Abstract:

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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<em>Cassia grandis</em> Lf nanodispersion is a hypoglycemic product with a potent α-glucosidase and pancreatic lipase inhibitor effect

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.

^{Pharmacy Department, Faculty of Natural Sciences, University of Oriente, Patricio Lumumba s/n, Santiago de Cuba, CP 84500 Santiago de Cuba, Cuba}

^{Division of Postgraduate Studies in Health, University of La Sierra del Sur, Calle Guillermo Rojas Mijangos S/N, Esq. Av. Universidad Colonial, Miahuatlán de Porfirio Díaz, C.P. 70800 Oaxaca, Mexico}

^{Laboratory of Innovation and Development in Pharmaceutical Technology (LIDETEF), Faculty of Pharmaceutical Sciences, Federal University of Amazonas, Ave Rodrigo Otavio Ramos, 6200, Barrio Coroado, CEP 69077-000 Manaus, AM, Brazil}

^{Laboratory of Biological Activity, Pharmaceutical Sciences Faculty, Federal University of Amazonas, Ave. Rodrigo Otavio Ramos 6200, Coroado, CEP 69077-000 Manaus, AM, Brazil}

^{Drug Research Laboratory, Federal University of Amapá, Rodovia Juscelino Kubitschek, km 2, Jardim Marco Zero, CEP: 68903-419 Macapá, AP, Brazil}

Jesus Rafael Rodriguez Amado: moc.liamg@9002allibirij

^{Corresponding author at: Laboratório de Inovação e Desenvolvimento em Tecnología Farmacéutica (LIDETEF), Faculty of Pharmaceutical Sciences, Federal University of Amazonas, Ave. Rodrigo Otavio Ramos 6200, Coroado, CEP 69077-000 Manaus, AM, Brazil.}moc.liamg@9002allibirij

Jesus Rafael Rodriguez Amado: moc.liamg@9002allibirij

Received 2018 Mar 30; Accepted 2018 Oct 16.

This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

DLN, extract-loaded nanoparticle, Statistical differences at p < 0.05.

Different letters in a row mean statistical differences at p < 0.05.

Footnotes

Peer review under responsibility of King Saud University.

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