Development of ibuprofen-loaded nanostructured lipid carrier-based gels: characterization and investigation of in vitro and in vivo penetration through the skin.
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.
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Szeged, Hungary.
Blanka
B
Sütő
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Szeged, Hungary.
Szilvia
S
Berkó
Department of Applied and Environmental Chemistry, University of Szeged, Szeged, Hungary.
Gábor
G
Kozma
Department of Applied and Environmental Chemistry, University of Szeged, Szeged, Hungary; MTA-SZTE "Lendület" Porous Nanocomposites Research Group, University of Szeged, Szeged, Hungary.
Ákos
Á
Kukovecz
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Szeged, Hungary.
Mária
M
Budai-Szűcs
Department of Dermatology and Allergology, University of Szeged, Szeged, Hungary; Department of Oral Biology and Experimental Dental Research, University of Szeged, Szeged, Hungary.
Gábor
G
Erős
Department of Dermatology and Allergology, University of Szeged, Szeged, Hungary.
Lajos
L
Kemény
Department of Pharmacodynamics and Biopharmacy, University of Szeged, Szeged, Hungary.
Anita
A
Sztojkov-Ivanov
Department of Pharmacodynamics and Biopharmacy, University of Szeged, Szeged, Hungary.
Róbert
R
Gáspár
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Szeged, Hungary.
Erzsébet
E
Csányi
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry*; D005782:Gels; D007052:Ibuprofen / Q000008:administration & dosage / Q000494:pharmacology*; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D018625:Microscopy, Atomic Force; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects*; D013059:Spectrum Analysis, Raman; D014961:X-Ray Diffraction
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D005782:Gels; D008055:Lipids; D007052:Ibuprofen
SKH-1 hairless mice; ibuprofen; nanostructured lipid carriers; osteoarthritis; skin penetration