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

• Published in: International journal of nanomedicine 2016-01, Vol.11 (default), p.1201-1212
• Main Authors: Sütő, Blanka, Berkó, Szilvia, Kozma, Gábor, Kukovecz, Ákos, Budai-Szűcs, Mária, Erős, Gábor, Kemény, Lajos, Sztojkov-Ivanov, Anita, Gáspár, Róbert, Csányi, Erzsébet
• Format: Article
• Language: English
• Subjects: Administration, Cutaneous; Animals; Anti-Inflammatory Agents, Non-Steroidal - pharmacology; Antiarthritic agents; Arthritis; Chemistry, Pharmaceutical - methods; Cytotoxicity; Drug Carriers - chemistry; Drug delivery systems; Gels; Homogenization; Hydrogels; Ibuprofen; Ibuprofen - administration & dosage; Ibuprofen - pharmacology; In Vitro Techniques; Lipids; Lipids - chemistry; Male; Mice; Mice, Hairless; Microscopy, Atomic Force; Nanoparticles; Nanoparticles - administration & dosage; Nanoparticles - chemistry; Nanostructured lipid carriers; Nanostructures - chemistry; Nonsteroidal anti-inflammatory drugs; Original Research; Osteoarthritis; Pain; Particle Size; Pharmaceuticals; SKH-1 hairless mice; Skin; Skin - drug effects; Skin - metabolism; Skin Absorption - drug effects; Skin penetration; Spectrum Analysis, Raman; Studies; Surfactants; X-Ray Diffraction
• ISSN: 1178-2013; 1176-9114; 1178-2013
• DOI: 10.2147/IJN.S99198

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.