Formulation of cross-linked and non-crosslinked chitosan-based microparticles for oral delivery of praziquantel filled in hard-gelatin capsules

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

Congreso; X Congreso de Protozoología y Enfermedades Parasitarias; 2014

The interest of novel drug delivery systems has been focused on oral controlled-release dosage forms. They distribute more uniformly in the gastrointestinal tract, resulting in more reproducible release profiles, more predictable gastric emptying, reduced local irritation, and a minimized risk of dose dumping. In this study, the development of novel microparticulate solid dosage form of Praziquantel (PZQ), an anthelmintic drug, mainly used to treat shistososomiasis, was investigated. PZQ was loaded into polymeric microparticles based on chitosan or chitosan-sodium lauryl sulfate, and then included into hard gelatin capsules. Spray drying technique was applied to produce the PZQ microparticles. The product was evaluated by X-ray powder diffractometry, infrared spectroscopy and scanning electron microscopy. Non-crosslinked microparticles were prepared without sodium lauryl sulfate. The results obtained suggested that spray-drying is a good technique for the preparation of both non-crooslinked and crosslinked PZQ-chitosan microparticles. The dissolution rate of the drug from all chitosan microparticles was significantly higher than that of drug alone. Unexpectedly, the reinforced crosslinked microparticles exhibited a higher dissolution rate in comparison with the non-crosslinked microparticles, probably due to the gelation process. Regarding the behavior of the particles when incorporated into hard gelatin capsules, it was found that the PZQ dissolution from crosslinked chitosan formulations was faster than the reference capsule. The characterization of the polymeric matrix indicated a clear ionic interaction between the polymer and the surfactant that would be responsible for the modified dissolution rate. In conclusion, chitosan-sodium lauryl sulphate microparticles prepared by spray drying, is a promising approach to deliver PZQ in hard gelatin capsules.