuromuscular junction, producing a botox‐like effect. Therefore, it is used as a safe needle‐free alternative to botox treatment. In this work we investigated the presence of Argireline in cosmetic creams and sera by application of reversed phase liquid chromatography and tandem mass spectrometry (RP‐HPLC‐MS and MS/MS). The analysis revealed the presence of argireline and its oxidized form in several different cosmetics. The methionine residue in Argireline sequence was indicated as oxidation point according to neutral loss MS studies. The developed sample preparation strategy minimizes and monitors methionine oxidation, bringing to our attention the question of impact of ingredients on the stability of cosmetic product.
... 24,25 Another class of cosmeceuticals includes bioactive peptides, such as palmitoyl pentapeptide-4, which has been showed in vitro to simulate collagen and clinical studies have shown improvement in signs of aging (e.g., wrinkle and fine line reduction). 26,27 As such, replenishing the dermis and epidermis through HA, antioxidants, and peptides is an intuitive approach to reverse the signs of photoaging and to prevent further deterioration. ...
BACKGROUND: The neck is one of the most common areas affected by the aging process. A novel two product combination system composed of a serum and cream with hyaluronic acid and multiple strong antioxidants were investigated to determine their efficacy and safety in neck rejuvenation. OBJECTIVE: The objective of this prospective, randomized, double-blind, placebo-controlled clinical trial was to assess the efficacy and safety of a novel serum containing fractionated hyaluronic acid, peptides, and antioxidants for photodamage of the neck. METHODS: This was an institutional review board (IRB)-approved, randomized, double blind, placebo-controlled clinical trial involving 31 healthy subjects with moderate-to-severe neck wrinkling corresponding to at least a Grade 2 in wrinkles and score of 4 in elastosis on the Fitzpatrick-Goldman Wrinkle Scale. Twenty subjects were randomized to receive the active cream and serum system, while 11 subjects were randomized to receive the vehicles alone in serum and cream format for a course of two months. RESULTS: Both active and placebo cream and serum showed improvement of wrinkles, laxity, pigmentation, erythema, dryness, and texture of the skin, and high patient satisfaction scores. Histology of one of the active serums and cream samples revealed improvement in the quality of papillary dermal collagen and increase in the number of elastic fibers in the upper dermis after treatment. CONCLUSION: Our prospective, randomized controlled trial showed that the novel serum and cream showed improvement in skin aging on the neck, was well-tolerated by patients, and had a high degree of patient satisfaction.
... 7 Synthetic bioactive peptides-short sequences of amino acids derived from endogenous proteins (matrikines 10 )-have been shown to afford remarkable skincare and repair properties both in vitro and in clinical studies via synthesis and remodeling of the extracellular matrix. 11,12 Topical peptides improve skin tightness, elasticity, and firmness, reduce the appearance of rhytides, and lessen other manifestations of photodamage and hyperpigmentation. 13 Palmitoyllysyl-dioxymethionyl-lysine (palmitoyl tripeptide-38) is one such matrikine-mimetic peptide. ...
Background
Allegations on the benefits of incorporating vitamin C, vitamin E, and combinations thereof in topical skincare formulations are mostly based on in vitro and ex vivo experiments and/or limited protocols of specific stress conditions (pollution, UV exposure, laser irradiation,…).
Objective
To evaluate the instrumentally measurable effects and quantitative consumer perceptions of a protective and reparative serum on a panel of volunteers under normal nonstressed conditions of use, employing FOITS technology and innovative self‐assessment methods.
Method
In an open‐label study women of ≥40 years with visible signs of photoaging applied a serum comprising l‐ascorbic acid USP (15% w/v), tocopheryl acetate USP, and 5 ppm palmitoyl tripeptide‐38 to the face once daily for 56 days. Skin roughness and isotropy changes were evaluated on days 0, 28, and 56, visual instrumental evaluation of skin‐tone parameters was assessed on days 0 and 56. Subjects completed self‐assessment questionnaires every third day of the trial period for radiance, homogeneity, and wrinkle appearance.
Results
Skin‐roughness parameters decreased significantly by 8%‐9% (P < .05) and subjects experienced a significant increase in skin isotropy (P < .05). Photographic analysis revealed significant improvements in skin tone, with a 9% decrease in redness and 8% increase in homogeneity (P < .0001 for both), in excellent agreement with subjects' perception of significant improvements of radiance, complexion, and wrinkles.
Conclusion
The study confirms statistically significant correlation between objectively measured and quantitative subjectively perceived benefits of the bespoke serum containing antioxidants and a matrix‐restoring peptide.
... In vivo studies on 93 women, including placebo subjects, and conducted in a double-blind clinical study, show that an application of that palmitoylated peptide improves reduction of fine lines and wrinkles (Robinson et al., 2005). An advanced study on new analogs of Pentapetide-3 was recently published (Tałałaj et al., 2019). ...
