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采用W/O/W溶剂蒸发法和超声处理制备的具有毛囊递送特性的米诺地尔包封聚(L-丙交酯-共-乙交酯)纳米粒。

Minoxidil-encapsulated poly(L-lactide-co-glycolide) nanoparticles with hair follicle delivery properties prepared using W/O/W solvent evaporation and sonication.

作者信息

Takeuchi Issei, Hida Yukari, Makino Kimiko

机构信息

Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641, Yamazaki, Noda, Chiba 278-8510, Japan.

Center for Drug Delivery Research, Tokyo University of Science, 2641, Yamazaki, Noda, Chiba 278-8510, Japan.

出版信息

Biomed Mater Eng. 2018;29(2):217-228. doi: 10.3233/BME-171724.

Abstract

BACKGROUND

Nanoparticles with a diameter of 100-150 nm prepared using poly(lactide-co-glycolide) can be delivered to hair follicles. Moreover, it was shown that drug release from nanoparticles was prolonged by using poly(L-lactide-co-glycolide) (PLLGA).

OBJECTIVE

The aim of this study was to prepared minoxidil-encapsulated PLLGA nanoparticles and accumulate minoxidil in hair follicles utilizing its drug delivery properties for effective treatment of male and female androgenetic alopecia.

METHODS

Minoxidil-encapsulated PLLGA nanoparticles were prepared using W/O/W solvent evaporation and sonication, and the ability of PLLGA nanoparticles to deliver to hair follicles was evaluated by in vivo transdermal delivery study using C3H/He mice and tape stripping and cyanoacrylate skin surface biopsy.

RESULTS

Eight hours after administration of samples, minoxidil-encapsulated PLLGA nanoparticles delivered 3.1 times more minoxidil in stratum corneum and 2.5 times more in hair follicles r compared to minoxidil aqueous solution. In addition, we found that 4.8% of the dose of minoxidil-encapsulated PLLGA nanoparticles were delivered to the hair follicles.

CONCLUSIONS

In this study, it was shown that nanoparticulation using PLLGA7510 suppressed minoxidil release from nanoparticles and improved drug delivery amount to hair follicles.

摘要

背景

使用聚(丙交酯-共-乙交酯)制备的直径为100 - 150纳米的纳米颗粒可被递送至毛囊。此外,研究表明使用聚(L-丙交酯-共-乙交酯)(PLLGA)可延长纳米颗粒的药物释放时间。

目的

本研究旨在制备米诺地尔包裹的PLLGA纳米颗粒,并利用其药物递送特性使米诺地尔在毛囊中蓄积,以有效治疗男性和女性雄激素性脱发。

方法

采用W/O/W溶剂蒸发法和超声处理制备米诺地尔包裹的PLLGA纳米颗粒,并通过使用C3H/He小鼠进行体内透皮递送研究以及胶带剥离和氰基丙烯酸酯皮肤表面活检来评估PLLGA纳米颗粒递送至毛囊的能力。

结果

给药8小时后,与米诺地尔水溶液相比,米诺地尔包裹的PLLGA纳米颗粒在角质层中的米诺地尔递送量多3.1倍,在毛囊中的递送量多2.5倍。此外,我们发现米诺地尔包裹的PLLGA纳米颗粒剂量的4.8%被递送至毛囊。

结论

在本研究中,结果表明使用PLLGA7510制备纳米颗粒可抑制米诺地尔从纳米颗粒中的释放,并提高药物向毛囊的递送量。

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