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Solid dispersion of praziquantel enhanced solubility and improve the efficacy of the schistosomiasis treatment

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Abstract Praziquantel (PZQ) is an anthelmintic of choice in the treatment of schistosomiasis. Solvent evaporation technique produced three different Solid Dispersions (SD) (drug: polymer, w/w) with sodium alginate (ALG) or… Click to show full abstract

Abstract Praziquantel (PZQ) is an anthelmintic of choice in the treatment of schistosomiasis. Solvent evaporation technique produced three different Solid Dispersions (SD) (drug: polymer, w/w) with sodium alginate (ALG) or carboxymethylcellulose (CMC). Characterization was done by X-Ray Diffraction (XRD), Fourier Transformed Infrared spectroscopy (FTIR) and Scanning Electron Microscopy (SEM), thermal analysis (DSC/TG), cell viability and in vitro assay against S. mansoni . The results of SD with different ratios revealed that the 1:0.25 ratio of PZQ with ALG showed higher solubility. The morphological structure change to the lamellar structure that it was confirmed with XRD. Then, thermal analyses and FTIR indicating a significant interaction between PZQ and polymer in SD indicate a change in the molecular mobility of the drug. In a culture of S. mansoni , we observed that SD is leading the death of the parasites. Regarding cytotoxicity, SD does not show toxicity in fibroblasts cells.

Keywords: schistosomiasis; solid dispersion; treatment; dispersion praziquantel; solubility; praziquantel

Journal Title: Journal of Drug Delivery Science and Technology
Year Published: 2018

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