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Microencapsulación de secnidazol mediante secado por aspersión

Abstract:

Secnidazole is a synthetic derivative of the nitroimidazoles series that has antiparasitic activity, it is two times more active than metronidazole. This drug is used for the treatment of the parasitosis by Giardia lamblia, Entamoeba histolytica, Gardnerella vaginalis and Trichomonas vaginalis. It has a low acceptance of powder for oral suspension that is the conventional way of administration for children and that has a greater efficiency, due to its shows an unpleasant taste referred as a metallic taste. Moreover, the current drug is degradable in the stomach and for this reason it is not absorbed at 100% in the intestinal tract, place where parasites often stay, so the main aim of this investigation was to microencapsulate secnidazole by spray drying method. For this work, polymers Eudragit® S-100, L-100 and L-100-55 were used from EVONIK INDUSTRIES, dispersions of drug were prepared in the different polymers, using a drug-polymer ratio of 40:60. The samples were dried in a mini-spraydryer Büchi B-191 using an atomization air flow of 600 L/h and temperatures of input and output of 150 and 85 °C respectively. With the collected samples, the process yield and the microencapsulation efficiency were determined using differential scanning calorimetry and comparing by diffraction (XRD) to select the best polymer. The best yield obtained was 72.3 ± 0.8% with Eudragit® L-100, and a microencapsulation efficiency of 98.96%, that seems to be greater than the ones achieved by other methods studied, coinciding with the XRD results. The results showed a high efficiency of the Eudragit® L-100 in the microencapsulation of the secnidazole