Optimization of valencene containing lipid vesicles for boosting the transungual delivery of itraconazole.

The objective of the present study was to prepare valencene (sesquiterpene) containing invasomes for itraconazole (ITZ) transungual delivery using central composite design. The phospholipid (X 1) and valencene (X 2) were selected as an independent variables, while vesicles size (Y 1), entrapment efficiency (Y 2) and in vitro drug release (Y 3) were chosen as dependent variables. The antifungal activity of optimized formulation was screened against Trichophyton rubrum, a common causative onychomycosis pathogen, by cup plate method. The optimized ITZ-loaded invasomes formulation presented vesicles size of 176.8 ± 6.03 nm, entrapment efficiency of 83.21 ± 4.11% and in vitro drug release of 75.22 ± 5.03%. The ITZ-loaded invasomes gel formulation showed good homogeneity, pH 6.5 ± 0.23, viscosity 7.33 ± 0.67 Pa s and drug content 94.13 ± 1.13%. The spreadability and extrudability of developed ITZ-loaded invasomes gel were found to be 7.85 ± 0.24 gcm/s and 162 ± 2.74 g, respectively. The ITZ-loaded invasomes gel presented 71.11 ± 3.65% cumulative permeation of drug via goat hooves. The in vitro antifungal activity depicted that the ITZ-loaded invasomes gel and marketed preparation were presented zone of inhibition of 21.42 mm and 10.64 mm against T. rubrum respectively. Hence the prepared ITZ-loaded invasomes formulation could therefore be a promising topical dosage to mitigate the indications and hasten the cure for onychomycosis than conventional available therapies. © King Abdulaziz City for Science and Technology 2021.