Among the many aspects that contribute to the wellness of each individual, healthy and younger-looking skin play a relevant role, as clearly shown by the important growth of the skin-care products market observed in recent years. In this scenario, the field of cosmeceuticals appears particularly promising, being based on cosmetic products containing active ingredients. Among these, several peptides were proposed for cosmeceutical applications, thanks to their specific interaction with biological targets. In this mini-review, we report some of the most investigated and used peptides for cosmetic formulations, taking into account that cosmeceutical peptides are basically divided into three main categories (i.e., neurotransmitter inhibitors, carriers, and signal peptides). Special attention was payed to the scientific studies supporting the claimed biological activity of these peptides, as a fundamental aspect that should underpin the growth of this field in the framework of a sustainable wellness economy.
... Matrixyl has been structurally characterized and it has been shown to organize into giant fibrillar nanotapes with lengths extending to at least 10-100mm (Castelletto et al., 2010a). Clinical trials on Caucasian female subjects (n = 93, aged 35-55) have demonstrated that in 12 weeks fine line/wrinkles improvements were noticed in the subjects that were topically applying the matrixyl cream compared to the controls (Robinson et al., 2005) ...
Peptide and proteins are involved in a wide range of brain disease but they don't cross the blood brain barrier because of their hydrophilic nature and size. Nanofibrous systems are attracting increasing interest in the field of drug delivery and regenerative medicine. The aim of this work is to investigate the therapeutic applicability of peptide nanofibres as new drug delivery system to the Central Nervous System. Our working hypothesis was to choose a model hydrophilic peptide unable to enter the brain, make a lipophylic derivative from which monodomain nanofibres were constructed, in order to test them as a peptide carrier to the brain. Dalargin, a hexapeptide analogue of Leu-enkephalin, which is unable to cross the blood brain barrier was chosen as a model drug. On direct injection into the brain, Dalargin acts on brain opioid receptors, resulting in analgesia. An amphipatic derivative of dalargin, palmitoyl Dalargin (pDal) was synthesized resulting in a surfactant like peptide able to form high-axial-ratio nanostructures in aqueous environments. The self-assembly of the peptide amphilphile has been assessed experimentally and in silico. Intravenous injection of formulation of nanofibres resulted in analgesic response in mice. Brain peptide delivery was assessed with Raman microscopy as well as by measuring analgesia and peptide nanofibres pharmacokinetic profiles in biological matrices. While Dalargin was not detected in any of the tissue samples, palmitoyl Dalargin was measured in the brain tissue confirming the ability of peptide palmitoyl dalargin nanofibres to deliver the peptide across the blood brain barrier. Furthermore Raman microscopy revealed the presence of palmitoyl dalargin in the brain parenchyma. We conclude that peptide nanofibres offer a unique method for delivering hydrophilic peptides across the blood brain barrier.
... The antiaging property of the facial cream having GHK-Cu was examined by Abdulghani and coworkers by applying it on the skin of female volunteers and the result was much satisfactory (Abdulghani et al. 1998). The peptide named Palmitoyl KTTKS has found to enhance the penetration into skin as compared to placebo and so it is being used widely into the cosmetic industry and is much satisfactory comparator (Osborne et al. 2005;Robinson et al. 2005). The effectivity of the acetyl hexapeptide-3 (Argireline1) is also much famous as the examination of 30 days resulted in 30% decrease in the wrinkle's depth by Argireline1 as compared to decrease by placebo that was found to be only 10% (Blanes-Mira et al. 2002). ...
Today’s consumer perception and expectations of personal care have gone beyond merely cleansing, moisturizing, and makeup products, focusing more on the reduction or elimination of signs of aging. Cosmeceuticals, developed to create a more youthful appearance, commonly contain substances with therapeutic and physiological effects. The development of cosmeceutical products containing peptides, biotic ingredients, and marine-based compounds has become a highly popular strategy to enhance anti-aging effects and better address consumer demands. Peptides are frequently used in anti-aging products due to their effects on enhancing fibroblast proliferation and collagen synthesis, contributing to the skin’s barrier function, and reducing skin pigmentation. Meanwhile, biotic components are extensively evaluated for their potential to improve barrier function by maintaining the balance of the skin microflora. On the other hand, the increasing interest of cosmetic consumers in natural and eco-friendly products, along with the rich biodiversity in the oceans and seas, has made marine-derived substances highly significant for the cosmetic industry. Marine polysaccharides are particularly valuable as biopolymers, offering useful properties for gel formation in cosmetic formulations. This review discusses scientific studies and commercially available products using peptides, biotic and marine-based compounds in cosmetic formulations, their cosmetic and cosmeceutical benefits, and the challenges in the formulation design of these products.
