IQUIR   05412
INSTITUTO DE QUIMICA ROSARIO
Unidad Ejecutora - UE
congresos y reuniones científicas
Título:
FORMULATION AND CHARACTERIZATION OF PRAZIQUANTEL NANOPARTICLES BY A GELATION PROCESS.
Autor/es:
ARRÚA E; SALOMON C.
Reunión:
Conferencia; ICCC / EUCHIS 2015-12th International Conference of the European Chitin Society; 2015
Resumen:
Praziquantel (PZQ) is the drug of choice for schistosomiasis, a neglected parasitic disease. It is classified as Class II in the Biopharmaceutic Classification System, and its low aqueous solubility hinders its performance in biological systems. A useful tool to solve this drawback is the incorporation of the drug into nanoparticulate systems. The objective of this study was to develop chitosan (85.5% DD; MW 239.2 KD) nanoparticles as carrier for the development of novel PZQ delivery systems. Several experiments were performed to evaluate how the physicochemical properties of the PZQ nanoparticles was influenced by systematically varying process parameters including type and ratio of crosslinking agent (EDTA, succinic acid and sodium lauryl sulphate) effect of surfactant (Span 60) and type of drying (lyophilized or drying chamber). The particles were characterized by particle size analysis, zeta potential, aqueous solubility, encapsulation efficiency, infrared spectroscopy, X-ray diffractometry, and in vitro drug release. Particle size of PZQ nanoparticles was between 124 and 455 nm depending on both the crosslinking agent and the type of drying. The drug encapsulation efficiency was found to be around 69 and 99%. Crystalline structure of PZQ partially dimished or transformed into an amorphous phase depending which crosslinking agent was selected. Drug release studies from nanoparticles showed an increase of PZQ dissolution in comparison with the raw material. In all samples the smaller particle size resulted in higher solubility and faster dissolution rate. Thus, the nanoencapsulation of PZQ by a gelation process is a convenient approach to improve the antiparasite therapy.