Development of Diclofenac and Capsaicin Emulgel for the Management of Inflammation in Rheumatoid Arthritis http://www.doi.org/10.26538/tjnpr/v7i6.28
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Abstract
The topical application of diclofenac for the management of inflammation in rheumatoid arthritis has minimized systemic adverse effect by providing local therapeutic action around the joints. Capsaicin – a naturally occurring compound obtained from plants of the genus Capsicum has antiinflammatory and analgesic property which when combined with diclofenac may lead to enhanced activity. Therefore, a diclofenac-capsaicin emulgel topical formulation was developed and evaluated for its anti-inflammatory activity. Emulgel formulations containing capsaicin, diclofenac, or diclofenac-capsaicin were prepared and subjected to physicochemical characterization, anti-inflammatory activity, skin irritation test and histopathology study in rats. All the formulations had off-white, smooth texture, and glossy appearance. The pH and viscosities of all formulations ranged from 5.51 - 6.23 and 10452 - 52920 mPa.s respectively. All formulations possessed good spreadability and bioadhesive strength, however, the formulations with smaller amount of the alkyl acrylate polymer (1% Carbopol®) as gelling agent had a better spreadability but lesser bioadhesiveness than those with higher gel content (1.5% Carbopol®). The release of diclofenac from all formulations followed the Higuchi model. The diclofenac-capsaicin formulations containing 0.2 and 0.3% capsaicin respectively had a higher anti-inflammatory effect than the diclofenac formulation (p<0.05); the 0.2% formulation had the highest anti-inflammatory effect. The formulations showed no symptoms of allergy nor changes in the microstructure of the skin upon application. The formulations possessed desired physicochemical properties and safety for application to the skin. The spreadability and bioadhesive property of the formulation is dependent on the concentration of carbopol®. The diclofenac-capsaicin emulgel formulation showed improved anti-inflammatory effect when compared with the diclofenac formulation.
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