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Liposomal formulation for co-delivery of paclitaxel and lapatinib, preparation, characterization and optimization

Fatemeh Ravar1, Ebrahim Saadat1, Pouya Dehghan Kelishadi1

  • 1a Department of Pharmaceutics, Faculty of Pharmacy , Tehran University of Medical Sciences , Tehran , Iran and.

Journal of Liposome Research
|August 13, 2015
PubMed

Insights

This study developed a novel liposomal co-delivery system for paclitaxel (PTX) and lapatinib (LPT) to overcome multidrug resistance (MDR) in cancer. The optimized formulation demonstrated enhanced cytotoxicity against cancer cells compared to free drugs.

Area of Science:

  • Nanomedicine
  • Drug Delivery Systems
  • Cancer Therapeutics

Background:

  • Paclitaxel (PTX) is a potent anticancer drug, but its efficacy is limited by hydrophobicity and multidrug resistance (MDR).
  • Lapatinib (LPT), a tyrosine kinase inhibitor, can overcome MDR by inhibiting p-glycoproteins, a key efflux pump.
  • Co-delivery of PTX and LPT offers a promising strategy to enhance anticancer efficacy and combat MDR.

Purpose of the Study:

  • To develop and optimize a novel liposomal formulation for the co-delivery of paclitaxel (PTX) and lapatinib (LPT).
  • To investigate the potential of this formulation in overcoming paclitaxel-related multidrug resistance (MDR).
  • To evaluate the physicochemical properties, drug release kinetics, and in vitro cytotoxicity of the optimized liposomal formulation.

Main Methods:

  • D-optimal response surface methodology was employed for optimizing the liposomal formulation.
  • Encapsulation efficiency, particle size distribution, and morphology were characterized using various analytical techniques.
  • In vitro drug release studies were conducted under sink conditions.
  • Differential scanning calorimetry (DSC) was used to analyze the drug state within the liposomes.
  • Cytotoxicity was assessed against 4T1 murine mammary cells.

Main Results:

  • The optimized liposomal formulation achieved high encapsulation efficiencies for both LPT (52 ± 3%) and PTX (68 ± 5%).
  • The formulation exhibited a narrow particle size distribution (average 235 ± 12 nm) with spherical, discrete liposomes observed via TEM.
  • In vitro release studies showed significant drug release over 40 hours (93% for PTX, 71% for LPT).
  • DSC analysis confirmed the conversion of both drugs to a molecular state within the lyophilized formulation.
  • The liposomal formulation demonstrated superior cytotoxicity compared to a binary mixture of free drugs.

Conclusions:

  • A novel liposomal formulation capable of co-delivering PTX and LPT was successfully developed and optimized.
  • This formulation effectively overcomes limitations associated with PTX, including hydrophobicity and MDR.
  • The enhanced in vitro cytotoxicity suggests significant therapeutic potential for this dual-drug delivery system in cancer treatment.
Keywords:
D-optimal designlapatinibliposomemultidrug resistancepaclitaxelresponse surface methodology

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