摘要
目的制备包载羟基喜树碱(HCPT)的甘草次酸修饰的PEI-PLGA(GA-PEI-PLGA)纳米粒。方法采用超声乳化-减压溶剂挥发法制备HCPT/GA-PEI-PLGA纳米粒。在单因素实验基础上,选取药物/载体比、油相/水相体积比、超声时间、超声功率为考察因素,以包封率和载药量为考察指标,通过正交设计实验对载药纳米粒的制备工艺进行优化,并对其粒径及Zeta电位进行测定。结果超声乳化-减压溶剂挥发法成功制得HCPT/GA-PEI-PLGA纳米粒,其中药物/载体比对载药纳米粒制备的影响最大。优化后的处方工艺为:药物/载体比3∶10、油相/水相体积比1∶9、超声功率570 W、超声时间15 min。制得的载药纳米粒包封率高达(87.52±3.91)%,载药量为(20.10±4.72)%;平均粒径(218.1±3.23)nm,Zeta电位为(34.98±3.56)m V。结论超声乳化-减压溶剂挥发法适于制备HCPT/GA-PEI-PLGA纳米粒,制得的载药纳米粒包封率和载药量较高、粒径分布均匀、稳定性好。
Objective To prepare hydroxycamptothecin（HCPT）loaded glycyrrhetinic acid modified polyethyleneimine- poly（lactic-co-glyeolie acid） （GA-PEI-PLGA）nanoparticles. Methods Emulsion-solvent evaporation method was used to prepare HCPT-loaded GA-PEI-PLGA nanoparticles. Based on the single-faetor experiments, drug/GA-PEI-PLGA ratio, oil phase/water phase ratio, sonieation timeand power were further investigated. The formulation and process were optimized by orthogonal testingdesign using entrapment efficieney and drug loading efficiency as indexes. HCPT-loaded GA-PEI-PLGA nanopartieles＂ diameter and zeta potential were determined. Results HCPT-loaded GA-PEI-PLGA nanopartieles were successfully prepared by emulsion-solvent evaporation method.Drug/GA-PEI-PLGA ratio, in particular, had the uniform particle on the preparation of HCPT-loaded nanopartieles.The optimal process was as follows：drug/GA-PEI-PLGA ratio of 3 tol0, oil phase/water phase ratio of 1 to 9, sonieation power of 570 W and sonieation time of 15 min.The entrapment efficiency and drug loading effieieney of HCPT-loaded GA-PEI-PLGA nanopartieles were （ 87.52 ± 3.91 ） % and （ 20.10 ± 4.72 ） %, respectively. The average particle size was（218.1±3.23）nm and the zeta potential was（34.98±3.56） mV. Conclusion Emulsion-solvent evaporation method was feasible for preparing HCPT-loaded GA-PEI-PLGA nanoparticles, with uniform particel size distribution, good stability, high entrapment and drug loading efficiency.
作者
梁劲康
吴得天
胡巧红
吴雅琼
LIANG Jingkang WU Detian HU Qiaohong WU Yaqiong(College of Pharmacy Guangdong Provincial Key Laboratory of Advanced Drug Delivery, Guangdong Pharmaceutical University, Guangzhou 510006, China)
出处
《医药导报》
CAS
2016年第11期1254-1258,共5页
Herald of Medicine
基金
广东药学院大学生创新创业训练项目(201510573043)
