Preparation and in vitro and in vivo evaluation of folate-BSA-coated cationic nanostructure lipid carriers
10.11665/j.issn.1000-5048.20150109
- VernacularTitle: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
- Author:
Shengying CHU
1
;
Weiling SUN
;
Guoxi ZHANG
;
Wenzhong CHEN
;
Sai LI
;
Kaoxiang SUN
;
Qineng PING
Author Information
1. 烟台大学药学院；南京绿叶思科药业有限公司
- Publication Type:Journal Article
- Keywords:
folic acid;
bovine serum albumin;
paclitaxel;
nanostructure lipid carriers;
active targeting;
characte-rization;
pharmacokinetics
- From:
Journal of China Pharmaceutical University
2015;46(1):73-77
- CountryChina
- Language:Chinese
-
Abstract:
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.
