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Saudi Pharmaceutical Journal 2019-Feb

Cassia grandis Lf nanodispersion is a hypoglycemic product with a potent α-glucosidase and pancreatic lipase inhibitor effect.

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Ariadna Prada
Hady Keita
Tatiane de Souza
Emerson Lima
Leonard Acho
Márcia da Silva
José Carvalho
Jesus Amado

Ключевые слова

абстрактный

Purpose
This study aimed to evaluate the hypoglycemic effect, antioxidant, α-glucosidase and lipase inhibitory activity, and the cytotoxicity of the Cassia grandis nanodispersion (CgND).

Methods
The hypoglycemic effect was evaluated in alloxan-induced diabetic mice. The particle size, polydispersion index, ζ-potential, and conductivity, as well as the drug-loaded content, were monitored in shelf-live, along a year. The delivery profile was evaluated in simulated intestinal fluids at pH 6.5 and 7.4. The antioxidant effect was evaluated as DPPH and ABTS inhibition. The murine α-glucosidase inhibitory activity and the lipase-inhibitory effect were evaluated in vitro. Cytotoxicity was evaluated by the Alamar blue test.

Results
CgND remained stable for a year in shelf conditions. The hypoglycemic effect in a dose of 10 mg/kg was not statistically different from glibenclamide 25 mg/kg. Nanoparticles released 100% of extract in 120 min at pH 6.5 and 7.4. Nanodispersion exhibited a potent α-glucosidase and lipase-inhibitory effect with IC50 of 3.96 and 0.58 µg/mL, respectively. A strong antioxidant activity against DPPH (IC50 0.65 µg/mL) and ABTS (0.48 µg/mL) was also observed. The hypoglycemic effect could occur, at least in part, via antioxidant and α-glucosidase inhibition. CgND is non-cytotoxic in MRC-5 line cell. This nanodispersion is a promising nanotechnological product that could be used in pharmaceuticals for the treatment of Type II diabetes and related complications as obesity.

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