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Fairness via formulations: A review of cosmetic skin-lightening ingredients

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Abstract and Figures

Skin-lightening cosmetics are in big demand across Asia, and the quest for fairness has led to identification of many new ingredients. The mechanisms underlying pigmentation have been researched extensively and the knowledge is being updated regularly. This review serves to list the ingredients that are commercially available for that purpose and the modes of action through which the lightening is effected. Skin-lightening ingredients are also classified based on their sources; it is significant that far more botanicals have made the list than have synthesized compounds. Tyrosinase inhibition as a means of skin lightening is still the most reported method, followed by other methods such as Mitf inhibition, down regulation of MC1R activity, interference with melanosomal transfer, and melanocyte loss.
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J. Cosmet. Sci., 63, 43–54 ( January/February 2012)
Fairness via formulations: A review of cosmetic
skin-lightening ingredients
R. KAMAKSHI, Cavinkare Research Centre,
Ekkatuthangal, Chennai 600 032, India.
Accepted for publication August 31, 2011.
Skin-lightening cosmetics are in big demand across Asia, and the quest for fairness has led to identifi cation
of many new ingredients. The mechanisms underlying pigmentation have been researched extensively and
the knowledge is being updated regularly. This review serves to list the ingredients that are commercially
available for that purpose and the modes of action through which the lightening is effected. Skin-lightening
ingredients are also classifi ed based on their sources; it is signifi cant that far more botanicals have made the
list than have synthesized compounds. Tyrosinase inhibition as a means of skin lightening is still the most
reported method, followed by other methods such as Mitf inhibition, down regulation of MC1R activity,
interference with melanosomal transfer, and melanocyte loss.
The defi nition of fair skin is given as “not dark and free from spots, specks, dirt or imper-
fection; unblemished; clean; pure.” The booming cosmetics industry in recent decades can
be partly attributed to the elusive search for fair and fl awless skin (1,2). With the vast
information that is accessible in the 21st century, one has an option to choose methods
ranging from that of Cleopatra (soaking in donkey milk that is rich in AHA) to recent
advances in skin-lightening procedures such as dermabrasion, ultrasound, and laser ther-
apies, to name a few (3–9).
Skin-lightening agents are any ingredient or combination of ingredients that interfere
in any step of the melanogenesis pathway, melanin transfer, or desquamation that results in
lowering pigmentation on the surface of the skin (10). Skin-lightening cosmetics are in
big demand across the world, and this review serves to list the ingredients that are com-
mercially available for that purpose and the modes of action through which the lighten-
ing is effected. There are many reports of skin-lightening agents obtained from both
natural and synthetic sources. However, many ingredients in their original form may not
be compatible in cosmetic formulations for application to the skin due to various factors
such as cytotoxicity, insolubility, instability, and their sensitive nature to external condi-
tions. However, consistent efforts are being made by industry to arrive at compatible,
minimally toxic, and highly effi cacious ingredients that serve the purpose.
The color of our skin is due to the polymeric, amorphous, non-proteinaceous pigment
called melanin. Melanin is produced in the skin through a biochemical process called
melanogenesis. Dermal melanin is produced by melanocytes, which are found in the stra-
tum basale of the epidermis. The pathway of melanogenesis as elucidated by Raper (18)
and Mason (19) is shown below (Figure 1).
The difference in skin color between fair people and dark people is due not to the number
(quantity) of melanocytes in their skin, but to the melanocytes’ level of activity (quantity
and relative amounts of eumelanin and pheomelanin). In skin that exhibits a dark color
the melanosomes are well distributed in the keratinocytes, which absorb radiation (11).
Pigmentation in skin is determined by various physiological processes occurring at
different stages (12):
(a) Development of melanocytes
(b) Density of melanocytes
(c) Expression of the enzymatic and structural constituents of melanosomes
(d) Synthesis of melanin
(e) Transport of melanosomes to dendrites
(f) Transfer of melanosomes to keratinocytes
(g) Distribution of melanin in the supra basal layers of the skin
Figure 1. Raper-Mason pathway of melanogenesis.
The fi rst three stages are completely controlled genetically, while the next four stages
are targets for manipulation through skin-lightening agents. The most important
factor other than inheritance affecting skin pigmentation is ultraviolet (UV) radiation
(Figure 2). Exposure to UV triggers the following reactions that cause darkening of the
skin (13–15):
(a) Oxidation and polymerization of melanin
(b) Redistribution of melanosomes
(c) Activation of MITF (microphthalmia-associated transcription factor) leading to
increased melanin content
(d) Increase in expression of α-MSH (melanocyte-stimulating harmone) leading to
enhanced melanocyte responses
(e) Transfer of melanin from the lower to the upper epidermis to prevent damage from
A very effective method of reducing UV-induced pigmentation would be to incorporate
sunscreens in the vehicle used for skin lightening. Physical sunscreens like zinc oxide and
titanium oxide are available to suit delivery vehicles like creams, lotions, gels, etc. Chem-
ical sunscreens may be chosen from a variety of synthetic compounds such as ethyl hexyl
methoxy cinnamate, butyl methoxydibenzoylmethane, phenyl benzimidazole sulfonic
acid, and other substituted salicylates.
