Development of diclofenac potassium gel from hydrophobically modified HPMC

Abstract

An improved topical gel was developed which could allow fast release of drug and having appropriate organoleptic (texture) and rheological properties (viscosity). In vitro release of diclofenac potassium from hydrophobically modified hydroxypropyl methyl cellulose (hm-HPMC, 90L grade) based gels (F1, F2 and F3 at 1, 1.5 and 2 % (w/v) concentration, respectively) was compared with conventional hydrophilic hydroxypropyl methylcellulose (HPMC, 50 mPa s) based gels (F4 and F5 at 12 and 15 % (w/v) concentration, respectively). This study was performed in Franz diffusion cell using cellulose dialysis membrane. The hm-HPMC-based gels of higher viscosity release remarkable quantity of the drug in comparison to conventional hydrophilic HPMC-based gels of lower viscosity. So in the drug-release process polymer concentration is more important and a determinant factor compared to viscosity. Texture profile and viscosity of hm-HPMC-based gels were compared with a commercial gel and all the rheological data obtained from the experiments confirm the suitability of these hm-HPMC-based gels for use as a topical drug delivery system. In order to achieve percutaneous penetration of drug, permeation enhancers (n-octanol and propylene glycol) were added in hm-HPMC-based gels. Both enhancers have shown enhancement of drug penetration through rat skin. Propylene glycol at both lower concentration (2 %) and higher concentration (5 %) exhibited a greater increase in the permeation flux as well as more antinociceptive activity than formulations without enhancer or with n-octanol as enhancer.