转铁蛋白修饰的喜树碱-树枝状高分子复合物的药动学研究

Study on tumor active targeting with Transferrin-PEG-PAMAM dendrimer-CPT conjugate

目的探讨转铁蛋白修饰的主动靶向纳米载药复合物在大鼠体内的药动学行为。方法碱水解后采用HPLC法测定大鼠尾静脉给药后血浆中的药物浓度。结果经转铁蛋白修饰的主动靶向复合物能显著提高喜树碱在大鼠体内的半衰期及平均滞留时间,比未经转铁蛋白修饰的载药复合物的半衰期的平均滞留时间短。结论转铁蛋白-聚乙二醇-聚酰胺-胺树枝状分子-喜树碱复合物具有显著的长循环效果。关键词:聚酰胺-胺树枝状聚合物;转铁蛋白;聚乙二醇;喜树碱;

Objective To explore the pharmacokinetics characteristic of transferrin modified PEG ylated polyamidoamine dendrimers（PEG-PAMAM） as the carrier for tumor targeting of the anticancer drug camptothecin（CPT） in rats.Methods CPT solution and PEG-PAMAM-CPT were used as control,transferrin modified PEG-PAMAM-CPT was injected via the tail vein.The plasma concentration of CPT in rats was determined by HPLC following alkaline hydrolysis.Results Transferrin modified PAMAM-PEG-CPT could enhance half-life and mean residence time comparing with that of CPT solution,but were relative shorter than that of CPT-PAMAM-PEG.Conclusion Transferrin modified PAMAM-PEG-CPT had a better long-circulating effect in rats.