Development and Comparison of Nanosponge and Niosome based Gel for the Topical Delivery of Tazarotene

Abstract

Background: Tazarotene is used as topical retinoid for the treatment of acne, psoriasis and sun damaged skin. But its topical formulation has many side-effects including itching, burning, dryness, redness, stinging, rash blistering, skin discolouration, peeling at the site of application and low bioavailability.

Objective: The present study focuses on the reduction of side effects and enhancement of solubility and topical bioavailability of tazarotene by formulating nanosponge and niosomes based gel for topical application.

Methodology: Nanosponge and niosomes of tazarotene were prepared by emulsion solvent evaporation technique and thin film hydration method respectively. The prepared formulations were characterized for drug content, morphology, size distribution, PDI, viscosity, % swelling and in vitro permeation. The nanosponge and niosome formulations were incorporated into carbomer 940 (gel matrix) to convert them into nanosponge and niosome based gel. The gel formulations were subjected to drug content determination, pH determination, spreadability, viscosity, rheological behaviour and in vitro permeation studies using wistar rat skin by Franz diffusion cell for optimization. The optimized nanosponge (NSG1) containing ethyl cellulose, PVA and dichloromethane and optimized niosomes (NMG5) containing tween 20, cholesterol, chlororform were formulated into gels and compared with nanosponge (NS1), niosomes (NM5), plain drug gel and marketed formulation (Tazaorac) for skin permeation and retention characteristics.

Results: The nanosponge (NSG1) and niosome (NMG5) gel formulations had lower cumulative amount of drug permeated, flux, enhancement ratio and higher skin retention within the skin layers and local accumulation efficiency (LAE) than plain drug gel and marketed formulation.

Conclusion: Thus, the study showed that nanosponge and niosome based gel formulation can be a possible alternative to conventional formulations of tazarotene with enhanced bioavailability and skin retention characteristics for topical application.

Keywords: Gel; nanosponge; noisome; permeation; tazarotene; topical..