丹参酮ⅡA固体脂质纳米粒的制备及大鼠在体肠吸收研究

Studies on the preparation of tashinone ⅡA solid lipid nanoparticles and absorption in rat intestine in situ

目的制备丹参酮ⅡA固体脂质纳米粒(TA-SLN),并考察其性质及大鼠在体肠吸收特性。方法 以乳化蒸发法制备丹参酮ⅡA固体脂质纳米粒,透射电镜观察其形态,建立测定纳米粒和肠回流液中丹参酮ⅡA的HPLC。结果纳米粒平均粒径为119.7nm,Zeta电位为-31.6mV,载药量为3.8％,包封率为87.7％。肠吸收实验表明,随给药剂量的增加,TA-SLN吸收速率常数Ka呈下降趋势,吸收半衰期t1/2延长,TA-SLN的大鼠小肠吸收优于丹参酮ⅡA溶液。结论TA-SLN能够促进丹参酮ⅡA在大鼠小肠的吸收,其转运机制可能为主动转运或促进扩散。

OBJECTIVE To prepare tashinone ⅡA solid lipid nanoparticles(TA-SLN) and investigate its properties and the absorption character in rat intestine in situ. METHODS Solvent emulsification/ evaporation method was used to prepare tashinone ⅡA solid lipid nanoparticles. Its morphology was examined by transmission electron microscope. A HPLC method for the determination of tashinone ⅡA in the nanoparticles and intestinal flux was established. RESULTS The mean diameter of TA-SLN was 119.7 nm .The Zeta potential were 31.6mV.The drug loading and entrapment efficiency were 3.8% and 87.7% respectively.The result of TA-SLN absorption in small intestinal indicated that Ka was decreased and the absorption t1/2 increased gradually with the increase of dosage. The rat small intestinal absorption of TA-SLN was better than that of tashinone ⅡA solution. CONCLUSION TA-SLN can improve the absorption of tashinone ⅡA in rat small intestine. The transport mechanism may be active transport or facilitated diffusion.