Skin-lightening agents are those that cause depigmenting activity on human skin, and
they have been widely used in dermatology and cosmetics. A huge number of actives
(both from biological sources and synthetic chemical compounds) have been reported in
the literature (16,17). Their mechanism of action is generally through:
(a) Tyrosinase inhibition
(b) Mitf inhibition
(c) Down regulation of MC1R activity
Figure 2. Schematic representation of the effect of UV rays on skin leading to pigmentation.
(d) Interference with melanosome maturation and transfer
(e) Melanocyte loss, exfoliation
Successful treatments mostly combine two or more modes of action to achieve a synergis-
tic effect.
Skin-lightening ingredients can also be classifi ed by their source, such as the classes to
which they belong. The important classes are:
(i) Chemical tyrosinase inhibitors (hydroquinone and similar type of compounds)
(ii) Botanicals (essentially from plants and algae)
(iii) Anti-oxidants
(iv) Vitamins—A, B, C, E
(v) Peptides
(vi) Alpha and beta hydroxyl acids and derivatives
The inhibition of tyrosinase is the most widely reported screening method in the litera-
ture for skin-lightening ingredients. Tyrosinase is a copper-containing enzyme present in
melanocytes that catalyzes the production of melanin. The biosynthetic pathway of mela-
nin synthesis was fi rst elucidated by Raper (18). Tyrosinase inhibition may be achieved by
inhibitors from chemical or biological sources.
(i) Chemical tyrosinase inhibitors (Figure 3). There has been tremendous activity in the iden-
tifi cation of tyrosinase inhibitors that are of synthetic origin. Such compounds are gener-
ally highly pure and potent. Synthetic compounds of various classes like hydroquinone
and derivatives, phenolic amines, coumarins, chalcone analogs, hydroxy stilbene deriva-
tives, benzaldehyde analogs, biphenyls, and trihydroxy fl avones have been studied for
their tyrosinase inhibitory properties (21–33).
However, many of these compounds have been screened through in vitro assays and their
effi cacy and adverse effects need to be established through clinical trials. Chemical com-
pounds with depigmenting activity have been used in cosmetics for a long time. Some of
the best known tyrosinase inhibitors are hydroquinone, kojic acid, and similar types of
(a) HYDROQUINONE AND DERIVATIVES. Hydroquinone is considered to be the gold standard for
depigmenting agents. Hydroquinone interacts with copper at the active site of the en-
zyme tyrosinase, thus decreasing its activity by nearly 90% (34). It not only limits ty-
rosinase but also oxidizes membrane lipids and proteins through generation of reactive
oxygen species (35). The radicals generated inhibit cellular metabolism by affecting
DNA and RNA synthesis (36). It is generally administered at concentrations ranging from
1.5% to 5% concentration. The use of hydroquinone in cosmetics has diminished because
of adverse side effects due to its cytotoxic nature. Monobenzyl ether of hydroquinone
(MBEH) and monomethyl ether of hydoquinone (MMEH) also demonstrate tyrosinase
inhibitory properties (37–39). Further, they also cause melanocyte loss through genera-
tion of free radicals. However, the use of these compounds for depigmentation is limited
by their adverse effects, similar to those of hydroquinone.
(b) ARBUTIN. Arbutin is a naturally occurring β,D-glycopyranoside derivative of hydro-
quinone. Although it shows tyrosinase inhibition, it is not found to affect RNA synthe-
sis as does hydroquinone. The α-derivative shows a stronger inhibitory effect on tyrosinase
and melanosome maturation (40,41). It is also present in many of the botanical extracts.
Arbutin is highly pH-sensitive and can hydrolyze to hydroquinone at both acidic and
alkaline pH. Hence, care should be taken during use in commercial skin-lightening
(c) KOJIC ACID. Kojic acid is a powerful tyrosinase inhibitor. It functions by the chelation of
copper at the active site of the enzyme tyrosinase (42). Further, it acts as an antioxidant
and a free radical scavenger. Although powerful, the use of kojic acid is under scrutiny by
dermatologists because of its adverse side effects such as allergic dermatitis (43). It
is found to be unstable in formulations and may also cause discoloration. Some stable
derivatives, such as kojic acid dipalmitate, are being used to enhance effectiveness by
enhanced skin penetration. Thus there exists a demand for safe and effective alternative
botanicals as preferred skin-lightening ingredients.
Figure 3. Structures of some skin-lightening agents.
