edoc

Combining mechanochemistry and spray congealing for new praziquantel pediatric formulations in schistosomiasis treatment

Albertini, Beatrice and Perissutti, Beatrice and Bertoni, Serena and Zanolla, Debora and Franceschinis, Erica and Voinovich, Dario and Lombardo, Flavio and Keiser, Jennifer and Passerini, Nadia. (2019) Combining mechanochemistry and spray congealing for new praziquantel pediatric formulations in schistosomiasis treatment. International journal of molecular sciences, 20 (5). p. 1233.

[img] PDF - Published Version
Available under License CC BY (Attribution).

4004Kb

Official URL: https://edoc.unibas.ch/69848/

Downloads: Statistics Overview

Abstract

Praziquantel (PZQ) is the first line drug for the treatment of schistosome infections and is included in the WHO Model List of Essential Medicines for Children. In this study, the association of mechanochemical activation (MA) and the spray congealing (SC) technology was evaluated for developing a child-friendly PZQ dosage form, with better product handling and biopharmaceutical properties, compared to MA materials. A 1:1 by wt PZQ-Povidone coground-was prepared in a vibrational mill under cryogenic conditions, for favoring amorphization. PZQ was neat ground to obtain its polymorphic form (Form B), which has an improved solubility and bioactivity. Then, activated PZQ powders were loaded into microparticles (MPs) by the SC technology, using the self-emulsifying agent Gelucire; ®; 50/13 as a carrier. Both, the activated powders and the corresponding loaded MPs were characterized for morphology, wettability, solubility, dissolution behavior, drug content, and drug solid state (Hot Stage Microscopy (HSM), Differential Scanning Calorimetry (DSC), X-Ray Powder Diffraction Studies (PXRD), and FT-IR). Samples were also in vitro tested for a comparison with PZQ against; Schistosoma mansoni; newly transformed schistosomula (NTS) and adults. MPs containing both MA systems showed a further increase of biopharmaceutical properties, compared to the milled powders, while maintaining PZQ bioactivity. MPs containing PZQ Form B represented the most promising product for designing a new PZQ formulation.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Helminth Drug Development (Keiser)
UniBasel Contributors:Lombardo, Flavio and Keiser, Jennifer
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Molecular Diversity Preservation International
ISSN:1422-0067
Note:Publication type according to Uni Basel Research Database: Journal article
Language:English
Identification Number:
Last Modified:20 Mar 2019 13:46
Deposited On:20 Mar 2019 13:46

Repository Staff Only: item control page