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含有非那雄胺的局部用制剂。第二部分:使用差异剥离技术测定非那雄胺向毛囊的渗透情况。

Topical formulations containing finasteride. Part II: determination of finasteride penetration into hair follicles using the differential stripping technique.

作者信息

Tampucci Silvia, Burgalassi Susi, Chetoni Patrizia, Lenzi Carla, Pirone Andrea, Mailland Federico, Caserini Maurizio, Monti Daniela

机构信息

Department of Pharmacy, University of Pisa, Pisa, I-56126, Italy.

出版信息

J Pharm Sci. 2014 Aug;103(8):2323-9. doi: 10.1002/jps.24045. Epub 2014 Jun 10.

Abstract

The differential stripping technique consists of a tape-stripping phase followed by a cyanoacrylate biopsy. This technique not only allows the quantification of drug retained in the stratum corneum (SC) and in the hair follicles but also differentiates transepidermal from transfollicular penetration. Our study aimed at both validating the differential stripping procedure on hairless rat skin and assessing the role of the hair follicle in the cutaneous penetration of finasteride (FNS) after application of two experimental formulations for 6 or 24 h: P-08-016, a hydroxypropyl chitosan (HPCH)-based formulation and P-10-008, an anhydrous formulation devoid of HPCH. Microscopic and histological evaluation showed that after 15 tape strips both the SC and the viable epidermis were completely removed. A subsequent cyanoacrylate skin surface biopsy led to the removal of the infundibula content. The largest amounts of FNS were found in the epidermis and in the appendages after application of P-08-016, regardless of the time from application. In contrast, smaller and statistically significant amounts of FNS were recovered with P-10-008 6 h after application, compared with that at 24 h. In conclusion, the differential stripping technique allowed determination of the amount of FNS localized in different skin districts, focusing particularly on the follicular contribution.

摘要

差异剥离技术包括胶带剥离阶段,随后进行氰基丙烯酸酯活检。该技术不仅能够对保留在角质层(SC)和毛囊中的药物进行定量,还能区分经表皮渗透和经毛囊渗透。我们的研究旨在验证无毛大鼠皮肤上的差异剥离程序,并在应用两种实验制剂6小时或24小时后,评估毛囊在非那雄胺(FNS)皮肤渗透中的作用:P - 08 - 016,一种基于羟丙基壳聚糖(HPCH)的制剂;以及P - 10 - 008,一种不含HPCH的无水制剂。显微镜和组织学评估表明,经过15次胶带剥离后,角质层和活表皮均被完全去除。随后的氰基丙烯酸酯皮肤表面活检导致漏斗部内容物被去除。无论给药时间如何,在应用P - 08 - 016后,在表皮和附属器中发现的FNS量最大。相比之下,与24小时时相比,应用P - 10 - 008 6小时后回收的FNS量较少且具有统计学意义。总之,差异剥离技术能够确定不同皮肤区域中FNS的含量,尤其关注毛囊的贡献。

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