Advanced search
Start date
Betweenand
Related content
(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Development and physicochemical characterization of solid dispersions containing praziquantel for the treatment of schistosomiasis

Full text
Author(s):
Dametto, P. R. ; Dametto, A. C. ; Polese, L. ; Ribeiro, C. A. ; Chorilli, M. ; de Freitas, Osvaldo
Total Authors: 6
Document type: Journal article
Source: JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY; v. 127, n. 2, p. 1693-1706, FEB 2017.
Web of Science Citations: 3
Abstract

Praziquantel (PZQ) is an anthelminthic agent active against parasitic flatworms of the Schistosoma type and the most important drug for the treatment and morbidity control of schistosomiasis. In this study, a high-performance liquid chromatography method was employed for quantification of PZQ in the physical mix (PM) and solid dispersion (SD) prepared by Fusion Method utilizing the carriers Gelucire(A (R)) 50/13 and mannitol in ratio 3:1; 1:1; 1:3 PZQ/carrier. Furthermore, PM and SD were characterized by Thermogravimetry-Differential Thermal Analysis, Differential Scanning Calorimetry, Infrared Spectroscopy, X-Ray Diffraction, and Scanning Electron Microscopy. Solubility assay was made to evaluate the solubility of PZQ in purified water, in 0.1 mol L-1 HCl solution and 0.2 mol L-1 buffered phosphate solution. PZQ dissolution test was carried out in 0.1 mol L-1 HCl and 0.2 M buffered phosphate (pH 6.8). The interaction between PZQ and carriers in PMs and SDs was evidenced due to experimental enthalpy, which was different from expected enthalpy. However, this interaction did not affect the solubility of the drug. In PZQ dissolution test, the best result was for SD 1:1 PZQ/Gelucire, which presented higher dissolution rate and release extension than PM and PZQ. Thus, SD may be a strategy to enhance the solubility and dissolution, a crucial step in the development of a pharmaceutical dosage form containing PZQ for possible application in the treatment of schistosomiasis. (AU)

FAPESP's process: 11/11586-0 - Solid dispersions as a strategy to increase the availability of poorly soluble drugs
Grantee:Patrícia Roberta Dametto
Support Opportunities: Scholarships in Brazil - Post-Doctoral