Preparation and liver targeting of floxuridinyl dibutyrate solid lipid nanoparticles.
- Author:
Jin-juan LI
1
;
Guang-de YANG
;
Hong-ying WANG
;
San-qi ZHANG
Author Information
1. Institute of Pharmaceutical Science, School of Medicine, Xi' an Jiaotong University, Xi' an 710061, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Antimetabolites, Antineoplastic;
administration & dosage;
pharmacokinetics;
Area Under Curve;
Drug Carriers;
Drug Compounding;
Drug Delivery Systems;
Female;
Floxuridine;
administration & dosage;
blood;
pharmacokinetics;
Galactosides;
chemistry;
Lipids;
chemistry;
Liver;
metabolism;
Male;
Mice;
Nanoparticles;
Particle Size;
Tissue Distribution
- From:
Acta Pharmaceutica Sinica
2008;43(7):761-765
- CountryChina
- Language:Chinese
-
Abstract:
This paper described the preparation and liver targeting traits of new solid lipid nanoparticles (SLN) containing floxuridinyl dibutyrate (FUDRB) modified with beta-D-galactosides (G2). FUDRB-SLN and FUDRB-G2SLN were prepared by thin layer ultrasonic technique. Transmission electron microscopy micrograph analysis demonstrated that the particle sizes of FUDRB-SLN and FUDRB-G2SLN were (137.5 +/- 11.1) nm and (95.0 +/- 10.7) nm. Drug loading were 9.64% and 8.56%, and entrapment efficiency were 99.81% and 96.23%, respectively. The concentrations of floxuridine (FUDR) in serum and some organs (liver, kidney and lung) were determined by RP-HPLC after iv administration of SLN. FUDR release was confirmed, and a significant enrichment of SLN modified with G2 was observed in liver with G2 complex (targeting rates of SLN-G2 was 8.28 for liver) in comparison with FUDR-sol (targeting rate was 2.56). FUDR could be detected in liver in mice at 480 min after iv administration of FUDRB-G2SLN. These results suggested that incorporation of G2 (4%-5%, g/g) into SLN enhanced the liver targeting-ability of FUDRB. SLN containing G2 could be a useful drug carrier system for liver targeting.
