Lu B, Zhang J Q, Yang H
West China School of Pharmacy, Sichuan University, #17, 3rd Block, Renmin South Road, Chengdu 610041, China.
Int J Pharm. 2003 Oct 20;265(1-2):1-11. doi: 10.1016/s0378-5173(03)00332-6.
Carboplatin (CPt) was incorporated in the gelatin microspheres by the method of emulsion and the drug content determined spectrophotometrically. The arithmetic mean diameter of the microspheres was 13.20 microm with 98% of the microspheres ranging from 5.0 to 28.6 microm. The average carboplatin content was 23.76% and the yield of the microspheres 85.12%. The microspheres were stable for three months when stored at 37 degrees C/RH 75%, showing insignificant change in appearance and drug content. The in vitro release profile of the microspheres could be described by a biexponential equation, and the release t(1/2) was 49.7 min and 92.04% released in 10h; while for the original drug, CPt, under the same conditions, 92.15% released in the first half an hour. Very high lung-targeting efficiency in vivo was proved by the results of targeting parameters. The S-180 lung neoplasm models were established by i.v. cancer cells in mice and the number of pulmonary nodules examined for evaluation of the treatment effect. The results of therapeutic tests showed that the antitumour effects were increased by injection of the microspheres compared with the injection of CPt solution: half of the dose in the microspheres showed comparable effect to the original drug.
采用乳化法将卡铂（CPt）载入明胶微球中，并通过分光光度法测定药物含量。微球的算术平均直径为13.20微米，98%的微球直径在5.0至28.6微米之间。卡铂的平均含量为23.76%，微球产率为85.12%。微球在37℃/相对湿度75%条件下储存三个月时稳定，外观和药物含量无明显变化。微球的体外释放曲线可用双指数方程描述，释放t(1/2)为49.7分钟，10小时内释放92.04%；而在相同条件下，原药CPt在半小时内释放92.15%。靶向参数结果证明微球在体内具有很高的肺靶向效率。通过给小鼠静脉注射癌细胞建立S-18肿瘤模型，并检查肺结节数量以评估治疗效果。治疗试验结果表明，与注射CPt溶液相比，注射微球可增强抗肿瘤效果：微球中一半剂量的效果与原药相当。
