利福布汀-PLGA纳米粒的制备

目的:制备利福布汀(RB)-聚乳酸-羟基乙酸共聚物(PLGA)纳米粒,并对制备工艺进行优化。方法:采用改良的自乳化溶剂挥发法制备;通过单因素法考察对包封率影响较大的因素,在此基础上以包封率为指标采用正交设计优化纳米粒的制备工艺并进行验证。结果:对纳米粒包封率影响较大的因素是RB与PLGA投药比、PLGA浓度、混合有机相中丙酮比例及油水相比;上述各因素的最佳水平分别是1:2、40mg·mL-1、70%、1:5。验证试验中所制纳米粒平均粒径为(201±19)nm、包封率为(59.1±5)%、载药量为(15.1±2.4)%。结论:本文的制备方法简单,所得纳米粒粒径小、质量稳定。

Preparation of Rifabutin-PLGA Nanoparticles

OBJECTIVE： To prepare Rifabutin （RB）-PLGA nanoparticles, and to optimize the preparation technology. METH- ODS： Modified self-emulsification-solvent evaporation method was adopted. The main influential factors of encapsulation coefficen- cy were investigated by single factor, and the preparation technology of nanoparticles was optimized with orthogonal design using encapsulation coefficency as index. RESULTS： The prominent factors towards encapsulation coefficency were ratio of RB to PLGA, concentration of PLGA, the proportion of acetone and ratio of oil to water. The above index of optimal preparation technol- ogy was 1：2, 40 mg.mL -1, 70% and 1：5. The average diameter of prepared nanoparticles was （201± 19） nm, encapsulation coef- ficency was （59.1 ± 5）%, and drug-loading amount was （15.1 ± 2.4）%. CONCLUSIONS： The method is simple, and prepared nanoparticles have small particle size and stable in quality.