Formulation development,in vitroandin vivoevaluation of microemulsion-based gel loaded with ketoprofen

Abstract

Background: Anti-inflammatory agents are widely used to relieve inflammation caused by various factors. Aim: This study was initiated with the intention to deliver low aqueous soluble ketoprofen to enhance its solubility by developing microemulsion system as a template and then incorporating it into gel phase. Materials and methods: Initially ketoprofen was solubilized into microemulsion preparation made up of clove oil, Tween 20 and propylene glycol as oil phase, surfactant and co-surfactant respectively, then it was incorporated into different concentration of gelling phase using gelling agents namely Carbopol 940, Carbopol 934 and hydroxypropyl methyl cellulose K 4 M (HPMC K 4 M). Formulated emulgels were evaluated for their physical appearance, pH, rheological properties, globule size, extrudability, drug content, spreadability, bioadhesion strength, in vitro and ex vivo drug release, skin irritation test and anti-inflammatory activity. Results: Microemulsion had shown globule size 396 nm, pH 6-6.7, viscosity 29.4 cps and zeta potential À12 mV indicating good stability. Formulated emulgels showed good physical appearance, skin acceptable pH 6-6.9, non-Newtonian shear thinning system, drug content 99.28 AE 0.16%, bioadhesion strength 48.4 gram force, globule size 473 nm, spreadability 22.96 gm.cm/s, good extrudability, in vitro release, ex vivo release did not showed any irritation reaction and possess a good anti-inflammatory activity. Conclusions: Selected batch showed enhanced drug release (92.42 AE 4.66%) as compared to marketed gel (65.94 AE 3.30). Similarly ex vivo release of formulation showed 72.22% release through mice skin compared with marketed gel. Formulations followed Korsmeyer-Peppas diffusion kinetic model. It was observed from the results that the formulated emulgel can provide promising delivery of ketoprofen.

Development of gellan gum containing formulations for transdermal drug delivery: Component evaluation and controlled drug release using temperature responsive nanogels

“…Propylene glycol, Isopropyl alcohol and DMSO were selected due because of their wide use as penetration enhancers (Williams and Barry, 2004) wehereas mineral oil and Tween 20 were selected for the oil phase and the surfactant, respectively for the semisolid gel (Nikumbh et al, 2015;Williams and Barry, 2004) Gellan gum was slowly incorporated into the liquid mixture under constant stirring and dissolved by heating at 75°C. When the gellan gum dissolved, mineral oil was added and the mixture was slowly cooled under high speed stirring (1200 rpm) for 30 minutes until an emulsion formed.…”

Ketoprofen-loaded polymer carriers in bigel formulation: an approach to enhancing drug photostability in topical application forms

“…34 Samples of 0.300 g bigel, containing the drug or KP-NPs equivalent of 2.5% KP, were applied onto a cellulose membrane (MWCO 12,500 Da), which had been previously soaked in distilled water for 24 hours. 28 The cellulose membrane with bigel was fixed to the baskets. Three hundred mL of freshly prepared phosphate buffer pH 5.5 was used as a test medium.…”

“…28 The measurement was done 3 times, and the result of pH of the bigel was represented as a mean value ± SD.…”

Advances in nanotechnology-based carrier systems for targeted delivery of bioactive drug molecules with special emphasis on immunotherapy in drug resistant tuberculosis – a critical review

“…Microemulsions are mainly clear, transparent, thermodynamically stable, isotropic dispersions composed of an aqueous component and oily component (Nikumbh et al, 2015). Microemulsion also contains emulsifying agents, surfactant or co-surfactant mixtures (Kaur et al, 2014b).…”