羟基喜树碱阳离子聚合物纳米粒的制备和体外性质评价  

Preparation and property evaluation in vitro of 10-hydroxycamptothecin cationic polymer nanoparticles

作　　者：杨经安[1] 李娟[1] 王晶[1] 

机构地区：[1]中国药科大学药剂学教研室,南京210009

出　　处：《中国新药杂志》2013年第3期274-278,共5页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2009ZX09310-004)

摘　　要：目的:合成直链聚乙烯亚胺(linear polyethyleneimine,LPEI)接枝单甲氧基聚乙二醇(methoxypolyethylene,mPEG)/聚己内酯(polyε-Caprolactone,PCL)的双亲性阳离子聚合物(mPEG-LPEI-PCL)用于制备阳离子型10-羟基喜树碱纳米粒(10-hydroxycamptothecin nanoparticles,HCPT-NPs),并对其体外性质进行评价。方法:通过IR和1H-NMR表征聚合物结构;采用改进的薄膜分散法制备HCPT-NPs,然后考察纳米制剂的粒径、电势、包封率、稳定性和形态,透析法研究HCPT-NPs的体外释放。结果:HCPT-NPs平均粒径为(155.6±9.6)nm,Zeta电位为(29.6±3.2)mV,包封率和载药量分别为(92.6±1.1)%和(4.49±0.02)%,释放速率随pH值升高而加快。结论:成功合成双亲性聚合物mPEG-LPEI-PCL,该聚合物能自组装形成核-壳结构纳米粒,4℃下稳定性良好。Objective：To synthesize linear polyethyleneimine grafted mPEG and PCL （mPEG-LPEI-PCL） as an amphiphilic cation polymer used to prepare cationic 10-hydroxycamptothecin nanopartieles （HCPT-NPs） and to evaluate its properties in vitro, nethods：IR and X H-NMR were used to characterize the structure of the polymer, and HCPT-NPs were prepared by modified film dispersion method. Thereafter, the size, Zeta potential, entrapment efficiency, stability and morphology were studied. Additionally, the drug release performance of HCPT-NPs was test- ed using dialysis method in vitro. Results：The mean diameters, Zeta potential, entrapment efficiency and drug load- ing of HCPT-NPswere （155.6±9.6） nm,（29.6±3.2） mV,（92.6±1.1）% and （4.49±0.02）%,respectively. The drug release speed appeared faster with pH value increasing. Conclusion：The amphiphilic polymer mPEG- LPEI-PCL is successfully synthesized, which enables self-assembly to form cationic core-shell structure nanoparti- cles. The nanoparticles have good stability when stored at 4 ℃.

关 键 词：10-羟基喜树碱 阳离子纳米粒 薄膜分散法 体外释放 

分 类 号：R943.42[医药卫生—药剂学] R979.1[医药卫生—药学]