Abstract
Purpose: To develop polymeric nanosponge based hydrogel system of fluconazole (FZ) for improved delivery for topical application.Method: Six different nanosponge preparations of fluconazole were formulated by oil-in-water (o/w) emulsion solvent diffusion method using various drug to polymer (ethylcellulose, EC) ratios. Polyvinyl alcohol (PVA) and dichloromethane were used to prepare the aqueous and dispersed phases, respectively. The nanosponges (NS) were studied for entrapment efficiency, particle size, structural properties, size and appearance, and in vitro drug release. Furthermore, the hydrogel formulation was evaluated for ex vivo permeation characteristics.Results: Morphological studies revealed porous nanosized particles with the outer surface resembling orange peel. The nanosponges had particle size in the range of 220.2 ± 4.5 to 624.1 ± 10.4 nm. Release studies showed 43.9 ± 3.2 % drug release at 6 h, confirming the sustained release pattern of the drug-loaded nanosponges. Powder x-ray diffraction (PXRD) and Fourier transform infra-red (FTIR) analyses indicate complex formation in the nanosponge structure. Out of six nanosponge formulations prepared, F3 containing FZ and EC in the ratio of 1:0.7 showed optimum physicochemical and release characteristics and, therefore, was selected for hydrogel formulation. Kinetic analysis of the permeation data revealed a Higuchi diffusion pattern. Ex vivo permeation studies indicate that the hydrogel preparation displayed adequate drug permeation through rat abdominal skin.Conclusion: A nanosponge-loaded hydrogel of fluconazole for improved permeation of the drug through skin has been successfully developed. Safety and toxicity tests are required to ascertain its potential suitability for use in humans.Keywords: Fluconazole, Nanosponges, Ethylcellulose, Drug release, Franz diffusion cell, Higuchi diffusion
Highlights
Conventional topical systems such as ointments and creams are less effective for skin permeation due to their poor efficiency and are associated with side effects such as burning, contact dermatitis and stinging sensations owing to uncontrolled release of drug [1,2]
Nanosponges can be prepared by solvent method, cross linking of β-cyclodextrins, ultra sound assisted method and emulsion solvent diffusion method which is one of the effective and economical method for preparation of NS [9]
Being an anti-fungal agent, it normally requires a long duration of therapy, which can lead to higher incidence of adverse effects after systemic administration
Summary
Nanosponges can be prepared by solvent method, cross linking of β-cyclodextrins, ultra sound assisted method and emulsion solvent diffusion method which is one of the effective and economical method for preparation of NS [9]. Being an anti-fungal agent, it normally requires a long duration of therapy, which can lead to higher incidence of adverse effects after systemic administration. This requires development of topical FZ preparation to avoid these untoward effects. Majority of topical delivery systems in the market have insufficient residence time and results into inadequate therapeutic effects [11] Due to their low efficacy as delivery system, these formulations normally need a high amount of active pharmaceutical agent to get desired therapeutic effect. Emulsion-solvent diffusion method was employed for formulation of FZ loaded nanosponges as described earlier [8]. Dispersed phase was prepared by ultrasonic stirring of EC and FZ in 20 mL dichloromethane. Samples were kept in disposable cuvette and measurements were made at 372.0 kcps (count rate) for 20 s
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