Apatinib-loaded CalliSpheres Beads for embolization in a rabbit VX2 liver tumor: characterization
            <i>in vitro</i>
            , pharmacokinetics and tumor response
            <i>in vivo</i>

Shi, Qing; Lu, Yongning; Huang, Songjiang; Zhou, Chen; Yang, Chongtu; Liu, Jiacheng; Ma, Jinqiang; Xiong, Bin

doi:10.1080/10717544.2020.1818881

Cited by 13 publications

(18 citation statements)

References 32 publications

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“…For example, Shi et al. prepared an “Apatinib-loaded CalliSpheres Beads” for embolization and examined the pharmacokinetics and tumor response in a rabbit VX2 liver tumor model ( 67 ). The strategy of this study is fundamentally different from these studies: these studies must use microspheres made of polymer materials (such as CalliSpheres Beads) to physically adsorb molecular targeted drugs, and the chemical properties of molecular targeted drugs affect the drug-amount carried by microspheres; and the drug-loaded microspheres obtained in these strategies are mainly the microspheres themselves, and the drug content is limited.…”

Section: Discussionmentioning

confidence: 99%

Novel Microcrystal Formulations of Sorafenib Facilitate a Long-Acting Antitumor Effect and Relieve Treatment Side Effects as Observed With Fundus Microcirculation Imaging

Wang

Zhao³

et al. 2021

Front. Oncol.

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The tyrosine kinase inhibitors (TKIs), including sorafenib, remain one first-line antitumor treatment strategy for advanced hepatocellular carcinoma (HCC). However, many problems exist with the current orally administered TKIs, creating a heavy medical burden and causing severe side effects. In this work, we prepared a novel microcrystalline formulation of sorafenib that not only achieved sustainable release and long action in HCC tumors but also relieved side effects, as demonstrated by fundus microcirculation imaging. The larger the size of the microcrystalline formulation of sorafenib particle, the slower the release rates of sorafenib from the tumor tissues. The microcrystalline formulation of sorafenib with the largest particle size was named as Sor-MS. One intratumor injection (once administration) of Sor-MS, but not Sor-Sol (the solution formulation of sorafenib as a control), could slow the release of sorafenib in HCC tumor tissues and in turn inhibited the in vivo proliferation of HCC or the expression of EMT/pro-survival–related factors in a long-acting manner. Moreover, compared with oral administration, one intratumor injection of Sor-MS not only facilitated a long-acting antitumor effect but also relieved side effects of sorafenib, avoiding damage to the capillary network of the eye fundus, as evidenced by fundus microcirculation imaging. Therefore, preparing sorafenib as a novel microcrystal formulation could facilitate a long-acting antitumor effect and relieve drug-related side effects.

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Section: Discussionmentioning

confidence: 99%

Novel Microcrystal Formulations of Sorafenib Facilitate a Long-Acting Antitumor Effect and Relieve Treatment Side Effects as Observed With Fundus Microcirculation Imaging

Wang

Zhao³

et al. 2021

Front. Oncol.

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“…The agents were physically adsorbed to the microspheres. As an example, the results from Shi et al, 2020 shown that prepared the Apatinib as loaded CalliSpheres Beads for embolization could achieved the good pharmacokinetics feature and tumor response in liver tumor model (115). However, the usage of the microspheres still has some shortcomings: the microspheres such as CalliSpheres Beads were made by the polymer materials and these polymer materials may not be biodegradable.…”

