Optimized Loading of Idarubicin in CalliSpheres® Drug-Eluting Beads and Characterization of Release Profiles and Morphological Properties

Lu, Enhao; Shao, Guoliang; Ma, Jingqin; He, Yejun; Gong, Yuanchuan; Yan, Zhi‐Ping; Sha, Xianyi

doi:10.3390/pharmaceutics13060799

Cited by 6 publications

(5 citation statements)

References 15 publications

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“…Notably, CB is reported as an ideal drug carrier of apatinib, idarubicin, arsenic trioxide, etc. [ 10 , 41 , 42 ]. Combined with previous literatures, we concluded that the lidocaine/CalliSpheres ® composites were successfully prepared, and exhibited preliminary application potential as drug carriers.…”

Section: Resultsmentioning

confidence: 99%

One-step fabrication of lidocaine/CalliSpheres® composites for painless transcatheter arterial embolization

et al. 2022

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Background Transcatheter arterial embolization (TAE) is one of the first-line treatments for advanced hepatocellular cancer. The pain caused by TAE is a stark complication, which remains to be prevented by biomedical engineering methods. Methods Herein, a commercial embolic agent CalliSpheres® bead (CB) was functionally modified with lidocaine (Lid) using an electrostatic self-assembly technique. The products were coded as CB/Lid-n (n = 0, 5, 10, corresponding to the relative content of Lid). The chemical compositions, morphology, drug-loading, and drug-releasing ability of CB/Lid-n were comprehensively investigated. The biocompatibility was determined by hemolysis assay, live/dead cell staining assay, CCK8 assay, immunofluorescence (IHC) staining assay and quantitative real-time PCR. The thermal withdrawal latency (TWL) and edema ratio (ER) were performed to evaluate the analgesia of CB/Lid-n using a plantar inflammation model. A series of histological staining, including immunohistochemistry (IL-6, IL-10, TGF-β and Navi1.7) and TUNEL were conducted to reveal the underlying mechanism of anti-tumor effect of CB/Lid-n on a VX2-tumor bearing model. Results Lid was successfully loaded onto the surface of CalliSpheres® bead, and the average diameter of CalliSpheres® bead increased along with the dosage of Lid. CB/Lid-n exhibited desirable drug-loading ratio, drug-embedding ratio, and sustained drug-release capability. CB/Lid-n had mild toxicity towards L929 cells, while triggered no obvious hemolysis. Furthermore, CB/Lid-n could improve the carrageenan-induced inflammation response micro-environment in vivo and in vitro. We found that CB/Lid-10 could selectively kill tumor by blocking blood supply, inhibiting cell proliferation, and promoting cell apoptosis. CB/Lid-10 could also release Lid to relieve post-operative pain, mainly by remodeling the harsh inflammation micro-environment (IME). Conclusions In summary, CB/Lid-10 has relatively good biocompatibility and bioactivity, and it can serve as a promising candidate for painless transcatheter arterial embolization.

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Section: Resultsmentioning

confidence: 99%

One-step fabrication of lidocaine/CalliSpheres® composites for painless transcatheter arterial embolization

et al. 2022

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“…CalliSpheres DLMS is a new type of drug-loaded microsphere system, and its volume will be signifcantly reduced after drug loading. After 20 days of interventional therapy, with the gradual release of chemotherapy drugs, the volume of CalliSpheres DLMS will gradually recover, so it can efectively block the blood vessels supplying tumors and prolong the recanalization time of the blood vessels supplying tumors [13,14].…”

Section: Discussionmentioning

confidence: 99%

Magnetic Resonance Diffusion-Weighted Imaging to Evaluate the Clinical Efficacy of CalliSpheres Drug-Loaded Microspheres in the Treatment of Advanced Bladder Cancer

