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肽类树枝状大分子:自组装胶束及药物释放研究
Polypeptide dendrimers:Self-assembly and drug delivery
【摘要】 本文以三代聚谷氨酸肽类树枝状分子(G3-Glu)为大分子引发剂,引发N-羧基-L-苯丙氨酸-环内酸酐(NCA-Phe)的开环聚合反应,制备聚谷氨酸树枝状大分子-聚苯丙氨酸嵌段共聚物.嵌段共聚物通过自组装形成以聚苯丙氨酸链段为核,聚谷氨酸树枝状大分子为壳的胶束.将抗肿瘤药物阿霉素负载到高分子胶束中,研究其药物释放性能及体外抗肿瘤效果.结果表明,共聚物胶束具有良好的生物相容性.载药胶束具有药物缓释效果,药物持续释放时间可达60h.载药胶束的体外抗肿瘤实验表明其对肝癌细胞HepG2具有很好的杀灭效果,共培养48h后对癌细胞的杀死率可高达75%.
【Abstract】 Amphiphilic dendritic poly(glutamic acid)-b-polyphenylalanine copolymers were synthesized using generation 3 dendritic poly(glutamic acid) as the macroinitiator in the ring-opening polymerization of NCA-Phe.The block copolymers self-assembled micelles with polyphenylalanine segments as core and dendritic poly(glutamic acid) segments as shell.The biocompatibility of the micelles was studied.The release of the anticancer drug doxorubicin from the micelles was investigated in vitro.The results showed that the sustaining release of the drug could last for 60 h.The micellar drug release system was efficient in inhibiting the proliferation of HepG2 liver cancer cells,75% cancer cells were killed under appropriate in vitro incubation.
【Key words】 self-assembly; dendritic polypeptide block copolymer; drug delivery;
- 【文献出处】 中国科学:化学 ,Scientia Sinica(Chimica) , 编辑部邮箱 ,2011年02期
- 【分类号】TQ460.1
- 【被引频次】4
- 【下载频次】866