The standard of care for intermediate stage hepatocellular carcinoma is transarterial chemoembolization (TACE). Drug‐eluting bead TACE (DEB‐TACE) has emerged as a leading form of TACE, as it uses highly calibrated microspheres to deliver consistent embolization and controlled drug release to the tumor microenvironment. We report here on doxorubicin (DOX)‐loaded polyphosphate glass microspheres (PGM) as a novel resorbable, radiopaque, preloaded DEB‐TACE platform. Coacervate composed of polyphosphate chains complexed with Ba²⁺, Ca²⁺, and Cu²⁺ can be loaded with DOX prior to PGM synthesis, with PGM production achieved using a water‐in‐oil emulsion technique at room temperature yielding highly spherical particles in clinically relevant size fractions. In vitro, DOX release was found to be linear, pH dependent, and in accordance with Type II non‐Fickian transport. PGM degradation was characterized by an initial burst release of degradation products over 7 days, followed by a plateau in mass loss at approximately 75% over a period of several weeks. in vitro studies indicate that PGM degradation products, namely Cu²⁺, are cytotoxic and may interact with eluted DOX to impair its pharmacological activity. With additional compositional considerations, this approach may prove promising for DEB‐TACE applications.

中文翻译：

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用于经动脉化疗栓塞的载有阿霉素的多磷酸盐玻璃微球。

中期肝细胞癌的标准治疗是经动脉化疗栓塞 (TACE)。药物洗脱微珠 TACE (DEB-TACE) 已成为 TACE 的主要形式，因为它使用高度校准的微球向肿瘤微环境提供一致的栓塞和受控药物释放。我们在此报告了载有阿霉素 (DOX) 的多磷酸盐玻璃微球 (PGM) 作为一种新型可吸收、不透射线、预载 DEB-TACE 平台。由与 Ba ²⁺、Ca ²⁺和 Cu ²⁺复合的多磷酸链组成的凝聚层可以在 PGM 合成之前加载 DOX，在室温下使用油包水乳液技术实现 PGM 生产，产生临床相关尺寸分数的高度球形颗粒。在体外，发现 DOX 释放是线性的、pH 依赖性的，并且符合 II 型非 Fickian 转运。PGM 降解的特点是降解产物在 7 天内首次突然释放，然后在几周内质量损失达到约 75% 的平台期。体外研究表明，PGM 降解产物 Cu ²⁺具有细胞毒性，可能与洗脱的 DOX 相互作用而削弱其药理活性。考虑到额外的成分，这种方法可能被证明适用于 DEB-TACE 应用。