DEVELOPMENT AND EVALUATION OF CYCLODEXTRIN BASED NANOSPONGE LOADED TAZORETENE GELAbstract
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 were 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, sufficiently high particle size, and maximum solubilization efficiency. Tazarotene was loaded into five β-Cyclodextrin nanosponge formulations by freeze-drying method and evaluated. Owing to the better solubilization and drug loading capacity (45%) TZNS3 was selected for further studies. The particle size of 336 nm, the zeta potential of -23 mV, and maximum drug dissolution of 97%in 12h were displayed by TZNS3 hence formulated into a gel and evaluate. The optimized tazarotene-loaded nanosponge formulation (TZNS3) was incorporated into a model carbopol gel formulation and was evaluated for skin permeation and stability. The flux value for nanosponges based gel formulation (189.342 ± 3.879 μg cm−2 h−1) was found to be higher than that for plain tazarotene (106.765 ± 4.123 μg cm−2 h−1). Skin permeation studies demonstrated that the cumulative amount of tazarotene penetrating through the skin from gel formulation containing nanosponge encapsulated tazarotene was around 6 times more than that from gel formulation containing free tazarotene at 12 h. 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.