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Enhanced cellular uptake and cytotoxicity of vorinostat through encapsulation in TPGS-modified liposomes

Muhammad Asim Farooq1, Huang Xinyu1, Amna Jabeen2

  • 1Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu, 211198, PR China.

Colloids and Surfaces. B, Biointerfaces
|December 28, 2020
PubMed

Insights

TPGS-coated liposomes significantly enhance the delivery of vorinostat (VOR), a histone deacetylase inhibitor (HDACi), for breast cancer therapy. This formulation improves VOR

Area of Science:

  • * Pharmaceutical Sciences
  • * Nanotechnology
  • * Cancer Therapeutics

Background:

  • * Vorinostat (VOR) is a histone deacetylase inhibitor (HDACi) approved for cutaneous T cell lymphoma.
  • * Poor solubility, permeability, and limited anti-cancer activity challenge VOR's effective delivery.
  • * Biopharmaceutics Classification System Class IV drugs like VOR require advanced delivery systems.

Purpose of the Study:

  • * To enhance the physicochemical properties of VOR using TPGS-coated liposomes.
  • * To improve the cytotoxicity and cellular uptake of VOR in breast cancer cells.
  • * To evaluate TPGS-coated liposomes as a drug delivery system for hydrophobic anti-cancer agents.

Main Methods:

  • * Liposomes fabricated using film hydration and probe ultra-sonication.
  • * Characterization of particle size, polydispersity index (PDI), and stability.
  • * Assessment of encapsulation efficiency, solubility, and drug release kinetics.
  • * In vitro evaluation of cytotoxicity (MTT assay) and cellular uptake (fluorescence microscopy, flow cytometry).

Main Results:

  • * TPGS-coated liposomes (TPGS-VOR-LIPO) exhibited smaller particle size (176.99 nm) and better stability than conventional liposomes (OR-LIPO, 211.97 nm).
  • * Encapsulation efficiency exceeded 80%, with enhanced solubility and sustained VOR release over 48 hours.
  • * Transmission electron microscopy confirmed TPGS coating.
  • * Superior cytotoxic effect and enhanced cellular uptake observed in breast cancer cells compared to free VOR.

Conclusions:

  • * TPGS-coated liposomes significantly improve VOR's solubility, stability, and anti-cancer efficacy.
  • * Enhanced cellular uptake and cytotoxicity demonstrate the potential of TPGS-liposomes for breast cancer therapy.
  • * TPGS-coated liposomes represent a promising drug delivery platform for hydrophobic anti-cancer drugs.
Keywords:
Cancer therapyLiposomesSolubilityTPGSVorinostat

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