Abstract |
5-Fluorouracil-loaded N-succinyl-chitosan nanoparticles (5-FU-Suc-Chi/NP) were prepared by emulsification solvent diffusion. Biodistribution and tumor targeting were evaluated after i.v. administration of 5-Fu-Suc-Chi/NPs in Sarcoma 180-bearing mice. Also, pharmacokinetic profiles were evaluated after intravenous injection of 5-Fu-Suc-Chi/NP via the tail vein to rats. Our experimental results showed the 5-FU-Suc-Chi/NPs could be sustained at a high level in the blood for a very long time, implying its long systemic retention in the circulation. 5-FU-Suc-Chi/NPs were distributed mainly in tumors and liver, with small quantities being found in kidney and spleen. 5-FU-Suc-Chi/NPs accumulated only slightly in the heart and lung, and lowered the toxic effect of 5-FU in the heart and lung. Pharmacokinetic analysis in plasma showed the area under plasma concentration-time curve (AUC), elimination half-life (t(1/2)), and residence time (MRT) were increased 2.5-fold, 10.98-fold, and 10.8-fold for 5-FU-Suc-Chi/NP compared with that of free 5-FU, respectively. These results indicate that a long half-life in the circulation and tumor targeting of 5-FU-Suc-Chi/NPs are possible.
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Authors | Chengyun Yan, Jiwei Gu, Yuzhi Guo, Dawei Chen |
Journal | Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan
(Yakugaku Zasshi)
Vol. 130
Issue 6
Pg. 801-4
(Jun 2010)
ISSN: 0031-6903 [Print] Japan |
PMID | 20519858
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antimetabolites, Antineoplastic
- Drug Carriers
- Chitosan
- Fluorouracil
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Topics |
- Animals
- Antimetabolites, Antineoplastic
(pharmacokinetics)
- Biological Availability
- Chitosan
- Drug Carriers
- Fluorouracil
(administration & dosage, pharmacokinetics)
- Injections, Intravenous
- Male
- Mice
- Mice, Inbred BALB C
- Nanoparticles
- Neoplasm Transplantation
- Particle Size
- Rats
- Rats, Wistar
- Sarcoma 180
(metabolism)
- Tissue Distribution
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