乳糖化羧甲基壳聚糖包覆苦参碱脂质体在大鼠体内组织分布研究  

Preparation of Matrine Liposomes Coated by Carboxymethyl Galactosylate Chitosan and Its Tissue Distribution in Rats

作　　者：仵文英[1] 刘硕[2] 黄洁[3] 张抗怀[1] 王娜[1] 

机构地区：[1]西安交通大学第二附属医院药剂科,西安710004 [2]北京市胸科医院药剂科,北京101149 [3]西安交通大学医学院药学系,西安710061

出　　处：《中国药学杂志》2008年第6期439-443,共5页Chinese Pharmaceutical Journal

摘　　要：目的研究乳糖化羧甲基壳聚糖包覆的苦参碱脂质体的制备方法并考察其在大鼠体内的组织分布。方法采用逆相蒸发-短时超声法制备苦参碱脂质体。合成乳糖化羧甲基壳聚糖并用其包覆苦参碱脂质体。采用反相高效液相色谱法测定大鼠组织中的苦参碱浓度。结果包覆后脂质体的平均粒径无明显变化,Zeta电位由负转正,包封率为51.0%,渗漏率略有降低,包覆前后的脂质体的体外释放均符合Higuchi方程。乳糖化羧甲基壳聚糖包覆的苦参碱脂质体的肝脏AUC值相对于苦参碱脂质体和苦参碱溶液具有显著性差异(P<0.05),包覆后的苦参碱脂质体相对摄取率为肺脏>肝脏>脾脏。乳糖化羧甲基壳聚糖包覆的苦参碱脂质体、苦参碱脂质体和苦参碱溶液肝脏靶向效率分别为28.85%,20.93%和13.31%。结论与苦参碱溶液和普通脂质体相比,乳糖化羧甲基壳聚糖包覆的苦参碱脂质体可以提高肝靶向性。OBJECTIVE To prepare matrine liposomes coated by carboxymethyl galactosylate chitosan and to study its tissue distribution in rats. METHODS The matrine liposomes were prepared using the reverse-phase evaporation-ultrasonic technique. Carboxymethyl galactosylate chitosan was synthesized and used for coating matrine liposomes. The RP-HPLC was used for the determination of matrine concentration in rat tissue. RESULTS After being coated, the mean diameter had no obvious change, Zeta potential was reversed, entrapping efficiency was 51.0% , the leakage rate was decreased and the releasing process of them in vitro was fit for the Higuchi equation. Tissue distribution results proved that the area under the curve of liver was significantly difference among coated matrine liposomes, regular matrine liposomes and matrine solutions. The Re of coated matrine liposomes was lung 〉 liver 〉 spleen and the Te of three dosage forms were 28.85 % , 20.93 % and 13.31% , respectively. CONCLUSION Compared with regular matrine liposomes and matrine solutions, the coated matrine liposomes has the best targetability to liver in rats after intravenous injection.

关 键 词：乳糖化羧甲基壳聚糖 苦参碱脂质体 组织分布 肝靶向性 

分 类 号：R944[医药卫生—药剂学]