以卟啉衍生物为内核,采用可逆加成-断裂链转移(RAFT)聚合法合成了温度敏感性聚己内酯-聚N-异丙 基丙 烯 酰 胺。用FT-IR、1H NMR、GPC、TEM、分子荧光、变温紫外、粒度分布等手段对聚合物进行了表征,并以紫杉醇为模型药物分子,进行了药物释放测试。结果表明,聚合物自组装后,形成了平均直径为100nm左右的胶束。这种内部亲脂外部亲水的核壳结构能够稳定地载药,在温度为15℃的DMF中,12h内释放了37%的药物,而在温度为38℃的DMF中,12h药物释放量为81.4%。这种两亲性大分子聚合材料对紫杉醇的释放具有温度敏感性,有望在抗癌药物的控制释放领域得到广泛应用。
The thermosensitive copolymer poly(e-caprolactone)-b-poly(N-isopropylacrylamide) was synthesized by reversible addition-fragmentation chain transfer polymerization(RAFT) using a tetra-hydroxyethyl terminated porphyrin as a core initiator.The copolymer was characterized by fourier-transform infrared spectroscopy,1H NMR,gel permeation chromatography,transmission electron microscopy,molecule fluorescence,UV-Vis measurement and size distribution measurement.With Paclitaxel as model drug,the drug release behavior of the copolymeric micelles was studied.It was found that the sizes of copolymeric micelles were around 100nm after self-assembly.The paclitaxel loaded micelles were stable,in the release medium of 38℃ the release of paclitaxel was much quicker than that at 15℃.Therefore,the release of paclitaxel from the copolymeric micelles could be controlled by changing temperature.The SPPCL-PNIPAAm copolymeric micelles has a potential application in drug release.