Pharmacokinetics and Tissue Distribution of Vinorelbine Bitartrate after Intraveous Administration of Liposomal and Injectable Formulations

Abstract

A hydrophilic and temperature-induced degradation drug, vinorelbine bitartrate (VB)-loaded phosphatidylethanolamin liposomes (PSLs), was prepared by the thin-film hydration method. Liposomes were made of phosphatidylethanolamine: cholesteryl: oleic acid (PE: CHOL: OA, 3:3:1 mass/mass). The mean particle size of the PSLs ranged from 293.06 nm. The transmission electron microscope (TEM) images displayed that the shape of the PSLs was multilamellar vesicles with smooth surface. The highest entrapment efficiency (EE) and drug loading capacity (DL) could reach up to 68.5% and 6.23%, respectively. The PSLs was evaluated by comparing the rate of release of encapsulated VB in different phosphate buffer solution (PBS), and the result showed that the rate of drug release in acid medium was faster than in pH 7.4. Pharmacokinetic characteristics in vivo and the tissue distribution in mice were investigated, which provided experimental and theoretical basis for utilizing liposomes in malignant tumor chemotherapy.

Keywords:

• pH-sensitive liposomes
• phosphatidylethanolamin
• vinorelbine bitartrate

Acknowledgments

This work is supported by National Natural Science Foundation of Shandong Province, China (No. Y2007C141) and the Scientific Research Foundation for the Middleaged Scientist (No. 2007BS02002).

Notes

Note: Q is the fraction of drug release, t is the time, R is the regression coefficient.