The Use of Botanical Extracts in East Asia for Treatment of Hyperpigmentation: An Evidenced-Based Review.

Recent years have seen a growth in the Asian cosmeceutical industry and an expanding worldwide marketplace with increasing consumer use of plant-based skin care products. The rising prevalence of Asian cosmeceuticals has led to research studies assessing the safety and efficacy of these products. We seek to review current evidence on safety and efficacy of key ingredients used in Asian cosmeceuticals to treat disorders of hyperpigmentation. A comprehensive search on PubMed was conducted to identify hyperpigmentation-related research studies on eight popular ingredients used in Asian cosmeceuticals: green tea, soy, orchid, licorice, rice water, ginseng, bamboo, and aloe. Both in vitro studies and clinical trials involving human subjects were included. Of the ingredients reviewed, soy and licorice had the most clinical evidence supporting their efficacy, while all other ingredients were supported by in vitro studies. More research is needed to further evaluate the safety and efficacy of Asian cosmeceutical ingredients in treatment of hyperpigmentation. J Drugs Dermatol. 2020;19(7): doi:10.36849/JDD.2020.4776.

Development of a new eczema-like reconstructed skin equivalent for testing child atopic dermatitis-relieving cosmetics.

OBJECTIVE: Atopic dermatitis (AD) is the most common chronic inflammatory skin disease, and it has serious effects on children's and families' quality of life. We aimed to screen and evaluate the efficacy of different formulas on relieving of atopic dermatitis clinical symptoms by developing an eczema-like reconstructed human skin equivalent in vitro. METHOD: Some research has reported that thymic stromal lymphopoietin (TSLP) may be a potential therapeutic target for the treatment of AD. We developed an eczema-like in vitro skin equivalent by coculturing the cocktails polyinosinic-polycytidylic acid sodium salt (poly(I:C)) and lipopolysaccharides (LPS). The eczema-like skin equivalent was characterized by overexpression of TSLP and impaired skin barrier function. Three cosmetic formulas with the potential of anti-inflammation and skin barrier promotion were topically applied onto the eczema-like skin equivalent, mimicking in vivo application. The inhibitory effect on TSLP was examined by ELISA. Effects on tissue viability and skin barrier function were determined by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) method. CONCLUSION: The results show that eczema-like skin equivalent induced by cocktails of poly(I:C) and LPS can mimic the skin characters of the atopic dermatitis. The cocktails can induce high TSLP expression, impaired cell viability, and skin barrier function. The cosmetic formulas with the potential of anti-inflammation and skin barrier promotion were evaluated to be helpful to decrease and relieve the impact of AD with the decreased TSLP and the higher tissue viability than the eczema-like skin equivalent without any cosmetic application. The eczema-like skin equivalent can be used to screen and evaluate formulas on AD relieving.

Evaluation of moisturizing and irritation potential of sacha inchi oil.

OBJECTIVE: The moisturizing and irritation effects of sacha inchi oil were evaluated. STUDY DESIGN: The moisturizing effect on the skin was clinically assessed using a regression study design. Sacha inchi oil or olive oil (benchmark) was applied on the left or right lower leg of the subjects for 14 days followed by application discontinuation for 2 days. The TEWL, skin moisture content and dryness appearance were observed. METHODS: The fatty acid composition and characteristics of cold-pressed sacha inchi seed oil were determined. Skin tissues cultured ex vivo were used to assess primary irritation induced by the oil by examining keratin 1 expression and TNF-α and IL-1α release from the oil-applied tissues. RESULTS: The sacha inchi oil contained 42.3% linolenic acid and 39.5% linoleic acid. This oil's saponification, iodine, acid and peroxide values were 168.58 ± 1.55 mg KOH/g, 203.00 ± 0.04 g I2 /100 g, 1.68 ± 0.03 mg KOH/g, and 1.95 ± 0.26 mEq peroxide/kg, respectively. Compared with nontreated skin tissues, induced secretion of TNF-α and IL-1α and disruption of keratin 1 integrity in the stratum corneum layer were not found in the sacha inchi oil-treated tissues. In a clinical study with 13 volunteers, the improvement in moisture content and skin dryness appearance at the sacha inchi oil-applied site was comparable with that observed at the olive oil-applied site. CONCLUSIONS: The sacha inchi oil was mild to the skin and benefited dry skin.

