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目的:本研究以脂蟾毒配基(resibufogenin,RBG)为模型药物,以自制的乙交酯丙交酯共聚物-维生素E聚乙二醇1000琥珀酸酯(polylactide-co-glycolide-D-α-tocopheryl polyethylene glycol 1000 succinate,PLGA-TPGS)为载体材料,采用正交试验筛选制备脂蟾毒配基PLGA-TPGS纳米粒(RBG-loaded PLGA-TPGS nanoparticles,RPTN)的最佳处方和制备工艺,并对RPTN进行体外稳定性考察。方法:采用超声乳化-溶剂挥发法制备RPTN,用单一因素法分别考察主药与载体配比、TPGS水溶液浓度、超声功率、超声时间对RPTN的粒径、载药量和包封率的影响。根据单一因素考察的试验结果,设定因素水平表,通过正交试验筛选制备RPTN的最佳处方和制备工艺。采用影响因素、加速、长期试验考察RPTN的体外稳定性。结果:通过正交试验筛选出制备RPTN的最佳处方和制备工艺,即主药与载体比例为3∶10(W∶W),0.05%TPGS水溶液为乳化剂,超声功率250 W下超声10 min。6批RPTN的平均粒径、载药量和包封率分别为(152.3±2.5)nm、(18.4±0.3)%和(79.3±1.2)%(n=6)。在稳定性考察中,RPTN在影响因素、加速、长期试验中均表现出良好的稳定性。结论:筛选出制备RPTN的最佳处方和制备工艺,自制RPTN粒径较小、载药量和包封率较高,体外具有良好的稳定性。
OBJECTIVE: In this study, we investigated the effect of polylactide-co-glycolide-D- α-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) as carrier material, and the optimum prescription and preparation technology of RPG-loaded PLGA-TPGS nanoparticles (RPTN) , And in vitro stability of RPTN study. Methods: RPTN was prepared by phacoemulsification and solvent evaporation method. The effects of main drug carrier, carrier concentration, concentration of TPGS solution, ultrasonic power and ultrasonic time on the particle size, drug loading and entrapment efficiency of RPTN were investigated. According to the single factor test results, set the level of factors table, through orthogonal test screening RPTN preparation of the best prescription and preparation process. Using influencing factors, accelerated, long-term tests to investigate the in vitro stability of RPTN. Results: The optimal formulation and preparation process of RPTN were screened by orthogonal test. The ratio of main drug to carrier was 3:10 (W: W), 0.05% TPGS aqueous solution was used as emulsifier and ultrasonic power was 250 W for 10 min . The average particle size, drug loading and entrapment efficiency of six batches of RPTN were (152.3 ± 2.5) nm, (18.4 ± 0.3)% and (79.3 ± 1.2)% (n = 6), respectively. In the stability study, RPTN showed good stability in influencing factors, accelerating and long-term experiments. Conclusion: The best prescription and preparation technology of RPTN were screened out. The self-made RPTN has the advantages of smaller particle size, higher drug loading and entrapment efficiency, and good stability in vitro.