Abstract

Objective: Flutrimazole is a topical antifungal agent which displays potent broad spectrum in vitro activity against dermatophytes, filamentous fungi, and yeasts. The purpose of the present study is to formulate and evaluate microspheres loaded topical gel containing flutrimazole as model drug microspheres were prepared using aqueous ionotropic gelation method.
 Methods: Different polymers, the different drug to polymer(s) ratio(s) and other parameters were screened to study their effects on the properties of microspheres and to optimize each parameter. The controlled release emulgel was formulated by changing the polymer ratio. Fourier transform infrared study confirmed the purity of the drug, concede no interaction between the drug and excipients and analyze the parameters affecting the morphology and other characteristics of the resultant products employing scanning electron microscopy.
 Results: Microspheres loaded topical gel has been shown that encapsulation and controlled release of flutrimazole could reduce the side effect while also reducing percutaneous absorption when administered to the skin. The microspheres obtained were subjected to the preformulation studies such as bulk density, tapped density, angle of repose, Carr’s index, and Hausner’s ratio the results obtained were within the limit. The microspheres were characterized by percentage yield, drug entrapment efficiency, and particle size analysis, then the optimized microspheres formulation were incorporated into the gel prepared with various polymer(s) ratio(s) and were evaluated by parameters such as visual inspection, pH measurement, spreadability studies, viscosity, and in vitro drug release using Franz diffusion cell.
 Conclusion: The result of studies revealed that the optimized batch shows 97.24% release in 12 h and stable for around there. The microsphere loaded gel has advantages such as efficient absorption and more drug retention time.

Highlights

  • For many decenniums, medication of an acute disease or a chronic disease has been accomplished by delivering drugs to the patients through various pharmaceutical dosage forms such as tablets, capsules, pills, creams, ointments, liquids, aerosols, injectables, and suppositories as carriers

  • Microspheres loaded topical gel has been shown that encapsulation and controlled release of flutrimazole could reduce the side effect while reducing percutaneous absorption when administered to the skin

  • The microspheres were characterized by percentage yield, drug entrapment efficiency, and particle size analysis, the optimized microspheres formulation were incorporated into the gel prepared with various polymer(s) ratio(s) and were evaluated by parameters such as visual inspection, pH measurement, spreadability studies, viscosity, and in vitro drug release using Franz diffusion cell

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Summary

Introduction

Medication of an acute disease or a chronic disease has been accomplished by delivering drugs to the patients through various pharmaceutical dosage forms such as tablets, capsules, pills, creams, ointments, liquids, aerosols, injectables, and suppositories as carriers This results in a fluctuated drug level and undesirable toxicity and poor efficiency. Microspheres can be defined as solid, approximately spherical particles ranging in size from 1 to 1000 μm. They are made of polymeric, waxy, or other protective materials, that is, biodegradable synthetic polymers and modified natural products such as starches, gums, proteins, fats, and waxes. At the lower end of their size range, they have colloidal properties [6]

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