Highly Homogeneous Biotinylated Carbon Nanodots: Red-Emitting Nanoheaters as Theranostic Agents toward Precision Cancer Medicine

Cinzia Scialabba, Marco Cannas, Gennara Cavallaro, Nicolò Mauro, Gianpiero Buscarino, Gaetano Giammona, Fabrizio Messina, Giuseppina Roscigno, Nicolò Mauro, Gerolama Condorelli, Alice Sciortino

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8 Citazioni (Scopus)

Abstract

Very recent red-emissive carbon nanodots (CDs) have shown potential as near-infrared converting tools toproduce local heat useful in cancer theranostics. Besides, CDs seem very appealing for clinical applications combininghyperthermia, imaging, and drug delivery in a single platform capable of selectively targeting cancer cells. However, CDs stillsuffer from dramatic dot-to-dot variability issues such that a rational design of their structural, optical, and chemicalcharacteristics for medical applications has been impossible so far. Herein, we report for the first time a simple and highlycontrollable layer-by-layer synthesis of biotin-decorated CDs with monodisperse size distribution, well established polymericshell thickness, and degree of surface functionalization, endowed with strong red luminescence and the ability to convert NIRlight into heat. These CDs, henceforth named CDs-PEG-BT, consist of a carbonaceous core passivated with biotin-terminatedPEG2000 chains, which we demonstrate as active targeting groups to recognize cancer cells. The CDs-PEG-BT are designed toefficiently incorporate a high amount of anticancer drugs such as irinotecan (16−28%) and to act as NIR-activated nanoheaterscapable of triggering local hyperthermia and massive drug release inside tumors, thus provoking sudden and efficient tumordeath. The potential of the irinotecan-loaded CDs-PEG-BT (CDs-PEG-BT@IT) in fluorescence imaging was studied on 2Dcultures and on complex 3D spheroids mimicking in vivo tumor architectures, showing their capability of selectively enteringcancer cells through biotin receptors overexpressed in cell membranes. The efficient anticancer effect of these CDs wasthoroughly assessed on multicellular 3D spheroids and patient organoids (tumor-on-a-dish preclinical models) to predict thedrug response in humans in view of personalized medicine applications. CDs-PEG-BT@IT have a smart combination ofproperties, which pave the way to their real-world use as anticancer theranostic agents for image-guided photothermalapplications.
Lingua originaleEnglish
pagine (da-a)19854-19866
Numero di pagine13
RivistaACS APPLIED MATERIALS & INTERFACES
Volume11
Stato di pubblicazionePublished - 2019

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Medicine
Carbon
irinotecan
Polyethylene glycols
Tumors
Biotin
Cells
Imaging techniques
Medical applications
Cell membranes
Drug delivery
Pharmaceutical Preparations
Antineoplastic Agents
Luminescence
Fluorescence
Infrared radiation

All Science Journal Classification (ASJC) codes

  • Materials Science(all)

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title = "Highly Homogeneous Biotinylated Carbon Nanodots: Red-Emitting Nanoheaters as Theranostic Agents toward Precision Cancer Medicine",
abstract = "Very recent red-emissive carbon nanodots (CDs) have shown potential as near-infrared converting tools toproduce local heat useful in cancer theranostics. Besides, CDs seem very appealing for clinical applications combininghyperthermia, imaging, and drug delivery in a single platform capable of selectively targeting cancer cells. However, CDs stillsuffer from dramatic dot-to-dot variability issues such that a rational design of their structural, optical, and chemicalcharacteristics for medical applications has been impossible so far. Herein, we report for the first time a simple and highlycontrollable layer-by-layer synthesis of biotin-decorated CDs with monodisperse size distribution, well established polymericshell thickness, and degree of surface functionalization, endowed with strong red luminescence and the ability to convert NIRlight into heat. These CDs, henceforth named CDs-PEG-BT, consist of a carbonaceous core passivated with biotin-terminatedPEG2000 chains, which we demonstrate as active targeting groups to recognize cancer cells. The CDs-PEG-BT are designed toefficiently incorporate a high amount of anticancer drugs such as irinotecan (16−28{\%}) and to act as NIR-activated nanoheaterscapable of triggering local hyperthermia and massive drug release inside tumors, thus provoking sudden and efficient tumordeath. The potential of the irinotecan-loaded CDs-PEG-BT (CDs-PEG-BT@IT) in fluorescence imaging was studied on 2Dcultures and on complex 3D spheroids mimicking in vivo tumor architectures, showing their capability of selectively enteringcancer cells through biotin receptors overexpressed in cell membranes. The efficient anticancer effect of these CDs wasthoroughly assessed on multicellular 3D spheroids and patient organoids (tumor-on-a-dish preclinical models) to predict thedrug response in humans in view of personalized medicine applications. CDs-PEG-BT@IT have a smart combination ofproperties, which pave the way to their real-world use as anticancer theranostic agents for image-guided photothermalapplications.",
author = "Cinzia Scialabba and Marco Cannas and Gennara Cavallaro and Nicol{\`o} Mauro and Gianpiero Buscarino and Gaetano Giammona and Fabrizio Messina and Giuseppina Roscigno and Nicol{\`o} Mauro and Gerolama Condorelli and Alice Sciortino",
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language = "English",
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TY - JOUR

