CSK-conjugated PLGA nanoparticles enhance oral delivery of insulin
- VernacularTitle:黏膜特异性多肽修饰载胰岛素口服纳米粒的制备及其体内外评价
- Author:
Zhiqiang LIU
;
Xudong CHEN
;
Fangyi LONG
;
Huifeng ZHU
- Publication Type:Journal Article
- Keywords:
insulin;
nanoparticles;
hypoglycemic effect;
peptide
- From:
Chinese Journal of Biochemical Pharmaceutics
2014;(1):79-81
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate the effects of CSK-conjugated PLGA nanoparticles on oral delivery of insulin in vitro and in vivo.Method CSK-INS-NPs were prepared by double-emulsion. Nanoparticle size、zeta potential and entrapment efficiency were measured. The efficiency of cellular uptake on Caco-2 cells in vitro was evaluated. The hypoglycemic effects were evaluated by monitoring the glucose levels in diabetic rats. Results The average sizes was(134. 4 ± 15)nm and their PDI values were less than 0.3.The insulin entrapment efifciency was around 71%. The cellular uptake of CSK-INS-NPs by Caco-2 cells was 2.8 times higher than INS-NPs. The CSK-INS-NPs transferred more insulin across the Caco-2 cell monolayer than INS-NPs and insulin solution did. In vivo experiments,the CSK-INS-NPs could reduce the blood glucose level of diabetic rats after oral administration in 10 h.Conclusion Compared with insulin solution,CSK-INS-NPs enhanced the insulin through Caco-2 cell monolayer by transcellular pathway and may be a potential delivery system for Oral Delivery of Insulin.
