Design of Polyazamacrocyclic Gd 3+ Theranostic Agent Combining MRI and Two-Photon PDT - Université de Bretagne Occidentale Access content directly
Preprints, Working Papers, ... Year : 2020

Design of Polyazamacrocyclic Gd 3+ Theranostic Agent Combining MRI and Two-Photon PDT

Eniko Molnar
  • Function : Author
  • PersonId : 1025002
János Kiss
  • Function : Author
  • PersonId : 1070275
Cyrille Monnereau
Gyula Tircso
  • Function : Author
  • PersonId : 1025006
Olivier Maury

Abstract

New “all-in-one” theranostic systems, combining a magnetic resonance imaging (MRI) contrast agent with a biphotonic photodynamic therapy (2P-PDT) photosensitiser generating cytotoxic singlet oxygen, were envisaged and synthesised. They are based on azamacrocycles, regiospecifically functionalised by two-photon PDT π-conjugated dibromobenzene-picolinate photosensitisers and acetate, able to complex gadolinium(III) and allow an MRI signal. Our approach was to use two different macrocyclic platforms, tacn and pyclen, for modulating simultaneously the structures, properties and solubility of the complexes. Photophysical properties of the ligands and their gadolinium(III) complexes were fully investigated. The Gd3+-pyclen derivative showed the best water solubility and the greatest value of singlet oxygen generation of the series with φΔ = 0.53 enabling in vitro studies. The biological PDT activity under mono and biphotonic excitation was evaluated in human breast cancer cells (MCF-7). While a very low dark toxicity was observed, an almost total cell death was induced after only 3 successive irradiations of 1.57 sec. Finally, its relaxivity was measured in a DMSO/H2O solvents mixture with r1p = 11.21 and r2p = 24.60 mM-1s -1 at 3.0 T and T1- and T2-weighted phantom MR images were obtained highlighting a first generation of “all-in-one” PDT/MRI theranostic agents.
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Dates and versions

hal-03018923 , version 1 (23-11-2020)

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  • HAL Id : hal-03018923 , version 1

Cite

Laura Abad Galan, Nadège Hamon, Christopher Nguyen, Eniko Molnar, János Kiss, et al.. Design of Polyazamacrocyclic Gd 3+ Theranostic Agent Combining MRI and Two-Photon PDT. 2020. ⟨hal-03018923⟩
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