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Polymeric nanoparticles for topical delivery of alpha and beta arbutin: preparation and characterization

Ayumi NS, Sahudin S, Hussain Z, Hussain M, Samah NHA

Drug Deliv Transl Res, 2019 04;9(2):482-496.
PMID: 29569027 DOI: 10.1007/s13346-018-0508-6

To investigate the use of chitosan nanoparticles (CS-TPP-NPs) as carriers for α- and β-arbutin. In this study, CS-TPP-NPs containing α- and β-arbutin were prepared via the ionic cross-linking of CS and TPP and characterized for particle size, zeta potential, and dispersity index. The entrapment efficiency and loading capacity of various β-arbutin concentrations (0.1, 0.2, 0.4, 0.5, and 0.6%) were also investigated. SEM, TEM FTIR, DSC and TGA analyses of the nanoparticles were performed to further characterize the nanoparticles. Finally, stability and release studies were undertaken to ascertain further the suitability of the nanoparticles as a carrier system for α- and β-arbutin. Data obtained clearly indicates the potential for use of CS-TPP-NPs as a carrier for the delivery of α- and β-arbutin. The size obtained for the alpha nanoparticles (α-arbutin CSNPs) ranges from 147 to 274 d.nm, with an increase in size with increasing alpha arbutin concentration. β-arbutin nanoparticles (β-arbutin CSNPs) size range was from 211.1 to 284 dn.m. PdI for all nanoparticles remained between 0.2-0.3 while the zeta potential was between 41.6-52.1 mV. The optimum encapsulation efficiency and loading capacity for 0.4% α-arbutin CSNPs were 71 and 77%, respectively. As for β-arbutin, CSNP optimum encapsulation efficiency and loading capacity for 0.4% concentration were 68 and 74%, respectively. Scanning electron microscopy for α-arbutin CSNPs showed a more spherical shape compared to β-arbutin CSNPs where rod-shaped particles were observed. However, under transmission electron microscopy, the shapes of both α- and β-arbutin CSNP nanoparticles were spherical. The crystal phase identification of the studied samples was carried out using X-ray diffraction (XRD), and the XRD of both α and β-arbutin CSNPs showed to be more crystalline in comparison to their free form. FTIR spectra showed intense characteristic peaks of chitosan appearing at 3438.3 cm-1 (-OH stretching), 2912 cm-1 (-CH stretching), represented 1598.01 cm-1 (-NH2) for both nanoparticles. Stability studies conducted for 90 days revealed that both α- and β-arbutin CSNPs were stable in solution. Finally, release studies of both α- and β-arbutin CSNPs showed a significantly higher percentage release in comparison to α- and β-arbutin in their free form. Chitosan nanoparticles demonstrate considerable promise as a carrier system for α- and β-arbutin, the use of which is anticipated to improve delivery of arbutin through the skin, in order to improve its efficacy as a whitening agent.

Matched MeSH terms: Skin Lightening Preparations/chemistry*
Fulltext Estimation of Inhibitory Effect against Tyrosinase Activity through Homology Modeling and Molecular Docking

Nokinsee D, Shank L, Lee VS, Nimmanpipug P

Enzyme Res, 2015;2015:262364.
PMID: 26788364 DOI: 10.1155/2015/262364

Tyrosinase is a key enzyme in melanogenesis. Generally, mushroom tyrosinase from A. bisporus had been used as a model in skin-whitening agent tests employed in the cosmetic industry. The recently obtained crystal structure of bacterial tyrosinase from B. megaterium has high similarity (33.5%) to the human enzyme and thus it was used as a template for constructing of the human model. Binding of tyrosinase to a series of its inhibitors was simulated by automated docking calculations. Docking and MD simulation results suggested that N81, N260, H263, and M280 are involved in the binding of inhibitors to mushroom tyrosinase. E195 and H208 are important residues in bacterial tyrosinase, while E230, S245, N249, H252, V262, and S265 bind to inhibitors and are important in forming pi interaction in human tyrosinase.

