Resveratrol encapsulation in High Molecular Weight Chitosan-based Nanogels for applications in ocular treatments

BUOSI, FLORENCIA; ELÍAS FERNANDA; CASTAÑEDA CATAÑA MAYRA ALEJANDRA; MARTÍNEZ, KARINA; ALAIMO, AGUSTINA; GARCIA LINARES, GUADALUPE; CARLA C. SPAGNUOLO; PÉREZ, OSCAR EDGARDO; DI SANTO, MARIANA CAROLINA; ACEBEDO, SOFÍA LORENA; LEONARDO LIZARRAGA

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2020 vol. 165 p. 804 - 821

0141-8130

Oxidative stress and inflammation play a pivotal role in ocular diseases. Resveratrol(RSV) is a natural bioactive that has recently attracted attention due to it potentantioxidant and anti-inflammatory properties. However, RSV present poor aqueoussolubility and chemical instability. Besides, effective drug delivery to the posteriorsegment of the eye is challenge nowadays. Nanotechnology emerges as a possiblesolution to improve both limitations. Here, we developed and characterized nanogels(NG) based on high molecular weight chitosan (HCS) crosslinked with sodiumtripolyphosphate. The distribution size of NG presented a major population around 140nm with a ζ-potential value of 32 ± 2 mV. TEM and AFM images showed that NGexhibited a rounded morphology. RSV encapsulation efficiency was 59 ± 1%.Photodegradation experiments showed that HCS by its own protects RSV from UVlight-induced degradation. Biocompatibility assays revealed that NG were not cytotoxicneither inflammatory in human retinal pigment epithelial cells (ARPE-19), whichconstitutes the outer blood-retinal barrier. After cellular internalization, we report anendo‐lysosomal escape of NG, which is crucial for efficient nanocarriers deliverysystems. In conclusion, we envision that HCS based NG could constitute novel carriersfor RSV, opening the possibility of its application in ocular diseases.