%0 Journal Article
%T 叶酸-白蛋白包覆阳离子纳米脂质载体的制备及体内外评价
%A 初声英
%A 孙维玲
%A 张国喜
%A 陈文忠
%A 李赛
%A 孙考祥
%A 平其能
%J 中国药科大学学报
%D 2015
%X 合成叶酸-白蛋白靶向材料，通过薄膜分散法制备白蛋白包覆阳离子脂质纳米载体(BSA-cNLCs)和叶酸-白蛋白包覆阳离子脂质纳米载体(FA-BSA-cNLCs)。对两者粒径、外观、包封率、载药量、体外细胞摄取、血液和肿瘤药代动力学和药效学进行考察。结果表明，BSA-cNLCs和FA-BSA-cNLCs粒径分别为81.4和79.8 nm，Zeta电位分别为+5.12和+3.74 mV，透射电镜照片表明两者均为圆整的类球形结构。两者紫杉醇包封率都大于97%，载药量在3.7%左右。体外细胞试验证实，高表达叶酸受体的SKOV3对FA-BSA-cNLCs的摄取显著高于BSA-cNLCs，说明FA-BSA-cNLCs对SKOV3具有明显的靶向性。血液及肿瘤药代动力学显示两者体内药代动力学行为明显差异，证实表面修饰叶酸不影响制剂的体内行为。药效学试验显示，BSA-cNLCs和FA-BSA-cNLCs抑瘤率分别为72.08%和80.75%。可见FA-BSA-cNLCs在一定程度上提高了体内外抗肿瘤疗效，在肿瘤的治疗中具有较好应用前景。</br>Folic acid(FA)was conjugated with bovine serum albumin(BSA)to form targeting material. BSA-coated cationic nanostructure lipid carriers(BSA-cNLCs)and folate-BSA-coated cationic nanostructure lipid carriers(FA-BSA-cNLCs)were prepared by film dispersion. The particle sizes of BSA-cNLCs and FA-BSA-cNLCs were 81. 4 nm and 79. 8 nm, while their Zeta potentials were +5. 12 mV and +3. 74 mV. Both nanostructure lipid carriers showed spherical shape. Paclitaxel encapsulation efficiency of them were more than 97%, with drug loading efficiency of about 3. 7%. In vitro experiments confirmed that the uptake of FA-BSA-cNLCs by overexpressed folate receptor SKOV3 cells was significantly higher than that of BSA-cNLCs, demonstrating that FA-BSA-cNLCs were obviously targeted to SKOV3. Blood and tumor pharmacokinetics showed that there was no significant differences between BSA-cNLCs and FA-BSA-cNLCs. This suggested that modified FA on the surface of the preparation had no effect on its in vivo behavior. Tumor inhibition of BSA-cNLCs and FA-BSA-cNLCs were 72. 08% and 80. 75%, repectively, which indicateds that FA-BSA-cNLCs improve anticancer efficacy in vitro and in vivo, and that it could be a potential preparation for the treatment of cancer
%K 叶酸 白蛋白 紫杉醇 脂质纳米载体 主动靶向 表征 药代动力学&lt
%K /br&gt
%K folic acid bovine serum albumin paclitaxel nanostructure lipid carriers active targeting characte-rization pharmacokinetics
%U http://www.zgykdxxb.cn/jcpu/ch/reader/view_abstract.aspx?file_no=20150109&flag=1