隐丹参酮纳米结构脂质载体的制备及药动学研究

目的制备隐丹参酮纳米结构脂质载体,并研究其药动学。方法高压均质法制备纳米结构脂质载体后,测定粒径、Zeta电位、包封率、载药量、体外释药。大鼠分别灌胃给予隐丹参酮及其纳米结构脂质载体混悬液(15 mg/kg),HPLC法测定隐丹参酮含有量,计算主要药动学参数,绘制血药浓度-时间曲线。结果所得隐丹参酮纳米结构脂质载体平均粒径为(175. 26±6. 07) nm,PDI为0. 068±0. 009,Zeta电位为(-34. 2±3. 4) m V,包封率为(87. 69±1. 97)%,载药量为(3. 75±0. 38)%,36 h内累积释放度为64. 13%。与隐丹参酮比较,其纳米结构脂质载体tmax、t1/2、Cmax、AUC0~t、AUC0~∞升高(P<0. 05,P<0. 01),相对生物利用度增加到226. 06%。结论隐丹参酮纳米结构脂质载体具有明显的缓释特征,口服吸收生物利用度有所改善。

Preparation and pharmacokinetics for nanostructured lipid carriers of cryptotanshinone

AIM To prepare the nanostructured lipid carriers of cryptotanshinone and to study their pharmacokinetics. METHODS For the nanostructured lipid carriers prepared by high presure homogenization method,particle size,Zeta potential,encapsulation efficiency,drug loading and in vitro drug release were determined. Rats were given intragastric administration of the suspensions of cryptotanshinone and its nanostructured lipid carriers(15 mg/kg),respectively,after which HPLC was adopted in the content determination of cryptotanshinone,main pharmacokinetic parameters were calculated,and plasma concentration-time curves were drawn. RESULTS The obtained nanostructured lipid carriers of cryptotanshinone demonstrated the average particle size of(175. 26±6. 07)nm,PDI of 0. 068±0. 009,Zeta potential of(-34. 2 ± 3. 4) mV,encapsulation efficiency of( 87. 69 ± 1. 97) %,drug loading of(3. 75±0. 38) % and accumulative release rate within 36 h of 64. 13%. Compared with cryptotanshinone,the nanostructured lipid carriers of cryptotanshinone demonstrated elevated tmax,t1/2,Cmax,AUC0-t and AUC0-∞(P< 0. 05,P < 0. 01),and relative bioavailability was increased to 226. 06%. CONCLUSION The cryptotanshinone nanostructured lipid carriers exhibit obvious sustained-release characteristics,along with improved bioavailability of oral absorption.