[Preparation of valaciclovir loaded bovine serum albumin nanoparticles surface-modified with glycyrrhizin and its characteristics of targeting to liver].
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.
Mao
Shengjun
S
West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Hou
Shixiang
S
Zhang
Liangke
L
Wei
Dapeng
D
Zhang
Jifen
J
Qiao
Xiaorong
X
He
Ru
R
D000212:Acyclovir / Q000031:analogs & derivatives* / Q000494:pharmacology; D002478:Cells, Cultured; D016503:Drug Delivery Systems; D019695:Glycyrrhizic Acid / Q000494:pharmacology*; D022781:Hepatocytes / Q000166:cytology / Q000378:metabolism*; D006801:Humans; D008863:Microspheres; D049329:Nanostructures; D036103:Nanotechnology; D010316:Particle Size; D012710:Serum Albumin, Bovine / Q000494:pharmacology*; D013678:Technology, Pharmaceutical / Q000379:methods; D000077483:Valacyclovir; D014633:Valine / Q000031:analogs & derivatives* / Q000494:pharmacology
D012710:Serum Albumin, Bovine; D019695:Glycyrrhizic Acid; D014633:Valine; D000077483:Valacyclovir; D000212:Acyclovir