Yang

Chen

2023

Concepts in Magnetic Resonance Part A

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The MR diffusion-weighted imaging technique was used to evaluate the efficacy and safety of CalliSpheres drug-loaded microspheres for transarterial chemoembolization in the treatment of advanced bladder cancer. 35 patients with advanced bladder cancer were treated with CalliSpheres DLMS for transarterial chemoembolization. Imaging techniques such as magnetic resonance (MR) diffusion-weighted imaging were used to evaluate the therapeutic effect. The changes in serum tumor markers, immune function indexes, and oxidative stress indexes in patients before and after treatment were compared, and the quality of life of patients and the incidence of adverse reactions during follow-up were also evaluated. The results showed that the overall response rate (ORR) was 74.29% and that the disease control rate (DCR) was 97.14%. Compared with that before treatment, the ADC value of the tumor in patients with advanced bladder cancer detected by MR diffusion-weighted imaging technology was significantly increased after treatment and the maximum tumor diameter was significantly decreased P < 0.05 . Compared with those before treatment, the levels of serum tumor markers (CA199, CA724, and CA125) in advanced bladder cancer patients after treatment decreased P < 0.05 . The levels of T-lymphocyte subsets (CD3+ and CD4+) decreased, and CD8+ levels increased P < 0.05 . The levels of superoxide dismutase decreased P > 0.05 . At the same time, the subscale evaluation of function, symptoms, quality of life, adverse reactions, and economics of patients with advanced bladder cancer on the QLQ-C30 scale improved after treatment, and the incidence rate and recurrence rate during the follow-up period were 8.57% and 11.43%, respectively. It showed that CalliSpheres DLMS had a good clinical effect and high safety in the treatment of advanced bladder cancer and was a safe and feasible treatment method. The use of MR diffusion-weighted imaging technology could achieve quantitative evaluation of clinical efficacy of advanced bladder cancer.

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“…It carries an anionic sulfonic acid group and cationic amino group of chemotherapy drugs for exchange to complete drug loading. Studies have shown that DEB can accelerate the loading of drugs in a 5% glucose solution [ 40 – 42 ]. DEB can be divided into five types according to the diameter: 100 ~ 300, 300 ~ 500, 500 ~ 700, 700 ~ 900, and 900 ~ 1200 μm.…”

Section: Callisperes ® Of Drug-loaded Microspherementioning

confidence: 99%

Clinical research progress of callisperes® of drug-loaded microsphere arterial chemoembolisation in the treatment of solid tumors

Wang,

Zhu,

Sheng

2024

Discov Onc

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The incidence and mortality of cancer is ever-increasing, which poses a significant challengesto human health and a substantial economic burden to patients. At present, chemotherapy is still a primary treatment for various cancers. However, chemotherapy kills tumors but also induces the related side effects, whichadversely impacting patient quality of life and exacerbating suffering. Therefore, there is an urgent need for new and effective treatments that can control tumor growth while reducing the side effects for patients. Arterial chemoembolization has been attracted much attentionwhich attributed to the advantage of ability to embolize tumor vessels to block blood and nutrition supplies. Thus, to achieve local tumor control, it has become an effective means of local tumor control and has been widely used in clinical practice. Despite its efficacy, conventional arterial chemoembolization techniques, limited by embolization materials, have been associated with incomplete embolization and suboptimal drug delivery outcomes. Gradually, researchers have shifted their attention to a new type of embolic material called CalliSperes® drug-eluting embolic bead (DEB). DEB can not only load high doses of drugs, but also has strong sustained drug release ability and good biocompatibility. The integration of DEBs with traditional arterial chemoembolization (DEB-TACE) promises targeted vascular embolization, mitigated tumor ischemia and hypoxia, and direct intravascular chemotherapy delivery. It can prevent cancer cell differentiation and accelerate their death, meanwhile, directly injecting chemotherapy drugs into the target blood vessels reduced the blood concentration of the whole body, thus reduced the toxic and side effects of chemotherapy. Furthermore, DEB-TACE's sustained drug release capability elevates local drug concentrations at the tumor site, amplifying its antitumor efficacy. Therefore, DEB-TACE has become a hot spot in clinical research worldwide. This review introduces the pathogenesis of solid tumors, the background of research and biological characteristics of DEB, and the action mechanism of DEB-TACE, as well as its clinical research in various solid tumors and future prospects. This review aims to provide new ideas for the treatment of DEB-TACE in various solid tumors.

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Optimized Loading of Idarubicin in CalliSpheres® Drug-Eluting Beads and Characterization of Release Profiles and Morphological Properties

Cited by 6 publications

References 15 publications

One-step fabrication of lidocaine/CalliSpheres® composites for painless transcatheter arterial embolization

One-step fabrication of lidocaine/CalliSpheres® composites for painless transcatheter arterial embolization

Magnetic Resonance Diffusion-Weighted Imaging to Evaluate the Clinical Efficacy of CalliSpheres Drug-Loaded Microspheres in the Treatment of Advanced Bladder Cancer

Clinical research progress of callisperes® of drug-loaded microsphere arterial chemoembolisation in the treatment of solid tumors

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