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目的制备PAMAM-PEG-C_(12)-hyd-DOX酸敏感高分子聚合物胶束,延长其在体内的循环时间。方法树状高分子聚酰胺通过酸敏感的腙键共轭阿霉素形成两亲性高分子聚合物。通过改良的薄膜溶剂法自组装形成胶束,~1HNMR法与紫外分光光度法分别确证PEG与阿霉素的接枝率,粒度仪测定其粒径及电位,并对阿霉素胶束的体外释放药物特性进行了研究。结果树状高分子聚酰胺通过腙键键合阿霉素聚合物胶束的平均粒径为(68.4±2.4)nm,Zeta电位为-8.42 mV。通过酰胺键连接的聚合物的平均粒径为(163.4±3.6)nm,Zeta电位为36.03 mV。PAMAM-PEG-C_(12)-hyd-DOX聚合物胶束较PAMAM-PEG-C_(12)-amide-DOX聚合物胶束具有明显的pH敏感性。结论该载体材料具有良好的物理特性和缓释效果,作为抗肿瘤药物的靶向传递系统具有良好的应用前景。
Objective To prepare PAMAM-PEG-C_ (12) -hyd-DOX acid-sensitive macromolecule micelles and prolong their cycle time in vivo. Methods Dendrimer polyamides form amphipathic polymers via acid-sensitive hydrazone bonds. The micelles were self-assembled by modified thin film solvent method. The grafting degree of PEG and doxorubicin were confirmed by ~ 1HNMR and UV spectrophotometry respectively. The particle size and potential of PEG and doxorubicin were determined by particle size analyzer. Drug release characteristics were studied. Results The mean particle size of dendrimer polymer micelles was (68.4 ± 2.4) nm and the zeta potential was -8.42 mV via hydrazone bond. The average particle diameter of the polymer linked by the amide bond was (163.4 ± 3.6) nm and the zeta potential was 36.03 mV. PAMAM-PEG-C_ (12) -hyd-DOX polymer micelles have obvious pH sensitivity than PAMAM-PEG-C_ (12) -amide-DOX polymer micelles. Conclusion The carrier material has good physical properties and sustained release effect, and has good application prospect as a target delivery system of anti-tumor drugs.