In-vitro evaluation of griseofulvin loaded lipid nanoparticles for topical delivery

In this work, the potential of targeting griseofulvin (GF) into the skin by topical application was evaluated by in-vitro studies. Griseofulvin loaded lipid nanoparticles (GF-LN) were prepared using high pressure homogenization method without any penetration enhancer or solubilizing solvent. The formulations were freeze dried to increase stability of the lipid nanoparticles (LN). The optimum formulation showed a mean particle size of 179.8 nm with polydispersity index of 0.306 and zeta potential of −27.9 mV and the loading of griseofulvin was 0.77%. Morphology and the degree of crystallinity of the LN were investigated using transmission electron microscope (TEM) and differential scanning calorimetry (DSC). In-vitro cytotoxicity studies showed the LN has better safety profile in human keratinocyte cells (HaCaT) with four-folds reduction in cytotoxicity (IC50 30 ± 2.37 μg/mL). In the in-vitro antifungal susceptibility tests, the GF-LN demonstrated comparable antifungal activity against Trichophyton rubrum (MIC 0.5 μg/mL) and Trichophyton mentagrophytes (MIC 0.25 μg/mL). In-vitro skin penetration and retention studies were carried out on porcine skin. The GF-LN demonstrated sufficient skin permeation with penetration flux of 0.067 ± 0.003 μg/cm2/hr. The retention of griseofulvin was found four-folds higher in the epidermis (14.9 ± 0.483 μg/cm2) on comparison to the dermis.

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