Pharmaceutical Research

, Volume 27, Issue 8, pp 1687–1702 | Cite as

Evaluation of Docetaxel-Loaded Intravenous Lipid Emulsion: Pharmacokinetics, Tissue Distribution, Antitumor Activity, Safety and Toxicity

  • Mingming Zhao
  • Min Su
  • Xia Lin
  • Yanfei Luo
  • Haibing He
  • Cuifang Cai
  • Xing Tang
Research Paper



The purpose of this study was to carry out a detailed evaluation of an intravenous lipid emulsion for docetaxel (DLE) without Tween 80 before clinical administration.


The pharmacokinetics in rats and beagle dogs, tissue distribution, antitumor activity, safety test and toxicity of DLE have been investigated systematically to evaluate the formulation and compared with Taxotere® (DS).


The pharmacokinetic study in rats revealed that DLE exhibited higher plasma concentrations and AUC than DS, and a good correlation was observed between AUC and dose, while, in beagle dogs, the DLE was bioequivalent to DS. The tissue distribution study showed that the profiles of the two formulations were similar, indicating the DLE did not change the distribution of docetaxel in vivo. Furthermore, DLE was as safe as DS in the safety investigation and displayed significant antitumor activities against the A549, BEL7402 and BCAP-37 cell lines in nude mice, similar to DS. The corresponding results of the long-term toxic study demonstrated the DLE was less toxic than DS, and the toxic effects could be reversed.


The DLE investigated in this paper was found to be an attractive new formulation and an appropriate choice for the clinical administration of docetaxel.


docetaxel evaluation lipid emulsion 



the A549 human pulmonary adenocarcinoma cell line




alkaline phosphatase


alanine transaminase


aspartate transaminase


the BCAP-37 human breast cancer cell line


the BEL7402 human hepatocellular carcinoma cell line


blood urea nitrogen


creatinine kinase




coagulation time


WBC differential count


lipid emulsion for docetaxel






gama glutamyl transferase










mean corpuscular hemoglobin concentration


mean corpuscular volume


blood platelet count


the red blood cell count


reticulocyte count


the relative tumor volume


the percentage of tumor growth rate


total bilirubin


tert-butyl methyl ether


total cholesterol




the percentage of tumor growth inhibition rate


total protein


bilirubin in urine


urobilinogen in urine


white blood cell count



Professor Hui Zheng from Department of Pharmacology, China National Institute for Radiological Protection is kindly acknowledged for his assistance in the antitumor activity, safety test and long-term toxicity. Dr. David B Jack is gratefully thanked for correcting English of the manuscript.


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Copyright information

© Springer Science+Business Media, LLC 2010

Authors and Affiliations

  • Mingming Zhao
    • 1
  • Min Su
    • 1
  • Xia Lin
    • 1
  • Yanfei Luo
    • 1
  • Haibing He
    • 1
  • Cuifang Cai
    • 1
  • Xing Tang
    • 1
  1. 1.Department of PharmaceuticsShenyang Pharmaceutical UniversityShenyangPeople’s Republic of China

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