OCULAR DRUG DELIVERY: NANOFORMULATIONS BASED ON ARGENTINIAN CHITOSAN FOR RESVERATROL ENCAPSULATION

BUOSI FLORENCIA; ALAIMO, AGUSTINA; CASTAÑEDA CATAÑA, MAYRA ALEJANDRA; MARTÍNEZ, KARINA; DI SANTO, MARIANA CAROLINA; DOMINGUEZ RUBIO, ANA PAULA; ACEBEDO, SOFÍA LORENA; SPAGNUOLO, CARLA CECILIA; PÉREZ, OSCAR EDGARDO

Ciudad Autónoma de Buenos Aires

Jornada; IX Jornadas de Jóvenes Investigadores; 2019

Facultad de Ciencias Veterinarias

The retinal tissue has the highest oxygen uptake and glucose oxidation relative to any other tissue, which makes it more susceptible to oxidative stress. Constant light irradiation, atmospheric oxygen and environmental chemicals contribute to oxidative stress as the key factor for the ocular degenerative diseases. Whenever the antioxidant defense systems are depleted or not functional, vision impairment might be observed. For this reason antioxidantsare fundamental agents in prophylactic forms of oxidative diseases. However, considering its sensitive structure, nanotechnology becomes an option in antioxidant protection, stability, bioavailability, and therapeutic efficacy. Therefore, the aim of this work is to develop nanoparticles (NPs) as carriers of antioxidants for the ocular diseases prevention. Particularly, there is an increased interest in the therapeutic effects of Resveratrol (RSV).RSV is a naturally occurring polyphenolic compound, mainly found in black grapes and peanuts. Previous studies have demonstrated the various beneficial effects of RSV on human health, including its neuroprotection, anti-inflammatory action, potent antioxidant activity and anti-aging effects. Chitosan (CHI) is a naturally occurring and abundantly available polysaccharide extensively studied for drug delivery systems due to the biological properties such as its relative non toxicity, biocompatibility, biodegradability, cationic properties andmucoadhesive characteristics. CHI and the cross-linking agent tripolyphosphate-sodium (TPP) can form biocompatible spheres that can be efficiently employed in bioactives delivery. Hence, we designed and developed chitosan-based nanocarriers for RSV encapsulation to overcome this physicochemical and pharmacokinetic limitations. Our results included the design of colloidal NPs of CHI-TPP obtained by ionic gelation. The particle size distribution and the Z-potential were recorded by dynamic light scattering (DLS). The peak of the majority population was located at 144 nm and the obtained value of the Z-potential was 21±4 mV, indicating that the suspension of the NPs is relatively stable. We registered CHI-RSV interactions by fluorescence quenching. In addition, the protective effect of CHI against UV-induced photodegradation of RSV was determined. Also, we obtained TEM images for NPs size and shape characterization. They were rounded. Biological studies performed in human retinal pigment epithelial cells (ARPE-19 cells, ATCC) revealed that both free CHI and NPs were not cytotoxic. Also, uptake and intracellular incorporation was monitored through fluorescence microscopy. Finally, RSV loading- efficiency of the NPs was measured using spectrophotometry. RSV nanoencapsulation could be a potential carrier for the bioactive, opening the possibility of its application for ophthalmic uses.