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新型加湿器装置产生的水滴对亲水性药物咖啡因经皮渗透的改善作用。

Improvement of Skin Permeation of Caffeine, a Hydrophilic Drug, by the Application of Water Droplets Provided by a Novel Humidifier Device.

作者信息

Todo Hiroaki, Hasegawa Yuya, Okada Akie, Itakura Shoko, Sugibayashi Kenji

机构信息

Graduate School of Pharmaceutical Sciences, Josai University.

Faculty of Pharmacy and Pharmaceutical Sciences, Josai University.

出版信息

Chem Pharm Bull (Tokyo). 2021;69(8):727-733. doi: 10.1248/cpb.c21-00110.

DOI:10.1248/cpb.c21-00110
PMID:34334516
Abstract

Recently, a novel humidifier that sprays water fine droplets equipped with a copolymer, poly(3,4-ethylene dioxythiophene)-poly(styrene sulfonate) (PEDOT/PSS) was developed. PEDOT/PSS in the humidifier absorbs water from the environment and releases fine water droplets by heating. In the present study, the effect of hydration on the skin barrier, stratum corneum, was first determined by the application of fine water droplets using the humidifier. The skin-penetration enhancement effect of a model hydrophilic drug, caffeine, was also investigated using the humidifier and compared with a conventional water-evaporative humidifier. More prolonged skin hydration effect was observed after application of the fine water droplet release humidifier using PEDOT/PSS than that using a conventional humidifier. In addition, markedly higher skin permeation of caffeine was observed in both infinite and finite dose conditions. Furthermore, higher skin permeation of caffeine from oil/water emulsion containing caffeine was observed in finite dose conditions by pretreatment with the humidifier using PEDOT/PSS. This device can provide water droplets without replenishing water, so it is more convenient for enhancing the skin permeation of chemical compounds from topical drugs and cosmetic formulations.

摘要

最近,一种新型加湿器被开发出来,它能喷出带有共聚物聚(3,4-亚乙基二氧噻吩)-聚(苯乙烯磺酸盐)(PEDOT/PSS)的微小水滴。加湿器中的PEDOT/PSS从环境中吸收水分,并通过加热释放微小水滴。在本研究中,首先通过使用该加湿器施加微小水滴来确定水合作用对皮肤屏障——角质层的影响。还使用该加湿器研究了模型亲水性药物咖啡因的皮肤渗透增强作用,并与传统的蒸发式加湿器进行了比较。与使用传统加湿器相比,使用含PEDOT/PSS的微小水滴释放加湿器后观察到了更持久的皮肤水合作用效果。此外,在无限剂量和有限剂量条件下均观察到咖啡因的皮肤渗透率明显更高。此外,在有限剂量条件下,通过用含PEDOT/PSS的加湿器进行预处理,观察到含咖啡因的油/水乳液中咖啡因的皮肤渗透率更高。该装置无需补充水就能提供水滴,因此对于增强局部药物和化妆品配方中化合物的皮肤渗透更为方便。

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