Formulation and evaluation of microsponge gel for topical delivery of fluconazole for fungal therapy

Nirav Patel; Niyati Padia; Neha Vadgama; Mihir Raval; Navin Sheth

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자료유형: 학술저널

저자정보: Nirav Patel (Saurashtra University India) Niyati Padia (Saurashtra University India) Neha Vadgama (Saurashtra University India) Mihir Raval (Saurashtra University India) Navin Sheth (Saurashtra University India)

저널정보: 한국약제학회 Journal of Pharmaceutical Investigation Journal of Pharmaceutical Investigation 제46권 제3호

발행연도: 2016.6

수록면: 221 - 238 (18page)

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The aim of the present research was to develop Fluconazole loaded microsponge-based topical delivery system for controlled release and enhanced drug deposition in the skin. Microsponges containing fluconazole were prepared by an emulsion solvent diffusion method. The effect of formulation variables (drug: polymer ratio, internal phase volume and amount of emulsifier) and process variables (stirring time and stirring speed) on the physical characteristics of microsponges like Production yield, Mean particle size, Entrapment efficiency were investigated. The effect of internal phase volume and amount of emulsifier on the physical characteristics of microsponges were examined on optimized drug/polymer ratio, stirring speed and stirring time by 32 factorial design. The optimized microsponges were dispersed into a hydrogel and evaluated. In vitro drug release, Ex vivo drug deposition, primary skin irritancy study and In vivo antibacterial activity of fluconazole-loaded formulations were studied. Spherical and porous FLU microsponge particles were obtained. From 32 factorial design, it was concluded that optimized microsponge possess particle size, production yield and entrapment efficiency of 2.45 lm, 77.38 and 92.33 %, respectively. Microspongeloaded gels demonstrated controlled release, no irritancy to rat skin and antifungal activity. An In vivo skin deposition study demonstrated four fold higher retention in the stratum corneum layer as compared with marketed cream. Microsponges-based gel formulations showed prolonged efficacy in mouse surgical wound model infected with Candida spp. Fluconazole was stable in topical formulations and showed enhanced retention in the skin indicating better potential of the delivery system for treatment of primary and secondary skin infections.

#Microsponge loaded gel #Formulation and process variables #Factorial design #Ex vivo drug deposition #Primary skin irritancy study #In vivo antibacterial activity

참고문헌 (32)

참고문헌 신청

Allen L. / 2005 / Ansel’s pharmaceutical dosage forms and drug delivery systems / Lippincott Williams & Wilkins

Amrutiya N. / 2009 / Development of microsponges for topical delivery of mupirocin / AAPS PharmSciTech 10:402~409

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Behan N. / 2002 / Synthesis and in-vitro drug release of insulin-loaded poly(n-butyl cyanoacrylate)nanoparticles / Macromol Biosci 2:336~340

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