Formulation and characterization of praziquantel and benznidazole-loaded lipid nanocapsules.

EVA CAROLINA ARRUA; GUILLAUME BASTIAT; CLAUDIO JAVIER SALOMON

Rosario

Congreso; 4º Reunión Internacional de Ciencias Farmacéuticas; 2016

FORMULATION AND CHARACTERIZATION OF PRAZIQUANTEL AND BENZNIDAZOLE-LOADED LIPID NANOCAPSULES. Arrua E.1, Bastiat G.2, Salomon C.1,3 arruacarolina@gmail.com1IQUIR-CONICET, Rosario, Argentina. 2MINT, INSERM U1066, IBS-CHU, Angers, France 3Área Técnica Farmacéutica, Departamento Farmacia. Facultad de Ciencias Bioquímicas y Farmacéuticas, UNR.The aim of this study was to explore the feasibility of encapsulating benznidazole (BNZ) and praziquantel (PZQ), two lipophilic antiparasitic agents, into lipid nanocapsules (LNC) for oral delivery. The process was carried through the phase inversion method that allows the formulation of nanocapsules by a thermal manipulation of an oil/water system. Briefly, a solution of BZN or PZQ in acetone were incorporated in Labrafac and sonicated for 15 minutes. Then, these solutions were heated to evaporate completely acetone. This phase was mixed with Lipoid® S75-3, sodium chloride, Kolliphor® HS15 and heated under magnetic stirring up to 90 oC ensuring that the phase inversion temperature is passed. The cooling step was then performed until a temperature of 50 oC was reached, again, completely passing the phase inversion zone. This cycle was repeated twice before adding 5ml of distilled water at 4 oC. The hydrodynamic diameter, polydispersity index and zeta potential of LNC were determined by dynamic light scattering, each measurement was done in triplicate at 25 °C. It was evaluated the activation of the complement system in normal human serum by measuring the residual hemolytic system capacity after being in contact with LNC. The results showed that loaded and non-loaded LNC with both BNZ and PZQ exhibited a very similar average size of 50nm and a polydispersity index less than 0.07, which would indicate homogeneous size distribution. It was observed that activation of the complement system by all loaded LNC formulations was similar to that obtained with the non-loaded LNC, which could confirm the encapsulation of the drug into the LNC core. In addition, the loaded LNC presented similar results regarding the surviving cells for 24 and 48 hours after the start. Thus, LNC prepared with BNZ and PZQ may represent an attractive alternative for the efficient delivery of these antiparasitic agents. Studies are currently under way to further investigate the in vivo performance of these LNC.