Simultaneus multiresponse optimization applied to the development of albendazole microparticles

LAMAS, M.C. ; LEONARDI, D.; SALOMÓN, C.J.; OLIVIERI, A.C.

Barcelona

Congreso; 6th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology; 2008

Albendazole (ABZ), methyl [5-(propyl-thio)-1-H-benzimidazole-2yl] carbamate, is a benzimidazole derivative with a broad antihelmintic spectrum. ABZ is useful against several gastrointestinal parasites, as well as those producing hydatidosis. The latter disease, caused by Echinococcus granulosus, produces hydatidic cysts in kidney, liver and lung.. Although ABZ is poorly soluble in water it is the most commonly drug used in the medical treatment of echinococcosis. Different studies have been carried out to improve the aqueous solubility and dissolution rate of ABZ, such as the preparation of solid dispersions with polyvinylpyrrolidone (PVP), inclusion complexes with cyclodextrins, and incorporation into an hydrophobic micellar coreusing surfactants. Another tool used to increase the dissolution rate of poorly water soluble drugs is the microencapsulation with different polymers. The obtained microparticulesshow different physicochemical properties as compared to the drug itself, and therefore its dissolution rate will be modified. The purpose of this study is to develop ABZ-chitosan microspheres with high dissolution rate and encapsulation efficiency, in order to obtain a systemic action for the treatment of different hydatidic cysts. The achievement of certain predictable quality with desired and predetermined specifications is referred with the broad term "Quality by design" (QBD) The purpose of this study is to develop ABZ-chitosan microspheres with high dissolution rate and encapsulation efficiency, in order to obtain a systemic action for the treatment of different hydatidic cysts.