Effects of the Molecular Weight of PLGA on Degradation and Drug Release In vitro from an mPEG-PLGA Nanocarrier  

作　　者：LIU Rui WANG Yan MA Yudan WU Yi GUO Yi XU Li 

机构地区：[1]Key laboratory for Molecular Enzymology and Engineering, Ministry of Education, National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun 130012, P. R. China [2]Department of Endocrinology, China-Japan Union Hospital, Jilin University, Changehun 130033, P. R. China [3]College of Pharmacy, Jilin University, Changchun 130021, P. R. China [4]Jilin Research Institute of Sports Science, Changchun 130022, P. R. China

出　　处：《Chemical Research in Chinese Universities》2016年第5期848-853,共6页高等学校化学研究（英文版）

基　　金：Supported by the National Natural Science Foundation of China（Nos.81271697, 81571791, 31571017）.

摘　　要：We successfully synthesized four kinds of copolymers with varying molecular weights of poly（lactide- co-glycolide）（PLGA） to yield methoxy-poly（ethylene glycol）-block-poly（lactide-co-glycolide）（mPEG-PLGA） nano- carriers： mPEG-PLGA（3k）, mPEG-PLGA（9k）, mPEG-PLGA（llk） and mPEG-PLGA（16k）. An antitumor drug, 10-hydroxycamptothecin（HCPT）, was encapsulated into the mPEG-PLGA nanocarrier cores by self-assembly in dialysis. The lower molecular weight nanocarriers degraded more quickly, resulting in mass loss, pH decline, and a rapid HCPT release rate in vitro. The degradation and drug release of the nanocarriers were dependent on the PLGA molecular weight. However, the larger molecular weight nanocarriers could not increase the loading content and encapsulation efficiency. Considering the antitumor effect of these nanocarriers, the mPEG-PLGA（9k） nanocarrier, which had the highest drug loading content[（7.72±0.57）%] and a relatively high encapsulation efficiency [（22.71±5.53）%], is an optimum agent for drug delivery.We successfully synthesized four kinds of copolymers with varying molecular weights of poly（lactide- co-glycolide）（PLGA） to yield methoxy-poly（ethylene glycol）-block-poly（lactide-co-glycolide）（mPEG-PLGA） nano- carriers： mPEG-PLGA（3k）, mPEG-PLGA（9k）, mPEG-PLGA（llk） and mPEG-PLGA（16k）. An antitumor drug, 10-hydroxycamptothecin（HCPT）, was encapsulated into the mPEG-PLGA nanocarrier cores by self-assembly in dialysis. The lower molecular weight nanocarriers degraded more quickly, resulting in mass loss, pH decline, and a rapid HCPT release rate in vitro. The degradation and drug release of the nanocarriers were dependent on the PLGA molecular weight. However, the larger molecular weight nanocarriers could not increase the loading content and encapsulation efficiency. Considering the antitumor effect of these nanocarriers, the mPEG-PLGA（9k） nanocarrier, which had the highest drug loading content[（7.72±0.57）%] and a relatively high encapsulation efficiency [（22.71±5.53）%], is an optimum agent for drug delivery.

关 键 词：Poly（lactide-co-glycolide） 10-HYDROXYCAMPTOTHECIN NANOCARRIER Drug delivery 

分 类 号：O[理学]