摘要
目的制备吴茱萸碱固体脂质纳米粒,并评价其抗肿瘤活性。方法吴茱萸碱溶于混合溶剂(丙酮-无水乙醇)中,加入Precirol ATO 5并水浴加热,作为有机相,将其缓慢倒入泊洛沙姆188溶液(水相)中,冷冻干燥后制得纳米粒。分子模拟考察其处方组成。以Precirol ATO 5用量、药脂比、泊洛沙姆188用量为影响因素,在单因素试验基础上通过Box-Behnken设计优化制备工艺,再进行表征与体外抗肿瘤(人宫颈癌He La细胞)活性实验。结果最佳条件为30 mg Precirol ATO 5,药脂比1∶3,93 mg泊洛沙姆188,所得纳米粒圆整,分布均匀,平均粒径268.9 nm,平均载药量1.65%,对He La细胞有较好的抑制作用,并呈剂量依赖关系。结论固体脂质纳米粒可有效改善吴茱萸碱的分散性与透膜吸收。
AIM To prepare evodiamine-loaded solid lipid nanoparticles and to evaluate their antitumor activity. METHODS Evodiamine was dissolved in the mixed solution of acetone and anhydrous alcohol and added into Precirol ATO 5 exposed to bath heating. As an organic phase,it was then slowly poured into Poloxamer 188 solution（ water phase）,and the nanoparticles were prepared after freeze-drying. The formulation composition was investigated by molecular simulation. With the volume consumption of Precirol ATO 5 and Poloxamer 188,and ratio of drug to lipid as influencing factors,the preparation was optimized by Box-Behnken design on the basis of single factor test,then the characterization and in vitro antitumor（ human cervical carcinoma He La cells） test were carried out. RESULTS The optimal conditions were determined to be 30 mg Precirol ATO 5,1 ∶ 3 for ratio of drug to lipid,and 93 mg Poloxamer 188. The obtained round nanoparticles,with uniform distribution,an average particle size of 268. 9 nm and an average drug-loading rate of 1. 65%,exhibited a good inhibitory effect against Hela cells in a dose-effect relationship. CONCLUSION The solid lipid nanoparticles can effectively improve evodiamine＇s dispersion and the permeable membrane absorption for it.
出处
《中成药》
CAS
CSCD
北大核心
2016年第10期2149-2156,共8页
Chinese Traditional Patent Medicine
基金
2013年国家级大学生创新训练项目(201313705004)