The review on this fast-evolving field of neuro cosmetics, at the intersection of neuroscience and cosmetic science, has interestingly led to innovative skincare treatment approaches. The paper progresses from a basic discovery of neurogenic inflammation made by substance P in 1996 the more recent skin-brain axis of 2015 to its applications. The review focuses on neurotransmitters such as acetylcholine and serotonin, neuropeptides such as substance P and Calcitonin Gene-Related Peptide (CGRP), and the neuroendocrine cells, Merkel, and Langerhans cells, to achieve skin homeostasis, inflammation control, and aging. The article looks at neurocosmetic applications such as anti-aging, skin barrier enhancement, and pigmentation management to active ingredients such as acetyl hexapeptide-8, niacinamide, and cannabidiol. Also reviewed are delivery systems including nanoencapsulation, microneedle technology, and iontophoresis in enhancing bioavailability and penetration of neuroactive compounds. A meta-analysis of clinical trials is shown. One study, which lasted up to 24 w, registered a 27% decrease in wrinkles and an 18% increase in elasticity with the peptide complex; the second one described a 45% decrease in rosacea erythema with Alpha-Melanocyte Stimulating Hormone (α-MSH) and Transient Receptor Potential Vanilloid (TRPV1) antagonists. In this review, emerging areas for future research are AI-driven personalized neurocosmetics, interventions of the gut-brain-skin axis, chronocosmetics, epigenetic modulation, smart nanocarriers, and bioelectronic skin therapies. Safety and regulatory issues that arise are commented on, emphasizing long-term studies and standardized approaches. The review is apt for any researcher or dermatologist looking for a comprehensive overview of how neurocosmetics hold transformative promise in topical peptide formulations.
Lipoic acid is a biocompatible compound with antioxidant activity that is of considerable interest in cosmetic formulations, and the disulfide group in the N‐terminal ring confers redox activity. Here, we study the self‐assembly and aspects of the bioactivity of a lipopeptide (peptide amphiphile) comprising the KTTKS collagen‐stimulating pentapeptide sequence conjugated to an N‐terminal lipoic acid chain, lipoyl‐KTTKS. Using SAXS, SANS and cryo‐TEM, lipoyl‐KTTKS is found to form a population of curly fibrils (wormlike micelles) above a critical aggregation concentration. Upon chemical reduction, the fibrils (and β‐sheet structure) are disrupted because of the breaking of the disulfide bond, which produces dihydrolipoic acid. Lipoyl‐KTTKS also undergoes photo‐degradation in the presence of UV radiation. Through cell assays using fibroblasts, we found that lipoyl‐KTTKS has excellent cytocompatibility across a wide concentration range, stimulates collagen production, and enhances the rate of cell coverage in a simple in vitro scratch assay of ‘wound healing’. Lipoyl‐KTTKS thus has several notable properties that may be useful for the development of cosmetics, cell scaffolds or tissue engineering materials.
The increasing demand for youthful, radiant skin has driven the skincare industry to innovate, particularly through the development of natural cosmeceuticals. This chapter explains the efficacy of these products, focusing on their capacity to reduce skin wrinkles—a primary sign of aging. The authors examine clinical trials and case studies to understand the cellular and molecular mechanisms by which natural ingredients contribute to skin health and their anti-wrinkle effects. Additionally, the authors address challenges related to the stability and compatibility of natural ingredients in formulations, alongside their alignment with consumer preferences and market trends. The chapter concludes by assessing the potential benefits of natural cosmeceuticals in antiaging treatments and identifying key areas for future research. The goal of the presented chapter is to advance skincare science by pragmatically leveraging antiaging research to enhance product development.
Background
Photoaging is a process of the architecture of normal skin damaged by ultraviolet radiation. Topical cosmeceuticals have been used to treat this condition. The authors aimed to understand the mechanism and level of evidence of different commonly used cosmeceuticals used to treat photodamaged skin.
Objective
A range of commonly used topical cosmeceuticals (botanicals, peptides, and hydroquinone) has been used in cosmetic medicine for many years to treat photodamaged skin. This review article compares their efficacy and level of evidence.
Material and methods
This study was a systematic review to evaluate the efficacy of different topical cosmeceuticals. Keywords including “Photoaging,” “Azelaic acid,” “Soy,” “Green Tea,” “Chamomile,” “Ginkgo,” “Tea Tree Oil,” “Resveratrol,” “Cucumber,” “Ginseng,” “Centella asiatica,” “Licorice Root,” “Aloe Vera,” “Peptides,” “Argireline,” “Hydroquinone,” were typed on OVID, PUBMED, MEDLINE for relevant studies published on photoaging treatment.
Results
Most of the evidence behind cosmeceuticals is of high‐quality ranging from Level I to Level II. In particular, the evidence base behind peptides is the strongest with most studies achieving Level Ib status in the evidence hierarchy.
Conclusion
Topical cosmeceuticals like botanicals, peptides and hydroquinone can effectively treat photodamaged skin
Milk is the most necessary food for humans because it provides almost all nutrients such as the most
nutritious protein, calcium, essential fatty acids, water-soluble vitamins, and other bioactive
compounds responsible for maintaining health and other physiological functions. Milk has also been
used effectively in the Unani system of medicine for centuries to improve complexion and to treat
other ailments (especially dermatological disorders). For skin brightening, Unani physicians
mentioned the use of the paste made up of powdered tukhm e kharpazah (seeds of musk melon), aarad
e nakhud (powdered chickpea) each 2 parts, arad e baqla(powdered broad beans), aarad e jau
(powdered barley) each 1 part, adas muqashshar (powdered lentil), nishasta (corn flour), kateera
(tragacanth gum) each half part, tukhm e turb (radish seeds) 1/4th part, za’fran (saffron) a little and
milk at night on the face and advice to wash the face with the decoction of banafsha (sweet violet) and
post kharpaza (musk melon fruit epicarp) in the morning. Milk has several therapeutic actions too e.g.
