Rheological Properties and Composition Affecting the Skin Permeation of a Model of a Hydrophilic Drug in Lecithin Reverse Wormlike Micelles.

IF 1.7 4区 医学 Q3 PHARMACOLOGY & PHARMACY Biological & pharmaceutical bulletin Pub Date : 2024-01-20 Epub Date: 2023-12-14 DOI:10.1248/bpb.b23-00704
Yoshiyuki Miyasaka, Kaname Hashizaki, Kohsuke Shibasaki, Makiko Fujii, Hiroyuki Taguchi
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Abstract

We investigated the effect of the rheological properties and composition of lecithin reverse wormlike micelles (LRWs) on the skin permeation of a model of a hydrophilic drug to determine whether LRWs support uniform hydrophilic drug/oil-based formulations and good drug penetrate into skin. Here, we prepared LRWs with D (-)-ribose (RI) or glycerol (GL) as polar compounds, liquid paraffin (LP) or isopropyl myristate (IPM) as oils, and 6-carboxyfluorescein (CF) as a model for a hydrophilic drug, and evaluated the rheological properties and skin penetration characteristics of the preparations. The LRWs showed moderate viscosity at 25 °C, a typical storage temperature, but decreasing viscosity at 32 °C, the surface temperature of human skin, suggesting that the LRWs would penetrate the microstructure of skin (e.g., wrinkles and hair follicles). The highest skin permeability of CF was observed when IPM was used as the oil, suggesting that both the stratum corneum and hair follicle routes are involved in drug permeation. The penetration of CF into hair follicles is influenced not only by the rheology of the formulation but also by the interaction between IPM and sebum in the hair follicles.

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影响卵磷脂反向蠕虫状胶束中亲水性药物模型皮肤渗透的流变特性和成分
我们研究了卵磷脂反向蠕虫状胶束(LRWs)的流变特性和组成对亲水性药物模型的皮肤渗透的影响,以确定 LRWs 是否支持均匀的亲水性药物/油基制剂和良好的药物皮肤渗透。在此,我们以 D (-)- 核糖(RI)或甘油(GL)为极性化合物,液态石蜡(LP)或肉豆蔻酸异丙酯(IPM)为油,6-羧基荧光素(CF)为亲水性药物模型制备了 LRWs,并评估了制剂的流变特性和皮肤渗透特性。在 25°C 的典型储存温度下,LRWs 显示出中等粘度,但在 32°C 的人体皮肤表面温度下,其粘度却在下降,这表明 LRWs 可渗透皮肤的微观结构(如皱纹和毛囊)。当使用 IPM 作为油时,CF 的皮肤渗透性最高,这表明药物渗透的途径包括角质层和毛囊。CF 对毛囊的渗透不仅受制剂流变学的影响,还受 IPM 与毛囊中皮脂相互作用的影响。
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来源期刊
CiteScore
3.50
自引率
5.00%
发文量
247
审稿时长
2 months
期刊介绍: Biological and Pharmaceutical Bulletin (Biol. Pharm. Bull.) began publication in 1978 as the Journal of Pharmacobio-Dynamics. It covers various biological topics in the pharmaceutical and health sciences. A fourth Society journal, the Journal of Health Science, was merged with Biol. Pharm. Bull. in 2012. The main aim of the Society’s journals is to advance the pharmaceutical sciences with research reports, information exchange, and high-quality discussion. The average review time for articles submitted to the journals is around one month for first decision. The complete texts of all of the Society’s journals can be freely accessed through J-STAGE. The Society’s editorial committee hopes that the content of its journals will be useful to your research, and also invites you to submit your own work to the journals.
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