碳铂壳聚糖缓解释微球的制备

The manufacture of chitoson polymer microsphere with carboplatin

碳铂由于其水溶性高、半衰期短极大地限制了它在颅脑恶性肿瘤化疗中的使用 ,为此我们选用了壳聚糖作为载体制备了碳铂壳聚糖缓释微球用于颅脑恶性肿瘤瘤内化疗。方法 :我们参照了GuptaPK的统计学处理方法 ,引入“理想函数”全面优化微球的制备工艺 ,得到的微球载药量大 ,粒径分布适宜 ,工艺重现性好。通过多元线性回归分析 ,我们发现壳聚糖的浓度、固化时间、壳聚糖材料的类型及搅拌速度可能对粒径分布影响较大(P <0 .0 1) ,而壳聚糖的浓度与投药量的比例决定药物的包封率。结果 :在我们制备的药物包封率为 10 %的微球中的到了良好的外观性状、达两周的控释能力和很好的微球刚性 ,体外释放实验证实药物微球的释放曲线平缓无突释现象。结论 :我们制备的碳铂壳聚糖缓解微球物理性状良好 ,载药适中控释能力强 ,具有临床实际使用价值。

Objective:Because of high water resoluble and short half life, the carboplatin is much limited in the use of treatment in craniocerebral malignant tumor. We manufactured carboplatin polymer microsphere with chitoson as the carrier to improve the treatment effect of carboplatin in craniocerebral malignant tumor. Methods:After careful consideration, we use 'idea function' to arrange our manufacture process. We find that the concentration of chitoson, solid time, the type of chitoson structure and mixture speed affect the diameter of microsphere, but the concentration of chitoson and drug proportion affect drug envelopment into the microsphere. Results:Finally our chitoson polymer microsphere which carried 10% carboplatin have a good appearance without drug crystal on surface, have stable structure even after drug released two weeks, have a smooth release curve without any 'burst effect'. Conclusion:The chitoson polymer microsphere carried with carboplatin we made have a excellent physical quality, powerful controlled release ability and promising clinical future.