Section: Discussionmentioning

confidence: 99%

A Novel Microcrystalline BAY-876 Formulation Achieves Long-Acting Antitumor Activity Against Aerobic Glycolysis and Proliferation of Hepatocellular Carcinoma

et al. 2021

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BAY-876 is an effective antagonist of the Glucose transporter type 1 (GLUT1) receptor, a mediator of aerobic glycolysis, a biological process considered a hallmark of hepatocellular carcinoma (HCC) together with cell proliferation, drug-resistance, and metastasis. However, the clinical application of BAY-876 has faced many challenges. In the presence study, we describe the formulation of a novel microcrystalline BAY-876 formulation. A series of HCC tumor models were established to determine not only the sustained release of microcrystalline BAY-876, but also its long-acting antitumor activity. The clinical role of BAY-876 was confirmed by the increased expression of GLUT1, which was associated with the worse prognosis among advanced HCC patients. A single dose of injection of microcrystalline BAY-876 directly in the HCC tissue achieved sustained localized levels of Bay-876. Moreover, the single injection of microcrystalline BAY-876 in HCC tissues not only inhibited glucose uptake and prolonged proliferation of HCC cells, but also inhibited the expression of epithelial-mesenchymal transition (EMT)-related factors. Thus, the microcrystalline BAY-876 described in this study can directly achieve promising localized effects, given its limited diffusion to other tissues, thereby reducing the occurrence of potential side effects, and providing an additional option for advanced HCC treatment.

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“…Donafenib has a similar chemical formula to sorafenib, 18 and both carry a positive charge (NH + ) ( Figure 1A ). Composed of polyvinyl alcohol hybrid hydrogel linked to sulfonate group, CBs are net-like spheres carrying negative charge, 19 , 20 allowing drugs charged positively for interaction. The DCBs characterizations were explored as described in the previous literature.…”

Section: Methodsmentioning

confidence: 99%

Donafenib-Loaded Callispheres Beads Embolization in a VX2 Liver Tumor: Investigating Efficacy, Safety, and Improvement of Tumor Angiogenesis After Embolization

Li¹,

Shi²,

Liu³

et al. 2021

JHC

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Objective To investigate the efficiency and safety of callispheres beads loaded with donafenib (DCBs) for embolization in a VX2 liver tumor, as well as the improvement of tumor angiogenesis following embolization. Methods Forty New Zealand white rabbit VX2 liver tumors were treated with four different drugs via the hepatic artery: NS (normal saline), CB (blank callispheres beads), ACB (adriamycin-loaded callispheres beads) and DCB (DCBs). Hematoxylin-eosin staining was performed to assess tumor necrosis, while MRI was employed to detect the changes in tumor size. The safety was evaluated by the liver and kidney function parameters, and the immunofluorescence and immunohistochemical staining were performed to reflect the tumor hypoxia and tumor angiogenesis following embolization. Results The DCB group had the smallest tumor growth rate, but the tumor necrosis rate was the highest of the four groups. Compared to the CB and ACB groups, the DCB group did not aggravate the liver damage and had no influence on kidney function. The staining results showed that, although the tumor hypoxia deteriorated after DCBs embolization, the expression of VEGF (vascular endothelial growth factor) reduced, thus inhibiting tumor angiogenesis. Conclusion DCB administration via hepatic artery is an effective and safe treatment for a preclinical liver cancer model, with the unique benefit of suppressing tumor angiogenesis following embolization.

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Apatinib-loaded CalliSpheres Beads for embolization in a rabbit VX2 liver tumor: characterization in vitro , pharmacokinetics and tumor response in vivo

Cited by 13 publications

References 32 publications

Novel Microcrystal Formulations of Sorafenib Facilitate a Long-Acting Antitumor Effect and Relieve Treatment Side Effects as Observed With Fundus Microcirculation Imaging

Novel Microcrystal Formulations of Sorafenib Facilitate a Long-Acting Antitumor Effect and Relieve Treatment Side Effects as Observed With Fundus Microcirculation Imaging

A Novel Microcrystalline BAY-876 Formulation Achieves Long-Acting Antitumor Activity Against Aerobic Glycolysis and Proliferation of Hepatocellular Carcinoma

Donafenib-Loaded Callispheres Beads Embolization in a VX2 Liver Tumor: Investigating Efficacy, Safety, and Improvement of Tumor Angiogenesis After Embolization

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