title: Microemulsion for topical delivery of fenoprofen calcium: in vitro and in vivo evaluation.
abstract: The aim of this study was to investigate microemulsion (ME) based topical delivery system for fenoprofen calcium (FPCa) to eliminate its oral gastrointestinal adverse effects. ME was prepared by the water titration method using oleic acid as oil phase, tween 80 as a surfactant and propylene glycol as a cosurfactant. Oleic acid was selected as oil phase due to its good solubilizing capacity. ME existence region was determined using pseudo-ternary phase diagrams for preparing different formulations. Six different formulations were selected with various values of oil (25-68%), water (2-3%), and the mixture of surfactant and cosurfactant (1:1) (24-67%). The selected ME formulae were characterized for optical birefringence, transmission electron microscopy (TEM), pH, % transmittance, electronic conductivity, drug content, droplet size, rheological properties and stability evaluation. In vitro release study of FPCa from ME s through the synthetic membrane and hairless rat skin were evaluated. The optimized formula ME5 consisting of 5% w/w FPCa, 60% w/w oleic acid as oil phase, 3% w/w aqueous phase, and 32% w/w of surfactant phase containing Tween 80 and propylene glycol (1: 1) showed the highest transdermal flux and highest skin permeation rate. Finally, the % inhibition of carrageenan-induced rat paw edema of the optimized formula ME5 was highly significant (p < 0.001) as compared to plain gel of FPCa. In conclusion, ME is a promising technique for topical delivery of FPCa.
authors.affiliation: a Department of Pharmaceutics , The Applied Research Center of Medicinal Plants "ARCMP", National Organization for Drug Control and Research "NODCAR" , El-Haram, Giza , Egypt.
authors.forename: Dalia Ali
authors.initials: DA
authors.lastname: Farghaly
authors.affiliation: b Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Cairo University , Kasr El-Aini St, Cairo , Egypt , and.
authors.forename: Ahmed A
authors.initials: AA
authors.lastname: Aboelwafa
authors.affiliation: c Department of Pharmaceutics , National Organization for Drug Control and Research "NODCAR" , Agouza , Giza , Egypt.
authors.forename: Manal Y
authors.initials: MY
authors.lastname: Hamza
authors.affiliation: b Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Cairo University , Kasr El-Aini St, Cairo , Egypt , and.
authors.forename: Magdy I
authors.initials: MI
authors.lastname: Mohamed
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000633:toxicity; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D065546:Drug Liberation; D004655:Emulsions; D005279:Fenoprofen / Q000008:administration & dosage / Q000494:pharmacology* / Q000633:toxicity; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry; D019301:Oleic Acid / Q000737:chemistry; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D051381:Rats; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D012995:Solubility; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry; D013816:Thermodynamics
chemical_list: D000935:Antifungal Agents; D004337:Drug Carriers; D004655:Emulsions; D008081:Liposomes; D011136:Polysorbates; D013501:Surface-Active Agents; D019301:Oleic Acid; D005279:Fenoprofen
keywords: Fenoprofen calcium; anti-inflammatory activity; microemulsion; oleic acid; skin permeation; topical delivery