Matched MeSH terms: Skin Lightening Preparations
Mercury contamination in facial skin lightening creams and its health risks to user

Ho YB, Abdullah NH, Hamsan H, Tan ESS

Regul Toxicol Pharmacol, 2017 Aug;88:72-76.
PMID: 28554823 DOI: 10.1016/j.yrtph.2017.05.018

This study aims to determine concentrations of mercury in facial skin lightening cream according to different price categories (category I: skin lightening creams were determined during a preliminary market survey. Thereafter, twenty samples were purchased from various locations such as cosmetic stalls, beauty shops, pharmacies and street vendors based on their stratified price categories. Samples were extracted using microwave digester and analyzed using cold vapor atomic absorption spectrometry (CV-AAS). Non-carcinogenic chronic health risks for application of facial skin lightening cream were calculated using Dermal Absorption Dose (DAD) and Hazard Quotient (HQ). Concentrations of mercury in samples were less than the United States Food and Drug Administration (USFDA) permitted trace levels (<1 ppm) except for one sample from category III which was manufactured in China. Concentrations of mercury in facial skin lightening creams ranged from not detected to 1.13 mg kg-1. There was no significant association between concentrations of mercury with price categories (p = 0.12). There was no significant non-carcinogenic health risk due to daily application of the facial skin lightening creams based on assumption of 30 years exposure period (HQ

Matched MeSH terms: Skin Lightening Preparations/administration & dosage; Skin Lightening Preparations/analysis*
Fulltext A Zebrafish Embryo as an Animal Model for the Treatment of Hyperpigmentation in Cosmetic Dermatology Medicine

Lajis AFB

Medicina (Kaunas), 2018 May 25;54(3).
PMID: 30344266 DOI: 10.3390/medicina54030035

For years, clinical studies involving human volunteers and several known pre-clinical in vivo models (i.e., mice, guinea pigs) have demonstrated their reliability in evaluating the effectiveness of a number of depigmenting agents. Although these models have great advantages, they also suffer from several drawbacks, especially involving ethical issues regarding experimentation. At present, a new depigmenting model using zebrafish has been proposed and demonstrated. The application of this model for screening and studying the depigmenting activity of many bioactive compounds has been given great attention in genetics, medicinal chemistry and even the cosmetic industry. Depigmenting studies using this model have been recognized as noteworthy approaches to investigating the antimelanogenic activity of bioactive compounds in vivo. This article details the current knowledge of zebrafish pigmentation and its reliability as a model for the screening and development of depigmenting agents. Several methods to quantify the antimelanogenic activity of bioactive compounds in this model, such as phenotype-based screening, melanin content, tyrosinase inhibitory activity, other related proteins and transcription genes, are reviewed. Depigmenting activity of several bioactive compounds which have been reported towards this model are compared in terms of their molecular structure and possible mode of actions. This includes patented materials with regard to the application of zebrafish as a depigmenting model, in order to give an insight of its intellectual value. At the end of this article, some limitations are highlighted and several recommendations are suggested for improvement of future studies.

Matched MeSH terms: Skin Lightening Preparations/pharmacology*
Fulltext Depigmenting effect of Kojic acid esters in hyperpigmented B16F1 melanoma cells

Lajis AF, Hamid M, Ariff AB

J Biomed Biotechnol, 2012;2012:952452.
PMID: 23091364 DOI: 10.1155/2012/952452

The depigmenting effect of kojic acid esters synthesized by the esterification of kojic acid using Rhizomucor miehei immobilized lipase was investigated in B16F1 melanoma cells. The depigmenting effect of kojic acid and kojic acid esters was evaluated by the inhibitory effect of melanin formation and tyrosinase activity on alpha-stimulating hormone- (α-MSH-) induced melanin synthesis in B16F1 melanoma cells. The cellular tyrosinase inhibitory effect of kojic acid monooleate, kojic acid monolaurate, and kojic acid monopalmitate was found similar to kojic acid at nontoxic doses ranging from 1.95 to 62.5 μg/mL. However, kojic acid monopalmitate gave slightly higher inhibition to melanin formation compared to other inhibitors at doses ranging from 15.63 to 62.5 μg/mL. Kojic acid and kojic acid esters also show antioxidant activity that will enhance the depigmenting effect. The cytotoxicity of kojic acid esters in B16F1 melanoma cells was significantly lower than kojic acid at high doses, ranging from 125 and 500 μg/mL. Since kojic acid esters have lower cytotoxic effect than kojic acid, it is suggested that kojic acid esters can be used as alternatives for a safe skin whitening agent and potential depigmenting agents to treat hyperpigmentation.