Musammin e Badan (adipogenous), Muhallil (anti-inflammatory), Mugharri (glutinous- Mugharri drug
is a cold and dry substance with a small amount of viscid moisture that coats the surface and constricts
pores. It moisturizes the skin and makes it appear lighter), Mohsin e laun (fairness activity), Ghassal
(irrigator), Tiryaq (antidote), and Muqawwi (general tonic), etc. There are some scientific reports on
the anti-hyperpigmentation effect of cow milk in which a paste of cow milk and powdered roasted red
lentils was tested to enhance the complexion. They found significantly effective result on the
Fitzpatrick scale, enhanced complexion, and reduced tanning as well as dullness. The main objective of
this article is to present cow milk's nutritional and therapeutic activity.
Topical antiaging therapies provide noninvasive delivery of active therapeutics. Exosomes, or extracellular nanovesicles, and peptides, small strings of amino acids, have shown promise as topical therapies in early trials, but neither is FDA approved. This review aims to elucidate the current and future landscape of topical exosomes and peptides as therapeutics for skin rejuvenation. A literature search was conducted using the keywords “peptides” OR “exosomes” AND “skin” OR “rejuvenation.” Primary endpoints included mechanisms of action in humans or live animals as well as clinical data supporting the use of exosomes or peptides topically for skin rejuvenation or wound healing. Secondary endpoints were safety, side effects, and efficacy. The articles were collected, organized, and sorted using the Covidence software (Melbourne, Australia) for systematic review. Nine articles evaluating topical application of exosomes and 9 of peptides met inclusion criteria. Topical exosomes were found to increase collagen deposition, accelerate wound healing, and improve overall cosmesis. Several clinical trials are currently underway. Topical peptides were found to improve appearance of fine lines and wrinkles, elasticity and viscoelasticity, skin texture, skin thickness, and the potential for accelerated wound healing. Peptides are quite common in “cosmeceutical” products, and several patents have been filed for topical peptide products aimed at increasing skin rejuvenation. This could indicate a movement toward pursuing FDA approval. The future of topical exosome and peptide products for the purpose of skin rejuvenation appears promising. Preliminary data from the studies reviewed here indicates that these products have the potential to be safe and effective.
Level of Evidence: 3
This book delves into the world of natural sources from medicinal plants, microbes, and fungi, to lichen, algae, and clay minerals that have been used for centuries in traditional medicine. These sources are rich in bioactive secondary metabolites that have a wide range of applications in various industries, including cosmetics and personal care products.
This book provides a comprehensive guide to secondary metabolites for cosmeceutical purposes, regulatory perspectives for cosmeceuticals in different countries, and allergic responses from these secondary metabolites. Additionally, this book discusses the impact of nanotechnology on cosmetic products such as skin and hair care.
Bioprospecting of Natural Sources for Cosmeceuticals is a valuable resource for researchers and graduate students in chemistry, botany, biotechnology, microbiology, cosmetic science, and the pharmaceutical sciences. It is also useful for those researching traditional medicine systems and those in the microbiology, biotechnology, pharmaceutical, and nanoscience industries.
The term cosmeceutical refers to a category of skincare products that are purported to have active ingredients whose physiological or pharmacological actions are capable of inducing cosmetic enhancements to the skin. Given a demand for brighter, healthier, younger‐appearing skin, and relatively limited regulatory control, thousands of different cosmeceutical formulations have found their way onto store shelves and onto the skin of hopeful consumers, despite a lack of scientific evidence. This chapter summarizes new and old, common and rare cosmeceutical ingredients; their uses and side effects; and the science, where available, behind the claims.
Background:
Neck skin is thinner and has a more delicate dermal layer than facial skin. The studied product was specifically formulated for the neck combining a hydrating delivery system with a trifunctional corrective technology composed of 0.2% pure retinol, 2.5% tripeptide concentrate, and 5.0% glaucine complex to help improvement in signs of aging.
Objectives:
To evaluate cosmetic and histologic changes 3 months after treatment using immunostains for Type I collagen, Type III collagen, and glycosaminoglycan (GAGS). In addition, overall clinical improvement in photoaged skin was measured by both Griffith's photonumeric photoaging scale, photographic improvement, and questionnaires.
Methods:
This study was an open-label, blinded clinical trial evaluating a combined retinol, tripeptide, and glaucine containing cream in the treatment of photo-aged skin. The study enrolled a total of 20 healthy male or female subjects, who applied the product for 3 months to their face and neck.
Results:
Clinical as well histologic changes were consistent with improvement in all 20 subjects.