(ii) Botanical extracts. Extracts mostly contain a combination of two or more classes of com-
pounds that work synergistically to achieve skin lightening. Botanicals connote nature and
are hence more acceptable to people. Further, a large number of yet undiscovered plants are
available to provide for exotic products and claims for cosmetics. However, it should also be
observed that natural extracts may be highly unstable and may not be compatible within
formulations. A large number of ingredients (Table I) have been studied for tyrosinase inhi-
bition and have been processed to make them viable for use in cosmetic products. These are
available commercially through suppliers for use as skin-lightening agents.
(iii) Antioxidants as skin-lightening agents. Antioxidants serve to reduce oxidation of tyrosine
to DOPA quinone and therefore are shown to have skin-lightening activity (64).
In addition, they act in the melanogenesis pathway, reducing the synthesis of melanin.
Exposure to UV radiation results in the generation of free radicals. It has been identifi ed
that ROS (reactive oxygen species) are able to oxidize tyrosinase and DOPA to melanin,
and this is one of the major causes for tanning (65). Although antioxidants are present in
tissues, they may not be able to reduce the radicals, depending on the extent of UV expo-
sure. Infl ammation is a source of free radicals. Hence the quenching of free radicals would
also help in reducing the synthesis of melanin, thereby contributing to skin depigmenta-
tion effects (66). The use of phytic acid, glutathione (Figure 4), and ubiquinone as popu-
lar skin-lightening agents is due to their strong antioxidant nature (67–68). Melanin
synthesis in melanocytes is accompanied by the generation of hydrogen peroxide that
can lead to the formation of ROS that further increase the proliferation of melanocytes.
Table I
Botanicals That are Mostly Used in Skin-Lightening Cosmetics
S. No. Extract Type Reference
1Morus alba extract 2-Oxyresveratrol 44
2Aloe barbadensis leaf extract Aloesin 45
3Crocus sativus extract Kaempferol 46
4Uva ursi Arbutin 47
5 Licorice extract Glabridin 48
6Camelia sinesis extract ECG 49
7Phylanthus embelica extract Vitamin C 50
8Citrus limonum extract Hisperidin 51
9Punica granatum extract Ellagitannins 52
10 Vitis vinifera (grape) fruit extract Procyanidins 53
11 Anise extract Anisic acid 54
12 Cumin seed extract Cumic acid 55
13 Cinnamonum cassia extract Trans-cinnamaldehyde 56
14 Artocarpus lakoocha heartwood extract 2-Oxyresveratrol 57
15 Purus comunis (pear) extract Arbutin 58
16 Geranium extract Ellagic acid 59
17 Ramulus mori extract 2-Oxyresveratrol 60
18 Ginseng extract p-Coumaric acid 61
19 Malpighia punicifolia (Acerola) fruit extract Polyphenols 62
20 Mushroom (Agaricus blazei Muril) extract Tri-terpenoids 63
Most of the natural extracts contain fl avanoids that provide antioxidant effects and are
thus used as skin-lightening agents (69).
(iv) Vitamins as skin-lightening agents. Vitamins have been known to improve skin tone and
texture, and they have found remarkable acceptance among consumers. Most of the lead-
ing brands of skin-lightening agents that are available commercially utilize vitamins or
their derivatives as ingredients.
VITAMIN A. Vitamin A has been used for some decades for the removal of spots in Kligman’s
treatment (70). It is used along with hydroquinone and topical steroids for the treatment
of melasma. Tretinoin acts as a skin-lightening agent by inducing exfoliation. Further, it
accelerates the loss of epidermal melanin by increasing the turnover rate and by promoting
the proliferation of keratinocytes (71,72). However, users of tretinoin suffer from side
effects such as burning and increased photosensitization. Retinyl palmitate, a derivative
of retinoic acid, is used in skin-lightening cosmetic preparations.
VITAMIN B. Among the classes of vitamins that comprise vitamin B, two have been identi-
ed to have skin-lightening activity:
(a) Vitamin B3 (niacinamide): This is one of the most used hypopigmenting agents.
It is a well known antioxidant and interferes in melanasome transfer leading to skin
lightening. Using co-cultures of human melanocytes and keratinocytes, investiga-
tors have shown that niacinamide inhibits the transfer of melanosomes from mela-
nocytes to keratinocytes (73). The results of clinical studies using topically applied
niacin amide have demonstrated a reversible reduction in hyperpigmented lesions and
increased skin lightness compared with the vehicle alone after four weeks of use (74).
(b) Vitamin B5 (panthenoic acid): A derivative of vitamin B5, calcium pantetheine
sulfonate has been observed to interfere with the glycosylation of tyrosinase,
thereby leading to depigmenting effects (75).
