Halobetasol propionate-loaded solid lipid nanoparticles (SLN) for skin targeting by topical delivery

Abstract

The clinical use of halobetasol propionate (HP) is related to some adverse effects like irritation, pruritus and stinging. The purpose of this work was to construct HP-loaded solid lipid nanoparticles (HP-SLN) formulation with skin targeting to minimizing the adverse side effects and providing a controlled release. HP-SLN were prepared by solvent injection method and formula was optimized by the application of 3(2) factorial design. The nanoparticulate dispersion was evaluated for particle size and entrapment efficiency (EE). Optimized batch was characterized for differential scanning calorimetry (DSC), scanning electron microscopy, X-ray diffraction study and finally incorporated into polymeric gels of carbopol for convenient application. The nanoparticulate gels were evaluated comparatively with the commercial product with respect to ex-vivo skin permeation and deposition study on human cadaver skins and finally skin irritation study. HP-SLN showed average size between 200 nm and 84-94% EE. DSC studies revealed no drug-excipient incompatibility and amorphous dispersed of HP in SLN. Ex vivo study of HP-SLN loaded gel exhibited prolonged drug release up to 12 h where as in vitro drug deposition and skin irritation studies showed that HP-SLN formulation can avoid the systemic uptake, better accumulative uptake of the drug and nonirritant to the skin compared to marketed formulation. These results indicate that the studied HP-SLN formulation represent a promising carrier for topical delivery of HP, having controlled drug release, and potential of skin targeting with no skin irritation.

Enhancement of Skin Permeability of Econazole Nitrate Using Novel Flexisomal Nanocarriers by Implementing Quality by Design (Qbd) Approach

“…A weight of 0.5 kg was put on the upper glass plate for 5 min. The increase in the diameter due to spreading of gel sample was noted [35,37].…”

“…At each speed, dial reading on the viscometer was noted. Direct multiplication of the dial readings with factors given in the Brookfield viscometer catalogue gave the viscosity in centipoises [34][35][36][37].…”

“…From this solution, 1 ml was withdrawn and volume adjusted to 10 ml with methanol. The absorbance was taken at a λmax 264 nm by UV-Spectrophotometer [35][36][37].…”

“…UV-Visible spectrophotometer was used to analyze samples. The amount of EN permeated through human cadaver skin was plotted vs time [34,35].…”

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“…Attempts for maximizing therapeutic benefits of ultrapotent corticosteroid halobetasol propionate (HP) have been attempted which indicate the possibility of dose reduction with enhanced dermal localization of drug 11,12 .…”