Conclusion:
Use of a combined retinol, tripeptide, and glaucine containing cream led to both clinical and histologic improvement of phototoaging.
Background:
Crow's feet is one of the signs of skin aging. Many studies regarding skin aging have been carried out in Caucasians, as for Asians, there are different genotypes and phenotypes. Some anti-aging treatments carry a slightly higher risk of side effects and irritation in Asian skin. Currently, the use of topical active peptides for anti-aging, Acetylhexapeptide-3 (AHP-3) and Palmitoyl pentapeptide-4 (PPP-4), has been widely developed. This study aimed to investigate the anti-aging effects of AHP-3 and PPP-4 on the Asian patient with crow's feet.
Methods:
This study was a double-blind randomized trial using 21 Indonesian female subjects aged 26 to 55 years for eight weeks and divided into three groups: AHP-3 cream, PPP-4 cream, and placebo. The cream was applied twice daily to the periorbital area. The three groups were assessed using Corneometer, Tewameter, Cutometer, digital photography and Crow's Feet Grading Scale.
Results:
Based on clinical photos and data, improvements were found in several subjects using AHP-3 and PPP-4. PPP-4 appeared to demonstrate better results when compared to AHP-3 based on data, clinical photos, and self-assessment questionnaire.
Conclusion:
PPP-4 demonstrated better results when compared to AHP-3 and placebo. This initial study provides an opportunity for further study with a more adequate number of samples and duration.
The inherent natural human instinct to appear at their best self has always been the driving force which makes us reach out to cosmetics that can enhance our appearance. And with the never-ending quest of the researchers, another category of products called nanocosmeceuticals, superior to cosmetics, has made its appearance that claims to exert certain therapeutical benefits in addition to their beautification purpose. In this chapter, various nanobased vehicles that are explored for cosmeceutical purposes are briefly canvased and the main emphasis has been given to the dermatopharmacokinetics of the nanocosmeceuticals, which is the most significant parameter to assess their efficacy. The possible mechanism of action by which this spectrum of products exerts their action has also been covered.
Wound healing is one of the most complex biological processes. Studies show that Matrixyl (MTI), known as a cosmetic peptide, can lead to a faster healing process. The contribution of MTI to collagen formation during wound healing also depends on its mode of delivery and its release over time. Here, we investigate two modes of MTI-delivery system, the influence of MTI patch for wound healing application in comparison with MTI cream. In this study, animals were randomly divided into seven groups and studied for 21 days: patches containing two different concentrations a negative control (sham) group. To study the wound healing process, the change in collagen density, angiogenesis, epitheliogenesis, histopathology, immunohistochemical analysis, and wound area through imaging was monitored and measured. The macroscopic results showed that wound healing was improved from 63.5 up to 81.81% in treatment groups compared to that in the negative control group (P < 0.05 and P < 0.001). In addition, C-MTI-1 and P-MTI-1 had a larger impact on wound healing compared to that in the positive control group (Comfeel, P < 0.05). In hematoxylin and eosin (H&E) staining analysis, the rejuvenation of skin appendage was visible in both groups of cream and patches with MTI. According to the obtained results, the re-epithelialization had a higher range for the patch with MTI in comparison with cream containing MTI and positive control.
Extracellular matrix (ECM) proteins confer biomechanical properties, maintain cell phenotype and mediate tissue repair (via release of sequestered cytokines and proteases). In contrast to intracellular proteomes, where proteins are monitored and replaced over short time periods, many ECM proteins function for years (decades in humans) without replacement. The longevity of abundant ECM proteins, such as collagen I and elastin, leaves them vulnerable to damage accumulation and their host organs prone to chronic, age-related diseases. However, ECM protein fragmentation can potentially produce peptide cytokines (matrikines) which may exacerbate and/or ameliorate age- and disease-related ECM remodelling. In this review, we discuss ECM composition, function and degradation and highlight examples of endogenous matrikines. We then critically and comprehensively analyse published studies of matrix-derived peptides used as topical skin treatments, before considering the potential for improvements in the discovery and delivery of novel matrix-derived peptides to skin and internal organs. From this, we concluded that while the translational impact of matrix-derived peptide therapeutics is evident, the mechanisms of action of these peptides are poorly defined. Further, well-designed, multimodal studies are required.
Peptides are biologically active communication tools that direct skin functioning. Peptides, proteins, and amino acids are often mislabeled and the terms applied as if they were interchangeable, yet they are different in their characteristics, uses, biological activities, and cosmetic potential. Peptides perform many important biologic signal functions. The incorporation of peptides into various galenic forms of skin care products can be challenging. The term matrikines is used to describe naturally occurring fragments of matrix macromolecules endowed with stimulatory, tissue repair activity. Concepts derived from wound healing research are but one approach to peptide‐based anti‐aging treatments. Neurotensin, vasointestinal peptide, neuropeptide Y, substance P, and calcitonin gene‐related peptide, although endowed with potent biological activity, are not candidates for cosmetic applications because of their size and irritation potential. Structural proteins are building blocks for the organs and tissues of the human body. Superoxide dismutase, an antioxidant enzyme, is present at the surface of the skin.
