Design Development and Optimization of Novel Anti acne Formulations of Dapsone

Abstract

Backgound: Acne is a most common and multifactorial disorder which is currently incurable with available treatment and knowledge. Acne treatment lasts from months to years. To avoid systemic side effects of anti-acne agents, topical route is the most preferred way to provide local treatment which has bioavailability issues. In recent scenarios, most physicians use combination therapy (systemic and topical) to quickly get rid of acne. Successful management of acne needs careful selection of anti-acne agents for treatment according to type/level of acne and individual patient needs. To overcome these challenges, it was hypothesized to prepare one-month depot injection in the form of microspheres which provides long term treatment and to prepare topical dosage form with higher skin penetration and retention. newlineAim and Objective: Aim was to prepare dapsone containing intramuscular microspheres for long term treatment and topical nanogel with high retention and penetration effect for the management of acne vulgaris. So, the objective is to develop and optimize the microspheres as depot injection and to develop and optimize topical nanogel followed by In-vivo evaluation. newlineMaterials and methods: newlineFormulation 1: Dapsone for injectable suspension (Microspheres) newlineIn the present study, dapsone was selected as an active model drug because of its activity against P. acne (Propionibacterium acne) bacteria. Microsphere as injectable suspension was selected as a dosage form to improve patient compliance by providing long term treatment with minimum systemic side effects. Poly (lactide-co-glycolic acid) (50:50) was selected as a polymeric carrier as it is biocompatible and biodegradable in nature. newlineSolvent extraction and evaporation techniques were used to prepare microspheres by adopting risk based systemic approaches like identification of critical quality attributes, risk assessment, identification of critical process parameters, optimization using design expert software. Further optimized formulation was evaluate