Increased systemic efficacy of aphidicolin encapsulated in liposomes

  • Authors:
    • Martin Michaelis
    • Andreas Zimmer
    • Hiromi Ninomiya
    • Nganou Handjou
    • Jaroslav Cinatl
    • Jindrich Cinatl
  • View Affiliations

  • Published online on: January 1, 2005     https://doi.org/10.3892/or.13.1.157
  • Pages: 157-160
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Abstract

Aphidicolin, a tetracyclic diterpene antibiotic produced by Cephalosporium aphidicola, is under investigation as anti-cancer drug. Because of its poor solubility in water, it cannot be administered directly in vivo. Systemic application of aphidicolin glycinate or aphidicolin γ-cyclodextrin complexes resulted in tumour growth inhibition but not in cures. To improve the pharmacokinetics, a liposomal preparation of aphidicolin was developed and tested in neuroblastoma-bearing (UKF-NB-3) mice. The loading capacity of these liposomes was limited. Therefore, 4.5 mg aphidicolin/kg body weight was the maximum aphidicolin dose that could be applied as liposomal preparation in this approach. Comparison of effects on tumour growth exhibited by aphidicolin liposomes (4.5 mg aphidicolin/kg) given for 15 consecutive days to those of γ-cyclodextrin inclusion complexes (15 mg aphidicolin/kg) revealed comparable tumour growth inhibition, although aphidicolin concentrations were approximately 3-fold lower. This shows that liposomal encapsulation is a promising strategy for the improvement of systemic anti-cancer activity of aphidicolin.

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January 2005
Volume 13 Issue 1

Print ISSN: 1021-335X
Online ISSN:1791-2431

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APA
Michaelis, M., Zimmer, A., Ninomiya, H., Handjou, N., Cinatl, J., & Cinatl, J. (2005). Increased systemic efficacy of aphidicolin encapsulated in liposomes. Oncology Reports, 13, 157-160. https://doi.org/10.3892/or.13.1.157
MLA
Michaelis, M., Zimmer, A., Ninomiya, H., Handjou, N., Cinatl, J., Cinatl, J."Increased systemic efficacy of aphidicolin encapsulated in liposomes". Oncology Reports 13.1 (2005): 157-160.
Chicago
Michaelis, M., Zimmer, A., Ninomiya, H., Handjou, N., Cinatl, J., Cinatl, J."Increased systemic efficacy of aphidicolin encapsulated in liposomes". Oncology Reports 13, no. 1 (2005): 157-160. https://doi.org/10.3892/or.13.1.157