VITAMIN C. Vitamin C is required for the production of collagen and is a photoprotectant as
it deactivates UV-induced free radicals and decreases erythema. Further, Vitamin C also
acts as a tyrosinase inhibitor, thereby lightening the skin (76). Although most effective,
ascorbic acid is a highly unstable compound. Stable derivatives of ascorbic acid in the
Figure 4. Structures of (a) glutathione and (b) phytic acid.
form of sodium ascorbyl phosphate (SAP), magnesium ascorbyl phosphate (MAP), and
ascorbyl palmitate are widely used in cosmetic products (77).
VITAMIN E. Vitamin E is the most important lipid-soluble antioxidant in the body. It is
abundant in the sebum and acts to absorb the oxidative stress of sunlight and skin expo-
sure. It has been demonstrated that vitamin E provides protection against UV-induced
infl ammation and hyperpigmentation (78). Vitamin E has also been studied in combina-
tion therapies with other vitamins as well as in other classes of skin-lightening com-
pounds (79,80).
Vitamins B, C, and E are used individually or in combination in many skin-lightening
treatment therapies.
(v) Peptides in skin lightening. Peptides are reported to reduce pigmentation through inter-
action with the protease-activated receptor 2 (PAR-2) of keratinocytes. PAR-2 activation
in involved in cell growth, differentiation, and infl ammatory processes and was shown to
affect melanin and melanosome ingestion by human keratinocytes (81). The protease-
activated receptor-2 upregulates keratinocyte phagocytosis. The peptide-based antago-
nist for PAR-2 can be used to regulate melanin ingestion by keratinocytes, thus effecting
Short peptides have also been reported in reducing the enzymatic activity of tyrosinase
(82). The use of sericin, a high-molecular-weight soluble glycoprotein from silk, as
a tyrosinase inhibitor has also been documented (83). Peptide residues that act as MSH
inhibitors have been known to lighten the skin. Soy trypsin inhibitors have been identi-
ed as interfering in melanosomal transfer, thereby reducing skin pigmentation (84).
(vi) Alpha and beta hydroxyl acids and derivatives. Alpha and beta hydroxyl acids have been
the most important class of compounds that are most widely used in cosmetic prepara-
tions. These act as superfi cial chemical peels that target the stratum corneum to improve
skin color and tone. They are comparatively pure and inexpensive, and they may be used
in higher amounts without many side effects (85). They are generally used in conjunction
with other skin-lightening agents to improve performance. Also referred to as fruit acids,
they improve skin texture by promoting desquamation or the shedding of the outer layers
of the stratum corneum. Alpha hydroxyl acids (AHA) have also been noted to increase
the enzymatic activity leading to epidermolysis. They are also employed in microderm-
abrasion techniques. In addition, they act as moisturizers and promote the synthesis of
elastin fi bers, leading to improved skin tone. However, care should be taken to neutralize
the skin after AHA treatment, as it might cause burning and erythema. The most com-
monly used AHAs are glycolic, lactic, citric, malic, pyurvic, and salicylic acids and their
Formulations for skin lightening have been majorly based on o/w emulsions that have a
higher aesthetic appeal. The fact that many of the ingredients get better dispersions is
also an added feature for the choice of such emulsions. Recently gel-based formulations
are being considered for suitability in certain skin types. Effi cacy studies for skin-lightening
formulations are carried out through clinical trails. Some of the techniques used in-
volve the use of the mexameter, chromameter, spectrophotometer, and VISIA, along with
dermatologist assessment. Also, other skin parameters such as moisturization, texture,
barrier integrity, pH, etc, are being evaluated to give picture of skin health after the use
of skin-lightening agents. This leads to screening the potentially harmful side effects of
hydroquinone-like substances in addition to the high-value claim proposition for the cos-
metics industry. With advances in technology in measurement techniques, it is becoming
easier to identify the effi cacy of formulations in different skin types.
Research in the area of skin-lightening agents in an expanding fi eld, with new ingre-
dients being added to the repertoire with every new discovery. Although tyrosinase
inhibition is still the most sought after mechanism skin lightening, newer pathways
are being identifi ed. It has been noted that ingredients that interfere with the path-
ways affecting melanin synthesis and transfer show promise as depigmenting agents.
Persistent research into skin lightening has also led to new mechanisms being discov-
ered in recent years.
The aspiration for light skin is on an upward curve and can be satisfi ed only when the
cosmetic in the bottle fulfi ls the promise of fair skin. A careful and complete investiga-
tion of the ingredient on the basis of its effi cacy and tolerance to individuals through
clinical trails is essential to ascertain that the product delivers the promise.
We thank Dr. Yash Kamath for reviewing the manuscript. Thanks are also due to
Dr. Usha Ranganathan and Dr. Lakshmi Madhavi for their help in the preparation of the
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... Figure 4 shows that the escalated level of free radicals that eventually caused the cancer pathology. Several studies had shown that elevation of free radicals level in cells such as reactive oxygen species (ROS) or reactive oxygen nitrogen (RONS) is closely related to the increase process of tumour generation (tumorigenesis) [23,44,45]. Normally functioned cells maintain ROS level inside a non-toxic range by regulating and maintaining the its generation as well as its scavenging systems [44]. ...