Vitamins are commonly used in topical skincare products designed to prevent skin aging and improve aged skin appearance, resilience, and health. Vitamins are organic compounds required for maintaining human health and are primarily obtained from the diet. Several forms of the oil‐soluble vitamin A are used cosmetically, the most widely utilized ones being retinol, retinyl esters, and retinaldehyde. There are three primary forms of the water‐soluble vitamin B 3 that have found utility in skin care products: niacinamide, nicotinic acid, and nicotinate esters. The niacinamide‐treated skin is then more resistant to environmental damage, as determined by exposure of the skin to the surfactant sodium lauryl sulfate and assessment of the resulting transepidermal water loss. Topical panthenol is extremely well tolerated by the skin, leading to wide topical use of the material and many reported skin effects. Vitamin C is well known as an antioxidant and has been utilized as a skin lightener.
With the emergence of social aging problem, people's demand for active ingredients for skin health protection and therapeutic efficacy increases. Bioactive peptides are the optimal substances for skin anti-aging with its great diversity of biological activities and high security, such as antioxidation, anti-aging, anti-diabetes, anti-hypertension, and antibacterial. In recent years, natural and synthetic anti-aging peptides have been extensively studied in vitro, in vivo and clinically. Anti-aging peptides, such as collagen peptides, can affect various physiological pathways of skin, and have significant skin protection effect when applied locally and eaten. These characteristics show that bioactive peptides can improve skin health by providing specific physiological functions. In this review, we summarized the research of anti-aging peptides and the finishing of anti-aging peptides on improving skin health which is mainly based on the collagen peptides and the related synthetic peptides.
Recently, several peptides are used as active ingredients in topical cosmetic formulations, few information are available on their dermal stability against proteases. In this study, it was developed a simple and reliable assay to evaluate the stability of cosmeceutical peptides in skin homogenates. The quantification of studied peptides was performed by liquid chromatography coupled with a triple quadrupole mass spectrometer operating in tandem mass spectrometry mode (LC–MS/MS) and the conditions were tuned through energy resolved MS/MS (ERMS) experiments. The sample preparation procedure was carried out on rat skin homogenates by employing pal-KTTKS (reference peptide and the parameters that may affect the assay results were evaluated, including substrate concentration, dilution of skin homogenate, protein concentration and batch-to-batch variation of the homogenate. The optimized conditions were applied to check the degradation profile of pal-KTTKS in human skin samples and the obtained results were compared. Finally, the degradation profiles of SA1-III and pamSA1-III, recently described as cosmeceutical peptides, in human skin homogenate were evaluated. The results showed that proposed peptides are stable toward proteases for up to 8 h of incubation. Thanks to this characteristic, these peptides can be considered very interesting candidates as active ingredients for creams intended for a daily application.
This review presents the current scientific literature data about structure, properties, and functions of collagen, which is known as one of the most abundant human and animal proteins. The building of collagen molecule from the primary structure to submolecular formations, the main stages of its synthesis and biodegradation are briefly described. The information about collagen diversity, its features and metabolic ways in various tissues, including skin, tendons, bones, etc. is presented. The problems of pathologies caused by collagen synthesis and breakdown disorders as well as age-related changes in collagen properties and their causes are discussed. A comparative analysis of the advantages and disadvantages of collagen and its derivatives obtaining from various sources (animals, marine, and recombinant) is given. The most productive methods for collagen extraction from various tissues are shown. The concept of collagen hydrolysis conditions influence on the physicochemical properties and biological activity of the obtained products is described. The applications of collagen and its products in various fields of industrial activity, such as pharmaceutical, cosmetic industry and medicine, are discussed. Further prospective directions of fundamental and applied investigations in this area of research are outlined.
The development of synthetic peptides for skin care dates to the 1980s. The cosmetic industry periodically launches new peptides, as they are promising and appealing active ingredients in the growing and innovative cosmetics market. In this study, trends in the use of peptides in anti-aging products were analyzed by comparing the composition of the products marketed in 2011 with products launched or reformulated in 2018. The scientific and marketing evidence for their application as active ingredients in anti-aging cosmetics was also compiled from products’ labels, suppliers’ technical data forms and online scientific databases. The use of peptides in anti-aging cosmetics increased by 7.2%, while the variety and the number of peptide combinations in products have increased by 88.5%. The most used peptides in antiaging cosmetic formulations are, in descending order, Palmitoyl Tetrapeptide-7, Palmitoyl Oligopeptide and Acetyl Hexapeptide-8. In 2011, the majority of peptides were obtained from synthesis, while in 2018, biotechnology processing was the dominant source. This study provides an overview of the market trends regarding the use of peptides in anti-aging products, providing meaningful data for scientists involved in the development of new peptides to identify opportunities for innovation in this area.
