Development Of Cyclodextrin Based Nanosponge Loaded Tazoretene Gel: Characterization & In Vivo Evaluation

Abstract

The objective of the present study was to develop cyclodextrin based nanosponge based topical gel of
tazoretene using cross-linker diphenylcarbonate and Carbopol® Ultrez 10 NF polymer. The β-Cyclodextrin
nanosponges prepared using various concentrations of β-Cyclodextrin and diphenyl carbonate and
characterized. Based on evaluation parameters the β-Cyclodextrin nanosponges formulations (NS2) displayed
narrow particle size maximum solubilization efficiency. Tazarotene was loaded into five β-Cyclodextrin
nanosponge formulations by freeze drying method and evaluated. The particle size of 336 nm, zeta potential of
-23 mV and maximum drug dissolution of 97% in 12h were displayed by TZNS3 hence formulated into gel and
evaluated. The optimized tazarotene loaded nanosponge formulation (TZNS3) was incorporated into a model
carbopol gel formulation and were evaluated for invivo animal studies, and stability. This reduction may be the
result of anti-oxidant and anti-inflammatory activity associated with chitin. Test 2 caused significant reduction
in IMQ induced inflammatory process with absence of parakeratosis and decrease in acanthosis. The results
collectively suggest that because of the controlled drug release, better skin permeation, and good storage
stability, cyclodextrin nanosponges based gel formulation of tazarotene has tremendous potential to serve as a
topical delivery system.