European Journal of Biomedical and Pharmaceutical Sciences

FORMULATION, DEVELOPMENT AND EVALUATION OF ANTIFUNGAL NANOGEL USING VORICONAZOLE AND VITAMIN-C FOR TOPICAL DRUG DELIVERY

Payal Deepak Daswadkar*, K.J. Kore, S.D. Bhise, Madhuri Keskar

ABSTRACT

In the present study the formulation of nanogel was prepared by solvent evaporation method. With a aim to improve water solubility of the poorly water soluble drug Voriconazole belonging to the BCS Class-II. Total fifteen formulations of drug were prepared with varying proportion of polymer Ethyl-cellulose along with the stabilizer Poloxamer F38. The formulated nanogel is evaluated for particle size analysis, saturation, solubility, poly-dispersity index, drug entrapment, in-vitro dissolution studies, zeta potential, short term stability studies and the result showed stable The objective of the research was to design a formulation that can be easily applied onto the skin by providing relief and retention of water (the major ability of hydrogel) for a prolonged period on dermatitis-affected dried skin and able to permeate through intact skin. Voriconazole is an antifungal agent of the triazole class and a new existing drug. It overcomes all side effects of fungal other medicines like Ketoconazole, Amphotericin B, Clotrimazole, and Miconazole. Even though it has some side effects in the oral and IV dosage forms. Voriconazole remains one of the most frequently prescribed triazoles because of its excellent bioavailability, tolerability, and side effect profile. The voriconazole nanoparticle nanogels were prepared on the different concentrations of four polymers, HPMC, Methylcellulose, Carbopol, and pectin. The formulation of voriconazole nanoparticle-loaded gel with HPMC showed favorable characteristics such as a good flow index, spreadability, and viscosity. This indicated its suitability for topical application. The release profile demonstrated sustained drug release over a prolonged period, suggesting the potential for a long therapeutic effect. In the in vitro permeation studies R² = 0.9046, the nanogel exhibited efficient drug permeation through a synthetic membrane with a controlled release profile. This indicated the nanogel's ability to deliver voriconazole to the target site effectively nanogel with nanosize __. L-ascorbic acid (vit-C) is a water soluble compound and most abundant anti-oxidant in human skin, but this vitamin is unstable and loses its potency with poor formulation strategies. Nanotechnology has been effectively used to promote stability and therapeutic activity of various drug molecules. The objective of this work was set to formulate a topical delivery system of Voriconazole and Vitamin C nanoparticles incorporated into polymeric gel. Saturation solubility of such nanogel reveals that the aqueous solubility of drug is significantly increased due to decrease in particle size (80-300 nm). The short term stability studies was performed at two set of temperature 25oC and 37oC proves that the drug in nanogel can be remain stable at temperature 25oC. Zeta potential was found to be optimum which show the formulation is stable. From the above studies it is concluded that the Poloxamer F38 stabilizer (Pluronic F38) can be used for formulating stable nanogel with varying concentration in range of 0.5-1.0 %. It gives effective size as well as stability to nanogel. The ratio of Drug, polymer and stabilizer (Drug, Ethyl cellulose and Poloxamer F38) is important to obtain the stable nanogel formulation.

Keywords: Development, Evaluation, Nanogel, Antifungal Drug and Topical Delivery.