Abstract

The purpose of present work was to formulate Fluconazole loaded microsponge-based topical delivery system for modified release. Microsponges with varied drug–polymer ratios were prepared by emulsion solvent diffusion technique using Ethyl cellulose as release retard material. Prepared microsponges were studied for particle size and physical characterization. Scanning electron microscopy (SEM) images showed the microsponges porous and spherical in shape. The microsponges were then incorporated in carbopol gel and evaluated for pH, viscosity, spreadability, drug content, in-vitro release. The In vitro drug release showed that microsponges with 1:1.5 drug–polymer ratios (F3) were more efficient to give sustained release of 74.2% at the end of 8 hr. All the microsponge gel formulations (i.e.F1- F10) showed better results like pH between 6.5-7.0, viscosity between 25,030-47,390 cps, spreadability 2-4 cm/s and drug content of 76.20±0.02% to 96.41±0.01%. Hence, the fabricated microsponge based formulation of Fluconazole would be anticipation and promising substitute to conventional therapy of skin infections.

Highlights

  • Fluconazole is a synthetic antifungal agent belonging to the group of triazole

  • Alongside most of the time the parenteral administration of fluconazole led to skin rashes and itching (Doaa et al, 2012)

  • The conventional gel formulation of fluconazole causes cutaneous irritation and prolonged use led to dermal hypersensitivity

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Summary

Introduction

Fluconazole is a synthetic antifungal agent belonging to the group of triazole. It is one of the commonly used antifungal agents for most kinds of fungal infections including superficial and invasive fungal infections (Vinod et al, 2012). Alongside most of the time the parenteral administration of fluconazole led to skin rashes and itching (Doaa et al, 2012). For these reasons, a day’s advance localized and transdermal delivery has gained a lot of importance (Niethard et al, 2005; Kulkarni et al, 2011). Microspongebased delivery systems (MDS) give assurance of drug localization on skin surface and within epidermis without entering in systemic circulation in greater extent; thereby reducing systemic and local cutaneous adversities. They offer an advantage of programmable release and are biologically safe. This technology presents quite a lot of benefits via drug entrapment by means of better formulation flexibility, abridged side effects, improved elegance and superior stability (D’souza and More, 2008; Vyas et al, 2010; Vyas and Khar, 2002; Won, 1987)

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