Neurotoxicity and brain permeability of targeted polymeric nanoparticles

Domínguez, A. ¹ , Di Mauro, P. P. ² , Suárez Merino , B. ¹ , Borrós, S. ² , Llop, J. ³ & Goñi de Cerio, F. . ¹

1 GAIKER Technology Centre, Biomedicine Unit, Parque Tecnológico Ed 202, Zamudio, Vizcaya, Spain
2 Sagetis Biotech & Grup d'Enginyeria de Materials, Institut Químic de Sarrià, Universitat Ramon Llull, Barcelona, Spain
3 CIC biomaGUNE, Radiochemistry, Molecular Imaging Unit. Paseo Miramón 182, Parque Tecnológico San Sebastián, Guipúzcoa, Spain.

Neurotoxicity and brain permeability of targeted polymeric nanoparticles

Domínguez A.1, Di Mauro P.2, Suarez-Merino B.1, Borrós S.2, Llop J.3 and Goñi-de-Cerio F1.

1 GAIKER Technology Centre, Biomedicine Unit, Parque Tecnológico Ed 202, Zamudio, Vizcaya, Spain.
2 Sagetis Biotech & Grup d'Enginyeria de Materials, Institut Químic de Sarrià, Universitat Ramon Llull, Barcelona, Spain.
3 CIC biomaGUNE, Radiochemistry, Molecular Imaging Unit. Paseo Miramón 182,Parque Tecnológico San Sebastián, Guipúzcoa, Spain.

Health safety is an important concern in nanoparticles development. In particular, their penetration in the central nervous system is an issue of outmost importance. Regarding this matter, blood brain barrier (BBB) in vitro models can be used as a useful tool for the study of nanoparticles brain permeability.

In this study we perform neurotoxicological studies of a polymeric nanoparticle alone or targeted with two different peptide ligands in order to enhance drug delivery to the brain. To this aim, glial cells, neurons and cerebral microvascular endothelial cells were employed. Subsequently, BBB permeability of the aforesaid nanoparticles was tested employing a BBB in vitro model composed of microvascular brain endothelial cells (bEND.3) and glial cells to verify if the peptide ligands improve the nanoparticle ability to cross the endothelial monolayer.

Brain permeability studies employing nanoparticles concentrations selected in neurotoxicological studies, revealed a differential ligand capacity to enhance nanoparticles permeability depending on the employed peptide.