... Several studies had shown that elevation of free radicals level in cells such as reactive oxygen species (ROS) or reactive oxygen nitrogen (RONS) is closely related to the increase process of tumour generation (tumorigenesis) [23,44,45]. Normally functioned cells maintain ROS level inside a non-toxic range by regulating and maintaining the its generation as well as its scavenging systems [44]. The excessive and chronic increase of ROS endogenous level and other free radicals will lead to adaptive alterations that contribute to the tumorigenesis, metastasis, and drug resistance in various categories of cancer cells [44,45]. ...
... Normally functioned cells maintain ROS level inside a non-toxic range by regulating and maintaining the its generation as well as its scavenging systems [44]. The excessive and chronic increase of ROS endogenous level and other free radicals will lead to adaptive alterations that contribute to the tumorigenesis, metastasis, and drug resistance in various categories of cancer cells [44,45]. Apart from the evidence of free radicals increases the cancer growth and expansion, uncontrolled free radicals generation also can result in the adverse injury to DNA, lipid and cellular protein. ...
Clinacanthus nutans is largely cultivated in Asia tropical regions and predominantly native to Malaysia, Indonesia, Thailand and China. It is an important species from the Acanthaceae family and regarded as one of the primary contributor to the medicinal plants. This plant had been traditionally used as treatment of poisonous snake bites, skin rashes, dysentery, haematoma, rheumatism and injuries. Public Health Ministry of Thailand had used it as the primary therapy for lesion treatment due to virus. Phytochemicals recovered from this plant are chlorophyll derivatives, flavones, isoflavones and sulphur-containing glucosides. They exhibited various pharmacological effects such as anti-herpes simplex virus, anti-inflammatory and anti-cancer via various mechanisms. They also can potentially be exploited as the main ingredients in the cosmetic products including the lightening, anti-aging as well as anti-acne products since it exhibited the presence of compounds that had been proven to have anti-tyrosinase activity (melanin reduction), anti-oxidants (protection from UV radiation), anti-microbial towards Propionibacterium acnes and anti-inflammatory activities.
... The skin whitening compound which is widely used for depigmentation is hydroquinone. The compound overcomes hyperpigmentation by inhibiting the tyrosinase enzyme, but it is cytotoxic for melanocyte cells in long-term use [5]. Therefore, it is necessary to explore alternative natural ingredients for skin whitening compounds. ...
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The study aimed to determine genistein content and tyrosinase inhibition activity of 70% ethanolic and ethyl acetate extracts of edamame (Glycine max) with an extraction time of 15, 30, and 60 minutes. Extraction was performed using the ultrasonication method. Determination of genistein content was carried out using TLC-densitometry. Furthermore, all samples were tested for their tyrosinase inhibition activity using the spectrophotometric assay. Ethyl acetate extract with 60 min of extraction time exhibited the highest extraction yield (6.414% w/w), the highest genistein content (0.169 ± 0.007% w/w), and the highest tyrosinase inhibition activity (IC50 = 72.420 ± 0.550 µg/mL). It was known that the genistein content of 70% ethanolic and ethyl acetate extracts affected tyrosinase inhibition activity with correlation coefficient (r) values of 0.9973 and 0.9826, respectively. G. max was suggested as a tyrosinase inhibitor agent from natural sources for skin whitening product development due to its isoflavones content, mainly genistein.
... Dark skin or skin hyperpigmentation is a result of exposure to ultraviolet light or chemical irritants, and also is a manifestation in several skin disorders such as melasma, solar lentigines, or post-inflammatory hyperpigmentation [4]. The use of skin-lightening agents aims to reduce the level of melanin, the main pigment in the skin, resulting in a brighter skin tone [5,6]. ...
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Background: Paper mulberry is one of the most common skin-lightening agents in the beauty industry due to its strong anti-tyrosinase activity. This narrative review aims to summarize the chemical composition, biological activities, and applications of paper mulberry in cosmetics. Method: The literature for this article was acquired from the PubMed, Web of Science, and Google Scholar databases before September 2022. The keywords for searching included “paper mulberry”, “Broussonetia papyrifera”, “skin-lightening”, “skin-whitening”, “depigmentation”, “pharmacological activity”, and “biological activity”. Results: Paper mulberry consists of various components, including flavonoids, tannins, alkaloids, phenols, saponins, coumarins, glycosides, and polysaccharides, which possess a wide range of pharmacological properties. Apart from its anti-tyrosinase activity, paper mulberry and its compounds exhibited anti-inflammatory, antioxidant, antimicrobial, antiviral, anticancer, antidiabetic, anticholinesterase, antigout, antinociceptive, and hepatoprotective effects. Phenols and flavonoids were demonstrated to be the main contributors to the biological activities of paper mulberry. Paper mulberry is widely applied in cosmetics for skin lightening and skin moisturizing purposes and shows potential for application in hair care products due to the hair nourishing effects. The safety of paper mulberry for topical application was proven in clinical studies. Conclusion: The current review provides a better understanding of paper mulberry’s properties and allows us to extend the application of this plant and its bioactive components in cosmetics.