T1 - Highly Homogeneous Biotinylated Carbon Nanodots: Red-Emitting Nanoheaters as Theranostic Agents toward Precision Cancer Medicine

AU - Scialabba, Cinzia

AU - Cannas, Marco

AU - Cavallaro, Gennara

AU - Mauro, Nicolò

AU - Buscarino, Gianpiero

AU - Giammona, Gaetano

AU - Messina, Fabrizio

AU - Roscigno, Giuseppina

AU - Mauro, Nicolò

AU - Condorelli, Gerolama

AU - Sciortino, Alice

PY - 2019

Y1 - 2019

N2 - Very recent red-emissive carbon nanodots (CDs) have shown potential as near-infrared converting tools toproduce local heat useful in cancer theranostics. Besides, CDs seem very appealing for clinical applications combininghyperthermia, imaging, and drug delivery in a single platform capable of selectively targeting cancer cells. However, CDs stillsuffer from dramatic dot-to-dot variability issues such that a rational design of their structural, optical, and chemicalcharacteristics for medical applications has been impossible so far. Herein, we report for the first time a simple and highlycontrollable layer-by-layer synthesis of biotin-decorated CDs with monodisperse size distribution, well established polymericshell thickness, and degree of surface functionalization, endowed with strong red luminescence and the ability to convert NIRlight into heat. These CDs, henceforth named CDs-PEG-BT, consist of a carbonaceous core passivated with biotin-terminatedPEG2000 chains, which we demonstrate as active targeting groups to recognize cancer cells. The CDs-PEG-BT are designed toefficiently incorporate a high amount of anticancer drugs such as irinotecan (16−28%) and to act as NIR-activated nanoheaterscapable of triggering local hyperthermia and massive drug release inside tumors, thus provoking sudden and efficient tumordeath. The potential of the irinotecan-loaded CDs-PEG-BT (CDs-PEG-BT@IT) in fluorescence imaging was studied on 2Dcultures and on complex 3D spheroids mimicking in vivo tumor architectures, showing their capability of selectively enteringcancer cells through biotin receptors overexpressed in cell membranes. The efficient anticancer effect of these CDs wasthoroughly assessed on multicellular 3D spheroids and patient organoids (tumor-on-a-dish preclinical models) to predict thedrug response in humans in view of personalized medicine applications. CDs-PEG-BT@IT have a smart combination ofproperties, which pave the way to their real-world use as anticancer theranostic agents for image-guided photothermalapplications.

AB - Very recent red-emissive carbon nanodots (CDs) have shown potential as near-infrared converting tools toproduce local heat useful in cancer theranostics. Besides, CDs seem very appealing for clinical applications combininghyperthermia, imaging, and drug delivery in a single platform capable of selectively targeting cancer cells. However, CDs stillsuffer from dramatic dot-to-dot variability issues such that a rational design of their structural, optical, and chemicalcharacteristics for medical applications has been impossible so far. Herein, we report for the first time a simple and highlycontrollable layer-by-layer synthesis of biotin-decorated CDs with monodisperse size distribution, well established polymericshell thickness, and degree of surface functionalization, endowed with strong red luminescence and the ability to convert NIRlight into heat. These CDs, henceforth named CDs-PEG-BT, consist of a carbonaceous core passivated with biotin-terminatedPEG2000 chains, which we demonstrate as active targeting groups to recognize cancer cells. The CDs-PEG-BT are designed toefficiently incorporate a high amount of anticancer drugs such as irinotecan (16−28%) and to act as NIR-activated nanoheaterscapable of triggering local hyperthermia and massive drug release inside tumors, thus provoking sudden and efficient tumordeath. The potential of the irinotecan-loaded CDs-PEG-BT (CDs-PEG-BT@IT) in fluorescence imaging was studied on 2Dcultures and on complex 3D spheroids mimicking in vivo tumor architectures, showing their capability of selectively enteringcancer cells through biotin receptors overexpressed in cell membranes. The efficient anticancer effect of these CDs wasthoroughly assessed on multicellular 3D spheroids and patient organoids (tumor-on-a-dish preclinical models) to predict thedrug response in humans in view of personalized medicine applications. CDs-PEG-BT@IT have a smart combination ofproperties, which pave the way to their real-world use as anticancer theranostic agents for image-guided photothermalapplications.

UR - http://hdl.handle.net/10447/359834

M3 - Article

VL - 11

SP - 19854

EP - 19866

JO - ACS APPLIED MATERIALS & INTERFACES

JF - ACS APPLIED MATERIALS & INTERFACES

SN - 1944-8244

ER -