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目的研究载多柔比星(DOX)的胆固醇修饰乙二醇壳聚糖纳米粒(DCN-16)在荷S180瘤小鼠体内的组织分布。方法将多柔比星和DCN-16分别给动物静脉注射给药,用高效液相色谱法测定荷瘤小鼠不同组织中多柔比星的含量,对药物的体内分布特征和靶向性进行评价。结果 DCN-16能够长时间滞留在小鼠血液中,在荷瘤鼠中的心、肺、肾中的血药浓度-时间曲线下面积(AUC0→∞)比多柔比星组显著减小(P<0.05),在肝、脾和肿瘤组织中的AUC0→∞显著增多(P<0.05)。DCN-16在肿瘤中的相对摄取率(Re)为2.56。结论应用胆固醇修饰乙二醇壳聚糖纳米粒负载多柔比星后,能够使药物在血液中长时间循环,增加肿瘤靶向治疗效果和降低心脏的毒副作用。
Objective To investigate the tissue distribution of cholesterol-modified glycol chitosan nanoparticles loaded with doxorubicin (DOX) in S180 tumor-bearing mice. Methods Doxorubicin and DCN-16 were administered to animals intravenously. The contents of doxorubicin in different tissues of tumor-bearing mice were determined by high performance liquid chromatography (HPLC). The distribution characteristics and targeting of drugs in vivo Evaluation. Results DCN-16 was able to remain in the blood of mice for a long time. The area under the plasma concentration-time curve (AUC0 → ∞) in heart, lung and kidney of tumor-bearing mice was significantly decreased compared with that of doxorubicine P <0.05). The AUC0 → ∞ in liver, spleen and tumor tissues were significantly increased (P <0.05). The relative uptake (DC) of DCN-16 in tumors was 2.56. Conclusion Cholesterol-modified ethylene glycol chitosan nanoparticles loaded with doxorubicin can prolong the circulation of drugs in the blood, increase the efficacy of targeted therapy and reduce the side effects of the heart.