Radiolabelling of nanomaterials for medical imaging and therapy

Pellico, Juan; Gawne, Peter J.; Rosales, Rafael T. M. de

doi:10.1039/d0cs00384k

Cited by 168 publications

(138 citation statements)

References 694 publications

(708 reference statements)

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“…Nanocarriers have been used in the delivery of chemotherapeutic drugs to reduce their toxic and side effects and enhance their anticancer activity (Piktel et al, 2016 ; Shi et al, 2017 ; Pellico et al, 2021 ). Many nanotechnology-based approaches have been studied for biomedical applications such as liposomes, albumin nanoparticles (NPs) or polymeric micelles.…”

Section: Introductionmentioning

confidence: 99%

Effect of XlogP and hansen solubility parameters on the prediction of small molecule modified docetaxel, doxorubicin and irinotecan conjugates forming stable nanoparticles

Zhong

Yao

et al. 2021

Drug Delivery

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Small molecule-chemotherapeutic drug conjugate nanoparticles (SMCDC NPs) has a great advantage in improving drug loading. However, the factors which influence these conjugates forming stable nanoparticles (NPs) are currently unclear. In our previous studies, we synthesized a series of fatty acid-paclitaxel conjugates and suggested that the changes in the hydrophobic parameters (XlogP), solubility parameters and crystallinity of these fatty acid-paclitaxel conjugates were the key factors for affecting these small molecule-chemotherapeutic drug conjugates (SMCDCs) forming stable NPs in water. Here, we selected clinically widely used chemotherapeutic drug (docetaxel (DTX), doxorubicin (DOX) and irinotecan (Ir)) as model drug, and chose three straight-chain fatty acids (acetic acid (Ac), hexanoic acid (HA) and stearic acid (SA)) and one branched small molecule (N-(tert-butoxycarbonyl) glycine (B-G)) to synthesize 12 SMCDCs. Our results indicated that our prediction criterions obtained from paclitaxel conjugates were also appropriated for these synthesized SMCDCs. We suggested that the present studies expanded the scope of application of the above-mentioned influencing factors, provided research ideas for the rational design of SMCDC forming NPs and a basis for screening NPs with good anticancer activity.

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Section: Introductionmentioning

confidence: 99%

Effect of XlogP and hansen solubility parameters on the prediction of small molecule modified docetaxel, doxorubicin and irinotecan conjugates forming stable nanoparticles

Zhong

Yao

et al. 2021

Drug Delivery

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“…To convert SNs into suitable probes for PET and SPECT imaging, we followed a chelator-mediated approach, which is one of the most used methods to radiolabel nanoparticles with radionuclides, such as 64 Cu, 68 Ga, 99m Tc or 111 In. 13 , 26 Labeling organic nanoparticles, and especially lipid nanoparticles, can be done by the use of lipid-derivative chelators. These conjugates can be inserted into the membrane of the lipid particles at the time of their preparation.…”

Section: Resultsmentioning

confidence: 99%

“… 12 Chelator-based radiolabeling strategies offer a high versatility for the incorporation of radionuclides with different properties, suitable for complementary imaging techniques and nanotheranostics. 13 …”

Section: Introductionmentioning

confidence: 99%

Biodistribution of 68/67Ga-Radiolabeled Sphingolipid Nanoemulsions by PET and SPECT Imaging

Díez‐Villares¹,

Pellico²,

Gómez-Lado³

et al. 2021

IJN

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Background and Purpose Non-invasive imaging methodologies, especially nuclear imaging techniques, have undergone an extraordinary development over the last years. Interest in the development of innovative tracers has prompted the emergence of new nanomaterials with a focus on nuclear imaging and therapeutical applications. Among others, organic nanoparticles are of the highest interest due to their translational potential related to their biocompatibility and biodegradability. Our group has developed a promising new type of biocompatible nanomaterials, sphingomyelin nanoemulsions (SNs). The aim of this study is to explore the potential of SNs for nuclear imaging applications. Methods Ready-to-label SNs were prepared by a one-step method using lipid derivative chelators and characterized in terms of their physicochemical properties. Stability was assessed under storage and after incubation with human serum. Chelator-functionalized SNs were radiolabeled with 67 Ga and 68 Ga, and the radiochemical yield (RCY), radiochemical purity (RCP) and radiochemical stability (RCS) were determined. Finally, the biodistribution of 67/68 Ga-SNs was evaluated in vivo and ex vivo. Results Here, we describe a simple and mild one-step method for fast and efficient radiolabeling of SNs with 68 Ga and 67 Ga radioisotopes. In vivo experiments showed that 67/68 Ga-SNs can efficiently and indistinctly be followed up by PET and SPECT. Additionally, we proved that the biodistribution of the 67/68 Ga-SNs can be conveniently modulated by modifying the surface properties of different hydrophilic polymers, and therefore the formulation can be further adapted to the specific requirements of different biomedical applications. Conclusion This work supports 67/68 Ga-SNs as a novel probe for nuclear imaging with tunable biodistribution and with great potential for the future development of nanotheranostics.

