辣椒碱多囊脂质体的制备及在大鼠体内的药动学研究

Preparation of Capsaicin multivesicular liposomes and its pharmacokinetics in the rats

目的制备辣椒碱多囊脂质体,并考察其包封率和在大鼠体内的药动学。方法采用复乳法制备辣椒碱多囊脂质体、单因素筛选处方,并考察大鼠sc辣椒碱多囊脂质体后的体内药动学。结果制备的辣椒碱多囊脂质体的外观圆整,大小均匀,包封率为71.9%±3.8%,平均粒径为8.1μm。大鼠sc辣椒碱多囊脂质体后,与辣椒碱溶液相比,Cmax分别为405.72±53.87、804.06±108.17 ng.mL-1;AUC0-t为16.7836±2.8541、3.7622±0.6651μg.h.mL-1;消除时间分别为32.31±2.64、3.23±0.34 h,72 h时血浆中仍可检测到药物。结论采用复乳法可成功将脂溶性药物辣椒碱载入多囊脂质体中,大鼠体内的药动学研究显示有明显的缓释特征。

OBJECTIVE To prepare Capsaicin multivesicular liposomes（MVLs） and investigate the encapsulation efficiency and the pharmacokinetics in rats.METHODS Capsaicin MVLs were prepared by double emulsion method,and optimized by single factor experiments.The pharmacokinetics of Capsaicin MVLs following subcutaneous injection in rats was studied.RESULTS Capsaicin MVLs seemed round and well-distributed with the encapsulation efficiency was 71.9%±3.8% and the average particle size was 8.1 μm.Following the subcutaneous injection in rats,the Cmax was 405.72±53.87 and 804.06±108.17 ng·mL-1;AUC0-t was 16.7836±2.8542,3.7622±0.6651 μg·h·mL-1;t1/2 was 32.31±2.64,3.23±0.34 h for Capsaicin MVLs and solution,respectively.The plasma concentration of Capsaicin maintained above the quantitative limitation 72 h after the administration of Capsaicin MVLs.CONCLUSION The lipid soluble drug Capsaicin could be successfully entrapped into the MVLs,and Capsaicin MVLs showed a significant sustained release property following subcutaneous injection in rats.