Improving the dissolution performance of naproxen from nanoparticles

LEDESMA, RJ; OKULIK, NB; PÉREZ ZAMORA, C; SEREMETA, KP; BEDOGNI, GR; SALOMON, CJ

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

UNC y UNR

Naproxen, a non-steroidal anti-inflammatory, belongs to Class II of the Biopharmaceutical Classification System. It shows a low aqueous solubility (0.0159 mg/mL) which limits its dissolution rate and, therefore, its absorption and oral bioavailability. Thus, the aim of this work was to reduce the drug particle size to the nano scale to overcome such drawback. Nanoparticles were obtained by nanoprecipitation using Soluplus® as polymeric matrix and Pluronic® F68 as surfactant. The resulting suspension was filtered, frozen and freeze-dried. The powder obtained was characterized in terms of size, Z-pot, yield, encapsulation efficiency (%EE), drug loading (%DL) and drug/polymer interaction. Drug release was evaluated using the dialysis membrane method and 0.1 N HCl with 0.5% Tween® 80 at 37 °C. The particle size before and after freeze-drying was of 97 and 105 nm, respectively, and the Z-pot was between -5.1 and -1.2 mV. The yield of process was 85.66% with %EE and %DL values of 98.32% and 18.29%, respectively. FT-IR/ATR studies showed the characteristic bands of naproxen in the nanoparticles. Dissolution efficiency of the nanoparticles was up to 2-fold greater than that of raw drug. In conclusion, this approach may constitute a valuable alternative for obtaining nanoparticles of hydrophobic drugs with improved dissolution.