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Development, characterization and in vitro evaluation of single or co-loaded imatinib mesylate liposomal formulations

Ana Catarina Pinto1, Susana Angelo, João Nuno Moreira

  • 1Bluepharma, Indústria Farmacêuticas S.A, S. Martinho do Bispo, 3045-016 Coimbra, Portugal.

Journal of Nanoscience and Nanotechnology
|July 5, 2012
PubMed

Insights

This study developed a novel liposomal drug delivery system for co-encapsulating imatinib and mitoxantrone, showing improved prostate cancer cell growth inhibition. This nanotechnology platform offers a promising strategy for hormone-refractory prostate cancer (HRPC) therapy.

Area of Science:

  • Nanotechnology
  • Drug Delivery Systems
  • Oncology

Background:

  • Mitoxantrone combinations are standard palliative care for hormone-refractory prostate cancer (HRPC) but lack survival benefits.
  • Imatinib shows preclinical activity in HRPC but limited clinical efficacy.
  • Previous in vitro studies indicated additive growth inhibition with combined imatinib and mitoxantrone in PC-3 cells.

Purpose of the Study:

  • To develop novel liposomal formulations co-encapsulating imatinib and mitoxantrone.
  • To achieve high drug loading and maximum physical stability in these formulations.
  • To optimize drug delivery for enhanced therapeutic efficacy in prostate cancer.

Main Methods:

  • Active co-loading of imatinib and mitoxantrone using a (NH4)2SO4 transmembrane gradient.
  • Characterization of encapsulation efficiency, mean size diameter, and drug retention.
  • Evaluation of the optimized formulation's efficacy in inhibiting tumor cell growth.

Main Results:

  • Optimized liposomal formulation achieved high encapsulation efficiency (>95%) for both drugs.
  • Enhanced drug retention was observed under tested storage and biological conditions.
  • The co-encapsulated formulation improved tumor cell growth inhibition, allowing a 2.6-fold reduction in mitoxantrone dosage.

Conclusions:

  • An effective active loading method for imatinib in liposomes was developed.
  • The optimized liposomal formulation demonstrates potential for improved prostate cancer therapy.
  • This nanotechnology-based drug delivery platform offers a promising strategy for HRPC treatment.

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