Aptamer nanovehiculization for the development of novel targeted molecular agents

CASTELLI, R.; FERNANDEZ M.; SICCO E.; IBARRA M.; CABRAL, P; CERECETTO H.; CALZADA V.; GLISONI R.J.

Buenos Aires Virtual

Conferencia; 1st Zooming into preclinical Nanomedicines in the era Covid-19; 2020

Asociación Argentina de Nanomedicinas

Aptamers are oligonucleotides that have the characteristic of recognizing a target with high affinityand specificity. The greatest challenges are to hinder the degradation by nucleases and toincrease blood circulation. Sgc8c is an aptamer that recognizes the PTK7 receptor, described as atumor target that has been previously studied by our research group, as a molecular imagingprobe. The purpose of this work was the nanovehiculization of Sgc8c to improve its delivery, aswell as its stability. For it, Sgc8c-(CH2)6-NH2 was conjugated to Alexa647 fluorophore (Sgc8cALEXA) and its vehiculization was studied using: preformed pegylated liposomes (LPS) andpolymeric micelles (PMs) based of PEO-PPO copolymers. The particle size and Zeta-potential ofloaded-systems were different to that of the free-systems. The images obtained by TEM and AFMshowed different morphology between them. In brief, these studies showed evidence that theprobe would be interacting with the nanoparticles.Finally, the biodistribution and pharmacokinetic studies in animals included the administration ofthe free-probe and the nanosystems/probe were done. Pharmacokinetic and biodistributionparameters were evaluating quantifying the fluorescent probe. All data obtained, suggest that LPSand PMs would increase the bioavailability of Sgc8c-ALEXA in short times.