更新制备盐酸小檗碱纳米脂质体粒径及对Hela细胞毒性作用研究  

Optimizing Preparation of Berberine Hydrochloride Liposomes Particle Diameter and Its Cytotoxicity Studies in Vitro

作　　者：戴小慧[1] 

机构地区：[1]杭州师范大学附属医院,浙江杭州310015

出　　处：《中华中医药学刊》2014年第5期1188-1190,I0021,共4页Chinese Archives of Traditional Chinese Medicine

摘　　要：目的:对盐酸小檗碱的理化毒性进行研究并优化盐酸小檗碱脂质体的制备条件,提高盐酸小檗碱脂质体的生物利用度。方法:盐酸小檗碱纳米脂质体采用主动载药法优化制备,对该脂质体的粒径、包封率、形貌等进行考察,并采用MTT法对该脂质体的生物安全性进行检测。结果:盐酸小檗碱脂质体的包封率随卵磷脂/胆固醇质量比比的增加呈逐渐下降趋势,其粒径在卵磷脂/胆固醇质量比为3∶1时,得到较高的包封率;其粒径随盐酸小檗碱含量的增加而增大,当盐酸小檗碱含量等于0.8mg/mL时,纳米盐酸小檗碱脂质体的包封率为最大;在较低浓度条件下(≤20μg/mL),小糪碱纳米脂质体样品作用48h后的细胞存活率仍然都保持在80%以上,与同一浓度纯品小糪碱样品相比,小糪碱纳米脂质体样品作用细胞后,细胞存活率提高明显。结论:优化盐酸小檗碱脂质体的制备条件,能够显著提高生物利用度,可以使粒径更小,小糪碱纳米脂质体比小糪碱纯品对Hela细胞的毒性作用更小,药物安全性高。Objective： To investigate the preparation conditions in vitro of cytotoxicity and optimization of berberine hydrochloride liposomes in order to improve the berberine hydrochloride solution bioavailability. Methods： Berberine hydrochloride liposomes were prepared by active loading method. The particle size of the liposomes, entrapment efficiency and morphology were investigated and the MTT method was used to detect the biological safety of the liposome. Results ：The entrapment rate increase of berberine hydrochloride liposomes with lecithin/cholesterol mass ratio was decreased gradually, and the particle size in the lecithin/cholesterol mass ratio of 3 ： 1 had higher encapsulation efficiency. The particle size increased with the contents of berberine hydrochloride increasing. When the content of berberine hydrochlo- ride was equal to 0.8 mg/mL, berberine hydrochloride liposome encapsulation rate was the maximum. In the condition of lower concentrations （ ≤ 20 μg/mL） after 48 h,the cell survival rate still maintained above 80%. Compared with the same concentration of pure samples of berberine, berberine nano liposome samples cell survival rate was increased. Conclusion： The preparation optimizing conditions of berberine hydrochloride liposome can significantly improve the bio- availability and make the particle size smaller. Berberine nano liposome has less toxicity effect on Hela cells than pure berberine and high safety.

关 键 词：主动载药法 盐酸小檗碱 纳米脂质体 

分 类 号：R284[医药卫生—中药学]