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Design and development of PEGylated liposomal formulation of HER2 blocker Lapatinib for enhanced anticancer activity

Richa Shrivastava1, Shruti Trivedi2, Pankaj Kumar Singh3

  • 1Division of Toxicology and Experimental Medicine, CSIR-Central Drug Research Institute, Lucknow, Uttar Pradesh, 226031, India; Academy of Scientific and Innovative Research, (AcSIR), New Delhi, 110025, India.

Biochemical and Biophysical Research Communications
|June 17, 2018
PubMed

Insights

This study developed PEGylated liposomal Lapatinib to improve breast cancer treatment. The new formulation enhanced anti-tumor effects and reduced cardiotoxicity compared to free Lapatinib.

Area of Science:

  • Oncology
  • Nanotechnology
  • Pharmacology

Background:

  • Breast cancer is a leading cause of death in women, with HER2/neu receptor overexpression in 20-30% of cases.
  • Lapatinib, a dual tyrosine kinase inhibitor, targets EGFR and HER2 but faces clinical limitations due to poor solubility (Class II BSC) and cardiotoxicity.
  • HER2 receptors on cardiomyocytes contribute to Lapatinib-induced cardiotoxicity.

Purpose of the Study:

  • To design and characterize a PEGylated liposomal formulation of Lapatinib.
  • To evaluate the enhanced anticancer potential and reduced cardiotoxicity of this novel formulation.
  • To investigate the anti-tumor mechanisms, including apoptosis induction.

Main Methods:

  • Lapatinib liposomes were prepared using the lipid layer hydration method.
  • Formulation characterization included particle size, zeta potential, entrapment efficiency, and in vitro release profiling.
  • Anticancer efficacy and cardiotoxicity were assessed in chick embryo xenograft models (MDA-MB-453 cells), with flow cytometry and immunofluorescence used for apoptosis analysis.

Main Results:

  • PEGylated liposomal Lapatinib significantly reduced tumor size compared to free Lapatinib.
  • Enhanced apoptotic potential was confirmed via flow cytometry and cleaved PARP antibody staining.
  • Serum SGOT levels, a marker for cardiotoxicity and hepatotoxicity, were significantly decreased in the liposomal Lapatinib group.

Conclusions:

  • PEGylated liposomal Lapatinib demonstrates enhanced anti-tumor activity and reduced cardiotoxicity.
  • This formulation represents a promising therapeutic strategy for HER2-positive breast cancer.
  • It can be used as a standalone treatment or in combination with other therapies.
Keywords:
Chorioallantoic membraneHER2 receptorLapatinibPEGylated liposomes

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