TY - JOUR
T1 - An in vitro and in vivo study of peptide-functionalized nanoparticles for brain targeting
T2 - The importance of selective blood–brain barrier uptake
AU - Bode, Gerard H.
AU - Coué, Gregory
AU - Freese, Christian
AU - Pickl, Karin E.
AU - Sanchez-Purrà, Maria
AU - Albaiges, Berta
AU - Borrós, Salvador
AU - van Winden, Ewoud C.
AU - Tziveleka, Leto Aikaterini
AU - Sideratou, Zili
AU - Engbersen, Johan F.J.
AU - Singh, Smriti
AU - Albrecht, Krystyna
AU - Groll, Jürgen
AU - Möller, Martin
AU - Pötgens, Andy J.G.
AU - Schmitz, Christoph
AU - Fröhlich, Eleonore
AU - Grandfils, Christian
AU - Sinner, Frank M.
AU - Kirkpatrick, C. James
AU - Steinbusch, Harry W.M.
AU - Frank, Hans Georg
AU - Unger, Ronald E.
AU - Martinez-Martinez, Pilar
N1 - Publisher Copyright:
© 2016 Elsevier Inc.
PY - 2017/4/1
Y1 - 2017/4/1
N2 - Targeted delivery of drugs across endothelial barriers remains a formidable challenge, especially in the case of the brain, where the blood–brain barrier severely limits entry of drugs into the central nervous system. Nanoparticle-mediated transport of peptide/protein-based drugs across endothelial barriers shows great potential as a therapeutic strategy in a wide variety of diseases. Functionalizing nanoparticles with peptides allows for more efficient targeting to specific organs. We have evaluated the hemocompatibilty, cytotoxicity, endothelial uptake, efficacy of delivery and safety of liposome, hyperbranched polyester, poly(glycidol) and acrylamide-based nanoparticles functionalized with peptides targeting brain endothelial receptors, in vitro and in vivo. We used an ELISA-based method for the detection of nanoparticles in biological fluids, investigating the blood clearance rate and in vivo biodistribution of labeled nanoparticles in the brain after intravenous injection in Wistar rats. Herein, we provide a detailed report of in vitro and in vivo observations.
AB - Targeted delivery of drugs across endothelial barriers remains a formidable challenge, especially in the case of the brain, where the blood–brain barrier severely limits entry of drugs into the central nervous system. Nanoparticle-mediated transport of peptide/protein-based drugs across endothelial barriers shows great potential as a therapeutic strategy in a wide variety of diseases. Functionalizing nanoparticles with peptides allows for more efficient targeting to specific organs. We have evaluated the hemocompatibilty, cytotoxicity, endothelial uptake, efficacy of delivery and safety of liposome, hyperbranched polyester, poly(glycidol) and acrylamide-based nanoparticles functionalized with peptides targeting brain endothelial receptors, in vitro and in vivo. We used an ELISA-based method for the detection of nanoparticles in biological fluids, investigating the blood clearance rate and in vivo biodistribution of labeled nanoparticles in the brain after intravenous injection in Wistar rats. Herein, we provide a detailed report of in vitro and in vivo observations.
KW - Brain
KW - Nanoparticles
KW - Peptides
KW - Targeting
UR - http://www.scopus.com/inward/record.url?scp=85013813669&partnerID=8YFLogxK
U2 - 10.1016/j.nano.2016.11.009
DO - 10.1016/j.nano.2016.11.009
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C2 - 27884636
AN - SCOPUS:85013813669
SN - 1549-9634
VL - 13
SP - 1289
EP - 1300
JO - Nanomedicine: Nanotechnology, Biology, and Medicine
JF - Nanomedicine: Nanotechnology, Biology, and Medicine
IS - 3
ER -