论文部分内容阅读
目的:利用自制的羧基结尾的嵌段聚合物甲氧基聚乙二醇-聚乳酸(mPEG-PLA-COOH)和7-乙基-10-羟基喜树碱(SN38)合成聚合物-药物连接物mPEG-PLA-SN38,并评价其质量。方法:利用自制的两亲性嵌段共聚物mPEG-PLA-COOH与抗癌药物SN38合成mPEG-PLA-SN38连接物,1H-NMR法表征结构,HPLC法考察纯度;UV法测定载药量,考察连接物水分散体的粒径和体外释药行为。结果:mPEG-PLA-SN38的纯度达到99.51%;载药量为3.6%;水分散体平均粒径在70 nm以下,多分散系数为0.24;体外96 h累积释药8.8%。结论:成功制备了mPEG-PLA-SN38连接物,该连接物具有良好的缓释特征。
OBJECTIVE: To synthesize polymer-drug conjugates by using self-made carboxyl-terminated block copolymers of methoxypolyethylene glycol-polylactic acid (mPEG-PLA-COOH) and 7-ethyl-10-hydroxycamptothecin MPEG-PLA-SN38 and evaluated its quality. Methods: The mPEG-PLA-SN38 conjugate was synthesized by self-made amphiphilic block copolymer mPEG-PLA-COOH and antitumor drug SN38. The structure was characterized by 1H-NMR and the purity by HPLC. The particle size and in vitro release behavior of the aqueous dispersions were investigated. Results: The purity of mPEG-PLA-SN38 reached 99.51%. The drug loading was 3.6%. The average particle size of the aqueous dispersion was under 70 nm. The polydispersity index was 0.24. CONCLUSION: The mPEG-PLA-SN38 conjugate has been successfully prepared and has good sustained-release characteristics.