Preparation of valaciclovir loaded bovine serum albumin nanoparticles surface-modified with glycyrrhizin and its characteristics of targeting to liver.
- Author:
Shengjun MAO
1
;
Shixiang HOU
;
Liangke ZHANG
;
Dapeng WEI
;
Jifen ZHANG
;
Xiaorong QIAO
;
Ru HE
Author Information
1. West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
- Publication Type:Journal Article
- MeSH:
Acyclovir;
analogs & derivatives;
pharmacology;
Cells, Cultured;
Drug Delivery Systems;
Glycyrrhizic Acid;
pharmacology;
Hepatocytes;
cytology;
metabolism;
Humans;
Microspheres;
Nanostructures;
Nanotechnology;
Particle Size;
Serum Albumin, Bovine;
pharmacology;
Technology, Pharmaceutical;
methods;
Valine;
analogs & derivatives;
pharmacology
- From:
Journal of Biomedical Engineering
2004;21(4):570-574
- CountryChina
- Language:Chinese
-
Abstract:
The valaciclovir was used as the model drug, the bovine serum albumin nanoparticles (BSA-NP) were prepared by desolvation process. Glycyrrhizin (GL) was oxidized by sodium periodate to be conjugated to surface reactive amino groups (SRAG) of the VACV-BSA-NP. Gel filtration method combined with HPLC method verified that GL was covalent coupling to the surface of VACV-BSA-NP with mean 9 GL residues per albumin molecule. The mean diameter of the VACV-BSA-NP-GL was 268 +/- 23 nm, the drug loading was 1.35%, and embedding ratio was 68.76%. The characteristics of release in vitro were in accord with two-phase kinetics. The uptake amount of VACV-BSA-NP-GL by primary cultured rat hepatocytes in vitro was higher, compared to the control-VACV-BSA-NP. 69.89% and 64.82% of the VACV were concentrated in liver at 15 min after i.v. VACV-BSA-NP-GL and VACV-BSA-NP, respectively. There is a significant difference between surface-modified group and control group (P<0.10). VACV-BSA-NP-GL was successfully prepared, which is considered to be a novel drug delivery system for targeting to hepatocytes.