Skin permeation mechanism of aceclofenac using novel nanoemulsion formulation.
The aim of the present study was to investigate the skin permeation mechanism of aceclofenac using a novel nanoemulsion formulation. An optimized oil-in-water nanoemulsion of aceclofenac was prepared by the spontaneous emulsification method. The optimized nanoemulsion contained 2% w/w aceclofenac, 10% w/w Labrafil, 5% w/w Triacetin, 35.33% w/w Tween 80, 17.66% w/w Transcutol P and 32% w/w distilled water. The skin permeation mechanism was evaluated by FTIR spectroscopy, DSC thermography, activation energy measurement and histopathological examination. FTIR spectra of skin treated with the nanoemulsion formulation indicated breaking of the hydrogen bond network at the head of ceramides. DSC thermograms indicated that intracellular transport could be a possible mechanism of permeation enhancement and that permeation occurred due to the extraction of SC lipids by the nanoemulsion. The significant decrease in activation energy for aceclofenac permeation across rat skin indicated that the SC lipid bilayers were significantly disrupted (p < 0.05). Photomicrography of skin showed disruption and extraction of lipid bilayers as distinct voids and empty spaces visible in the epidermal region. Overall these findings indicated that nanoemulsions can be successfully used to enhance skin permeation of drugs.
Shakeel
F
F
Department of Pharmaceutics, Faculty of Pharmacy, Al-Arab Medical Sciences University, Benghazi, Libya. faiyazs@fastmail.fm
Baboota
S
S
Ahuja
A
A
All
J
J
Shafiq
S
S
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D004008:Diclofenac / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D004655:Emulsions; D053758:Nanoparticles; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000473:pathology; D012869:Skin Absorption / Q000502:physiology*; D017550:Spectroscopy, Fourier Transform Infrared
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004655:Emulsions; D004008:Diclofenac; C056498:aceclofenac