Response surface method for optimization of asiatic acid nanoparticles modified with PEG and its enhancing effects on intestinal absorption.
- Author:
Xia-Ying HUANG
1
;
Ya-Wen ZHANG
1
;
Li-Na YIN
1
;
Ze-Hua LIANG
2
;
Liang ZHU
2
;
Sheng-Hao WANG
1
Author Information
- Publication Type:Journal Article
- Keywords: asiatic acid; central composite design-response surface method; hydrophilic modification with polyethylene glycol; intestinal perfusion in situ; nanostructured lipid carriers
- From: China Journal of Chinese Materia Medica 2016;41(17):3239-3243
- CountryChina
- Language:Chinese
- Abstract: A solvent diffusion method was used to prepare pegylated asiatic acid (AA) loaded nanostructured lipid carriers (p-AA-NLC). Then central composite design-response surface method was used to obtain optimum condition for preparation technology of p-AA-NLC, where PEG/lipid ratio was 8.0% and AA/lipid ratio was 22.0%. Under the optimum condition, the system had particle size of (111.2±2.9) nm, Zeta potential of (-37.1±0.9) mV, drug loading of (15.4±0.2)% and entrapment efficiency greater than 90%. The deviations between observed values and predicated values were all below 5%, indicating that the established model had a good predictability. Meanwhile, a low-speed single pass perfusion model of rat in situ was set up to estimate the absorption kinetics of p-AA-NLC in small intestine, where the effective permeability (Peff), absorption rate constant (Ka) and other parameters were used to evaluate the drug absorption. It turned out that Peff and Ka in p-AA-NLC group were significantly higher than those in unmodified group (P<0.05), indicating that asiatic acid loaded nanostructured lipid carriers (AA-NLC) could enhance the effects on intestinal absorption after being modified with hydrophilic PEG.
