5-FU纳米微粒的制备及其释药特性研究

Preparation of chitosan-5-fluorouracil nanometer particle and its drug-release characters

目的制备一种新型的载氟尿嘧啶（5-FU）纳米微粒并对其体内释药特性进行研究。方法运用聚合物交联法制备出壳聚糖载氟尿嘧啶纳米粒，通过扫描电镜、激光粒度分析仪对其表征进行检测，紫外分光光度法测定载药量，高效液相色谱法检测体内的释药特性。结果壳聚糖载氟尿嘧啶纳米粒呈圆形或椭圆形，分散性良好，粒径在120-150nm；载药量为31．000％±0．001％；壳聚糖-5-FU纳米粒注射入兔体内后，初期突释相约在1．5h，峰浓度为5069．6μg／L，随即进入缓释相，浓度维持在76μg／L，时间长达48h。结论壳聚糖纳米药物载体可改变5-FU在体内的药代动力学行为，延长其循环时间，具有良好的缓释作用。

Objective To prepare the nanometer particles （NPs） of chitosan-5-fluorouracil （5-FU）, and to study its characters of drug release in vivo. Methods Cross-linking polymer technique was employed to prepare the chitosan-5-FU NPs, and their characters were detected by scanning electron microscope and photon correlation spectroscope （PCS） ; the loaded capacity was measured by ultraviolet spectrophotometry; high-performance liquid chromatography was used to detect the characters of drug release in vivo. Results The chitosan-5-FU-NPs were found to be round or elliptic in shape, with 120 to 150nm in diameter and having a good dispersive ability. The loaded capacity was 31.000%±0. 001%. The blood concentration of 5-FU was controlled at 76μg/L, and it was maintained for 48h. Conclusion As a vehicle, chitosan-5-FU NPs can change the behavior of pharmacokinetics and prolong the cycle time of 5-FU in vivo. Chitosan-5-FU NPs ran reduce the initial burst and prolong the releasing time.