Desenvolvimento e avaliação da atividade antiinflamatória de sistemas poliméricos de carboidratos naturais para liberação colônica de triancinolona

Abstract

The polymeric associations of carbohydrates in the form of differential systems with chitosan and guar gum in selective enzymatic degradation properties for the well region, bioadhesion, water retention and controlled release under pH conditions simulating the intestinal fluid (ARGIN, KOFINAS, LO, 2014). This work aimed to obtain, characterize and evaluate an in vitro and in vivo anti-inflammatory action of new specified systems (SP) of chitosan and guar gum for the colonic release of triamcinolone (TRI). Systems employing the simple coacervation technique with the addition of sodium sulfate follow the spray drying drying method. After a previous test, standardized: an inlet temperature of 140° C and outlet of 90° C, blower 6.5 and atomization of air 0.1 ppm. Different drug-polymer ratios (1: 5, 1:10 and 1:20 w / w) and polymer-polymer (50:50, 25:75 and 75:25 w / w) were studied for yield (%), encapsulation efficiency , EE (%) and loading (mg TRI / g SP), infrared, DSC, TG, kinetics, swelling and in vivo study to optimize as preparation conditions of the obtained particulate systems. The systems seem to have a higher chitosan: gum ratio (75:25 w / w) showed better yield (%), between the particulate system (25:75 w / w) showed higher encapsulation efficiency (%) and loading (mg TRI / g SP), as well as a lower mass in the thermal analysis (TG). However, because of its low yield, it was chosen to use without in vivo study the polymer ratio 50:50 w / w with 1:10 triamcinolone, because of its yield and reasonable encapsulation efficiency. A characterization of the infrared systems is evidenced as interactions between the components of the formulation. A thermal analysis shown in systems with greater amount of chitosan presented a greater thermal stability. The kinetics study of the three polymer ratios with TRI 1:10 occurred in two phases, a first time with a rapid initial release (burst effect) in 1 hour and a second, more controlled release phase. After 24 hours almost 100% of triamcinolone was released. The swelling study showed the differential statistic from 24h to 48h, with p <0.05, the polymer ratio 75:25 p / p swelled more than other reasons. All specified systems swelled more than placebos. Therefore, the data ensure that a new technological system specialized by spray-drying from chitosan and guar gum, compresses the ability to modify the release of triamcinolone with potential as an anti-inflammatory application in ulcerative colitis.