Investigational New Drugs

, Volume 37, Issue 4, pp 771–778 | Cite as

Cyclodextrin polymers decorated with RGD peptide as delivery systems for targeted anti-cancer chemotherapy

  • Maurizio Viale
  • Rita Tosto
  • Valentina Giglio
  • Giuseppe PappalardoEmail author
  • Valentina Oliveri
  • Irena Maric
  • Maria Addolorata Mariggiò
  • Graziella VecchioEmail author


Polymeric cyclodextrin–based nanoparticles are currently undergoing clinical trials as nanotherapeutics. Using a non-covalent approach, we decorated two cross-linked cyclodextrin polymers of different molecular weights with an RGD peptide derivative to construct a novel carrier for the targeted delivery of doxorubicin. RGD is the binding sequence for the integrin receptor family that is highly expressed in tumour tissues. The assembled host–guest systems were investigated using NMR and DLS techniques. We found that, in comparison with free doxorubicin or the binary complex doxorubicin/cyclodextrin polymer, the RGD units decorating the cyclodextrin-based nanosystems improved the selectivity and cytotoxicity of the complexed doxorubicin towards cultured human tumour cell lines. Our results suggest that the nanocarriers under study may contribute to the development of new platforms for cancer therapy.


Carbohydrates Peptides Nanoparticles Cancer Doxorubicin 



The authors are grateful for support from Università degli Studi di Catania (Piano della Ricerca di Ateneo 2016-2018) and the Italian Ministero dell’Università e della Ricerca. Training grant PO FSE 2014-2020 (Tosto R.) is also gratefully acknowledged.


This study was funded by Università degli Studi di Catania (Piano della Ricerca di Ateneo 2016-2018) and PO FSE 2014-2020 (MIUR).

Compliance with ethical standards

Ethical approval

This article does not contain any studies with human participants or animals performed by any of the authors.

Conflict of interest

All the authors declare that they have no conflict of interest.

Informed consent

For this type of study, formal consent is not required.


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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  1. 1.IRCCS Ospedale Policlinico San Martino, U.O.C. BioterapieGenoaItaly
  2. 2.CNR Istituto di Biostrutture e Bioimmagini, Sede di CataniaCataniaItaly
  3. 3.Dipartimento di Scienze ChimicheUniversità degli Studi di CataniaCataniaItaly
  4. 4.Dipartimento di Scienze Biomediche ed Oncologia UmanaUniversità degli Studi di Bari Aldo MoroBariItaly

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