Statistically optimized calcipotriol fused nanostructured lipid carriers for effectual topical treatment of psoriasis

Abstract

Present work focuses on the development and optimization (Box-Behnken design) of calcipotriol (CP) loaded nanostructured lipid carrier (NLC) enriched nanogel for topical treatment of psoriasis. In this regard, CP-NLCs were prepared, optimized, and investigated in vitro for various physical parameters. Further, the optimized batch of CP-NLCs was loaded into a carbopol 931 gel base to achieve CP enriched nanogel (CPNG) formulation. Mean particle size, zeta potential, and percent entrapment efficiency of an optimized batch of CP-NLCs were found to be 123.60 ± 1.21 nm,-36.8 ± 8.85 mV, and 85.31 ± 1.18% respectively. TEM confirmed the spherical shape of CP-NLCs. DSC curve demonstrated the absolute dispersal of CP in the matrix. Drug release data verified prolonged drug release obeying the Higuchi model (r2 = 0.987). The developed nanogel formulations presented pH, viscosity, and spreadability in an acceptable range for easy topical application. Ex vivo permeation experiment revealed negligible permeation of drugs into the systemic circulation. Besides, the retention experiment furnished that the retention of CP from nanogel formulation was enhanced by 1.57 in the SC and increased by 3.67 folds in viable layers, as compared to pure CP containing gel formulation. Furthermore, no irritation was reported for developed nanogel formulation. In vivo study on mice tail animal model revealed significantly higher anti-psoriatic efficacy of nanogel formulation in terms of enhancement in % orthokeratosis of skin and % drug activity. Conclusively, the newly developed formulation is an expectant modality for the cure of psoriasis.