[Preparation and liver targeting of floxuridinyl dibutyrate solid lipid nanoparticles].
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.
Li
Jin-juan
JJ
Institute of Pharmaceutical Science, School of Medicine, Xi' an Jiaotong University, Xi' an 710061, China.
Yang
Guang-de
GD
Wang
Hong-ying
HY
Zhang
San-qi
SQ
D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage / Q000493:pharmacokinetics; D019540:Area Under Curve; D004337:Drug Carriers; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005260:Female; D005467:Floxuridine / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D005697:Galactosides / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D008099:Liver / Q000378:metabolism*; D008297:Male; D051379:Mice; D053758:Nanoparticles; D010316:Particle Size; D014018:Tissue Distribution
D000964:Antimetabolites, Antineoplastic; D004337:Drug Carriers; D005697:Galactosides; D008055:Lipids; C007816:beta-galactoside; D005467:Floxuridine