Development of topical drug delivery system with Sphaeranthus indicus flower extract and its investigation on skin as a cosmeceutical product.

BACKGROUND: Cosmetics are the products used to beautify the skin. Emulsion is a fine dispersion of two or more immiscible liquids. Sphaeranthus indicus is claimed to be used for skin beautification in folk medicine. Multiple emulsion was formulated containing the extract of S indicus flowers. AIMS: This research study indicates that extract of S indicus flowers contains sufficient amount of polyphenols and also possess good antioxidant activity with mushroom tyrosinase inhibition activity. METHOD: Further, stable multiple emulsion was developed and stability testing was performed for 180 days by keeping the multiple emulsion at 8°C ± 1, 25°C ± 1, 40°C ± 1, and 40°C ± 1 with 75% ± 1 RH. Parameters checked were color change, phase distribution, viscosity, droplet size and size distribution, pH determination, and electrical conductivity. Sun protection factor (SPF) was determined which also showed promising results. Skin testing on human volunteers was done for 3 months after biosafety profiling of the most stable multiple emulsion. RESULTS: This also showed remarkable effects. Skin erythema, melanin, and sebum were reduced. Skin hydration and elasticity were increased. There was also reduction in the number of skin large and small skin pores. Skin spot area was also reduced by the use of multiple emulsion loaded with S indicus flower extract. ANOVA test showed that all the effects produced on skin were significant, ie, P ≤ .05. CONCLUSION: A stable multiple emulsion was developed which produced significant cosmetic effects on human skin.

Anti-skin aging properties of protocatechuic acid in vitro and in vivo.

BACKGROUND: Protocatechuic acid has reported containing antioxidant effects. However, information on its other biological activities such as anti-wrinkle properties is limited AIMS: The objective of this study was to evaluate an antioxidant, collagen synthesis, MMP-1 inhibition (in vitro), and anti-wrinkle (in vivo) effects of protocatechuic acid (PCA) as a potent ingredient for wrinkle-care cosmetic. METHODS: Antioxidant effect was evaluated based on its scavenging activity for free radicals (DPPH, ABTS+). To evaluate the anti-skin aging potency of PCA, levels of MMP-1 and type I procollagen were measured using an ELISA kit in cultured human dermal fibroblasts. To further investigate if PCA could increase collagen synthesis, full-thickness human skin explants were immunostained with an anti-collagen I antibody. In an in vivo study, 22 female subjects were enrolled in a placebo-controlled trial. Facial wrinkle, especially crow's feet around eyes, was treated with lotion-containing 0.02% PCA for 8 weeks and compared with the placebo. RESULTS: In in vitro study, PCA showed high antioxidant activ ity. PCA also showed potential to induce the synthesis of type I collagen in human dermal fibroblast and skin explants. It inhibited MMP-1 secretion from UVA-irradiated human dermal fibroblast. An in vivo study, treatment with lotion-containing 0.02% PCA for 8 weeks significantly reduced the percentage of all skin wrinkle parameters. CONCLUSION: Based on the results of in vitro assays and in vivo skin testing in human subjects, PCA shows potential in anti-wrinkle or anti-skin aging treatments.

Nutraceuticals' Novel Formulations: The Good, the Bad, the Unknown and Patents Involved.

Traditional nutraceuticals and cosmeceuticals hold pragmatic nature with respect to their definitions, claims, purposes and marketing strategies. Their definitions are not well established worldwide. They also have different regulatory definitions and registration regulatory processes in different parts of the world. Global prevalence of nutraceuticals and cosmeceuticals is noticeably high with large market share with minimal regulation compared to traditional drugs. The global market is flooded with nutraceuticals and cosmeceuticals claiming to be of natural origin and sold with a therapeutic claim by major online retail stores such as Amazon and eBay. Apart from the traditional formulations, many manufacturers and researchers use novel formulation technologies in nutraceutical and cosmeceutical formulations for different reasons and objectives. Manufacturers tend to differentiate their products with novel formulations to increase market appeal and sales. On the other hand, researchers use novel strategies to enhance nutraceuticals and cosmeceuticals activity and safety. The objective of this review is to assess the current patents and research adopting novel formulation strategies in nutraceuticals and cosmeceuticals. Patents and research papers investigating nutraceutical and cosmeceutical novel formulations were surveyed for the past 15 years. Various nanosystems and advanced biotechnology systems have been introduced to improve the therapeutic efficacy, safety and market appeal of nutraceuticals and cosmeceuticals, including liposomes, polymeric micelles, quantum dots, nanoparticles, and dendrimers. This review provides an overview of nutraceuticals and cosmeceuticals current technologies, highlighting their pros, cons, misconceptions, regulatory definitions and market. This review also aims in separating the science from fiction in the nutraceuticals and cosmeceuticals development, research and marketing.

