Development of a Drug Delivery System Based on Chitosan Nanoparticles for Oral Administration of Interferon-α

CÁNEPA, CAMILA; IMPERIALE, JULIETA C.; BERINI, CAROLINA A.; LEWICKI, MARIANELA; BIGLIONE, MIRNA M.

BIOMACROMOLECULES

AMER CHEMICAL SOC

Lugar: Washington; Año: 2017

1525-7797

Despite the good clinical efficacy of interferon-12 alpha (IFNα) to treat some types of cancer and viral infections,13 this biological drug is underused given its severe adverse effects14 and high dosing parenteral regimens. Aiming to achieve a15 breakthrough in therapy with IFNα, this work reports for the16 first time on the design and full characterization of a novel17 nanomedicine of IFNα-2b-loaded chitosan nanoparticles (IFN-CT18 NPs) for oral delivery. IFN-CT NPs produced by ionotropic19 gelation, encapsulating approximately 100% of the drug, showed a20 size of 36 ± 8 nm, zeta potential of +30 mV (dynamic light scattering), and spherical morphology (transmission electron21 microscopy). The antiviral activity of IFN-CT NPs in vitro was comparable to that of commercial IFNα. Remarkably, both22 treatments stimulated the expression of IFN genes to a similar extent in both noninfected and infected cells with Human23 Lymphotropic-T Virus type 1. Finally, oral administration of IFN-CT NPs (0.3 MIU) to CF1 mice showed detectable levels of24 IFNα in plasma after 1 h, whereas no IFNα was detected with a commercial formulation. These results are encouraging and open