Nanosuspension of fenbendazole as novel strategy to enhance its dissolution performance

BEDOGNI, GR; SEREMETA, KP; OKULIK, NB; SALOMON, CJ

Encuentro; 6ta Reunión Internacional de Ciencias Farmacéuticas (RICiFa 2020+1); 2021

UNC y UNR

Fenbendazole is a highly hydrophobic benzimidazole with a great potential to be repositioned as an anticancer drug. Therefore, the aim of this work was to develop fenbenzadole nanocrystals (FNB-nc) with improved dissolution characteristics. A nanosuspension was prepared by adding dropwise fenbendazole dissolved in a hydrochloric-acid ethanolic solution over an aqueous solution of poloxamer P407. FNB-nc were recovered by freeze-drying and a physicochemical characterization was performed. Release profiles were obtained in HCl pH 1.2 and phosphate buffer pH 7 applying the dialysis membrane method at 37±0.5 °C. FNB-nc exhibited a hydrodynamic diameter of 185±16.96/458.8±17.37 nm before/after freeze-drying respectively, with polydispersion index under 0.470, while zeta potential was -3.97±1.10 and 2.23±1.36 mV before and after drying, respectively. FNB-nc thermogram obtained by differential scanning calorimetry indicated that 64% of FNB exhibited an amorphous state, while FTIR-ATR spectra revealed characteristic peaks of the drug. Release profiles obtained for the nanosuspension and raw drug showed that statistically significant differences were obtained in HCl (p