... However, there is a limitation in the clinical efficacy of the currently used tyrosinase inhibitors, as these inhibitors were specifically chosen based on their ability to inhibit mushroom tyrosinase [59]. This is also a widely reported screening method in the literature for skin-lightening ingredients [60]. Tyrosinase is an enzyme responsible for synthesizing melanin through melanogenesis [61]. ...
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This article reviews the use of Kojic Acid (KA) as a skin-lightening ingredient in the cosmetics industry. In 1907, Saito discovered KA, a natural product; it has since become one of the most investigated skin-lightening agents. This paper highlights the findings of the research conducted on this agent. It has been found that KA has certain disadvantages, and researchers have attempted to mitigate these disadvantages by designing new equivalents of KA that are more efficient in tyrosinase inhibition. These equivalents are also safe to use and have improved properties and solubility. The Cosmeceutical Ingredient Review (CIR) indicates that this ingredient can be safely used at a concentration not higher than 1% due to its cytotoxicity. Other scientific data also support its safety at a concentration of 2% or less. It was shown to be helpful in the treatment of hyper pigmentary disorders, such as freckles, age spots, post-inflammatory hyperpigmentation, and melasma, which has been proven clinically.
... Alpha and beta hydroxyl acids and derivatives Among them botanical extracts mostly contains a combination of two or more classes of compounds that works synergistically to achieve skin lightening. Botanicals connote nature and are hence more acceptable to people (Kmakshi, 2012). ...
... The fatty matter is extracted using petroleum ether then evaporation and weighed. Water content was carried out by Karl Fischer method according to the standard methods by Kamakshi [60]. ...
For a long time, it could be found that appearance enhancement products fell into the cosmetic category. Therefore, more people want to appear beautiful, thus the desire to appear beautiful has been urgent since the early days. Skincare products, hair, perfumes, oral care, and nail products are used by women despite their containment of toxic chemicals harmful to health in a society that wants to look its best because it is a beauty freak. Different toxic components and dangerous chemicals utilized in cosmetics are integrated beyond acceptable limits. These heavy metals may reason dangerous sick influences on the skin causing carcinogenicity. Therefore, it begins to be a requirement for people to turn out having knowledge of the different dangers of heavy metals utilized in cosmetics.
... A wide range of active pharmaceutical ingredients (APIs) targets the skin for therapeutics or cosmetic purposes [1][2][3]. Since ancient times, topical delivery has been considered as a route for the delivery of pharmaceuticals. Skin diseases can be treated both by topical and oral medications. ...
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Combined therapies emerge as an interesting tool to overcome limitations of traditional pharmacological treatments (efficiency, side effects). Among other materials, metal-organic frameworks (MOFs) offer versatilities for the accommodation of multiple and complementary active pharmaceutical ingredients (APIs): accessible large porosity, availability of functionalization sites, and biocompatibility. Here, we propose topical patches based on water-stable and biosafe Fe carboxylate MOFs (MIL-100 and MIL-127), the biopolymer polyvinyl alcohol (PVA) and two co-encapsulated drugs used in skin disorders (azelaic acid (AzA) as antibiotic, and nicotinamide (Nic) as anti-inflammatory), in order to develop an advanced cutaneous combined therapy. Exceptional MOF drug contents were reached (total amount 77.4 and 48.1 wt.% for MIL-100 and MIL-127, respectively), while an almost complete release of both drugs was achieved after 24 h, adapted to cutaneous delivery. The prepared cutaneous PVA-MOF formulations are safe and maintain the high drug-loading capacity (total drug content of 38.8 and 24.2 wt.% for MIL-100 and MIL-127, respectively), while allowing a controlled delivery of their cargoes, permeating through the skin to the active target sites. The total amount of drug retained or diffused through the skin is within the range (Nic), or even better (AzA) than commercial formulations. The presented results make these drug combined formulations promising candidates for new cutaneous devices for skin treatment.
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Ultraviolet irradiation induces melanin accumulation, which can be reduced by the use of chemical whitening products. However, the associated safety concerns of such products have prompted the search for natural and harmless alternatives. This study aimed to identify a natural acidic formulation to reduce skin pigmentation. The metabolite propionic acid (CH 3 CH 2 COOH, PA) was the most abundant fatty acid in the filtrate from Pluronic F68 (PF68) fermentation of Cutibacterium acnes ( C. acnes ) and reduced the DOPA-positive melanocytes by significantly inhibiting cellular tyrosinase activity via binding to the free fatty acid receptor 2 (FFAR2). Moreover, 4 mM PA treatment did not alter melanocyte proliferation, indicating that it is an effective solution for hyperpigmentation, causing no cellular damage. The reduced DOPA-positive melanocytes and tyrosinase activity were also observed in mice ear skin tissue injected with a mixture of C. acnes and PF68, supporting that the inhibition of melanogenesis is likely to be mediated through fermentation metabolites from C. acnes fermentation using PF68 as a carbon source. Additionally, PA did not affect the growth of its parent bacteria C. acnes , hence is a potent fermentation metabolite that does not disrupt the balance of the skin microbiome.
