Fabrication and in-vivo evaluation of lipid nanocarriers based transdermal patch of colchicine

The present study deals with the formulation and evaluation of Solid Lipid Nanoparticles (SLNs) based transdermal patch of colchicine. Colchicine loaded SLNs (C-SLNs) were prepared by ultrasonication method and optimized with respect to the concentration of lipid and surfactant by 32 full factorial design. Properties like particle size, shape, zeta potential, polydispersity index and percentage entrapment efficiency were determined. The transdermal potential of C-SLNs was evaluated by ex-vivo drug permeation using Wistar rat skin and fluorescence microscopy. The optimized formulation was fabricated into the transdermal patch and in-vivo pharmacokinetic and pharmacodynamic study (subcutaneous air pouch model) was carried out. Particle size, zeta potential and entrapment efficiency of the optimized formulation were found to be 107 nm, (−) 17.4 mV and 37.25% respectively. Formulation F5 showed highest transdermal flux (8.76 μg/cm2/hrs). Fluorescence study confirms that SLNs have more penetration potential through the skin. AUC0→∞ of C-SLNs patch was improved by 2.84 times more than colchicine patch. Significant (p < 0.001) reduction in exudate volume, leukocyte count, and collagen deposition was observed in animals treated with C-SLNs transdermal patch. Thus, SLNs based transdermal patch of colchicine could be a promising approach for the treatment of gout.

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