Matched MeSH terms: Skin Lightening Preparations/pharmacology*
Discovery of new depigmenting compounds and their efficacy to treat hyperpigmentation: Evidence from in vitro study

Lajis AFB, Ariff AB

J Cosmet Dermatol, 2019 Jun;18(3):703-727.
PMID: 30866156 DOI: 10.1111/jocd.12900

Human skin pigmentation is a result of constitutive and facultative pigmentation. Facultative pigmentation is frequently stimulated by UV radiation, pharmacologic drugs, and hormones whereby leads to the development of abnormal skin hyperpigmentation. To date, many state-of-art depigmenting compounds have been studied using in vitro model to treat hyperpigmentation problems for cosmetic dermatological applications; little attention has been made to compare the effectiveness of these depigmenting compounds and their mode of actions. In this present article, new and recent depigmenting compounds, their melanogenic pathway targets, and modes of action are reviewed. This article compares the effectiveness of these new depigmenting compounds to modulate several melanogenesis-regulatory enzymes and proteins such as tyrosinase (TYR), TYR-related protein-1 (TRP1), TYR-related protein-2 (TRP2), microphthalmia-associated transcription factor (MITF), extracellular signal-regulated kinase (ERK) and N-terminal kinases (JNK) and mitogen-activated protein kinase p38 (p38 MAPK). Other evidences from in vitro assays such as inhibition on melanosomal transfer, proteasomes, nitric oxide, and inflammation-induced melanogenesis are also highlighted. This article also reviews analytical techniques in different assays performed using in vitro model as well as their advantages and limitations. This article also provides an insight on recent finding and re-examination of some protocols as well as their effectiveness and reliability in the evaluation of depigmenting compounds. Evidence and support from related patents are also incorporated in this present article to give an overview on current patented technology, latest trends, and intellectual values of some depigmenting compounds and protocols, which are rarely highlighted in the literatures.

Matched MeSH terms: Skin Lightening Preparations/pharmacology*; Skin Lightening Preparations/therapeutic use
Fulltext Optimization and validation of a cell-based tyrosinase assay for screening of tyrosinase inhibitors

Chan, Y.Y., Kim, K.H., Cheah, S.H.

JUMMEC, 2011;14(2):1-4.
MyJurnal

Tyrosinase is a key enzyme that catalyzes melanogenesis in human skin. It oxidizes tyrosine to L-3,4-dihydroxyphenylalanine (L-DOPA) and subsequently to dopachrome, which further polymerizes to melanin pigments. Therefore finding an effective tyrosinase inhibitor, either from synthetic or natural sources, is not only useful as skin whitening agents in cosmetic application, but also beneficial in treating melanin-related disorders. The present study reports of the optimized and validated results of a cell-based tyrosinase assay using B16F10 murine melanoma cell line, which produces melanin pigments and has been used extensively in antimelanogenesis studies. The optimization studies involved 3 parameters (1) optimal seeding cell number per well for total protein extraction; (2) optimal dopachrome formation from enzymatic reaction between total protein (tyrosinase source) and L-DOPA (substrate); and (3) optimal incubation period after the addition of substrate. The present study demonstrates that using seeding cell number of 2 × 105 cells/well, total protein of 40 μg, L-Dopa of 5 mM,and at an incubation period of 1 hour at 37°C provided the optimal response on cultured melanoma cells. Kojic acid, a standard tyrosinase inhibitor, was used as a positive control in the optimized cell-based tyrosinase assay to validate the usefulness of the assay. CONCLUSION: The use of the mentioned protocol is sensitive to determine changes in melanoma cells as the result of tyrosine inhibitors.

Matched MeSH terms: Skin Lightening Preparations
Fulltext Phenolic composition, antioxidant, anti-wrinkles and tyrosinase inhibitory activities of cocoa pod extract

Karim AA, Azlan A, Ismail A, Hashim P, Abd Gani SS, Zainudin BH, et al.

BMC Complement Altern Med, 2014 Oct 07;14:381.
PMID: 25292439 DOI: 10.1186/1472-6882-14-381

BACKGROUND: Cocoa pod is an outer part of cocoa fruits being discarded during cocoa bean processing. Authors found out that data on its usage in literature as cosmetic materials was not recorded in vast. In this study, cocoa pod extract was investigated for its potential as a cosmetic ingredient.
METHODS: Cocoa pod extract (CPE) composition was accomplished using UHPLC. The antioxidant capacity were measured using scavenging assay of 1,2-diphenyl-2-picrylhydrazyl (DPPH), β-carotene bleaching assay (BCB) and ferric reducing antioxidant power (FRAP). Inhibiting effect on skin degradation enzymes was carried out using elastase and collagenase assays. The skin whitening effect of CPE was determined based on mushroom tyrosinase assay and sun screening effect (UV-absorbance at 200-400 nm wavelength).
RESULTS: LC-MS/MS data showed the presence of carboxylic acid, phenolic acid, fatty acid, flavonoids (flavonol and flavones), stilbenoids and terpenoids in CPE. Results for antioxidant activity exhibited that CPE possessed good antioxidant activity, based on the mechanism of the assays compared with ascorbic acid (AA) and standardized pine bark extract (PBE); DPPH: AA > CPE > PBE; FRAP: PBE > CPE > AA; and BCB: BHT > CPE > PBE. Cocoa pod extract showed better action against elastase and collagenase enzymes in comparison with PBE and AA. Higher inhibition towards tyrosinase enzyme was exhibited by CPE than kojic acid and AA, although lower than PBE. CPE induced proliferation when tested on human fibroblast cell at low concentration. CPE also exhibited a potential as UVB sunscreen despite its low performance as a UVA sunscreen agent.
CONCLUSIONS: Therefore, the CPE has high potential as a cosmetic ingredient due to its anti-wrinkle, skin whitening, and sunscreen effects.

