Cytoprotective and enhanced anti-inflammatory activities of liposomal piroxicam formulation in lipopolysaccharide-stimulated RAW 264.7 macrophages

Int J Nanomedicine. 2013:8:1245-55. doi: 10.2147/IJN.S42801. Epub 2013 Mar 22.

Abstract

Background: Liposomal drug delivery systems, a promising lipid-based nanoparticle technology, have been known to play significant roles in improving the safety and efficacy of an encapsulated drug.

Methods: Liposomes, prepared using an optimized proliposome method, were used in the present work to encapsulate piroxicam, a widely prescribed nonsteroidal anti-inflammatory drug. The cytotoxic effects as well as the in vitro efficacy in regulation of inflammatory responses by free-form piroxicam and liposome-encapsulated piroxicam were evaluated using a lipopolysaccharide-sensitive macrophage cell line, RAW 264.7.

Results: Cells treated with liposome-encapsulated piroxicam demonstrated higher cell viabilities than those treated with free-form piroxicam. In addition, the liposomal piroxicam formulation resulted in statistically stronger inhibition of pro-inflammatory mediators (ie, nitric oxide, tumor necrosis factor-α, interleukin-1β, and prostaglandin E2) than piroxicam at an equivalent dose. The liposome-encapsulated piroxicam also caused statistically significant production of interleukin-10, an anti-inflammatory cytokine.

Conclusion: This study affirms the potential of a liposomal piroxicam formulation in reducing cytotoxicity and enhancing anti-inflammatory responses in vitro.

Keywords: cytokines; interleukin-1β; liposomes; nitric oxide; piroxicam; prostaglandin E2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analysis of Variance
  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cryoprotective Agents / chemistry
  • Cryoprotective Agents / pharmacology*
  • Cytokines / metabolism
  • Dinoprostone / metabolism
  • Drug Delivery Systems
  • Lipopolysaccharides
  • Liposomes / chemistry
  • Liposomes / pharmacology*
  • Macrophages / drug effects*
  • Macrophages / metabolism
  • Mice
  • Nitric Oxide / metabolism
  • Piroxicam / chemistry
  • Piroxicam / pharmacology*

Substances

  • Anti-Inflammatory Agents
  • Cryoprotective Agents
  • Cytokines
  • Lipopolysaccharides
  • Liposomes
  • Piroxicam
  • Nitric Oxide
  • Dinoprostone