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微针对氨氯地平透皮渗透增强的作用。

Effect of microneedles on transdermal permeation enhancement of amlodipine.

作者信息

Nalluri Buchi N, Uppuluri Chandrateja, Devineni Jyothirmayee, Nayak Atul, Nair Karthik J, Whiteside Benjamin R, Das Diganta B

机构信息

Department of Pharmaceutics, KVSR Siddhartha College of Pharmaceutical Sciences, Vijayawada, 520010 AP, India.

Department of Chemical engineering, Loughborough University, Loughborough, LE11 3TU, UK.

出版信息

Drug Deliv Transl Res. 2017 Jun;7(3):383-394. doi: 10.1007/s13346-017-0361-z. Epub 2017 Feb 3.

Abstract

The present study aimed to investigate the effect of microneedle (MN) geometry parameters like length, density, shape and type on transdermal permeation enhancement of amlodipine (AMLO). Two types of MN devices viz. AdminPatch® arrays (ADM) (0.6, 1.2 and 1.5 mm lengths) and laboratory-fabricated polymeric MNs (PM) of 0.6 mm length were employed. In the case of PMs, arrays were applied thrice at different places within a 1.77-cm skin area (PM-3) to maintain the MN density closer to 0.6 mm ADM. Scaling analyses were done using dimensionless parameters like concentration of AMLO (C/C), thickness (h/L) and surface area of the skin (Sa/L). Microinjection moulding technique was employed to fabricate PM. Histological studies revealed that the PM, owing to their geometry/design, formed wider and deeper microconduits when compared to ADM of similar length. Approximately 6.84- and 6.11-fold increase in the cumulative amount (48 h) of AMLO permeated was observed with 1.5 mm ADM and PM-3 treatments respectively, when compared to passive permeation amounts. Good correlations (R  > 0.89) were observed between different dimensionless parameters with scaling analyses. The enhancement in AMLO permeation was found to be in the order of 1.5 mm ADM ≥ PM-3 > 1.2 mm ADM > 0.6 mm ADM ≥PM-1 > passive. The study suggests that MN application enhances the AMLO transdermal permeation and the geometrical parameters of MNs play an important role in the degree of such enhancement.

摘要

本研究旨在探讨微针(MN)的长度、密度、形状和类型等几何参数对氨氯地平(AMLO)透皮渗透增强的影响。使用了两种类型的微针装置,即AdminPatch®阵列(ADM)(长度分别为0.6、1.2和1.5毫米)和长度为0.6毫米的实验室自制聚合物微针(PM)。对于PM,在1.77平方厘米的皮肤区域内不同位置重复施加三次阵列(PM - 3),以使微针密度接近0.6毫米ADM。使用氨氯地平浓度(C/C)、厚度(h/L)和皮肤表面积(Sa/L)等无量纲参数进行标度分析。采用微注射成型技术制备PM。组织学研究表明,由于其几何形状/设计,与类似长度的ADM相比,PM形成了更宽、更深的微通道。与被动渗透量相比,1.5毫米ADM和PM - 3处理分别使AMLO的累积渗透量(48小时)增加了约6.84倍和6.11倍。标度分析中不同无量纲参数之间观察到良好的相关性(R > 0.89)。发现AMLO渗透增强的顺序为1.5毫米ADM≥PM - 3 > 1.2毫米ADM > 0.

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