INVESTIGADORES
RAMIREZ RIGO Maria Veronica
congresos y reuniones científicas
Título:
Solubility determination of praziquantel in polymeric and surfactant solutions.
Autor/es:
GONZALEZ A; RAMÍREZ RIGO MV; ´GONZALEZ VIDAL N
Lugar:
Rosario
Reunión:
Congreso; 4ta Reunión Internacional de Ciencias Farmacéuticas (RICiFa 2016); 2016
Institución organizadora:
Universidad de Rosario y UNC
Resumen:
Praziquantel (PZQ) is an antihelminticdrug, effective against a broad range of trematodes and cestodes. It hasa very low aqueous solubility, leading to erratic absorption and low bioavailability. A possible approachfor overcoming this issue is to increasedrug surface area by preparing nanosuspensions, through high pressure homogenization (HPH). This methodology is sensitive to the proper selection of stabilizers anddrug concentration. Therefore, the aim of this study was to determine the PZQsolubility in different stabilizer solutions, in order to assuresupersaturation conditions for the nanosuspensiondevelopment by HPH.Surfactant (P80-Polysorbate 80 and SLS-sodium lauryl sulfate) and polymeric (PVP-Polyvinylpyrrolidone, P188-Poloxamer 188, HPMC-Hypromellose and MD-Maltodextrin) agents were selected as stabilizers. Binary solutions (surfactant-polymer or polymer-polymer) were prepared in triple distilled water,being the total stabilizer concentration of 1% (w/v).Moreover, P188 was used, individually, at different concentrations (0.25%, 0.5%, 1% w/v). The solubility was determined by addition of an excess of PZQto the solvent (n=3). The mixturewas stirred in a thermostatic bath at 40°C (the highest temperature reached by the dispersion during the HPH process) for 96 hours. Subsequently, samples were centrifugated, filtered and assayed by UV-spectrophotometry (264 nm).PZQ solubility in triple distilled water was 0.33 mg/mL.The solubility range was comprised between 0.31 mg/mL and 2.51 mg/mL, valuescorresponding tostabilizer solution ofpure P188(0.25%)and the binary mixture HPMC-SLS (1%), respectively. Sixsamples (pure P188 orin binary mixtures with PVP, MD and P80) showed no significant differences with the PZQsolubility in water. In contrast, other five samples showed highly significant differences in solubility values with respect to water, where HMPC and SLS were responsible for this behavior.In conclusion, the selection of 1% (w/v) as PZQ concentration for nanosuspension development is a very conservative value to ensure supersaturation conditions.