聚酰胺-胺树状大分子及其PEG修饰物的合成、表征与载药性能

Synthesis,characterization and property of loading drug of polyamide-amine dendrimers and PEG-poly-amidiamine

目的合成并表征各代聚酰胺-胺(polyamide-amine,PAMAM)树状大分子及聚乙二醇(poly-ethylene glycol,PEG)修饰PAMAM,研究其对难溶性药物的包载及释放行为。方法用发散法合成1-5代PAMAM大分子及PEG化PAMAM,采用IR、NMR、端基滴定、GPC等方法对其进行表征,并以阿霉素为模型药物,比较PAMAM和PEG-PAMAM载药能力及释放效果。结果FTIR、NMR、端基滴定、GPC测定结果表明所合成的产物确为1-5代PAMAM树状大分子,IR测定结果表征PEG化PAMAM合成,PAMAM大分子及PEG-PAMAM对难溶性药物具有较强包载能力,其中PEG-PAMAM能够更好地延缓药物释放。结论PEG-PAMAM大分子具有良好的作为难溶性药物载体的潜力。

Objective To synthesize and characterize the 1-5 generation polymer of polyamide-amine（PAM- AM） and PEG-PAMAM, and study the capacity of loading drug and in vitro release. Methods The 1- 5 generation PAMAM dendrimers were synthesized by means of divergent procedure. Their structures were char-acterized by FTIR, ^1H NMR, end-group titration, and GPC. Using adriamycin as model drug, comparing the capacity of loading drug and in vitro release of PAMAM and PEG-PAMAM. Results The results of FTIR, ^1H-NMR, end-group titration, and GPC demonstrated the success in the synthesis of 1-5 generation PAMAM and PEG-PAMAM. Both PAMAM and PEG-PAMAM have good capacity of loading insoluble drug, and PEG-PAMAM can further sustained the release of adriamycin. Conclusions PEG-PAMAM have good potent of being used as carder of insoluble drug.