PRAZIQUANTEL-CHITOSAN MICROPARTICLES PREPARED THROUGH A CONVENTIONAL AND MODIFIED IONOTROPIC GELATION PROCESS. DEVELOPMENT OF A MICROPARTICULATE ORAL DOSAGE FORM.

ORLANDI S.; REAL D. ; LEONARDI D.; SALOMON C.

Munster

Conferencia; ICCC / EUCHIS 2015-12th International Conference of the European Chitin Society; 2015

Praziquantel (PZQ) is an anthelminthic drug widely used to treat schistosomiasis and others trematode and cestode neglected infections. PZQ has very low water solubility and high permeability, then, the rate-limiting process of absorption is the drug dissolution step, a key factor in formulation development. Microencapsulation into hydrophilic polymers is one of the useful tools to increase the aqueous solubility of lipophilic drugs including PZQ. Chitosan (85.5% DD; MW 239.2 KD) is a biodegradable natural hydrophilic polymer. It has low toxicity, biodegradability and good biocompatibility that make it suitable as carrier for pharmaceutical formulations. Therefore, the aim of the present work was the development of PZQ microparticles through the interaction of chitosan with sodium lauryl sulphate. Another aim of this work was the development of hard gelatin capsules, as final dosage form, containing the corresponding PZQ microparticles. All the prepared microparticles were characterized by infrared spectroscopy, scanning electron microscopy and X-ray diffractometry. In-vitro, dissolution rate of both the microparticles and capsules were carried out and compared with PZQ without treatment. Infrared spectra suggested the presence of a novel structure between chitosan and the anionic surfactant. The diffractometric profile of the drug revealed a significant reduction in the sharp peaks of PZQ indicating a loss of crystallinity. In comparison with the already established ionotropic gelation process, the modified technique produced a remarkably differences on the PZQ release rate. Thus, according the applied gelation process, dissolution studies showed that the percentage of drug dissolved increased up to 90 % within 30 min.