Radiolabeling and biological characterization of TPGS-based nanomicelles by means of small animal imaging

Tesan, Fiorella Carla; Portillo, Mariano Gastón; Morettón, Marcela A.; Bernabeu, Ezequiel; Salgueiro, M.; Zubillaga, Marcela

doi:10.1016/j.nucmedbio.2016.09.006

Cited by 12 publications

(7 citation statements)

References 25 publications

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“…Tesan et al reported that 99m Tc radiolabeled TPGS micelles and displayed excellent radiostability in vivo. 47 Hence, the radiolabeling of HA-CHEMS-Cur-TPGS NPs could be explained by the complexation of 99m Tc and carboxyl group or two close ester groups. The successful radiolabeling of 99m Tc was found to provide an opportunity for radionuclide 188 Re to be used as internal radionuclide therapy.…”

Section: Resultsmentioning

confidence: 99%

99mTc Radiolabeled HA/TPGS-Based Curcumin-Loaded Nanoparticle for Breast Cancer Synergistic Theranostics: Design, in vitro and in vivo Evaluation

Huang¹,

Chen²,

Zhang³

et al. 2020

IJN

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Background: Emerging cancer therapy requires highly sensitive diagnosis in combination with cancer-targeting therapy. In this study, a self-assembled pH-sensitive curcumin (Cur)loaded nanoparticle of 99m Tc radiolabeled hyaluronan-cholesteryl hemisuccinate conjugates (HA-CHEMS) and D-a-tocopheryl polyethylene glycol succinate (TPGS) was prepared for breast cancer synergistic theranostics. Materials and Methods: The synthesized amphiphilic HA-CHEMS conjugates and TPGS self-assembled into Cur-loaded nanoparticles (HA-CHEMS-Cur-TPGS NPs) in an aqueous environment. The physicochemical properties of HA-CHEMS-Cur-TPGS NPs were characterized by transmission electron microscopy (TEM) and dynamic lighter scattering (DLS). The in vitro cytotoxicity of HA-CHEMS-Cur-TPGS NPs against breast cancer cells was evaluated by using the methyl thiazolyl tetrazolium (MTT) assay. Moreover, the in vivo animal experiments of HA-CHEMS-Cur-TPGS NPs including SPECT/CT imaging biodistribution and antitumor efficiency were investigated in 4T1 tumor-bearing BALB/c mice; furthermore, pharmacokinetics were investigated in healthy mice. Results: HA-CHEMS-Cur-TPGS NPs exhibited high curcumin loading, uniform particle size distribution, and excellent stability in vitro. In the cytotoxicity assay, HA-CHEMS-Cur-TPGS NPs showed remarkably higher cytotoxicity to 4T1 cells with an IC50 value at 38 μg/ mL, compared with free curcumin (77 μg/mL). Moreover, HA-CHEMS-Cur-TPGS NPs could be effectively and stably radiolabeled with 99m Tc. The SPECT images showed that 99m Tc-HA-CHEMS-Cur-TPGS NPs could target the 4T1 tumor up to 4.85±0.24%ID/g at 4 h post-injection in BALB/c mice. More importantly, the in vivo antitumor efficacy studies showed that HA-CHEMS-Cur-TPGS NPs greatly inhibited the tumor growth without resulting in obvious toxicities to major organs. Conclusion: The results indicated that HA-CHEMS-Cur-TPGS NPs with stable 99m Tc labeling and high curcumin-loading capacity hold great potential for breast cancer synergistic theranostics.

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Section: Resultsmentioning

confidence: 99%

99mTc Radiolabeled HA/TPGS-Based Curcumin-Loaded Nanoparticle for Breast Cancer Synergistic Theranostics: Design, in vitro and in vivo Evaluation

Huang¹,

Chen²,

Zhang³

et al. 2020

IJN

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“…As with other NP types, several studies have reported the radiolabelling of polymeric micelles with 99m Tc using the direct labelling method. [390][391][392][393][394][395][396][397][398] Once again, this was shown to be a robust technique; with reported RCYs generally being 495% under optimised conditions and serum stability ca. 98% after 24 h. [395][396][397] The radioiodination of polymeric micelles has also been reported.…”

Section: Radiolabelling Of Organic Nanomaterialsmentioning

confidence: 97%

Radiolabelling of nanomaterials for medical imaging and therapy

2021

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“…One might hypothesize that a poor bioavailability of TPGS-1000 in cardiac tissue could explain this lack of effect. Although TPGS-1000 is well tolerated in vivo and has a good bioavailability, previous studies suggested that it has a weak tropism for cardiac tissue [31]. [33], and thus care must be taken for its use in drug delivery.…”

Section: Discussionmentioning

confidence: 99%

In vitro and in vivo cardioprotective and metabolic efficacy of vitamin E TPGS/Apelin

Goto

Cinato

Merachli

et al. 2020

Journal of Molecular and Cellular Cardiology

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Aims: Apelin and vitamin E have been proposed as signaling molecules, but their synergistic role is unknown. The aim of this work was to develop vitamin E TPGS/Apelin system to test their cardioprotective and metabolic efficacy in vitro and in vivo. Methods: FDA-approved surfactant D-αtocopheryl polyethylene glycol 1000 succinate (TPGS-1000) and Apelin complex were characterized by physico-chemical methods (CMC determination, dynamic light scattering and circular dichroism). In vitro studies were carried out on H9C2 cardiomyoblasts and isolated murine cardiomyocytes. In vivo studies were performed in isoproterenol-and high-fat diet-induced cardiac remodeling models in mice. Results: We found that vitamin E TPGS/Apelin provide cardioprotective and metabolic efficacy in vitro and in vivo. In vitro studies revealed that vitamin E TPGS/Apelin reduces hypoxiainduced mitochondrial ROS production in cultured cardiomyocytes and H9C2 cardiomyoblasts. In addition, vitamin E TPGS/Apelin confers apoptotic response to hypoxic stress in cells. In a mouse model of isoproterenol-induced cardiac injury, TPGS is not able to affect cardiac remodeling, however combination of vitamin E TPGS and Apelin counteracts myocardial apoptosis, oxidative stress, hypertrophy and fibrosis. Furthermore, combination treatment attenuated obesity-induced cardiometabolic and fibrotic remodeling in mice. Conclusion: Together, our data demonstrated the therapeutic benefits of vitamin E TPGS/Apelin complex to combat cardiovascular and metabolic disorders.

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Radiolabeling and biological characterization of TPGS-based nanomicelles by means of small animal imaging

Cited by 12 publications

References 25 publications

<p><sup>99m</sup>Tc Radiolabeled HA/TPGS-Based Curcumin-Loaded Nanoparticle for Breast Cancer Synergistic Theranostics: Design, in vitro and in vivo Evaluation</p>

<p><sup>99m</sup>Tc Radiolabeled HA/TPGS-Based Curcumin-Loaded Nanoparticle for Breast Cancer Synergistic Theranostics: Design, in vitro and in vivo Evaluation</p>

Radiolabelling of nanomaterials for medical imaging and therapy

In vitro and in vivo cardioprotective and metabolic efficacy of vitamin E TPGS/Apelin

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