Abstract

Purpose of present study was to develop eight formulations of chlorpheniramine (CPM) niosomes according to 2³ factorial design, characterise on the basis of various evaluation tests, i.e. in vitro drug release, SEM, FTIR, TGA and release kinetics, optimise the eight formulation on the basis in vitro drug release data, formulate gel of optimised dispersion, and to perform in vivo and histopathological study using gel of optimised dispersion on rabbits. Here, N3 having low level of cholesterol and span-80 but high level of span-60(0.1:0.2:0.05) was selected as optimised dispersion of niosomes that showed highest drug release i.e. 88.25% at pH 6 over 24 h of study and followed Korsmeyers-Peppas release kinetics with Fickian diffusion mechanism. After application of statistic by Analysis of variance (ANOVA) with 3D surface plots construction, gel of optimised dispersion of CPM niosomes was formulated, and evaluated by tests for i.e. viscosity, Spreadability, Extrudibility, drug content, drug entrapment, stability, SEM, FTIR, TGA, in vitro drug release, in vivo drug release following first order kinetics and histopathological study. Niosomal gel of CPM ensured successful development using suitable combination of non-ionic surfactants, and effective loading of drug for targeted delivery of drug.

摘要

本研究的目的是根据 2 ^{3因子设计开发 8 种扑尔敏 (CPM) 片剂，}在体外药物释放、SEM、FTIR、TGA 和释放动力学等各种评价试验的基础上进行表征，优化这 8 种剂型。根据体外药物释放数据，配制分散优化的凝胶，并在体内进行使用优化分散凝胶对兔进行组织病理学研究。在这里，选择具有低水平胆固醇和 span-80 但高水平 span-60 (0.1:0.2:0.05) 的 N3 作为 niosomes 的优化分散体，在 24 小时的研究中显示出最高的药物释放，即在 pH 6 时为 88.25%，并且遵循具有 Fickian 扩散机制的 Korsmeyers-Peppas 释放动力学。应用方差分析 (ANOVA) 统计并构建 3D 表面图后，配制 CPM niosomes 的优化分散凝胶，并通过粘度、铺展性、挤出性、药物含量、药物截留、稳定性、SEM、FTIR 等测试进行评估, TGA,体外药物释放,体内一级动力学和组织病理学研究后的药物释放。CPM的Niosomal凝胶确保了使用合适的非离子表面活性剂组合的成功开发，以及药物的有效负载以实现药物的靶向递送。