Abstract

The present study aimed to optimize insulin-loaded chitosan-coated W/O/W multiple emulsions (MEs) by investigating the effect of process variables on the response using Box–Behnken design. Effect of three independent factors, which are, the concentration of the lipophilic surfactant (Span 80) in the primary emulsion, the concentration of the hydrophilic surfactant (Tween 80) in the secondary emulsion, and phase volume ratio (W/O) in the primary emulsion, was studied on three dependent responses, which are particle size, zeta potential, and entrapment efficiency. The optimized ME showed particle size of 193.7 nm and −64.58 mV zeta potential with maximum entrapment efficiency of 91.84%. The in vitro drug release profile from W/O/W ME was studied under two simulated physiological conditions. In vitro drug release behavior followed the Peppas–Sahlin model and showed an initial and rapid release followed by a slower release. The results of the present investigation suggest the potential of the chitosan-coated W/O/W MEs as a promising oral drug delivery system for insulin.

摘要

本研究旨在优化胰岛素-通过使用 Box-Behnken 设计研究过程变量对响应的影响，加载壳聚糖包覆的 W/O/W 多重乳液 (ME)。三个独立因素的影响，即初级乳液中亲脂性表面活性剂 (Span 80) 的浓度、次级乳液中亲水性表面活性剂 (Tween 80) 的浓度和相体积比 (W/O)对初级乳液的三个相关响应进行了研究，即粒度、zeta 电位和截留效率。优化后的 ME 显示出 193.7 nm 的粒径和 -64.58 mV zeta 电位，最大包封效率为 91.84%。在两种模拟生理条件下研究了 W/O/W ME 的体外药物释放曲线。体外药物释放行为遵循 Peppas-Sahlin 模型，表现出初始快速释放，随后缓慢释放。本研究的结果表明，壳聚糖包覆的 W/O/W MEs 具有作为胰岛素口服给药系统的潜力。