Evaluation of mesoporous carbon aerogels as carriers of the non-steroidal anti-inflammatory drug ibuprofen

Int J Pharm. 2016 Dec 30;515(1-2):262-270. doi: 10.1016/j.ijpharm.2016.10.008. Epub 2016 Oct 4.

Abstract

Towards the development of novel drug carriers for oral delivery of poorly soluble drugs mesoporous aerogel carbons (CAs), namely CA10 and CA20 with different pore sizes (10 and 20nm, respectively), were evaluated. The non-steroidal anti-inflammatory lipophilic compound ibuprofen was incorporated via passive loading. The drug loaded carbon aerogels were systemically investigated by means of High-Resolution Transmission Electron Microscopy (HR-TEM), Nitrogen physisorption studies, X-ray diffraction (XRD), Differential Scanning Calorimetry (DSC), X-ray photon electron spectroscopy (XPS) and ζ-potential studies. In vitro release studies were performed in simulated intestinal fluids reflecting both fasted (FaSSIF) and fed (FeSSIF) state conditions. Cytotoxicity studies were conducted with human intestinal cells (Caco-2). Drug was in an amorphous state in the pores of the carbon carrier as shown from the physicochemical characterization studies. The results showed marked differences in the release profiles for ibuprofen from the two aerogels in the media tested whereas in vitro toxicity profiles appear to be compatible with potential therapeutic applications at low concentrations.

Keywords: Carbon aerogels; Oral delivery; Poorly soluble drugs; Simulated intestinal fluids.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Caco-2 Cells
  • Calorimetry, Differential Scanning / methods
  • Carbon / chemistry*
  • Cell Line, Tumor
  • Drug Carriers / chemistry*
  • Gels / administration & dosage
  • Gels / chemistry*
  • Humans
  • Ibuprofen / administration & dosage
  • Ibuprofen / chemistry*
  • Microscopy, Electron, Transmission / methods
  • Particle Size
  • Porosity
  • Solubility
  • X-Ray Diffraction / methods

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Gels
  • Carbon
  • Ibuprofen