Nanocarrier based topical gel of clofazimine: advanced therapeutic strategy for the treatment of leprosy

This study aims to formulate Clofazimine (CLOF)-loaded nanostructured lipid carriers (NLCs) for transdermal application, thereby improving the overall efficacy of the drug. NLCs loaded with clofazimine were developed using biocompatible lipids, characterised w.r.t. particle size, PDI and % entrapment efficiency and optimised using 'Box-Behnken design'. The optimum formulation was assessed for <i>in vitro</i> drug release, dermatokinetics & <i>in vivo</i> biocompatibility study. The characterisation of NLCs formulation revealed their globular shape with a particle size of around 192 nm, zeta potential of approximately of -30 mV and % EE of around 88.45%. Drug release demonstrated biphasic drug release from NLCs and follows the Higuchi release kinetics with a non-fickian release mechanism. The <i>ex vivo</i> study confirmed a 3.5 folds increase in permeation as compared with conventional gel formulation. Thus, the NLC based formulation exhibited around 350% increase in permeation as compared to plain gel of drug. The developed formulation was found to be biocompatible and exhibited no signs of irritancy or toxicity, according to the skin irritation study. Furthermore, formulation has good physicochemical stability with a shelf life of about 27 months. In conclusion the study suggests that NLC-loaded CLOF was applied topically to treat leprosy, providing improved skin penetration and effectiveness.