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目的 制备卡铂非离子型表面活性剂囊泡 ,以提高卡铂对肺癌的疗效并降低其毒副作用。方法 用薄膜分散法制备卡铂囊泡 ,紫外分光光度法测定药物的含量 ,二阶导数法测定体外释药。小鼠体内分布试验 ,用iv .S 180肿瘤细胞建立了肺肿瘤模型 ,计算瘤结节数。结果 卡铂囊泡平均粒径为 3 72 μm ,最小粒径为 2 0 μm ,最大粒径为 10 0 μm ,跨距为 0 6 6。卡铂囊泡包封率为 2 9 2 %。体外释药符合双指数方程的规律 ,释药T1/ 2 比原药延长9 14倍。体内分布研究表明 ,卡铂囊泡与原药相比 ,有明显的肺靶向性。卡铂泡囊对小鼠肺脏S 180肿瘤生长较原药的抑瘤作用有明显提高。结论 卡铂囊泡在体内有良好的肺靶向性
Objective To prepare carboplatin non-ionic surfactant vesicles to improve the efficacy of carboplatin in lung cancer and reduce its toxic and side effects. Methods Carboplatin vesicles were prepared by membrane dispersion method. The content of drugs was determined by UV spectrophotometry. The second derivative method was used to determine drug release in vitro. In vivo distribution of mice, a lung tumor model was established using iv.S 180 tumor cells, and the number of tumor nodules was calculated. Results The average particle size of carboplatin vesicles was 3 72 μm, the minimum particle size was 20 μm, the maximum particle size was 100 μm, and the span was 0 6 6 . Carboplatin vesicle entrapment efficiency was 292%. In vitro drug release is in accordance with the law of the double exponential equation, and the drug release T1/ 2 is 9 14 times longer than the original drug. In vivo distribution studies have shown that carboplatin vesicles have significant lung targeting compared to the original drug. The antitumor effect of carboplatin vesicles on the growth of mouse S 180 tumors was significantly higher than that of the original drug. Conclusion Carboplatin vesicles have good lung targeting in vivo