类紫杉醇脂质体体外释放的桨膜结合分析法研究

体外释放度是评价脂质体制剂质量的重要指标，目前各国药典中均未收载脂质体体外释放度评价方法，致使脂质体质量评价缺乏统一标准和无法提供安全性保障。本研究以自制类紫杉醇脂质体为例，通过优化外部释放条件建立的桨膜结合法模拟了在生理条件下类紫杉醇药物12 h的释放情况，结果表明以0.5% SDS-HEPES作为释放介质，采用截留分子量为1 000 kD的透析袋对脂质体水溶液进行释放的结果满足要求，且具有区分能力，为载药脂质体体外释放方法开发提供参考。

In vitro release of paclitaxel derivative liposome by paddle membrane binding assay

The in vitro release is an important index to evaluate the quality of liposome formulation.Currently, there is no evaluation method for the in vitro release of liposome in pharmacopoeia of various countries, which leads to the lack of unified standard and safety guarantee for the quality evaluation of liposome formulation.Taking the self-made paclitaxel derivative liposomes as an example, the paddle membrane binding method established by optimizing external release conditions was used to simulate the complete release of paclitaxel derivative drugs in 12 hours under physiological conditions.The results showed that using 0.5% SDS-HEPES as the release medium and a dialysis bag with a molecular weight cutoff of 1 000 kD to release the liposome solution met the requirements and had discrimination ability, providing a reference for the development of drug-loaded liposomes release methods in vitro.