This chapter focuses on the microscopical examination of hair in the forensic domain. It discusses the relevant biological aspects of hair to provide the necessary background information upon which forensic hair examinations are based. The chapter introduces the methodologies and techniques used by forensic hair examiners. It describes the basic chemistry and basic histology of hairs. Each individual hair progresses through a regular and predictable cycle. This cycle is classically described as having three major phases: anagen, catagen, and telogen. While a variety of methods can be used, forceps and tape lifts are the two most commonly employed techniques for collecting hairs. Most forensic hair cases involve the examination of human hair. Historically, the emphasis has been placed on human hair comparisons. The chapter provides general guidelines for the comparison of hairs. Finally, the interpretation and significance of the results obtained through a microscopical hair examination are considered.
The hair cuticle provides significant protection from external sources, as well as giving rise to many of its bulk properties, e.g., friction, shine, etc. that are important in many industries. In this work, atomic force microscopy-infrared spectroscopy (AFM-IR) has been used to investigate the nanometer-scale topography and chemical structure of human hair cuticles in two spectral regions. AFM-IR combines atomic force microscopy with a tunable infrared laser and circumvents the diffraction limit that has impaired traditional infrared spectroscopy, facilitating surface-selective spectroscopy at ultra-spatial resolution. This high resolution was exploited to probe the protein secondary structures and lipid content, as well as specific amino acid residues, e.g., cystine, within individual cuticle cells. Characterization across the top of individual cells showed large inhomogeneity in protein and lipid contributions that suggested significant changes to physical properties on approaching the hair edge. Additionally, the exposed layered sub-structure of individual cuticle cells allowed their chemical compositions to be assessed. The variation of protein, lipid, and cystine composition in the observed layers, as well as the measured dimensions of each, correspond closely to that of the epicuticle, A-layer, exocuticle, and endocuticle layers of the cuticle cell sub-structure, confirming previous findings, and demonstrate the potential of AFM-IR for nanoscale chemical characterization within biological substrates.
The NH2 and COOH propieces of fibril-forming collagens are cleaved off extracellularly and have been implicated in feedback regulation of their own synthesis. Recently, we showed that a subfragment of the carboxyl-terminal propeptide of type I collagen (residues 197-241) dramatically augments extracellular matrix production in subconfluent fibroblasts. This stimulation of type I collagen, type III collagen, and fibronectin production occurred in a dose- and time-dependent manner with no effect on total protein synthesis or on the ratio of secreted proteins to cell-associated proteins (Katayama, K., Seyer, J.M., Raghow, R., and Kang, A.H. (1991) Biochemistry 30, 7097-7104). In the present report, we have extensively dissected this subfragment of the propeptide and found that the pentapeptide Lys-Thr-Thr-Lys-Ser (residues 212-216) is the minimum sequence necessary for potent stimulation of collagen and fibronectin production in a variety of mesenchymal cells. We postulate that the extracellular matrix production in fibroblasts may be subject to either positive or negative feedback regulation depending on the repertoire of specific proteases during postinflammatory tissue regeneration and fibrosis.
Deep phenol peels were done on 11 middle-aged white women with severe actinic damage. Subsequently, face lifts were carried out after periods of 1.5 to 20 years. This made it possible to obtain a full-thickness specimen extending several centimeters on either side of the border between peeled and unpeeled skin. In contrast to the markedly abnormal elastotic appearance of unpeeled skin, a new band of connective tissue 2 to 3 mm in width was laid down in the subepidermal region. Fine elastic fibers formed a dense network in the band of regenerated collagen. The disarray and cytologic abnormalities of sun-damaged epidermis were also largely corrected. Melanocytes were not eliminated, but melanin synthesis was evidently impaired, accounting for the bleaching effects. The effects of a phenol peel are very long lasting and adequately account for the effacement of wrinkles and obliteration of actinic keratoses, mottling, and freckling.
We investigated the clinical, histologic, and molecular responses of normal human skin to all-trans-retinol (ROL) application, compared to those induced by topical all-trans-retinoic acid (RA), and measured ROL-derived metabolites. Up to 1.6% ROL, 0.025% RA in vehicle (70% ethanol/30% propylene glycol), or vehicle alone were applied in a double-blind fashion to normal buttock skin and occluded for 4 d. ROL produced from none to only trace erythema, which was clinically and statistically insignificant, whereas RA induced a significant 3.7-fold increase in erythema score compared to vehicle (n = 10, p < 0.01). However, ROL induced significant epidermal thickening (1.5-fold at 1.6% ROL, p < 0.01), similar to RA (1.6-fold at 0.025% RA, p < 0.01), relative to the vehicle. ROL, compared with vehicle, also increased mRNA levels of cellular retinoic acid binding protein (CRABP-II) and cellular retinol binding protein (CRBP) genes as determined by Northern analysis (5- 6-fold and 6-7-fold, respectively) and riboprobe in situ hybridization. CRABP-II and CRBP protein levels were also higher following ROL than vehicle treatment, as measured by ligand binding (3.2-fold, p < 0.001; n = 7) and Western analysis (3.6-fold, p < 0.003; n = 6), respectively. Epidermal retinyl ester (RE) content, measured after removal of stratum corneum, rose 240-fold (p < 0.005, n = 5) by 24 h of ROL occlusion. RA content, however, was undetectable or detectable only at trace amounts in all samples obtained at 0, 6, 24, and 96 h after ROL occlusion. Detectability of RA was not correlated with ROL treatment (compared to untreated normal skin, p = 0.86) or baseline skin ROL levels (average r = -0.1, p> 0.3).
