摘要
目的:合成聚乙二醇单甲醚-聚己内酯(m PEG-PCL)嵌段聚合物,制备聚合物囊泡并考察胰岛素(INS)-m PEG114-PCL152的体外释药行为。方法:利用开环反应制备不同相对分子质量的m PEG-PCL聚合物并对其结构进行表征确定。采用薄膜水化法制备聚合物囊泡,激光散射法测定粒径,透射电镜考察表观形态,芘荧光探针法测定临界聚集浓度值(CAC)。利用Bradford法测定INS-m PEG114-PCL152的载药情况及其体外释放行为。结果:空白囊泡粒径约200 nm,CAC均较小。20%投药比例制备的载药囊泡模型药物INS-m PEG114-PCL152利用度最大,包封率(62.80±2.14)%,载药量(11.10±0.34)%;体外释药考察前2 h突释19.28%,48 h后累积释药55.05%,符合Higuchi模型。结论:m PEG-PCL共聚物囊泡粒径适中,抗稀释能力强。INS-m PEG114-PCL152具有较明显突释效应,随着表面结合的INS的解离,逐渐呈良好缓释作用。
Objective： To prepare mPEG-PCL copolymer and polymersomes, then investigate in vitro release of INS-mPEG114-PCL152 polymersomes. Method： mPEG-PCL block copolymer was synthesized by ringopening polymerization method, chemical structure of these polymers were characterized by FT-IR and ^1H-NMR. Polymersomes were prepared by film hydration method, particle size and apparent morphology were examined by dynamic light scattering and transmission electron microscope, respectively; critical aggregation concentration （CAC） was detected by fluorescence techniques with pyrene as a probe. Encapsulation efficiency, drug loading and in vitro release characteristic of INS-mPEG114-PCL152 polymersomes were determined by Bradford method. Result： Average particle sizes of blank polymersomes were about 200 nm, CAC were all low value. These prepared INS-mPEG114-PCL152 with 20% drug-copolymer ratio had maximize utilizaiton ratio, average encapsulation efficiency （62.80 ± 2. 14）% as well as drug loading （11. 10 ± 0. 34）%. In vitro cumulative release of INS-mPEG114-PCL152 polymersomes in 48 h was about 55.05% , with relatively significant burst release at initial 2 h about 19.28%. Conclusion： These polymersomes have uniform particle size with a great anti-dilution capability. INS-mPEG114-PCL152 polymersomes show a significant burst release at initial stage and then a good sustained-release property with dissociation of surface model drug.
出处
《中国实验方剂学杂志》
CAS
北大核心
2014年第23期15-21,共7页
Chinese Journal of Experimental Traditional Medical Formulae
基金
广州市科技计划项目(12C32121550)
关键词
聚乙二醇单甲醚-聚己内酯
胰岛素
聚合物囊泡
载药量
体外释药特性
polyethylene glycol monomethyl ether-polycaprolactone
insulin
polymersomes
drug loading
in vitro release characteristics
