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溶剂和渗透促进剂对透皮递送姜黄素的影响:渗透和皮肤沉积研究。

Effects of solvents and penetration enhancers on transdermal delivery of thymoquinone: permeability and skin deposition study.

机构信息

a Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers , The State University of New Jersey , Piscataway , NJ , USA.

b Center for Dermal Research, Life Sciences Building, Rutgers , The State University of New Jersey , Piscataway , NJ , USA.

出版信息

Drug Deliv. 2018 Nov;25(1):1943-1949. doi: 10.1080/10717544.2018.1523256.

Abstract

Thymoquinone (TQ) is a quinone-based phytochemical that was first identified in 1963 in Nigella sativa (black cumin seed) by El-Dakhakhany. Based on the ideal characteristics of transdermal delivery, TQ is potentially an attractive candidate for transdermal drug delivery. The aim of this study was to investigate the feasibility of transdermal delivery of TQ and to assess the effect of an ethanol and propylene glycol donor solvent system along with various compositions of receptor solvents. The effects of penetration enhancers on the in vitro skin permeation and TQ skin absorption were studied using human cadaver skin in Franz diffusion cells. The permeation of saturated solutions of TQ was investigated with 5% v/v of each of the following enhancers: Azone (laurocapram), Transcutol® P (Tc), oleic acid, ethanol, Polysorbate 80 (Tween 80), and N-methyl-pyrrolidone (NMP). The results indicated that Azone, oleic acid, and Tc were able to provide adequate TQ flux and may be the agents of choice for use in a novel transdermal formulation of TQ. These penetration enhancers were also able to generate TQ reservoirs in the skin that may be useful to provide sustained release of TQ from the stratum corneum over longer periods of time.

摘要

百里醌(TQ)是一种基于醌的植物化学物质,于 1963 年由 El-Dakhakhany 首次在黑孜然种子(黑孜然种子)中鉴定出来。基于经皮给药的理想特征,TQ 可能是经皮药物递送的有吸引力的候选物。本研究旨在探讨 TQ 经皮给药的可行性,并评估乙醇和丙二醇供体溶剂系统以及受体溶剂的各种组合的效果。使用 Franz 扩散细胞中的人体尸体皮肤研究了渗透促进剂对 TQ 的体外皮肤渗透和 TQ 皮肤吸收的影响。研究了 TQ 饱和溶液在以下每种 5%v/v 的渗透增强剂中的渗透:氮酮(月桂氮酮)、Transcutol® P(Tc)、油酸、乙醇、聚山梨酯 80(吐温 80)和 N-甲基-吡咯烷酮(NMP)。结果表明,氮酮、油酸和 Tc 能够提供足够的 TQ 通量,可能是用于 TQ 新型经皮制剂的首选试剂。这些渗透促进剂还能够在皮肤中产生 TQ 储库,这可能有助于从角质层中长时间持续释放 TQ。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a73b/6249612/3f59072b341b/IDRD_A_1523256_F0001_C.jpg

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