Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier

Ilaria Monaco; Simona Camorani; David Colecchia; Erica Locatelli; Pierpaolo Calandro; Anais Oudin; Simone Niclou; Claudio Arra; Mario Chiariello; Laura Cerchia; Mauro Comes Franchini

doi:10.1021/acs.jmedchem.7b00527

Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier

Ilaria Monaco
, Simona Camorani
, David Colecchia
, Erica Locatelli
, Pierpaolo Calandro
, Anais Oudin
, Simone Niclou
, Claudio Arra
, Mario Chiariello^*
, Laura Cerchia
, Mauro Comes Franchini

^*Corresponding author for this work

Research output: Contribution to journal › Article › Research › peer-review

130 Citations (Scopus)

Abstract

Polymeric nanoparticles (PNPs) may efficiently deliver in vivo therapeutics to tumors when conjugated to specific targeting agents. Gint4.T aptamer specifically recognizes platelet-derived growth factor receptor β and can cross the blood-brain barrier (BBB). We synthesized Gint4.T-conjugated PNPs able of high uptake into U87MG glioblastoma (GBM) cells and with astonishing EC₅₀ value (38 pM) when loaded with a PI3K-mTOR inhibitor. We also demonstrated in vivo BBB passage and tumor accumulation in a GBM orthotopic model.

Original language	English
Pages (from-to)	4510-4516
Number of pages	7
Journal	Journal of Medicinal Chemistry
Volume	60
Issue number	10
DOIs	https://doi.org/10.1021/acs.jmedchem.7b00527
Publication status	Published - 25 May 2017

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10.1021/acs.jmedchem.7b00527

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title = "Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier",

abstract = "Polymeric nanoparticles (PNPs) may efficiently deliver in vivo therapeutics to tumors when conjugated to specific targeting agents. Gint4.T aptamer specifically recognizes platelet-derived growth factor receptor β and can cross the blood-brain barrier (BBB). We synthesized Gint4.T-conjugated PNPs able of high uptake into U87MG glioblastoma (GBM) cells and with astonishing EC50 value (38 pM) when loaded with a PI3K-mTOR inhibitor. We also demonstrated in vivo BBB passage and tumor accumulation in a GBM orthotopic model.",

author = "Ilaria Monaco and Simona Camorani and David Colecchia and Erica Locatelli and Pierpaolo Calandro and Anais Oudin and Simone Niclou and Claudio Arra and Mario Chiariello and Laura Cerchia and \{Comes Franchini\}, Mauro",

note = "Funding Information: University of Bologna and Istituto Toscano Tumori are acknowledged for funding this project. The work was supported in part by IG AIRC (n. 18753 to L.C.). S.C. was supported by a Fondazione Umberto Veronesi Fellowship. Publisher Copyright: {\textcopyright} 2017 American Chemical Society.",

year = "2017",

month = may,

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doi = "10.1021/acs.jmedchem.7b00527",

language = "English",

volume = "60",

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journal = "Journal of Medicinal Chemistry",

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TY - JOUR

T1 - Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier

AU - Monaco, Ilaria

AU - Camorani, Simona

AU - Colecchia, David

AU - Locatelli, Erica

AU - Calandro, Pierpaolo

AU - Oudin, Anais

AU - Niclou, Simone

AU - Arra, Claudio

AU - Chiariello, Mario

AU - Cerchia, Laura

AU - Comes Franchini, Mauro

N1 - Funding Information: University of Bologna and Istituto Toscano Tumori are acknowledged for funding this project. The work was supported in part by IG AIRC (n. 18753 to L.C.). S.C. was supported by a Fondazione Umberto Veronesi Fellowship. Publisher Copyright: © 2017 American Chemical Society.

PY - 2017/5/25

Y1 - 2017/5/25

N2 - Polymeric nanoparticles (PNPs) may efficiently deliver in vivo therapeutics to tumors when conjugated to specific targeting agents. Gint4.T aptamer specifically recognizes platelet-derived growth factor receptor β and can cross the blood-brain barrier (BBB). We synthesized Gint4.T-conjugated PNPs able of high uptake into U87MG glioblastoma (GBM) cells and with astonishing EC50 value (38 pM) when loaded with a PI3K-mTOR inhibitor. We also demonstrated in vivo BBB passage and tumor accumulation in a GBM orthotopic model.

AB - Polymeric nanoparticles (PNPs) may efficiently deliver in vivo therapeutics to tumors when conjugated to specific targeting agents. Gint4.T aptamer specifically recognizes platelet-derived growth factor receptor β and can cross the blood-brain barrier (BBB). We synthesized Gint4.T-conjugated PNPs able of high uptake into U87MG glioblastoma (GBM) cells and with astonishing EC50 value (38 pM) when loaded with a PI3K-mTOR inhibitor. We also demonstrated in vivo BBB passage and tumor accumulation in a GBM orthotopic model.

UR - https://www.scopus.com/pages/publications/85019721372

U2 - 10.1021/acs.jmedchem.7b00527

DO - 10.1021/acs.jmedchem.7b00527

M3 - Article

C2 - 28471660

AN - SCOPUS:85019721372

SN - 0022-2623

VL - 60

SP - 4510

EP - 4516

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 10

ER -

Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier

Abstract

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