Abstract
Dexibuprofen is a practically water-insoluble nonsterodial anti-inflammatory drug. Following previous experience on enhancing the solubility of the drug, a mixed hydrotropic solubilization technique was here applied in order to improve the aqueous solubility of the drug so that a soluble form of dexibuprofen was prepared and then could be used as a main active ingredient in transdermal films. Nine formulae were prepared applying 32 full factorial design using different amounts of hydroxypropylmethylcellulose (HPMC) and polyvinylpyrrolidone K30 (PVP K30). The prepared formulae were evaluated for their physical properties, loading efficacy and In-vitro dissolution studies adopting the USP XXII dissolution method type V paddle over disk apparatus method. Permeation studies were done for best three films showing higher dissolution rate using Franz cell apparatus and also bioavailability study was carried out on the best formula to compare the absorption of dexibuprofen from the prepared film (treatment A) to commercial tablets (treatment B) following administration of a single dose to rabbits. The prepared films were off-white color, opaque, smooth, moist and non-sticky. Increasing the amounts of HPMC and PVP K30 lead to increasing weight, folding endurance, tensile strength, moisture content and moisture absorption. Transdermal films containing higher concentrations of PVP K30 and lower concentration of HPMC showed higher rate and amount of dexibuprofen released from dissolution medium and Franz cell. The bioavailability study showed that (Tmax) in treatments A and B is 3 hours and 2 hours respectively. The average peak plasma concentration values (Cmax) were 28.98±3.36 and 34.67±0.61 ug/mL, respectively and the AUC0-∞ values were 145.82±13.09 and 117.44±3.15 µg·h/mL, respectively. There were significant differences between treatments A and B in Cmax, t(1/2)ab, Kel, t(1/2)el, TCR, AUC0-8, AUC0-∞, AUMC0-8, AUMC0-∞, and MRT. While the difference was insignificant in Kab.
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