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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 monomethoxy polyethylene glycol-polylactic acid-glycolic acid nanoparticles (mPEG-PLGA-NP) and to study its physicochemical properties and in vitro anti-stick properties. Methods: Using mPEG-PLGA with different mPEG molecular weight and content as carrier, self-emulsifying solvent diffusion method was used to prepare nanoparticles. The preparation process was investigated by single factor. Furan diene was used as a model drug to investigate the drug-loading properties of nanoparticles, and the in vitro mucin binding method was used to evaluate the anti-adhesion properties of the nanoparticles. Results: The optimal formulation of mPEG-PLGA-NP prepared by self-emulsifying solvent diffusion method was determined. Acetone was organic solvent, 0.2% polysorbate 80 was used as emulsifier, the amount of mPEG-PLGA was 25mg, the volume of organic phase and water phase The ratio is 1:15. Nanoparticles spherical, the appearance of regular, evenly distributed. The mPEG-PLGA-NP gradually decreased in size with the increase of mPEG content, and the absolute value of Zeta potential decreased gradually. Fumedoprene containing mPEG-PLGA-NP encapsulation efficiency of 50%, drug loading of about 10%. In vitro mucin binding experiments showed that the mPEG-modified nanoparticles exhibited 6-fold higher anti-adhesion than the unmodified ones and the anti-adhesion ability of mPEG-PLGA-NP gradually increased with the increase of the relative molecular weight and mPEG content. Conclusion: mPEG-PLGA-NP was successfully prepared and characterized in this experiment, and mPEG-PLGA-NP has good drug loading and anti-adhesion properties.