Chitosan cocrystals embedded alginate beads for enhancing the solubility and bioavailability of aceclofenac

Int J Biol Macromol. 2015 Mar:74:310-7. doi: 10.1016/j.ijbiomac.2014.12.038. Epub 2014 Dec 31.

Abstract

Enhanced oral bioavailability of aceclofenac has been achieved using chitosan cocrystals of aceclofenac and its entrapment into alginate matrix a super saturated drug delivery system (SDDS). Prepared SDDS were evaluated by various physiochemical and pharmacological methods. The result revealed that the primary cocrystals enhanced the solubility of the drug and the thick gelled polymer matrix that formed from swelling of calcium alginate beads makes it to release the drug in continuous and sustained manner by supersaturated drug diffusion. The Cmax, Tmax and relative bioavailability for aceclofenac cocrystal and aceclofenac SDDS were 2.06±0.42 μg/ml, 1 h, 159.72±10.84 and 2.01 μg/ml, 1 h, 352.76±12.91, respectively. Anti-inflammatory activity of aceclofenac was significantly improved with the SDDS. With respect to the results, it revealed that the SDDS described herein might be a promising tool for the oral sustained release of aceclofenac and likely for that of various other poorly soluble drugs.

Keywords: Aceclofenac; Anti-inflammatory; Cocrystal; SDDS; Sustained release.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alginates / chemistry*
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Biological Availability
  • Chitosan / chemistry*
  • Crystallization
  • Diclofenac / analogs & derivatives*
  • Diclofenac / chemistry
  • Diclofenac / pharmacokinetics
  • Disease Models, Animal
  • Drug Delivery Systems
  • Drug Liberation
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Inflammation / drug therapy
  • Male
  • Particle Size
  • Rats
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • X-Ray Diffraction

Substances

  • Alginates
  • Anti-Inflammatory Agents, Non-Steroidal
  • Hexuronic Acids
  • Diclofenac
  • Glucuronic Acid
  • Chitosan
  • aceclofenac