title: Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion.
abstract: Flurbiprofen, a potent nonsteroidal anti-inflammatory drug, is widely used for relief of pain in patients suffering from rheumatic diseases, migraine, sore throat and primary dysmenorrheal. However, this drug has many gastrointestinal side effects produced by its oral administration, such as gastric bleeding and peptic ulcer. These effects were responsible for non-compliance among patients, which ultimately results in treatment failure. The physicochemical properties of flurbiprofen, make it a suitable candidate for transdermal drug delivery, which can overcome the drawbacks of oral administration. In this sense, microemulsions have been proved to increase the cutaneous absorption of lipophilic drugs when compared to conventional drug delivery systems. The purpose of this study was to formulate and characterize gel based microemulsions, for topical delivery of flurbiprofen. Different gel bases, containing microemulsion and hydro-alcoholic solution of flurbiprofen, were developed and compared. In vitro study showed that gels containing microemulsion had a higher permeation rate than those containing hydro-alcoholic solutions. Additionally, formulation of Carbopol-I (microemulsion) showed higher percent of inhibition of inflammation than others bases. Further, skin irritation study demonstrated that Carbopol-I was none irritating. Flurbiprofen microemulsion incorporated on Carbopol-I showed physicochemical, in vitro and in vivo characteristics suitable for the development of alternative transdermal delivery formulation.
authors.affiliation: Department of Pharmacy, Faculty of Pharmacy and Alternative Medicine, Islamia University, Punjab, PK.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Naeem
authors.affiliation: Department of Pharmacy, Faculty of Pharmacy and Alternative Medicine, Islamia University, Punjab, PK.
authors.forename: Nisar
authors.initials: N
authors.lastname: Ur Rahman
authors.affiliation: Department of Biochemistry, Institute of Biology, State University of Campinas, Campinas, SP, BR.
authors.forename: Guilherme D
authors.initials: GD
authors.lastname: Tavares
authors.affiliation: Faculty of Pharmaceutical Sciences, Department of Pharmacy, University of Sao Paulo, São Paulo, SP, BR.
authors.forename: Sávio F
authors.initials: SF
authors.lastname: Barbosa
authors.affiliation: Faculty of Pharmaceutical Sciences, Department of Pharmacy, University of Sao Paulo, São Paulo, SP, BR.
authors.forename: Nádia B
authors.initials: NB
authors.lastname: Chacra
authors.affiliation: Faculty of Pharmacy and Pharmaceutical Sciences, Katz Group-Rexall Centre for Pharmacy and Health Research, University of Alberta, Edmonton, Alberta, CA.
authors.forename: Raimar
authors.initials: R
authors.lastname: Löbenberg
authors.affiliation: Faculty of Pharmacy and Pharmaceutical Sciences, Katz Group-Rexall Centre for Pharmacy and Health Research, University of Alberta, Edmonton, Alberta, CA.
authors.forename: Muhammad K
authors.initials: MK
authors.lastname: Sarfraz
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000009:adverse effects; D016503:Drug Delivery Systems / Q000379:methods; D004655:Emulsions / Q000008:administration & dosage; D005480:Flurbiprofen / Q000008:administration & dosage* / Q000009:adverse effects; D006801:Humans; D011817:Rabbits; D012869:Skin Absorption / Q000187:drug effects*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004655:Emulsions; D005480:Flurbiprofen