Abstract
Praziquantel is a broad spectrum antihelmintic agent and represents the drug of choice for the treatment of schistosomiasis. However, its low aqueous solubility and strong bitter taste highly affect the bioavailability and compliance in pediatric patients. Thus, the purpose of this study was to develop a dry nanosuspension, by a combination of high-pressure homogenization and spray drying, intended for redispersion in a pleasant taste vehicle for extemporaneous use. Three formulations, varying stabilizers to drug ratio, were developed and characterized in terms of particle size distribution, crystallinity, morphology, in vitro dissolution, and sedimentation-redispersibility behavior. A significant reduction in particle size was achieved after the high-pressure homogenization process, and the nanoparticles were further microencapsulated by spray drying technique. The redispersed dried powders exhibited a conserved particle size distribution (in the nanometric range) and certain crystallinity extent, with satisfactory redispersion ability. Besides, the enhancement of the dissolution performance obtained after comminution was conserved, even after drying and redispersion of the extemporaneous powdered formulation. In conclusion, the developed nanoparticle-loaded powders comprise an interesting tool for the administration of praziquantel to preschool-age children.
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Acknowledgments
The authors kindly thank the Universidad Nacional del Sur (PGI 24/ZB70, PGI 24/B252), Agencia Nacional de Promoción Científica y Tecnológica (PICT-2016-0976), and CONICET (PIP 11220150100704CO) for the financial support; Lic. F. Cabrera, Tec. T. Odoux (PLAPIQUI, Argentina), Dr. F. Prado (IFISUR, Argentina), C. Briones Nieva, and Dr. J.M. Bermudez (INIQUI Argentina) for their technical assistance; and Dr. A. Ayala (Universidade Federal do Ceará, Brazil) for the assistance in PXRD data analysis. M. A. Gonzalez is grateful to CONICET (Argentina) for the PhD fellowship.
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Gonzalez, M.A., Ramírez Rigo, M.V. & Gonzalez Vidal, N.L. Orphan Formulations in Pediatric Schistosomiasis Treatment: Development and Characterization of Praziquantel Nanoparticle—Loaded Powders for Reconstitution. AAPS PharmSciTech 20, 318 (2019). https://doi.org/10.1208/s12249-019-1548-z
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DOI: https://doi.org/10.1208/s12249-019-1548-z