Faizi Muzaffar & U. K. Singh . Int. Res. J. Pharm. 2017, 8 (9) 95 INTERNATIONAL RESEARCH JOURNAL OF PHARMACY www.irjponline.com ISSN 2230 – 8407 Research Article DESIGN DEVELOPMENT AND EVALUATION OF TOPICAL MICROEMULSION Faizi Muzaffar *, U. K. Singh Kharvel Subharti college of Pharmacy, Swami Vivekanand Subharti Univrsity, India *Corresponding Author Email: faizimuzaffar@gmail.com Article Received on: 12/08/17 Approved for publication: 18/09/17 DOI: 10.7897/2230-8407.089164 ABSTRACT A microemulsion based gel was designed for the topical and targeted delivery of sertaconazole nitrate for the treatment of superficial fungal infection. The microemulsion region was obtained using a ternary diagram, different ratio of oil and Smix were used. The microemulsion of sertaconazole containing 2% (w/w) of sertaconazole, 6.67% (w/w) of oil phase (Eugenol+Oleic acid 1:1), 60.18% (w/ w) of surfactant mixture 2:1 ratio (Tween-80 and Transcutol-P) and 33.15% (w/w) with distilled water. The prepared microemulsion gel and commercial cream of sertaconazole were evaluated for in-vitro and ex-vivo studies. The highest drug retention was achieved with Tween 80 and Transcutol P (T80TC45) when the optimized formulation was converted to a gel. The designed formulation MG2 was safe to be used over the skin as the PDI=0 when compared with commercial cream and MG1. The optimized formulation also posse’s anti -inflammatory activity. The average zone of inhibition of MG2 was (23.19 ± 0.478) which was more than the commercial cream (15.34 ± 0.382) or MG1 (17.78 ± 0.715). Candida albicans which may be due to better permeation and retention effect of microemulsion gel 2. The MG2 was found to be stable after six month. The results obtained in this research from in vitro and in vivo data it can be concluded that the developed microemulsions have great potential for topical drug delivery in the treatment of inflammation and fungal infection. Key words: Sertaconazole nitrate, microemulsion gels, skin retention, antifungal, anti-inflammatory effect INTRODUCTION Delivery of a drug via skin 1-2 found to be attractive and proven to be very beneficial, as the systemic load of API is avoided and thus side effect are reduced as compared to others routes, drug applied topically avoids a number of parameters. Plasma levels typical for repeated administration of rapidly eliminated drug circumvent the first pass effect and decrease gastrointestinal side effects of a drug administrated by the oral route. Local actions include actions on the stratum corneum, or within the dermis. Topical delivery 3-4 has become an important means of drug delivery. Delivery of drugs to skin for systemic and local effect is called topical delivery. Topical delivery involves in the availability of drug molecules continuously from the surface, through its layers, and maintain a constant concentration within. Thus it’s a valuable alternative to the conventional topical, oral and parenteral route of drug administration. Several topical therapeutic systems are being developed successfully and recently commercialized. The reason for selecting a skin, as the route of delivery of API, is mainly because of the fact that this method avoids the irritation to the GIT that can often occur, causing bleeding, etc. Additionally, in some instances administration through this route allows the drug to bypass the metabolism, allowing more of the drug's active ingredient to be utilized. Furthermore, a high drug concentration can be delivered to a particular diseased or affected area (e.g. bacterial or fungal infection). Ingredients selected must be tolerable to the patient and non-corrosive to the applied area. Absorption rate must be considered along with the total amount of drug delivered and the rate of elimination of active ingredient if found in the bloodstream. Microemulsion could be an alternative carrier in topical drug delivery and as it has high Solubilization capability and nanometer size, it is believed that microemulsion will be a better candidate in delivering drug topically. Microemulsions composed of surfactant, water, and oil having co-surfactants provide better therapeutic action when compared to the traditional cream and lotions. Chemically, Sertaconazole contains a benzothiophene ring which makes it unique from other imidazole antifungal. A benzothiophene ring is a sulfur analog of the indole ring found in the amino acid tryptophan. Tryptophan is found in the fungal membrane in addition to lipids such as ergosterol. The benzothiophene ring in Sertaconazole mimics tryptophan and increases the drugs ability to form pores in the fungal cell membrane. If the cell membrane is made sufficiently leaky by these pores the fungal cell will die. MATERIALS AND METHODS Sertaconazole nitrate was purchased from Hangzhou Holypharm Biotech Co. Ltd. (Zhejiang, China, Eugenol, Tween-80, propylene glycol was purchased from Sigma Aldrich Mumbai Transcutol P was gifted from gattefosse, India. All other chemicals used in the study were of analytical reagent grade. Screening of excipients Screening of excipients is most important criteria to find Sertaconazole solubility 5-6 in different excipients such as oil, surfactants, and cosurfactants. Maximum solubility is to be fined in each component and with the help of ternary diagram microemulsion region is obtained. Smix has a vital in the