Matched MeSH terms: Skin Lightening Preparations/analysis; Skin Lightening Preparations/pharmacology; Skin Lightening Preparations/chemistry
Efficacy and safety of topical depigmenting agent in healthy human fair skin female volunteers: A single-arm study

Shah S, Chew SK

J Cosmet Dermatol, 2018 Oct;17(5):830-839.
PMID: 29193788 DOI: 10.1111/jocd.12435

BACKGROUND: Skin hyperpigmentation is the darkening of skin due to the increased production of melanin in the body.
OBJECTIVES: To evaluate the efficacy and safety of a botanical-based Rosa E pigmentation serum in healthy fair skin female volunteers with wrinkles, skin tone, and pigmentation.
METHODS: This was a single-arm, open label study conducted in healthy Indian females; 18 subjects aged 30-55, having fair Caucasian-like skin with at least 2 dark skin pigments with facial wrinkles diagnosed by dermatologist were selected. Rosa E pigmentation serum was applied twice a day for 84 days. Effect was evaluated by (i) instrumental technique (spectrophotometer® 2600D), (ii) clinically by dermatologist regarding product efficacy (skin tone, antiwrinkle, pigmentation), and (iii) volunteers self-evaluation.
RESULTS: The L* value of spectrophotometer reading represents lightness in the skin pigment. Reduction in the pigment was reported from day 14, with significant reductions observed till day 84 compared with baseline. Significant (P < .0001) skin pigmentation lightening was seen on day 14 (1.11) vastly improving on day 84 (1.94) based on photographic assessments. The significant reduction in skin pigment was 76.85%, Felix von Luschan skin color score was 30.24% (P < .0001) with a 7.38-fold reduction in skin tone and 57% reduction in facial wrinkles at day 84 from baseline.
CONCLUSIONS: Rosa E pigmentation serum was found safe and effective in significant reduction in skin pigments, improvement of skin tone, and antiwrinkle properties instrumentally, clinically, and self-evaluation by volunteers. In these evaluations, best results were seen the longer the Rosa E was used.

Matched MeSH terms: Skin Lightening Preparations/therapeutic use*
Fulltext Algae Metabolites in Cosmeceutical: An Overview of Current Applications and Challenges

Thiyagarasaiyar K, Goh BH, Jeon YJ, Yow YY

Mar Drugs, 2020 Jun 19;18(6).
PMID: 32575468 DOI: 10.3390/md18060323

Cosmetics are widely used by people around the world to protect the skin from external stimuli. Consumer preference towards natural cosmetic products has increased as the synthetic cosmetic products caused adverse side effects and resulted in low absorption rate due to the chemicals' larger molecular size. The cosmetic industry uses the term "cosmeceutical", referring to a cosmetic product that is claimed to have medicinal or drug-like benefits. Marine algae have gained tremendous attention in cosmeceuticals. They are one of the richest marine resources considered safe and possessed negligible cytotoxicity effects on humans. Marine algae are rich in bioactive substances that have shown to exhibit strong benefits to the skin, particularly in overcoming rashes, pigmentation, aging, and cancer. The current review provides a detailed survey of the literature on cosmeceutical potentials and applications of algae as skin whitening, anti-aging, anticancer, antioxidant, anti-inflammation, and antimicrobial agents. The biological functions of algae and the underlying mechanisms of all these activities are included in this review. In addition, the challenges of using algae in cosmeceutical applications, such as the effectiveness of different extraction methods and processing, quality assurance, and regulations concerning extracts of algae in this sector were also discussed.

Matched MeSH terms: Skin Lightening Preparations/isolation & purification; Skin Lightening Preparations/pharmacology; Skin Lightening Preparations/therapeutic use; Skin Lightening Preparations/chemistry

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