Abstract

Taking advantage of the radiation properties of 99mTc and 186/188Re and the photophysical characteristics of the {M(CO)3}+ moiety (M = Re), we developed a multifunctional silica platform with the theranostic pair 99mTc/Re with high potential for (nano)medical applications. Starting with a general screening to evaluate the most suitable mesoporous silica construct and the development of appropriate chelate systems, multifunctional mesoporous silica microparticles (SBA-15) were synthesized. These particles act as a model towards the synthesis of the corresponding nanoconstructs. The particles can be modified at the external surface with a targeting function and labeled with the {M(CO)3}+ moiety (M = 99mTc, Re) at the pore surface. Thus, a silica platform is realized, whose bioprofile is not altered by the loaded modalities. The described synthetic procedures can be applied to establish a target-specific theranostic nanoplatform, which enables the combination of fluorescence and radio imaging, with the possibility of radio- and chemotherapy.

Highlights

  • IntroductionIn combination with isotopes 186 and 188 of its heavier homolog rhenium (186/188 Re), it represents one of the first “theranostic pairs” for nuclear medical diagnosis and therapy [6]

  • For many decades, the nuclear isomer technetium-99m (99m Tc, t1/2 = 6 h, Eγ = 141 keV) has been the most frequently used radio metal for applications in nuclear medical diagnostics [1,2,3,4,5]

  • To understand which type of mesoporous silica particle is suitable as a theranostic

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Summary

Introduction

In combination with isotopes 186 and 188 of its heavier homolog rhenium (186/188 Re), it represents one of the first “theranostic pairs” for nuclear medical diagnosis and therapy [6]. A conceptual extension of the “theranostic pair” Tc/Re was described by the combination of a 99m Tc-based bio-mimetic with its organometallic but non-radioactive rhenium homologue [7]. The rhenium complex should be therapeutically active through its structure, while the 99m Tc homologue allows for visualizing the pharmacology. Besides the use of Tc and Re as a “theranostic pair”, Stephenson et al demonstrated that the two homologues allow the development of multimodal imaging probes [8].

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