聚乙二醇化聚乳酸羟基乙酸纳米粒的制备及体外抗黏性能评价  

Preparation and properties of mPEG-PLGA nanoparticles and evaluation of their in vitro anti-adhesive ability

作　　者：谢鑫鑫[1] 王俊腾[1] 秦利芳[1] 闻真[1] 郭桂萍[1] 林东海[1] 

机构地区：[1]烟台大学药学院,山东烟台264005

出　　处：《中国医院药学杂志》2012年第21期1727-1731,共5页Chinese Journal of Hospital Pharmacy

基　　金：国家自然科学基金资助项目(编号:30973949);山东省自然科学基金资助项目(编号:ZR2009CM012)

摘　　要：目的:制备单甲氧基聚乙二醇-聚乳酸-羟基乙酸纳米粒(mPEG-PLGA-NP)并研究其理化性质及体外抗黏性能。方法:以不同mPEG分子量和含量的mPEG-PLGA为载体,采用自乳化溶剂扩散法制备纳米粒,并对其制备处方工艺进行单因素考察。以呋喃二烯为模型药考察纳米粒的载药性能,采用体外黏蛋白结合法评价纳米粒的抗黏性能。结果:确定自乳化溶剂扩散法制备mPEG-PLGA-NP的最佳处方,丙酮为有机溶剂,0.2%的聚山梨酯80为乳化剂,mPEG-PLGA的用量为25mg,有机相和水相的体积比为1∶15。纳米粒呈球形,外观规整,分布均匀。mPEG-PLGA-NP随着修饰的mPEG含量的增加粒径逐渐减小,Zeta电位的绝对值逐渐减小。载呋喃二烯的mPEG-PLGA-NP包封率为50%,载药量在10%左右。体外黏蛋白结合实验显示,经mPEG修饰的纳米粒抗黏性比未修饰的高6倍,并且随着修饰的mPEG相对分子质量和含量的增加,mPEG-PLGA-NP的抗黏性能逐渐增强。结论:本实验成功制备并表征了mPEG-PLGA-NP,并且mPEG-PLGA-NP具有良好的载药和抗黏性能。OBJECTIVE To prepare mPEG-PLGA nanoparticles and discuss its physicochemical characterization and anti-adhesive ability.METHODS mPEG-PLGA-NP was prepared by self-emulsion solvent diffusion technique with different amount of mPEG-PLGA as the carrier.The preparation conditions were optimized by means of monofactorial design.Drug-loaded properties of mPEG-PLGA-NP were studied with furanodiene.The in vitro anti-adhesive activity of nanoparticles was evaluated by pig gastric mucin（PM） binding experiments.RESULTS The optimized preparation conditions were obtained as follows： organic solvents was acetone,0.2% Tween-80 was emulsifiers,the amount of mPEG-PLGA was 25 mg,the volume ratio of organic and aqueous phase was 1：15.Particle size and the absolute value of Zeta potential of mPEG-PLGA-NP decreased gradually with the increase of mPEG content.Encapsulation efficiency of mPEG-PLGA-NP was about 50%,drug-loading of mPEG-PLGA-NP was about 10%.PM binding experiments showed that,the anti-adhesive activity of mPEG-PLGA-NP was six times higher than PLGA-NP,and it was increased gradually with the increase of mPEG molecular and content.CONCLUSION This study successfully prepared mPEG-PLGA-NP and characterized its properties.mPEG-PLGA-NP has good drug loading and anti-adhesive activity.

关 键 词：单甲氧基聚乙二醇-聚乳酸-羟基乙酸 纳米粒 呋喃二烯 黏蛋白 抗黏 

分 类 号：R943[医药卫生—药剂学]