Development of ibuprofen-loaded nanostructured lipid carrier-based gels: characterization and investigation of in vitro and in vivo penetration through the skin

Abstract

An ibuprofen-loaded nanostructured lipid carrier (IBU-NLC) was developed for enhanced skin penetration to improve the treatment of osteoarthritis and other musculoskeletal diseases. The mean particle size was 106 nm, with a spherical morphology, a smooth surface, and a zeta potential of −18.4 mV. X-ray diffraction studies revealed the amorphous state of the lipid matrix. Both Raman spectroscopy and Fourier transformation infrared analysis indicated no major shifts in the spectra of the formulations, which suggest rapid drug dissolution from the nanoparticles. The drug loading was 9.85%, and the entrapment efficiency was 98.51%. In vitro release of the NLC dispersion, in vitro permeation, and in vivo animal studies of IBU-NLC gel all confirmed that the permeation of IBU was significantly better than that of a reference after 6 hours. In conclusion, IBU-NLC gel is of great potential to enhance drug permeation through the skin and hence the efficacy of the treatment of chronic joint inflammation.

Keywords:

• ibuprofen
• nanostructured lipid carriers
• skin penetration
• SKH-1 hairless mice
• osteoarthritis

Acknowledgments

The authors would like to thank Miss Gabriella Farkas for analyzing the FT-IR spectra, Péter Sipos, PhD, for the Raman measurements and analysis, as well as Piroska Révész, PhD, DSc, for revising the manuscript critically for important intellectual content.

The authors would also like to thank Azelis Ltd, Sasol GmbH, and BASF SE for the gift samples.

The financial support of the Hungarian National Research Fund projects OTKA NN 110676 and K 112531 is acknowledged.

Disclosure

The authors report no conflicts of interest in this work.