灯盏花素壳聚糖纳米粒的构建及大鼠药动学研究

Construction of Breviscapine Chitosan Nanoparticles and Pharmacokinetics in Rats

目的:制备用于注射的灯盏花素壳聚糖纳米粒,考察其在大鼠体内药动学。方法:采用离子凝胶化法制备灯盏花素壳聚糖纳米粒,并观察其微观形态,测定粒径分布和Zeta电位,考察其体外释药特征;测定灯盏花素壳聚糖纳米粒在大鼠体内药动学情况。结果:本研究制备的灯盏花素壳聚糖纳米粒在透射电镜下可观察呈球状分布,其粒径为(98.5±16.4)nm,多分散系数(PdI)为(0.157±0.009),Zeta电位为(+12.2±1.8)mV,包封率为(95.4±1.5)%;灯盏花素壳聚糖纳米粒体外释药前期较快,后期缓慢;大鼠药动学结果显示,灯盏花素壳聚糖纳米粒的半衰期(t1/2)及药-时曲线下面积(AUC0~∞)分别是灯盏花素注射剂的2.57倍和3.92倍。结论:本研究制备的灯盏花素壳聚糖纳米粒可以延长循环时间,提高药物生物利用度。

Objective:To prepare breviscapine chitosan nanoparticles for injection,and investigate its pharmacokinetics in rats.Methods:Breviscapine chitosan nanoparticles were prepared by an ionic gelation method.The microscopic morphology was observed,and the particle size distribution and zeta potential were measured.The in vitro release characteristics were investigated.The pharmacokinetics of breviscapine chitosan nanoparticles in rats was determined.Results:The prepared breviscapine chitosan nanoparticles were found to be spherical with the particle size of(98.5±16.4)nm,PdI of(0.157±0.009),zeta potential of(+12.2±1.8)mV and encapsulation efficiency of(95.4±1.5)%.The breviscapine chitosan nanoparticles were released faster in the early stage and slower in the later stage.The pharmacokinetic results showed that the t1/2and AUC0-tof breviscapine chitosan nanoparticles was 2.57 times and 3.92 times higher than that of breviscapine injection.Conclusion:Breviscapine chitosan nanoparticles prepared in the study can prolong the cycle time and improve the bioavailability of drug.