Enhancement of Percutaneous Delivery of Dapsone by Microemulsion Gel

Abstract

Objective: The purpose of this study was to developed microemulsion based gel formulation for topical delivery of dapsone with an objective to increase the solubility and skin permeability of the drug for treatment of acne. Methodology: The solubility of dapsone in oils, surfactants and cosurfactants was evaluated by saturation solubility to screen the components of the microemulsion. The pseudoternary phase diagrams were constructed using capryol 90 and N-methyl-2 pyrrolidone as the oil phase, Kolliphor EL as surfactant and PEG 400 as the co-surfactant. The system were assessed for drug-loading efficiency and characterized for pH, conductance, viscosity, particle size, drug content, globule size, zeta potential and drug release. Optimized formulation systems were formulated into gel form by using poloxamer-407 and evaluated for viscosity, spreadability, drug content, stability, in-vitro skin permeation, steady state flux, permeability coefficient, enhancement ration and skin irritation study. Result and Discussion: Globule size of optimized microemulsion (F2) was found to be 27.53 nm, zeta potential was found to be-14.6 mV, permeability of drug from microemulsion within 8h was observed 82%, In-vitro diffusion study showed increase in flux of microemulsion based gel (392.43 µg cm-2 h-1) to that of simple dapsone gel (274.4 ± 0.78 µg cm-2h-1). Draize test revealed absence of irritation and inflammation on rat skin. Conclusion: Microemulsion based gel of dapsone formulation provided better application property and stability in comparison to simple gel. This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.

In-vitro diffusion study of caffeine from microemulsion gel system containing grape seed oil

“…Microemulsion containing surfactant and cosurfactant at a high concentration can act as penetrant enhancers. (Mahore et al, 2017). Linear regression analyses were employed for the release kinetic study (Table 4 and Figure 4).…”

Foray into Concepts of Design and Evaluation of Microemulsions as a Modern Approach for Topical Applications in Acne Pathology

“…In the first study of Mahore et al, the ME vehicles presented in Table 4 were composed of a S/CoS mixture formed with Kolliphor EL and PEG 400, using Capryol and N-methyl-2-pyrolidone as an oil phase. Poloxamer 407 was added in the optimal system, assuring the formation of a viscous system and modulating the retention time at the place of application [ 313 ]. In a recent study of Beheshti-Mall et al, valuable results were obtained when dapsone was incorporated in an O/W vehicle formulated with Tween 80 as a S, a CoS formed with Transcutol and ethanol, using isopropyl myristate as an oil phase.…”

Emerging Technologies to Target Drug Delivery to the Skin – the Role of Crystals and Carrier-Based Systems in the Case Study of Dapsone

“…Microemulsions (MEs) have also been reported in the literature to enhance both solubility and skin permeation of DAP incorporated into poloxamer 407 gel (106). The spontaneous emulsification method was selected to prepare MEs with propylene glycol monocaprylate and N-methyl-2-pyrrolidone as the oil phase constituents.…”