Objective: Melasma is an acquired hyperpigmentation disorder, and reactive oxygen species play important role in regulating melanin synthesis. Lycopene is one of the most effective oxygen neutralizers among tomato-derived carotenoids. Also, hydroquinone is a compound that has been used for the treatment of hyperpigmentation by mechanism of tyrosinase inhibition and can be found in wheat. Methods: An appropriate cream formulation containing 0.05% tomato lycopene and 3.45% wheat bran extract was prepared, and physicochemical characterization was performed. The prepared formulations were applied twice a day for three months in combination with SPF = 30 sunscreen by 22 patients diagnosed with melasma. MASI score in two groups was evaluated at weeks 0, 3, 6, 9, and 12 and 1 month after the treatment. Results: The prepared formulation shows smooth and homogeneous appearance with suitable spreadability and viscosity. The MASI score of intervention group from the sixth week until the end of the treatment was significantly decreased compared to the onset of the treatment (P < .05), and the mean difference of the MASI score and the rate of skin discoloration in intervention group (0.53 ± 0.47 and 3.73 ± 1.90, respectively) were significantly higher than in placebo group (0.14 ± 0.20 and 0.91 ± 0.07, respectively; P < .05). Size of melasma during the study was decreased significantly from 6.59 ± 3.47 to 5.97 ± 3.83 (P < .05). Conclusion: The data of mean difference of the MASI score indicated skin improvement in intervention group. Meanwhile, no recurrence was observed one month after the end of the treatment. These data suggest that the prepared formulation containing lycopene and wheat bran extract is safe and could be promising as an efficacious cosmetic treatment.
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The quest to be fair is not a concept of the new world. For centuries untold, having a lighter skin tone has been considered as a trait of beauty and supremacy. Society implicates fairness as a factor for getting a prospective life partner. Media portrays fair skin tone as a predecessor for success. These subtle influences affect young minds and drive them towards wanting fair skin. Physicians observe that it is one of the most common forms of body dysmorphic disorder. This article aims to highlight the psychosocial factors that mold this mentality and the possible ill effects it can have on a person, both psychologically as well as physically. This article is protected by copyright. All rights reserved.
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"Whiteness" or having white skin is considered an important element in constructing female beauty in Asian cultures. A dramatic growth of skin whitening and lightening products has occurred in Asian markets. Contemporary meanings of whiteness are influenced by Western ideologies as well as traditional Asian values and beliefs. In this study, we analyze print advertisements for skin whitening and lightening products in four Asian societies - India, Hong Kong, Japan and Korea. We compare the verbal messages and visual images for both global brands and local brands and across countries. We find that whiteness in these Asian cultures is both empowering and disempowering as well as both global and local in character.
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With the breakdown of traditional racial boundaries in many areas of the world, the widespread and growing consumption of skin-lightening products testifies to the increasing significance of colorism—social hierarchy based on gradations of skin tone within and between racial/ethnic groups. Light skin operates as a form of symbolic capital, one that is especially critical for women because of the connection between skin tone and attractiveness and desirability. Far from being an outmoded practice or legacy of past colonialism, the use of skin lighteners is growing fastest among young, urban, educated women in the global South. Although global in scope, the skin-lightening market is highly segmented by nation, culture, race, and class. This article examines the “yearning for lightness” and skin-lightening practices in various societies and communities and the role of transnational pharmaceutical and cosmetic corporations in fueling the desire for lighter skin through print, Internet, and television ads that link light skin with modernity, social mobility, and youth.
