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.

Encapsulation of Flurbiprofen by Chitosan Using a Spray-Drying Method with <i>In Vitro</i> Drug Releasing and Molecular Docking

“…A calibration curve of FP released to the medium was plotted by concentration against the absorbance. Releasing percentage of FP was calculated from the following equation [2]:…”

“…2 To minimize these side effects, biodegradable polymeric micro-and nano spheres have been developed for drug releasing. 3,4 Chitosan is a kind of biopolymer which is with its edible, biodegradable, biocompatible and nontoxic nature 5 and it was used for encapsulation of some compounds such as doxorubicin, 6 curcumin, 7 glycyrrhizin, 8 insulin 9 and cyclosporin A.…”

Intranasal Microemulgel as Surrogate Carrier to Enhance Low Oral Bioavailability of Sulpiride

“…However, some tiny agglomerates of carbopol 940 were observed as it was not properly swollen. It might attribute to the relatively high viscosity of ME and more time was consumed for the swelling of the polymer [21]. Moreover, this system showed a poor stability, non-uniformity and more air bubbles and lumps, when compared with MBG, swelled in water [11].…”

“…At the time intervals of 1, 2, 3 and 6 mo of storage, the formulations were tested for physical stability (phase separation or flocculation), the appearance, drug content, pH, and viscosity. Also, the formulations were characterized for accelerated centrifugation cycle (13000 rpm for 15 min) [21].…”

“…In the first case, carbopol 940 was swollen in the aqueous phase for 24 h and then it was incorporated in the oily phase containing a surfactant, cosurfactant, and drug resulting in a homogenous MBG formulation after pH was adjusted with triethanolamine. Formulations with no agglomerate were observed due to complete swelling of the polymer [21]. In the second case, carbopol 940 was added directly to the preformed ME without previous swelling in aqueous phase [25].…”