摘要
目的以聚乙二醇单甲醚-聚乳酸[methoxy poly(ethylene glycol)-poly(lactide),m PEG-PLA]嵌段共聚物为载体材料,制备他克莫司载药胶束,考察其制剂学性质。方法采用薄膜分散法制备他克莫司载药胶束。超速离心法测定他克莫司载药胶束的载药量和包封率。以载药量、包封率、粒径以及粒径分布为评价指标,采用单因素试验和正交试验优化他克莫司载药胶束制备处方。应用透射电镜、粒度测定仪和zeta电位分析仪对他克莫司载药胶束的形态、粒径和电位进行表征。结果在优化条件下制备的他克莫司载药胶束载药量为7.77%,包封率为84.31%,胶束粒子外观圆整且分散良好,平均粒径为23.20 nm,PDI为0.058,zeta电位为-0.831 m V。结论单因素试验联合正交试验可有效地优化他克莫司m PEG-PLA胶束处方和制备工艺。优化条件下制备的他克莫司载药胶束具有较高的载药量和包封率,粒径较小且分布均匀,24 h内稳定性良好。
Objective To prepare the tacrolimus-loaded miceUes using mPEG-PLA block copolymer and to characterize the physicochernical properties of the drug-loaded micelles. Methods Thin film dispersion method was applied to prepare tacrolimus-loaded micelles. Ultracentfifugation method was applied to measure the entrapment efficiency and loading content of the drug loaded micelles. Single-factor test and orthogonal design were used to optimize the formulation with entrapment efficiency, drug loading content, particle size and size distribution as indexes. The morphology, diameter and zeta-potential of the micelles were characterized by transmission electron microscopy and dynamic light scattering, respectively. Results The entrapment efficiency and loading content of tacrolimus-loaded micelles prepared according to the optimal conditions were 84. 31% and 7. 77% ,respectively. The micelles were globular in shape and the particle size was 23.20 nm with narrow distribution. The zeta potential of the micelles was - 0. 831 mV. Conclusions Single-factor test and orthogonal design can be successfully used to optimize the formulation and preparation process of tacrolimus-loaded micelles. The optimal tacrolimus-loaded micelles have relatively high entrapment efficiency, drug loading content and uniform particle size.
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2016年第9期679-685,695,共8页
Journal of Shenyang Pharmaceutical University
基金
国家自然科学基金资助项目(81273448)
关键词
他克莫司
聚乙二醇单甲醚-聚乳酸
薄膜分散法
胶束
单因素试验
正交试验
载药量
包封率
粒径
ZETA电位
tacrolimus
methoxy poly （ ethylene glycol ） -poly （ lactide ）
thin film dispersion method
micelle
single-factor test
orthogonal design
drug loading content
entrapment efficiency
particle size
zeta-potential
作者简介
董丽艳（1991-），女（汉族），辽宁沈阳人，硕士研究生，E-mail dongliyan4752@126．com；
通讯作者：乔明曦（1976-），男（汉族），辽宁盘锦人，副教授，博士，硕士生导师，主要从事药物制剂新技术与新型给药系统的研究，Tel．024-23986308，E-mallqiaomingxi@163．com。
