Albendazole-chitosan-hydroxypropylmethyl cellulose microparticulate systems obtained by controlled precipitation.

PRIOTTI, J.; LEONARDI, D.; SALOMON, C.; LAMAS, M. C.

Munster

Congreso; 13th International Conference on Chitin and Chitosan; 2015

European Chitin Society

Albendazole (ABZ) is a benzimidazole derivative with a broad anthelmintic spectrum useful against several gastrointestinal parasites, including Trichinella spiralis. The worms invade muscle tissues, including the heart and diaphragm. ABZ is poorly soluble in water (1 μg/mL at 25 °C), administered only by the oral route. An oral compound must dissolve in the gastric fluids in order to be absorbed, controlling the dissolution process the rate and degree of absorption. Therefore the aim of this work was to develop microparticles based on chitosan (CH) (MW >300 k Da, degree of deacetylation >85%) or hydroxypropylmethylcellulose (HPMC) to improve the ABZ dissolution rate, and the further anti-parasitic activity. Methods: ABZ (400 mg/mL) was solubilized in a mixture acetic acid / ethanol (1:1.5), the solution was dripped to a CH or HPMC solution (0.1 or 0.5% w/v each) with or without poloxamer 388 (0.02 % w/v). The systems were obtained by following a spraying drying methodology. The particles were characterized based on X ray diffraction patterns, size, morphology, yield, ABZ solubility, and ABZ dissolution rate. Results: Both, the highest yield (69 %) and ABZ dissolution rate (83% after 10 minutes assay) were achieve using CH (0.1% w/v) and poloxamer. Additionally, these particles presented the smallest range size (2 to 5 microns) and spheroid morphology. The X ray diffraction patterns showed a decrease in drug crystallinity of ABZ loaded into the microparticles. Conclusion: The microparticles were successfully achieved, improving the physicochemical properties of ABZ.