Formulation of Piperine-Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation

Molecules. 2021 May 29;26(11):3281. doi: 10.3390/molecules26113281.

Abstract

The present research work is designed to prepare and evaluate piperine liposomes and piperine-chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (-7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC50 when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.

Keywords: MCF-7; breast cancer; chitosan; liposomes; mucoadhesive; piperine.

MeSH terms

  • Alkaloids / chemistry*
  • Antineoplastic Agents / chemistry
  • Antioxidants / chemistry
  • Benzodioxoles / chemistry*
  • Cell Adhesion
  • Cell Survival
  • Chitosan / chemistry*
  • Drug Carriers / chemistry
  • Drug Delivery Systems
  • Drug Liberation
  • Humans
  • In Vitro Techniques
  • Inhibitory Concentration 50
  • Liposomes / chemistry*
  • MCF-7 Cells
  • Microscopy, Electron, Transmission
  • Particle Size
  • Permeability
  • Piperidines / chemistry*
  • Polyunsaturated Alkamides / chemistry*
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Alkaloids
  • Antineoplastic Agents
  • Antioxidants
  • Benzodioxoles
  • Drug Carriers
  • Liposomes
  • Piperidines
  • Polyunsaturated Alkamides
  • Chitosan
  • piperine