Development of Novel Topical Cosmeceutical Formulations from Nigella sativa L. with Antimicrobial Activity against Acne-Causing Microorganisms.

Acne vulgaris occurs due to the inflammation of sebaceous follicles in the skin. It is triggered by the activity of some bacterial species like Propionibacterium acnes, Staphylococcus aureus, and Staphylococcus epidermidis. Acquisition of antibiotic resistance by these microorganisms and adverse effects associated with the current treatment regimens necessitate the introduction of novel therapeutic agents for acne vulgaris. Thus, this study was undertaken to develop novel gel formulations from seeds of Nigella sativa L. and to evaluate the antibacterial potential against some acne-causing bacterial species. The antibacterial activity of seed extracts was initially screened against S. aureus and P. acnes by the agar well diffusion method. Thereafter, topical gels were formulated incorporating the ethyl acetate extract of seeds of N. sativa at three different concentrations. These topical formulations were subjected to antimicrobial activity studies while the stability was evaluated over a period of 30 days. All three formulations were capable of inhibiting the growth of S. aureus and P. acnes, with the highest antibacterial activity in the formulation comprising 15% of the seed extract. Interestingly, the antibacterial potency of this formulation against S. aureus surpassed the commercial synthetic product used as the positive control. Moreover, any alteration in color, odor, homogeneity, washability, consistency, and pH was not observed while the antibacterial potency was also retained during the storage period. The potent antibacterial activity in topical gel formulations developed from the ethyl acetate extract of N. sativa signposts their suitability as alternatives to existing antiacne agents in the management of acne vulgaris.

Relevant Topical Skin Care Products for Prevention and Treatment of Aging Skin.

Options for skin care are varied. New products are introduced constantly and it is important for the practitioner to have an understanding of products that impart beneficial results for aging skin. Educating patients to use products with scientifically proven benefits leads to better outcomes. Patients should be encouraged to use daily sunscreen, a topical retinoid every night, and a topical antioxidant daily. Supplementing the routine skin care regimen with alpha hydroxy acids, growth factors, heparin sulfate, and defensins can be addressed individually. Exogenous stem cells do not have sufficient evidence to warrant recommending them currently.

Clinical cosmeceutical repurposing of melatonin in androgenic alopecia using nanostructured lipid carriers prepared with antioxidant oils.

BACKGROUND: The present work aims to formulate nanostructured lipid carriers (NLCs) exhibiting high skin deposition and high inherent antioxidant potential to repurpose the use of melatonin hormone and some antioxidant oils in the treatment of androgenic alopecia (AGA). RESEARCH DESIGN AND METHODS: NLCs were characterized for their size, charge, drug entrapment, anti-oxidant potential, physical stability, in vitro release, surface morphology, and ex-vivo skin deposition. Their merits were clinically tested on patients suffering from AGA by calculating the degree of improvement, conduction of hair pull test, histometric assessment, and dermoscopic evaluation. RESULTS: Results revealed that melatonin NLCs showed nanometer size, negatively charged surface, high entrapment efficiency, and high anti-oxidant potential, in addition to sustained release for 6 h. Furthermore, NLCs displayed good storage stability and they were able to increase the skin deposition of melatonin 4.5-folds in stratum corneum, 7-folds in epidermis, and 6.8-folds in the dermis compared to melatonin solution. Melatonin NLCs displayed more clinically desirable results compared to the melatonin solution in AGA patients, manifested by increased hair density and thickness and decreased hair loss. CONCLUSIONS: The aforementioned system was shown to be a very promising treatment modality for AGA, which is worthy of futuristic experimentation.

Evidence for Anti-Aging South Korean Cosmeceuticals.