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“…Positron emission tomography (PET) and single-photon emission computed tomography (SPECT) are routinely used in clinical oncology in the diagnosis and follow-up of cancer patients. SPECT imaging relies on the use of radionuclides that emit single gamma ( γ )-ray photons with different energies and varying half-lives such as technetium-99 ( 99m Tc; Eγ = 140 keV, t 1/2 = 6 h), indium-111 ( 111 In, Eγ = 245 keV, t 1/2 = 2.8 days), or iodine-123 ( 123 I, Eγ = 159 keV, t 1/2 = 13.2 h), while PET makes use of tracers labelled with radioisotopes that decay by emission of a positron (β + particle), such as fluorine-18 ( 18 F; Eβ + = 634 keV, t 1/2 = 1.8 h), copper-64 ( 64 Cu, Eβ + = 653 keV, t 1/2 = 12.7 h), gallium-68 ( 68 Ga, Eβ + = 1899 keV, t 1/2 = 1.13 h), yttrium-86 ( 86 Y, Eβ + = 3150 keV, t 1/2 = 14.7 h) and zirconium-89 ( 89 Zr, Eβ β+ = 901 keV, t 1/2 = 78.4 h) [ 23 , 24 , 25 , 26 , 27 ]. The positron after interacting with nearby-electron produce two annihilation gamma photons of 511keV emitted in opposite directions generating high-quality images with increased sensitivity and spatial resolution, compared to single-photon emission tomography [ 27 , 28 ].…”

Section: Nuclear Imaging and Targeted Radionuclide Therapymentioning

confidence: 99%

Nanobody-Based Theranostic Agents for HER2-Positive Breast Cancer: Radiolabeling Strategies

Hrynchak

Santos

Falcão

et al. 2021

IJMS

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The overexpression of human epidermal growth factor 2 (HER2) in breast cancer (BC) has been associated with a more aggressive tumor subtype, poorer prognosis and shorter overall survival. In this context, the development of HER2-targeted radiotracers is crucial to provide a non-invasive assessment of HER2 expression to select patients for HER2-targeted therapies, monitor response and identify those who become resistant. Antibodies represent ideal candidates for this purpose, as they provide high contrast images for diagnosis and low toxicity in the therapeutic setting. Of those, nanobodies (Nb) are of particular interest considering their favorable kinetics, crossing of relevant biological membranes and intratumoral distribution. The purpose of this review is to highlight the unique characteristics and advantages of Nb-based radiotracers in BC imaging and therapy. Additionally, radiolabeling methods for Nb including direct labeling, indirect labeling via prosthetic group and indirect labeling via complexation will be discussed, reporting advantages and drawbacks. Furthermore, the preclinical to clinical translation of radiolabeled Nbs as promising theranostic agents will be reported.

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Radiolabelling of nanomaterials for medical imaging and therapy

Abstract: This review describes and critically evaluates the various strategies available to radiolabel organic and inorganic nanomaterials for in vivo imaging and therapy

Cited by 168 publications

References 694 publications

Effect of XlogP and hansen solubility parameters on the prediction of small molecule modified docetaxel, doxorubicin and irinotecan conjugates forming stable nanoparticles

Effect of XlogP and hansen solubility parameters on the prediction of small molecule modified docetaxel, doxorubicin and irinotecan conjugates forming stable nanoparticles

Biodistribution of 68/67Ga-Radiolabeled Sphingolipid Nanoemulsions by PET and SPECT Imaging

Nanobody-Based Theranostic Agents for HER2-Positive Breast Cancer: Radiolabeling Strategies

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