pH/温度双重敏感型纳米凝胶的制备及性质研究  

Preparation and Characterization of pH and Temperature Sensitive Nanoparticles

作　　者：李飞[1] 吴红[1] 张慧[1] 范黎[1] 张海涛[1] 任波[2] 

机构地区：[1]第四军医大学药学系化学教研室,陕西西安710032 [2]解放军第302医院,北京100039

出　　处：《解放军药学学报》2008年第5期377-381,共5页Pharmaceutical Journal of Chinese People's Liberation Army

基　　金：国家自然科学基金资助项目;No.30300456;30770573;全军医药卫生科研基金课题;No.06Q064

摘　　要：目的制备具有pH／温度双重敏感的聚（马来酰化葡聚糖／N-异丙基丙烯酰胺）[P（Dex-MA／NIPA）]纳米凝胶，研究释药特性。方法乳液聚合法制备不同配比的聚（马来酰化葡聚糖／N-异丙基丙烯酰胺）纳米凝胶，测定临界相变温度（LCST）以及不同pH下的粒径；以羟基喜树碱（HPCT）为药物模型，动态透析法研究其不同pH和温度下的智能释药特性。结果P（Dex-MA／NIPA）纳米凝胶的LCST与Dex／MA和NIPA的比例有关，并且可调节至35-45℃；pH2．0、7．5的缓冲液里，粒径分别为62、273nm，包裹率、载药率分别为62．94％、0．82％。37℃时在pH为2．0、5．0、7．5的缓冲液中12h后的药物释放累积率为11％、19．65％、33％；pH7．5时在37、40~C的介质中4h后药物释放累积率分别为15％、25％。结论P（Dex-MA／NIPA）纳米凝胶具有pH／温度双重敏感性，有望成为智能型控释和靶向性抗肿瘤药物载体。Aim To prepare pH and temperature sensitive p（Dex-MA/NIPA） nanoparticles, and study the prop- erties of the drug release. Methods P（ maleilated dextran/N-isopropylacrylamide） （p（Dex-MA/NIPA））nanopartieles were first synthesized by emulsion polymerization. At different pH, temperatures, size distribution and drug release of p（Dex-MA/NIPA） nanoparticles were determined. Results The size of nanoparticles was 62nm and 273nm in different pH buffer solutions, p （Dex-MA/NIPA） nanoparticles with lower critical solution temperatures （LCST） ranging from 35℃ to 45℃ were correlated to the molar fraction of maleilated dextran copolymerized with NIPA. Drug loading and encapsulation efficiency were 62.94% ,0.82% respectively. In vitro drug release there were sig- nificant differences in different pH and temperatures. Conclusion p （Dex-MA/NIPA） nanoparticles respond to pH and temperature stimulis, which are promising candidates for novel drug carriers with advantages of controlled re- lease and targeting effect.

关 键 词：N-异丙基丙烯酰胺(NIPA) 马来酰化葡聚糖(Dex-MA) 纳米凝胶 pH/温度敏感 

分 类 号：R944.2[医药卫生—药剂学]