Influence of the ratio between Poloxamer 188 and Poloxamer 407 on praziquantel dissolution profiles from solid dispersions

SANTIAGO N. CAMPOS; AILÉN L. SIBELLO ; JOSÉ M. BERMÚDEZ; CINTIA A. BRIONES; MERCEDES VILLEGAS; ANALÍA I. ROMERO; ELIO E. GONZO; ALICIA G. CID

Cordoba

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

Universidades Nacionales de Córdoba y Rosario

Abstract: Praziquantel (PZQ) is a commonly used antiparasitic drug, but its pour solubility difficults its formulation and causes a low bioavailability. In this work, solid dispersion (SD) technology was used as an alternative to improve PZQ solubility and dissolution rate. SDs were prepared by the fusion method using Poloxamer 188 (P188) and Poloxamer 407 (P188) in different proportions (0%, 50% and 100% in P188) as carriers loaded with 50% w/w of PZQ. Dissolution tests were performed and dissolution profiles were analyzed and compared with the corresponding physical mixtures (PMs) using the Lumped model. The initial dissolution rates of SDs and PMs were 23.13 and 4.14 %/min for 0%P188, 37.21 and 11.45 %/min for 50%P188, and 53.13 and 20.20 %/min for 100%P188, respectively, while for the pure PZQ it was 0.24 %/min. Although both PMs and SDs enhanced the dissolution rate and the solubility of PZQ, SDs showed the best performance increasing the initial dissolution rate more than PMs. Furthermore, the SD prepared with 100% P188 presented a near 2-fold increase in this parameter compared with 100% P407. These results allow concluding that PZQ SDs based on P188 would represent a valuable alternative to improve its dissolution behavior.