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KMID : 0369820090390050359
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Jorunal of Korean Pharmaceutical Sciences
2009 Volume.39 No. 5 p.359 ~ p.366
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Pharmacokinetic Behavior and Biodistribution of Paclitaxel-Loaded Lipid Nanosuspension
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Choi Sung-Up
Lee Jae-Hwi
Choi Young-Wook
Choi Woo-Sik
Park Jung-Min
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Abstract
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In this study, paclitaxel-loaded lipid nanosuspension (PxLN) was prepared and the in vivo profiles after intravenous administration in rats were investigated. We compared the manufacturing processes depending on the temperature: PxLN-H for a hot homogenization process and PxLN-C for solidification of lipid-drug mixtures by liquid nitrogen. Both formulations showed submicron size distribution and the similar drug loading efficiency of about 70%. In vitro release of PxLNs and Taxol performed by a dialysis diffusion method showed similar pattern for PxLN-H and Taxol, but the reduced release profile for PxLN-C. PxLN or Taxol was intravenously administered to the rats at a dose of 5 mg/kg as paclitaxel. The drug in blood samples were assayed by the HPLC/MS/MS method. The AUC of PxLN-H was 3.4-fold greater than that of Taxol. PxLN-H gave higher biodistribution in all tissues than did Taxol. In addition, it maintained the higher drug concentration for 12 h. This lipid nanosuspension might be a promising candidate for an alternative formulation for the parenteral delivery of poorly water-soluble paclitaxel.
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KEYWORD
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Paclitaxel, Lipid Nanosuspension, Pharmacokinetic Behavior, Biodistribution
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