BCNU缓释微球体内外释放与分布  

In vitro and in vivo release and disposition of BCNU sustained release microspheres

作　　者：章文斌[1] 马晓东[2] 张岩松[1] 刘宏毅[1] 常义[1] 周定标[2] 

机构地区：[1]南京医科大学附属脑科医院神经外科,210029 [2]中国人民解放军总医院神经外科

出　　处：《临床神经外科杂志》2007年第1期27-30,共4页Journal of Clinical Neurosurgery

摘　　要：目的探讨自制卡氮芥（BCNU）聚乳酸-羟基乙酸（PLGA）缓释微球的体内外药物释放过程以及在大鼠脑组织的分布与其生物相容性。方法应用高效液相色谱法检测BCNU在磷酸盐缓冲溶液和脑组织内自聚乳酸．羟基乙酸缓释微球释放的药物含量；应用3H标记BCNU，检测3H—BCNU缓释微球在正常大鼠脑组织及血清中的分布；BCNU缓释微球植入大鼠脑组织，常规HE染色，光镜下观察其生物相容性。结果BCNU-PLGA-MS在PBS和大鼠脑组织中均可持续释放药物2周以上；缓释剂植入侧脑组织药物浓度比对侧高6．70倍；大鼠脑组织表现为小胶质细胞反应。结论BCNU—PLGA缓释微球具有良好的缓释功能，而且安全性、生物相容性较好。Objective To explore the in vitro and in vivo course of BCNU released from BCNU-loaded PLGA mierospheres and location in rat brain tissue. Methods The concentrations of BCNU in PBS and brain tissue were determined by high performance liquid chromatography, and 3H-labeled BCNU was used to determine the location in normal brain tissue and serum. The biocompatibility of mierospheres was evaluated by the routine HE stain. Results The BCNU could be sustained released from BCNU-PLGA-MS over 2 weeks both in PBS and in brain tissue, and the concentrations of BCNU in ipsilateral side was 6 to 70 times higher than those in eontralateral. The rat brain tissue demonstrated gIial cell reaction. Conclusion BCNU-PLGA sustained release microspheres are safe and biocompatible.

关 键 词：BCNU PLGA 释放动力学 分布 生物相容性 

分 类 号：R730.53[医药卫生—肿瘤]