PLGA/O-CMC载药纳米微粒的体外降解及释药行为研究  

The Degradation and Release Behavior of 5-fluorouracil-loaded PLGA/O-CMC Nanoparticles In vitro

作　　者：胡云霞[1] 原续波[1] 郭毅[1] 常津[1] 宋存先[2] 

机构地区：[1]天津大学材料科学与工程学院纳米生物技术研究所,天津300072 [2]中国医学科学院生物医学工程研究所,天津300192

出　　处：《中国生物医学工程学报》2005年第4期492-497,共6页Chinese Journal of Biomedical Engineering

基　　金：国家自然科学基金资助项目(50373033)。

摘　　要：本研究以聚乳酸乙醇酸共聚物(PLGA)和自行制备的O羧甲基壳聚糖(OCMC)为原料,以5氟尿嘧啶(5FU)为抗癌药物模型,采用自身设计的改良复乳法制备了载药纳米微粒。微粒平均粒径为98.5nm,粒径分布指数为0.192,粒子表面ξ电位为61.48eV,载药率高达18.9%。然后用SEM动态监测载药纳米粒子降解过程中表面形貌的变化,并连续追踪粒子降解过程中的质量损失和降解介质的pH变化。载药纳米粒子在PBS中的释药行为研究表明,(1)前12h的释药动力学符合Huguchi方程,具有一级释放特性;(2)在20d内的释药动力学符合零级释放特性。细胞凋亡实验结果表明载药纳米粒子对TJ905脑胶质瘤细胞增殖有明显的抑制作用。Poly （ D, L-lactide-co-glycolic acid） （PLGA） and o-carboxymethyl chitosan （O-CMC） were chosen to microencapsulate 5-fluorouracil （5-FU）by improved W/O/W method due to their attractive degradation and physicochemical properties;The results of characterizing 5-FU-loaded nanoparticles（NPs）showed that the mean size of NPs was 98.5nm, polydispersity was 0.192, zeta potenial was 61.48eV, and 5-FU-loading level was 18.9% respectively. SEM was used to study the morphological change of NPs during the degradation;and the weight loss of NPs and pH change of degradation medium were also observed as well. The investigation of 5-FU release behavior from NPs showed that（ 1 ）the release kinetics of 5-FU from NPs in early 12 hours was coincided with Huguchi release equation; （2）the release kinetics in 20 days was coincided with zero-level release.

关 键 词：O-羧甲基壳聚糖 聚乳酸-乙醇酸共聚物 纳米微粒 抗癌药物 细胞凋亡 

分 类 号：R318.08[医药卫生—生物医学工程]