蛇床子素纳米结构脂质载体的制备及其体内药动学行为

Preparation of osthole-loaded nanostructured lipid carriers and the in vivo pharmacokinetic behaviors

目的制备蛇床子素纳米结构脂质载体,并考察其体内药动学行为。方法制备纳米结构脂质载体后,测定其包封率、载药量、粒径、Zeta电位、体外释药行为。然后,大鼠分别灌胃给予蛇床子素和纳米结构脂质载体,测定血药浓度,计算主要药动学参数。结果纳米结构脂质载体粒径为226.25nm,Zeta电位为-15.17mV,包封率为88.17%,载药量为5.06%,24h内累积释放度为77.12%。与蛇床子素组比较,纳米结构脂质载体组Tmax、T1/2、Cmax、AUC0~t、AUC0~∞显著升高(P<0.05,P<0.01)。结论纳米结构脂质载体可有效改善蛇床子素体内吸收,提高其生物利用度。

AIM To prepare osthole-loaded nanostructured lipid carriers and to investigate the in vivo pharmacokinetic behaviors.METHODS The nanostructured lipid carriers were prepared, after which their encapsulation efficiency, drug loading, particle size, Zeta potential and in vitro drug release behaviors were determined. Subsequently, rats were given intragastric administration of osthole and nanostructured lipid carriers, respectively, followed by the determination of plasma concentration and calculation of main pharmacokinetic parameters.RESULTS The nanostructured lipid carriers demonstrated the particle size, Zeta potential, encapsulation efficiency, drug loading and accumulative release rate within 24 h of 226.25 nm,-15.17 mV, 88.17%, 5.06% and 77.12%, respectively. Significantly increased Tmax, T1/2, Cmax, AUC0~t and AUC0~∞ were observed in nanostructured lipid carriers group as compared with those in osthole group(P<0.05, P<0.01).CONCLUSION Nanostructured lipid carriers can effectively improve osthole in vivo absorption and enhance its bioavailability.