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Objective To develop and introduce evidence-based guidelines for the treatment of vitiligo in children and in adults. Patients and Setting Patients, residents, and dermatologists from the Department of Dermatology, Academic Medical Center, University of Amsterdam, and the Netherlands Institute for Pigmentary Disorders in Amsterdam. Design Scientific evidence obtained from 3 systematic reviews of the literature was combined with the results of 2 questionnaires and interviews of potential users of the guidelines, 3 internal expert meetings, and 1 local expert meeting, during which preliminary guidelines were presented and commented on. A final version of the guidelines was synthesized and disseminated among potential users. Six months after the introduction of these guidelines, their use was evaluated. Results Before the development of the guidelines, there was no uniformity in treatment selection, and there was a variability in estimates of treatment outcome. The meta-analysis showed class 3 corticosteroids and narrowband UV-B to be the most effective and safest therapies for localized and for generalized vitiligo, respectively. From another systematic review, it could be concluded that patients with segmental, stable, or lip-tip vitiligo could be successfully treated with most autologous transplantation methods. For vitiligo universalis, results of the systematic review showed that depigmentation using monobenzone or a Q-switched ruby laser was equally effective. The final version of the guidelines consisted of a treatment scheme together with detailed treatment protocols. Implementation of the guidelines was evaluated in 5 physicians. After the introduction of these guidelines, they were followed in most adult cases with vitiligo (71% of patients with localized vitiligo, 82% with generalized vitiligo, 100% with stable or segmental vitiligo, and 80% with universal vitiligo). In children with vitiligo, the physicians adhered to the guidelines for 52% of the cases. Conclusions Guidelines for the treatment of vitiligo can be successfully developed and disseminated for daily clinical practice. The results of the implementation of these guidelines should be confirmed in other centers involving more clinicians.
Melanogenesis provides a unique target for the development of antitumour agents specific for malignant melanoma. Among the anti-melanoma compounds we have examined, 4-S-cysteaminylphenol (4-S-CAP), a phenolic amine, was found to have the most promising anti-melanoma effects. To further improve its efficacy as an anti-melanoma agent, we synthesized the R- and S-enantiomers (99% enantiomer excess) of α-methyl- 4-S-cysteaminylphenol (α-Me-4-S-CAP) and α-ethyl- 4-S-cysteaminylphenol (α-Et-4-S-CAP) by coupling 4-hydroxythiophenol with the oxazolines obtained from the (R)- and (S)-enantiomers of 2-amino-1-propanol and 2-amino-1-butanol, respectively. The enantiomers of α-Me-4-S-CAP and α-Et-4-S-CAP were found to be better substrates for tyrosinase than the natural substrate, l-tyrosine. In vitro experiments showed that all four enantiomers were highly cytotoxic to pigmented B16-F1 melanoma cells, the effect being 70-fold and 160-fold greater than that on non-pigmented B16-G4F melanoma cells and 3T3 fibroblasts, respectively. The cytotoxic effect against B16-F1 cells was completely inhibited by phenylthiourea, a tyrosinase inhibitor, or by N-acetyl-l-cysteine, which increases the intracellular reduced glutathione (GSH) level. 4-S-CAP and the enantiomers were taken up into B16-F1 cells at comparable rates, but showed varying rates of GSH depletion that were inversely correlated to the cytotoxicity. These results suggest that the use of enantiomers would increase the efficacy of tyrosinase-dependent cytotoxic phenols.
Complete depigmentation of the normal skin of adult male blacks was procured by the daily application for five to seven weeks of a formula consisting of 0.1% tretinoin, 5.0% hydroquinone, 0.1% dexamethasone, and hydrophilic ointment. Depigmentation was not attainable when any one of the components was omitted.The formula was therapeutically effective in treatment of melasma, ephelides, and postinflammatory hyperpigmentation. Senile lentigines were resistant to this therapy.
The photoaging index has been developed to determine the level of skin rejuvenation required to reduce the visible signs of aging. Minor photoaging is reversed with free-radical avoidance and peeling with a topical skin care regimen consisting of buffing grains, α-hydroxy acid normalizing tonics and vitamin A conditioning lotions. The reversal of moderate photoaging requires the addition of light-to-moderate peels using α-hydroxy acids combined with microdermabrasion. For the more advanced case the Jessner/trichloroacetic acid (TCA) combination peel (Monheit peel) is used which can be repeated once to twice a year. Laser resurfacing is especially useful to shrink the collagen and produce a ‘face-lift bypass’. The phenol peel remains the standard to reverse heavy lines. A new modified formula (Hetter) is used which contains less phenol and less croton oil. Dermabrasion is helpful for removing multiple actinic keratosis. With this combination of skin care, chemical peels, and dermabrasion it is possible to reverse the photoaging index.
By bioassay-guided fractionation using mushroom tyrosinase (EC, 2-hydroxy-4-methoxybenzaldehyde was characterized as the principal tyrosinase inhibitor from three East African medicinal plants, the root of Mondia whitei (Hook) Skeels (Asclepiaceae), the root of Rhus vulgaris Meikle (Anacardiaceae), and the bark of Sclreocarya caffra Send (Anacardiaceae). It inhibited the oxidation of L-3,4-dihydroxyphenylalanine (L-DOPA) by mushroom tyrosinase with an IDS, of 4.3 mu g/ml (0.03 mM). The inhibition kinetics analyzed by a Lineweaver-Burk plot found this simple benzaldehyde derivative to be a mixed type inhibitor for this oxidation and affects on the enzyme in several ways. Based on finding this potent tyrosinase inhibitor, various related analogues were also tested in order to gain new insights into their inhibitory functions on a molecular basis.