Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion.

Muhammad Naeem,Nádia B Chacra,Sávio F Barbosa,Guilherme D Tavares,Nisar Ur Rahman,Raimar Löbenberg,Muhammad K Sarfraz

doi:10.1590/0001-3765201520130436

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.

Highlights

Flurbiprofen is used in inflammation, rheumatic diseases and mild to moderate pain of migraine, sore throat and in primary dysmenorrheal (British National Formulary 2006, Schachtel et al.2014)
A number of gel bases were prepared by using different concentrations of Carbopol 934P and Xanthan gum
The viscosities of Carbopol 934P (0.70-1.20% w/w) and Xanthan gum (1.10-1.60% w/w) gel bases were in the range of 307-1522 cp and 151-460 cp respectively

Summary

Introduction

Flurbiprofen is used in inflammation, rheumatic diseases and mild to moderate pain of migraine, sore throat and in primary dysmenorrheal (British National Formulary 2006, Schachtel et al.2014). The physicochemical properties of flurbiprofen, i.e., lipophilicity, low molecular weight and short elimination half-life make it a suitable candidate for transdermal drug delivery, which can overcome the drawbacks of oral administration (Fang et al 2003). It is imperative to develop novel drug delivery systems aimed to improve its skin permeation and therapeutic compliance. In this sense, microemulsions have been proven to increase the cutaneous absorption of lipophilic drugs when compared to conventional vehicles (Nisha et al 2011). Microemulsions are fluid, transparent, thermodynamically stable oil and water systems, stabilized by a surfactant usually in conjunction with a cosurfactant that could be a short-chain alcohol, amine, or other weakly amphiphilic molecule. If more oil is added to a water/oil (w/o) system, the system becomes cloudy, but the addition of more co-surfactant again gives a clean transparent emulsion (Betageri and Prabhu 2007, Fouad et al 2013)

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