PEG化PAMAM树状大分子的合成及其作为药物载体的研究

Synthesis of PEGylated PAMAM Dendrimer as a Drug Carrier

研究经聚乙二醇(PEG)进行表面修饰的聚酰胺-胺树枝状大分子作为药物载体时对药物的包裹及释放能力。用经三氟乙基磺酸单甲氧基(Tresylate)活化的相对分子质量为5000的单甲氧基聚乙二醇(Tresylated MPEG-5000)对聚酰胺-胺G4.0-PAMAM树状大分子修饰,目标产物PEG化树状大分子用FT-IR1、H NMR进行结构表征。MTT研究其细胞毒性。通过包裹与释放实验研究该药物载体对抗癌药物甲氨蝶呤(MTX)的包裹及释放能力。每个修饰后的树状大分子可包裹33个抗癌药物甲氨蝶呤分子,细胞毒指数较低,释药速度减慢。修饰后的树状大分子与未PEG化的树状大分子载体相比具有更强的包裹能力,并具有一定的药物缓释功能;细胞毒性试验表明,其胞毒性与未PEG化的树状大分子相比明显偏低。

To investigate the drug host and release behaviors of PEG modified polyamidoamine（PAMAM） dendrimer.PEGylated PAMAM dendrimer was prepared by modifying G4.0 PAMAM dendrimer with tresylated MPEG-5000.The PEGylated PAMAM dendrimer was characterized by FT-IR and（）-1H NMR.The cytotoxicity of the PEGylated PAMAM dendrimer was tested by MTT.The potential of the PEGylated PAMAM dendrimer as an anti-tumor drug carrier was evaluated using methotrexate（MTX） as a model drug.Each PEGylated G4.0 PAMAM could host 33 MTX molecules.In addition,PEGylated PAMAM exhibited lower cytotoxicity and controlled release behavior in vitro.PEGylated PAMAM dendrimer exhibits a greater drug host and release capability as well as a lower cytotoxicity in comparison with non-PEGylated PAMAM dendrimer.