title: An insight on human skin penetration of diflunisal: lipogel versus hydrogel microemulsion.
abstract: Diflunisal is a NSAID used in acute and long term management of pain and inflammation associated with osteoarthritis, rheumatoid arthritis and symptoms of primary dysmenorrhea. However, its oral use is associated with side effects such as peptic ulceration, dyspepsia, gastrointestinal disturbances and bleeding. The aim of this work was to develop lecithin organogels (LO) transdermal delivery system for diflunisal and to study its human skin penetration ability in comparison with an optimized microemulsion-based hydrogel. Ternary phase diagrams were constructed using butyl lactate as an organic solvent and two commercial grades of lecithin. The formation of gel phase was lecithin concentration dependent with Phosholipion 85 G being capable of forming organogels at lower lecithin concentration than Lipoid S75. The gels prepared using butyl lactate were able to tolerate higher amounts of water than could be incorporated in the lipogels prepared with other organic solvents. All the investigated gels possessed acceptable physical properties and were able to deliver diflunisal through human skin. The lipogels delivered higher total drug amount through the skin than the hydrogel. The composition of lecithin seemed to have some effect on the skin permeability enhancement ability of the lipogel. Lecithin containing higher amount of phosphatidyl ethanolamine could provide better transdermal delivery. The elaborated lecithin organogels are potential carriers that create a good opportunity for transdermal delivery of diflunisal overcoming the side effects associating its oral route.
authors.affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University , Alexandria , Egypt.
authors.forename: Marwa Ahmed
authors.initials: MA
authors.lastname: Sallam
authors.forename: Adel Mohamed
authors.initials: AM
authors.lastname: Motawaa
authors.forename: Sana Mohamed
authors.initials: SM
authors.lastname: Mortada
mesh_terms: D000279:Administration, Cutaneous; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D004061:Diflunisal / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D005260:Female; D005782:Gels; D006801:Humans; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D054709:Lecithins / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D008875:Middle Aged; D009924:Organ Culture Techniques; D012869:Skin Absorption / Q000187:drug effects / Q000502:physiology*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004655:Emulsions; D005782:Gels; D054709:Lecithins; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate; D004061:Diflunisal
keywords: Butyl lactate; diflunisal; human skin; lecithin; microemulsion-based gel; organogel; transdermal