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制备并体内评价基于大豆卵磷脂的微球用于米诺地尔的经皮给药。

Preparation and in vivo evaluation of lecithin-based microparticles for topical delivery of minoxidil.

机构信息

College of Pharmacy, Chungbuk National University, 194-31, Osongsangmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju, Chungbuk, 28160, Republic of Korea.

Department of Pharmaceutical Engineering, Cheongju University, Cheongju, Chungbuk, 28530, Republic of Korea.

出版信息

Arch Pharm Res. 2017 Aug;40(8):943-951. doi: 10.1007/s12272-017-0934-x. Epub 2017 Aug 2.

DOI:10.1007/s12272-017-0934-x
PMID:28770536
Abstract

Minoxidil is widely used for treatment of androgenic alopecia. Commercial products containing minoxidil are usually in solution form. Repeated applications of minoxidil solution can lead to adverse effects such as skin irritation and horniness. The aims of this study were to prepare lecithin-based microparticle in minoxidil solution for enhancement of minoxidil topical delivery and skin protection and evaluate the ability of lecithin on in vitro delivery, in vivo hair growth, and skin trouble improvement compared to commercial minoxidil solution. In in vitro skin permeation study, minoxidil solution containing lecithin microparticle showed higher skin penetration rate and higher retention of drug inside the skin compared to minoxidil solution without lecithin. After topical application of minoxidil solutions with or without lecithin to C57BL/6 mice, minoxidil 5% solution containing lecithin microparticle showed hair re-growth as efficient as commercial product of minoxidil 5% solution. It also significantly improved skin troubles while commercial product presented horny substance and crust formation. Therefore, the lecithin-based microparticle in minoxidil 5% solution has good ability to promote hair growth without adverse effects.

摘要

米诺地尔广泛用于治疗雄激素性脱发。含有米诺地尔的商业产品通常为溶液形式。米诺地尔溶液的重复应用可能导致皮肤刺激和角质化等不良反应。本研究旨在制备基于大豆卵磷脂的米诺地尔溶液中的微粒,以增强米诺地尔的局部递送和皮肤保护,并评估与商业米诺地尔溶液相比,大豆卵磷脂在体外递药、体内毛发生长和皮肤问题改善方面的能力。在体外皮肤渗透研究中,与不含大豆卵磷脂的米诺地尔溶液相比,含有大豆卵磷脂微粒的米诺地尔溶液显示出更高的皮肤渗透速率和更高的药物在皮肤内的保留率。在将含有或不含有大豆卵磷脂的米诺地尔溶液局部应用于 C57BL/6 小鼠后,含有大豆卵磷脂微粒的 5%米诺地尔溶液显示出与商业 5%米诺地尔溶液一样有效的毛发生长作用。它还显著改善了皮肤问题,而商业产品则表现出角质物质和结痂形成。因此,5%米诺地尔溶液中的大豆卵磷脂基微粒具有良好的促进毛发生长的能力,而没有不良反应。

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