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Molecules 2018, 23(7), 1655; https://doi.org/10.3390/molecules23071655

Design, Synthesis and Characterization of Novel Co-Polymers Decorated with Peptides for the Selective Nanoparticle Transport across the Cerebral Endothelium

1
Department of Pharmacy, University of Naples Federico II, 80131 Napoli, Italy
2
Center for Advanced Biomaterials for Healthcare, Istituto Italiano di Tecnologia (IIT@CRIB), Largo Barsanti e Matteucci, 53, I-80125 Napoli, Italy
3
Interdisciplinary Research Centre on Biomaterials, (CRIB), University of Naples Federico II, I-80125 Napoli, Italy
4
Department of Chemical, Materials and Industrial Production Engineering, University of Naples Federico II, I-80125 Napoli, Italy
5
Nanobiointeractions & Nanodiagnostics, Istituto Italiano di Tecnologia (IIT), Via Morego, 30, I-16163 Genova, Italy
*
Author to whom correspondence should be addressed.
Received: 30 May 2018 / Revised: 18 June 2018 / Accepted: 28 June 2018 / Published: 6 July 2018
(This article belongs to the Special Issue Molecules for Biotechnologies)
Full-Text   |   PDF [3259 KB, uploaded 6 July 2018]   |  

Abstract

The development of new strategies for enhancing drug delivery to the brain represents a major challenge in treating cerebral diseases. In this paper, we report on the synthesis and structural characterization of a biocompatible nanoparticle (NP) made up of poly(lactic-co-glycolic acid) (PLGA)-polyethylene glycol (PEG) co-polymer (namely PELGA) functionalized with the membranotropic peptide gH625 (gH) and the iron-mimicking peptide CRTIGPSVC (CRT) for transport across the blood-brain barrier (BBB). gH possesses a high translocation potency of the cell membrane. Conversely, CRT selectively recognizes the brain endothelium, which interacts with transferrin (Tf) and its receptor (TfR) through a non-canonical ligand-directed mechanism. We hypothesize that the delivery across the BBB of PELGA NPs should be efficiently enhanced by the NP functionalization with both gH and CRT. Synthesis of peptides and their conjugation to the PLGA as well as NP physical-chemical characterization are performed. Moreover, NP uptake, co-localization, adhesion under dynamic conditions, and permeation across in vitro BBB model are evaluated as a function of gH/CRT functionalization ratio. Results establish that the cooperative effect of CRT and gH may change the intra-cellular distribution of NPs and strengthen NP delivery across the BBB at the functionalization ratio 33% gH–66% CRT. View Full-Text
Keywords: nanoparticles; peptides; blood-brain barrier; drug delivery; transport nanoparticles; peptides; blood-brain barrier; drug delivery; transport
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Falanga, A.P.; Melone, P.; Cagliani, R.; Borbone, N.; D’Errico, S.; Piccialli, G.; Netti, P.A.; Guarnieri, D. Design, Synthesis and Characterization of Novel Co-Polymers Decorated with Peptides for the Selective Nanoparticle Transport across the Cerebral Endothelium. Molecules 2018, 23, 1655.

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