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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。
Objective: To prepare rifabutin (RB) -polylactic acid-glycolic acid copolymer (PLGA) nanoparticles and to optimize the preparation process. Methods: The modified self-emulsifying solvent evaporation method was adopted. The factors affecting the entrapment efficiency were investigated by single factor method. On the basis of the entrapment efficiency, orthogonal design was used to optimize the preparation process of the nanoparticles . Results: The factors affecting the entrapment efficiency of nanoparticles were the ratio of RB to PLGA, the concentration of PLGA, the proportion of acetone in the mixed organic phase and the ratio of oil to water. The optimum levels of these factors were 1: 2 and 40 mg · mL -1,70%, 1: 5. The average diameter of nanoparticles prepared in the validation experiment was (201 ± 19) nm, the encapsulation efficiency was (59.1 ± 5)% and the drug loading was (15.1 ± 2.4)%. Conclusion: The preparation method of this paper is simple, the obtained nanoparticles have small particle size and stable quality.