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熊果苷包封的胶束改善了透皮给药并抑制细胞黑色素生成。

Arbutin encapsulated micelles improved transdermal delivery and suppression of cellular melanin production.

作者信息

Liang Ke, Xu Keming, Bessarab Dmitri, Obaje Jonathan, Xu Chenjie

机构信息

School of Chemical & Biomedical Engineering, Nanyang Technological University, 70 Nanyang Drive, Singapore, 637457, Singapore.

Urah® Transdermal Pte Ltd, 51 Ubi Avenue 1, #05-13, Singapore, 408933, Singapore.

出版信息

BMC Res Notes. 2016 Apr 30;9:254. doi: 10.1186/s13104-016-2047-x.

Abstract

BACKGROUND

Hyperpigmentation is a skin disorder characterized by elevated production of melanin. Current treatment approaches mainly rely on the application of skin lightening chemicals, most of which have safety issues. Efficacy of delivery of the active ingredients to the target organ has also been a challenge. Transdermal based drug delivery platform has been shown to improve drug bioavailability, avoiding the hepatic first pass metabolism, decrease gastrointestinal side effects, and eventually enhance patient compliance.

RESULTS

This article explores the utilization of micellar transdermal delivery technology to improve skin penetration and efficacy of arbutin, a hyperpigmentation agent. The suppression efficacy of cellular melanin production versus cell viability of four active ingredients commonly used in skin lightening products, namely allantoin, arbutin, glycolic acid, and hyaluronic acid were first compared. Arbutin was selected for the micellar delivery studies base on its comparatively low cytotoxicity and better performance in reducing melanin production. Micellar Arbutin cream was formulated using Urah® proprietary micellar technology and was assessed for its cellular melanin suppression efficacy and skin penetration capacity.

CONCLUSION

The results show that micellar arbutin cream improved both the delivery and cellular melanin suppression, suggesting that micellar transdermal delivery may have potential application in addressing hyperpigmentation skin disorders. Graphical abstract Transdermal delivery of arbutin with micelles for melanin production suppression.

摘要

背景

色素沉着是一种以黑色素生成增加为特征的皮肤疾病。目前的治疗方法主要依赖于使用美白化学品,其中大多数存在安全问题。将活性成分输送到靶器官的效果也是一个挑战。基于透皮的药物递送平台已被证明可以提高药物的生物利用度,避免肝脏首过代谢,减少胃肠道副作用,并最终提高患者的依从性。

结果

本文探讨了利用胶束透皮递送技术来提高色素沉着剂熊果苷的皮肤渗透性和疗效。首先比较了美白产品中常用的四种活性成分,即尿囊素、熊果苷、乙醇酸和透明质酸对细胞黑色素生成的抑制效果与细胞活力。基于其相对较低的细胞毒性和在减少黑色素生成方面的更好表现,选择熊果苷进行胶束递送研究。使用Urah®专有胶束技术制备了胶束熊果苷乳膏,并评估了其对细胞黑色素的抑制效果和皮肤渗透能力。

结论

结果表明,胶束熊果苷乳膏提高了递送效果和对细胞黑色素的抑制作用,表明胶束透皮递送在解决色素沉着性皮肤疾病方面可能具有潜在应用。图形摘要 用胶束透皮递送熊果苷以抑制黑色素生成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3ca5/4851826/a1d2ec2b2ec4/13104_2016_2047_Figa_HTML.jpg

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