The co-drug of conjugated hydroquinone and azelaic acid to enhance topical skin targeting and decrease penetration through the skin

Hsieh, Pei Wen; Al‐Suwayeh, Saleh A.; Fang, Chia Lang; Lin, Chwan Fwu; Chen, Chun Che; Fang, Jia You

doi:10.1016/j.ejpb.2012.03.006

Cited by 36 publications

(13 citation statements)

References 39 publications

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“…The aim is threefold: obtain a synergistic effect, increase cutaneous permeation, and increase the stability of the active ingredients by masking the most labile functions. As for cutaneous penetration, the gamble paid off in that the tests performed in vitro showed that the permeation of the codrug was two times greater than that obtained with the parent compounds alone [27].…”

Section: Hydroquinone and Its Derivativesmentioning

confidence: 99%

Overview of Skin Whitening Agents: Drugs and Cosmetic Products

2016

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Depigmentation and skin lightening products, which have been in use for ages in Asian countries where skin whiteness is a major esthetic criterion, are now also highly valued by Western populations, who expose themselves excessively to the sun and develop skin spots as a consequence. After discussing the various possible mechanisms of depigmentation, the different molecules that can be used as well as the status of the products containing them will now be presented. Hydroquinone and derivatives thereof, retinoids, alpha-and beta-hydroxy acids, ascorbic acid, divalent ion chelators, kojic acid, azelaic acid, as well as diverse herbal extracts are described in terms of their efficacy and safety. Since a genuine effect (without toxic effects) is difficult to obtain, prevention by using sunscreen products is always preferable.

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Section: Hydroquinone and Its Derivativesmentioning

confidence: 99%

Overview of Skin Whitening Agents: Drugs and Cosmetic Products

2016

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“…The defatted fresh skin homogenate was prepared as described by Hsieh et al with some modifications 30 . Using the freshly obtained skin, 5 g was sliced into small pieces and soaked in 30-ml borate buffer (pH ¼8) in the refrigerator.…”

Section: Dea Hydrolysis By Human Skin and Human Skin Viabilitymentioning

confidence: 99%

A prodrug approach to enhance azelaic acid percutaneous availability

Al-Marabeh

Khalil

Khanfar

et al. 2016

Pharmaceutical Development and Technology

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Azelaic acid is a dicarboxylic acid compound used in treatment of acne vulgaris. However, high concentration (ca 20%) is needed to guarantee the drug availability in the skin. The latter increases the incidence of side effects such as local irritation. The prodrug strategy to enhance azelaic acid diffusion through skin was not reported before. Thus, a lipophilic prodrug of azelaic acid (diethyl azelate [DEA]) was synthesized and investigated to improve percutaneous availability of azelaic acid, with a subsequent full physical, chemical, and biological characterization. Expectedly, DEA exhibited a significant increase in diffusion compared to azelaic acid through silicone membrane. In contrast, the diffusion results through human stratum corneum (SC) displayed weaker permeation for DEA with expected retention in the SC. Therefore, a desorption study of DEA from SC was conducted to examine the reservoir behavior in SC. Results showed an evidence of sustained release behavior of DEA from SC. Consequently, enhancement of keratolytic effect is expected due to azelaic acid produced from enzymatic conversion of DEA released from SC.

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“…Especially, hyperpigmentation is an important disease in the skin care industry, mainly due to prolonged exposure to ultraviolet light and excessive use of certain chemical drugs [3,4]. The common and effective treatments for all types of hyperpigmentary disorders are topical tyrosinase inhibitors and antimelanogenesis compounds, such as hydroquinone (HQ), kojic acid (KA), azelaic acid (AA), and phenylethyl resorcinol (PR) [5][6][7][8]. Specially, PR is an effective skin lightening agent compared with other commonly used skin lightening drugs and proved to be a highly safe ingredient [9].…”

Section: Introductionmentioning

confidence: 99%

Fabrication of Carboxylmethyl Chitosan Nanocarrier via Self-Assembly for Efficient Delivery of Phenylethyl Resorcinol in B16 Cells

2020

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Micro-molecular drugs have special advantages to cope with challenging diseases, however their structure, physical and chemical properties, stability, and pharmacodynamics have more requirements for the way they are delivered into the body. Carrier-based drug delivery systems can circumvent many limited factors of drug delivery and increase their bioavailability. In this context, stable drug nanocarriers of alkaline amino acids (arginine, Arg) modified conjugated linoleic acid-carboxymethyl chitosan (CLA-CMCS) conjugate were developed, which could generate supramolecular micelles to effectively encapsulate the tyrosinase inhibitor phenylethyl resorcinol (PR). The resulting CCA-NPs were spherical nanoparticles with a mean size around 175 nm. The 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay and cellular uptake investigation demonstrated that the CCA-NPs were non-cytotoxic and had excellent cell transport ability. In addition, these CCA-NPs were able to effectively deliver PR and inhibited melanin formation to reduce pigmentation by enhancing cellular uptake. In conclusion, our research indicated that nanocarriers based on self-assembly amphiphilic polymers constituted a promising and effective drug delivery system in hyperpigmentation targeting.

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The co-drug of conjugated hydroquinone and azelaic acid to enhance topical skin targeting and decrease penetration through the skin

Cited by 36 publications

References 39 publications

Overview of Skin Whitening Agents: Drugs and Cosmetic Products

Overview of Skin Whitening Agents: Drugs and Cosmetic Products

A prodrug approach to enhance azelaic acid percutaneous availability

Fabrication of Carboxylmethyl Chitosan Nanocarrier via Self-Assembly for Efficient Delivery of Phenylethyl Resorcinol in B16 Cells

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