新型树状大分子PAMAM-Poloxamer的合成及作为药物载体的体外试验

Synthesis of PAMAM-Poloxamer Dendrimers and in vitro Test as a Drug Carrier

作者：马丽芳(四川大学化工学院制药与生物工程系)；郑云(四川大学化工学院制药与生物工程系)；戴华胄(四川大学化工学院制药与生物工程系)；王宇飞(四川大学化工学院)；郭丽(四川大学华西药学院)

Author：Ma Li-fang()；()；()；王宇飞()；郭丽(West China School of Pharmacy, Sichuan University)

收稿日期：2010-01-20 年卷（期）页码：2011,43(1):190-194

期刊名称：工程科学与技术

Journal Name：Advanced Engineering Sciences

关键字：聚酰胺胺-泊洛沙姆树状大分子；合成；细胞毒性；药物载体

Key words：PAMAM-poloxamer dendrimers; synthesis; MTT; drug carrier

基金项目：其它

中文摘要

目的合成新型树状大分子聚酰胺胺-泊洛沙姆（PAMAM-Poloxamer），考察其作为药物载体的可行性。方法将泊洛沙姆188一端羟基以硫酸二甲酯甲基化，另一端羟基经过对硝基苯基氯甲酸酯活化，与PAMAM G2.0连接，目标产物PAMAM-Poloxamer用FT-IR、1HNMR进行结构表征。MTT研究其细胞毒性。通过体外增溶实验研究该药物载体对难溶抗癌药物喜树碱的增溶作用，以及pH对增溶作用的影响；通过光敏性试验研究其对喜树碱光敏性的稳定能力。结果通过上述方法成功合成树枝状大分子PAMAM-Poloxamer，其细胞毒性与PAMAM相比有所降低；对喜树碱有较好的增溶作用；对喜树碱光不稳定性具有很好的稳定作用。结论树枝状大分子PAMAM-Poloxamer有望成为一种新型药物载体材料。

英文摘要

Polymeric drug delivery systems are used to improve aqueous solubility and photostability. Camptothecin (CPT) is a plant alkaloid that is practically insoluble in water and photosensitive. In this study, PAMAM-Poloxamer dendrimers were synthesized and characterized by FT-IR and 1HNMR. Their cytotoxicity was investigated by MTT assay . The potential of PAMAM-poloxamer dendrimers as drug carriers of CPT by improving aqueous solubility and photostability was researched. The results showed that PAMAM-Poloxamer dendrimers exhibited lower toxicity in comparison with PAMAM., and could increase the solubility and photostability of CPT. These studies indicated that PAMAM-poloxamer dendrimers might be considered as a new drug carrier.

【关闭】

论文摘要

新型树状大分子PAMAM-Poloxamer的合成及作为药物载体的体外试验

Synthesis of PAMAM-Poloxamer Dendrimers and in vitro Test as a Drug Carrier