In vitro and in vivo behavior of ketoprofen intercalated into layered double hydroxides

J Mater Sci Mater Med. 2010 Nov;21(11):3009-18. doi: 10.1007/s10856-010-4151-0. Epub 2010 Sep 5.

Abstract

Ketoprofen (Ket) was intercalated into layered double hydroxides (ZnAlLDH and MgAlLDH) using the ionic exchange method. The drug intercalation was confirmed by X-ray diffraction (XRD) and FTIR spectroscopy. Ket release from the inorganic matrix was studied at pH 7.4 in continuous regime with a flow rate of 0.5 and respectively 1.0 ml/min. The kinetical data were interpreted using the Ritger and Peppas model. The data prove that the release kinetics and mechanism depend on the eluent flow rate. Quantification of gastric tolerance shows that the ulcerogenic effect of the intercalated drug is lower than the one of the raw Ket. The antinociceptive effect of both formulations was studied by the hot-plate method performed on mice. The MgAlLDH_Ket formulation shows a tendency towards a stronger antinociceptive effect than its ZnAlLDH_Ket counterpart during the 210 min recorded period.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / adverse effects
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Chemistry, Pharmaceutical / methods*
  • Drug Carriers / chemistry*
  • Drug Carriers / metabolism
  • Gastrointestinal Tract / drug effects
  • Gastrointestinal Tract / pathology
  • Hydroxides / chemistry*
  • Hydroxides / metabolism
  • Ketoprofen / administration & dosage
  • Ketoprofen / adverse effects
  • Ketoprofen / pharmacokinetics*
  • Male
  • Mice
  • Pain Measurement
  • Polymers / chemistry
  • Polymers / metabolism
  • Spectroscopy, Fourier Transform Infrared
  • Stomach Ulcer / chemically induced
  • Stomach Ulcer / epidemiology
  • Treatment Outcome
  • X-Ray Diffraction

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Hydroxides
  • Polymers
  • Ketoprofen