Abstract

DEVELOPMENT AND CHARACTERIZATION OF ALLOPURINOL BASED PRONIOSOMAL GEL FOR ANTI-GOUT ACTIVITY

Anurag Sharma*, Dr. Praveen Khirwadkar, Dr. Kamlesh Dashora

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Abstract

The objective of this study was to formulate and evaluate a proniosomal gel of allopurinol for effective transdermal delivery. Allopurinol, a xanthine oxidase inhibitor used in the treatment of gout, suffers from poor water solubility, limited oral bioavailability, and gastrointestinal side effects. To overcome these limitations, proniosomal gels were prepared using Span 40, Span 60, cholesterol, and soya lecithin via the Coacervation phase separation method. Preformulation studies including organoleptic evaluation, solubility analysis, partition coefficient determination, melting point, and FTIR spectroscopy confirmed drug-excipient compatibility and physicochemical stability. Nine formulations (F1–F9) were developed and evaluated for drug entrapment efficiency, pH, viscosity, spreadability, particle size, zeta potential, in vitro drug release, and stability. Among these, formulation F9—comprising Span 40 and Span 60 in a 1:1 ratio—exhibited the highest entrapment efficiency (89.93%), ideal pH (7.02), suitable viscosity (8690 cps), and superior spreadability (79.166 g·cm/s). In vitro drug release studies showed sustained release up to 12 hours, with a cumulative drug release of 93.47%. Kinetic modeling indicated that the release followed Korsmeyer-Peppas model and supported by Higuchi model for diffusion-controlled kinetics. Morphological studies using HR-TEM and SEM confirmed spherical, unilamellar nanosized vesicles with uniform distribution. Stability testing under varying storage conditions for 90 days confirmed the physical and chemical stability of the optimized formulation. The study concludes that F9 proniosomal gel offers a promising transdermal drug delivery system for allopurinol, with advantages including sustained release, enhanced stability, improved patient compliance, and reduced systemic side effects.

Keywords: Coacervation phase separation method, proniosomal gel, physicochemical stability, characterisation, Allopurinol, Kinetic modeling, Morphological studies, sustained release.