Preparation and in vitro/pharmacokinetic/pharmacodynamic evaluation of a slow-release nano-liposomal form of prednisolone

Drug Deliv. 2016 Oct;23(8):3008-3016. doi: 10.3109/10717544.2016.1138341. Epub 2016 Feb 1.

Abstract

A nano-liposomal carrier was prepared for the anti-inflammatory drug prednisolone acetate (PA). The drug showed remarkable loading in the nano-carriers. The drug-loaded nano-liposmes with average sizes of about 186 nm and zeta potentials of -20 mV were obtained. Our drug release studies showed an apparently zero-order trend with only 18% of the drug released in the first 120 h. Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) analyses showed no chemical interaction between the drug and carrier. Transmission electron microscopy (TEM) imaging showed near-spherical drug-containing nano-carriers. The intramuscular (IM) trial of the nanoformulation compared with the free drug showed both pharmacokinetic (lower Cmax, higher area under the curve (AUC)) and pharmacodynamic (higher and longer lasting anti-inflammatory effect, both macroscopically and biochemically) superiority for the nano-liposomal drug above the free prednisolone in rats.

Keywords: Nano-liposomes; pharmacodynamic evaluation; pharmacokinetic evaluation; prednisolone; slow-release.

MeSH terms

  • Animals
  • Area Under Curve
  • Calorimetry, Differential Scanning / methods
  • Chemistry, Pharmaceutical / methods
  • Delayed-Action Preparations / chemistry*
  • Delayed-Action Preparations / pharmacokinetics
  • Delayed-Action Preparations / pharmacology
  • Drug Carriers / chemistry
  • Drug Liberation
  • Liposomes / chemistry*
  • Male
  • Microscopy, Electron, Transmission / methods
  • Nanoparticles / chemistry*
  • Particle Size
  • Prednisolone / analogs & derivatives
  • Prednisolone / chemistry*
  • Prednisolone / pharmacokinetics
  • Prednisolone / pharmacology
  • Rats
  • Rats, Wistar
  • Spectroscopy, Fourier Transform Infrared / methods

Substances

  • Delayed-Action Preparations
  • Drug Carriers
  • Liposomes
  • prednisolone acetate
  • Prednisolone