Palmitoyl derivatives of interferon alpha2b (p-IFNalpha) were prepared by covalent attachment of the fatty acid to lysine residues in the protein through a reaction with N-hydroxysuccinimide palmitate ester. The p-IFNalpha was characterized by capillary electrophoresis (CE), mass spectrometry (MS), SDS-PAGE, and antiviral assay. Flow-through diffusion cells and human breast skins were used to measure cutaneous and percutaneous absorption. Formation of p-IFNalpha derivatives was demonstrated by CE to be dependent on reaction time and reagent: protein ratio. Electrospray MS of the crude p-IFNalpha mixture indicated three populations of IFNalpha derivatives with 10, 11, and 12 palmitoyl substitutions. The addition of palmitoyl residues to IFNalpha under the conditions described reduced the antiviral specific activity by 50%. However, the cutaneous absorption of p-IFNalpha was about 5-6 times greater than the parent protein. The amount of p-IFNalpha and IFN alpha in whole skin after 24 h of treatment was 2.106 +/- 1.216 microg/cm2 and 0.407 +/- 0.108 microg/cm2, respectively. Approximately two times higher flux was detected for p-IFNalpha compared to the nonfatty acylated IFNalpha. The total amount of drug diffused in 24 h was also approximately two times higher for the p-IFNalpha. The results indicate a potential for using fatty acylated derivatives of IFN alpha for dermal and transdermal delivery.
Cutaneous hyperpigmentation occurs in multiple conditions. In addition, many Asian women desire a lighter skin colour. Thus, there is a need for the development of skin lightening agents. Niacinamide is a possible candidate.
To investigate the effects of niacinamide on melanogenesis in vitro and on facial hyperpigmentation and skin colour in vivo in Japanese women.
Melanin production was measured in a purified mushroom tyrosinase assay, cultured melanocytes, a keratinocyte/melanocyte coculture model, and a pigmented reconstructed epidermis (PREP) model. The clinical trials included 18 subjects with hyperpigmentation who used 5% niacinamide moisturizer and vehicle moisturizer in a paired design, and 120 subjects with facial tanning who were assigned to two of three treatments: vehicle, sunscreen and 2% niacinamide + sunscreen. Changes in facial hyperpigmentation and skin colour were objectively quantified by computer analysis and visual grading of high-resolution digital images of the face.
Niacinamide had no effect on the catalytic activity of mushroom tyrosinase or on melanogenesis in cultured melanocytes. However, niacinamide gave 35-68% inhibition of melanosome transfer in the coculture model and reduced cutaneous pigmentation in the PREP model. In the clinical studies, niacinamide significantly decreased hyperpigmentation and increased skin lightness compared with vehicle alone after 4 weeks of use.
The data suggest niacinamide is an effective skin lightening compound that works by inhibiting melanosome transfer from melanocytes to keratinocytes.
Synopsis
Previous clinical testing of topical niacinamide (vitamin B3) has revealed a broad array of improvements in the appearance of aging facial skin. The study reported here was done to confirm some of those previous observations and to evaluate additional end points such as skin anti‐yellowing. Caucasian female subjects ( n = 50, aged 40–60 years) participated in a 12‐week, double‐blind, placebo‐controlled, split‐face, left–right randomized clinical study assessing two topical products: moisturizer control product versus the same moisturizer product containing 5% niacinamide. Niacinamide was well tolerated by the skin and provided significant improvements versus control in end points evaluated previously: fine lines/wrinkles, hyperpigmentation spots, texture, and red blotchiness. In addition, skin yellowing (sallowness) versus control was significantly improved. The mechanism by which this array of benefits is achieved with niacinamide is discussed.
Pentapeptide facilitates matrix regeneration of photo-aged skin
- K Lintner
- C Chamberlin
- P Mondon
Lintner, K., Mas-Chamberlin, C. and Mondon, P. Pentapeptide facilitates matrix regeneration of photo-aged skin. Ann. Dermatol. Venereol. 129, 1S401 (2002).
Relevance of antiwrinkle treatment of a peptide: 4 months clinical double blind study vs excipient
- C Mas-Chamberlin
- K Lintner
- L Basset
- H Adhoute
- J And Revuz
Mas-Chamberlin, C., Lintner, K., Basset, L., Adhoute, H. and Revuz, J. Relevance of antiwrinkle treatment of a peptide: 4 months clinical double blind study vs excipient. Ann. Dermatol. Venereol. 129, 1S456 (2002).
Pentapeptide facilitates matrix regeneration of photoaged skin
- Lintner K.