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微针类型对利扎曲普坦透皮渗透的影响。

Effect of Microneedle Type on Transdermal Permeation of Rizatriptan.

作者信息

Uppuluri Chandrateja, Shaik Ashraf Sultana, Han Tao, Nayak Atul, Nair Karthik J, Whiteside Benjamin R, Nalluri Buchi N, 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

AAPS PharmSciTech. 2017 Jul;18(5):1495-1506. doi: 10.1208/s12249-016-0702-0. Epub 2017 Jan 11.

Abstract

The present study was aimed to investigate the effect of salient microneedle (MN) geometry parameters like length, density, shape and type on transdermal permeation of rizatriptan (RIZ). Studies were carried out using two types of MN devices viz. AdminPatch® arrays (ADM) (0.6, 0.9, 1.2 and 1.5 mm lengths) and laboratory-fabricated polymeric MNs (PMs) of 0.6 mm length. In the case of the PMs, arrays were applied three times at different places within a 1.77-cm skin area (PM-3) to maintain the MN density closer to 0.6 mm ADM. Histological studies revealed that PM, owing to their geometry/design, formed wider and deeper microconduits when compared to ADM of similar length. Approximately 4.9- and 4.2-fold increases in the RIZ steady-state flux values were observed with 1.5 mm ADM and PM-3 applications when compared to the passive studies. A good correlation between different dimensionless parameters like the amount of RIZ permeated (C /C ), thickness (h/L) and surface area (S /L ) of the skin was observed with scaling analyses. Numerical simulations provided further information regarding the distribution of RIZ in MN-treated skin after application of different MNs. Overall, the study suggests that MN application enhances the RIZ transdermal permeation and the geometrical parameters of MNs play an important role in the degree enhancement.

摘要

本研究旨在探讨显著的微针(MN)几何参数,如长度、密度、形状和类型对利扎曲普坦(RIZ)经皮渗透的影响。使用两种类型的MN装置进行了研究,即AdminPatch®阵列(ADM)(长度为0.6、0.9、1.2和1.5毫米)和长度为0.6毫米的实验室制备的聚合物微针(PM)。对于PM,在1.77平方厘米的皮肤区域内不同位置应用三次阵列(PM-3),以保持MN密度更接近0.6毫米ADM。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。与被动研究相比,在应用1.5毫米ADM和PM-3时,观察到RIZ稳态通量值分别增加了约4.9倍和4.2倍。通过标度分析观察到不同无量纲参数之间的良好相关性,如RIZ渗透量(C /C )、皮肤厚度(h/L)和表面积(S /L )。数值模拟提供了关于应用不同MN后RIZ在MN处理皮肤中分布的进一步信息。总体而言,该研究表明MN的应用增强了RIZ的经皮渗透,并且MN的几何参数在增强程度中起着重要作用。

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