As the market for South Korean skin care products grows in the U.S. and worldwide, consumers will increasingly seek advice from dermatologists regarding their efficacy. In this paper, the evidence behind the anti-aging and skin whitening activity of ingredients in the most popular South Korean skin care products was reviewed and critically evaluated. Industry profit data from Euromonitor was obtained to identify the top cosmeceutical brands by retail value in South Korea. The top selling products and their ingredients were then identified from individual brand websites. A comprehensive literature search was conducted using Pubmed to identify and grade the anti-aging and whitening efficacy for nine popular ingredients: licorice, niacinamide, beta-glucan, snail mucus, ginkgo biloba, ginseng, green tea, pomegranate, and soy. Of the various ingredients reviewed, niacinamide, green tea, licorice, and soy have the most published data for anti-aging and whitening activity. Although the literature shows modest results, small sample sizes limit interpretation. High-level evidence to support the use of South Korean skin care products in anti-aging and skin whitening is lacking.

J Drugs Dermatol. 2017;16(4):358-364.

Efficacy and Tolerability of a Skin Brightening/Anti-Aging Cosmeceutical Containing Retinol 0.5%, Niacinamide, Hexylresorcinol, and Resveratrol.

Consumers are increasingly interested in over-the-counter skin care products that can improve the appearance of photodamaged and aging skin. This 10-week, open-label, single- center study enrolled 25 subjects with mild to moderate hyperpigmentation and other clinical stigmata of cutaneous aging including fine lines, sallowness, lack of clarity, and wrinkling. Their mean age was 53.4±7.7 years. The test product contained retinol 0.5% in combination with niacinamide 4.4%, resveratrol 1%, and hexylresorcinol 1.1% in a moisturizing base. Subjects were provided a skin care regimen including a cleanser, hydrating serum, moisturizer, and an SPF 30 sunscreen for daily use. The test product was applied only at night.

The use of this skin brightening/anti-aging cosmeceutical was found to provide statistically significant improvements in all efficacy endpoints by study end. Fine lines, radiance, and smoothness were significantly improved as early as week 2 (P<.001). By week 4, hyperpigmentation, overall skin clarity, evenness of skin tone, and wrinkles showed statistically significant improvement compared to baseline. Mild retinoid dermatitis including flaking and redness occurred early in the study as reflected by tolerability scores. By week 10, subjects reported no stinging, itching, dryness, or tingling.

The results of this open-label clinical study suggest that a topical cream containing retinol 0.5% in combination with niacinamide, resveratrol, and hexylresorcinol is efficacious and tolerable for skin brightening/anti-aging when used with a complementary skin care regimen including SPF 30 sun protection.

J Drugs Dermatol. 2016;15(7):863-868.

An Approach to Cosmeceuticals.

The cosmeceutical industry is a multi-billion dollar, consumer-driven market. Products promise highly desirable anti-aging benefits, but are not subject to regulation. We present an introduction to cosmeceuticals for the general and cosmetic dermatologist, including definitions and explanations of key terms, an approach to the evidence base, a dissection of chamomile and green tea, two paradigmatic cosmeceutical products, and a window into the underlying psychology of this vast marketplace.

Superior Efficacy of an Herbal-based Cosmeceutical Compared With Common Prescription and Cosmetic Antiaging Therapies.

INTRODUCTION: Research has shown that a disrupted stratum corneum permeability barrier coupled with chronic inflammation induce signs of extrinsic aging (photoaging). An novel herbal-based three product cosmeceutical regimen used to reverse these two anomalies that does not contain retinol, soy, niacinamide, tea, L-ascorbic acid or esters, hydroxy acids, tocopherol, or growth factors was tested in six human clinical trials to determine effectiveness and safety in reversing photoaging. MATERIALS AND METHODS: Six randomized split face, double blind, prospective, controlled clinical trials involving a total of 110 subjects compared a cosmeceutical blend of novel herbs in regimens consisting of one to three products to several common antiaging topical treatments. These comparative products include prescription tretinoin, physician strength idebenone, kinetin, polyhydroxy, lactic and glycolic acids in reversing signs of photoaging. RESULTS: The novel cosmeceutical blend regimen showed superior efficacy and safety in all six trials. DISCUSSION: These trials substantiate that herbs not used in common antiaging products effectively and safely mitigate and reverse photoaging signs and symptoms. The novel concept of treating photoaging and preventing its progression by repairing and optimizing the stratum corneum barrier, while reversing and inhibiting chronic cutaneous inflammation, has now been proven.