Transarterial chemo‐embolization with drug‐eluting embolic beads (DEB‐TACE) is still evolving. Recent developments include the introduction of radiopaque (X‐ray imageable) drug‐eluting particles. Here, we report on conceptually different radiopaque polymeric drug‐eluting embolic particles, which are (i), cross‐linked poly(methacrylates); (ii), radiopaque; (iii), microporous. Furthermore, the particles are not perfectly spherical: they have a large indentation in the sense that they are either a spherical/cup‐shaped or ellipsoid/mouth‐shaped. The micropores and the large indentation can confer useful features upon the particles, since they can be filled with a crystalline lipophilic chemotherapeutic drug. It is important, in this respect that (i), many potent chemotherapeutics are lipophilic and crystalline; (ii), available drug‐eluting beads (DEBs) have the limitation that they can only be used in combination with water‐soluble chemotherapeutic agents. Cup‐ and mouth‐shaped particles were obtained in a Cu(0) catalyzed free‐radical polymerization reaction. The microparticles could be charged with crystalline drug, in such a manner that the crystals reside in both the micropores and the large cavity, and in quantities that would be required for effective local chemotherapy. The antifungal drug voriconazole, lipophilic, and crystalline, was used to demonstrate this. We believe that the ability of the microporous/cavitated DEBs to carry lipophilic chemotherapeutic drugs is especially important. DEB‐TACE is likely to become a cornerstone method of interventional oncology in the years ahead, and the new embolic particles described herein hold the promise of becoming scope widening for the technique.

中文翻译：

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具有空腔的聚合物微粒，设计用于结晶药物制剂的经动脉化疗栓塞。

药物洗脱栓塞微珠（DEB-TACE）的经动脉化疗栓塞仍在不断发展。最近的发展包括引入不透射线（X 射线可成像）药物洗脱颗粒。在这里，我们报告了概念上不同的不透射线聚合物药物洗脱栓塞颗粒，它们是（i）交联聚（甲基丙烯酸酯）；(ii)，不透射线的；(iii)、微孔的。此外，这些颗粒不是完美的球形：它们具有较大的压痕，即它们是球形/杯形或椭圆形/嘴形。微孔和大压痕可以赋予颗粒有用的特征，因为它们可以填充结晶的亲脂性化学治疗药物。重要的是，在这方面 (i)，许多有效的化学治疗剂是亲脂性和结晶的；(ii), 现有的药物洗脱珠（DEBs）的局限性在于它们只能与水溶性化学治疗剂联合使用。在 Cu(0) 催化的自由基聚合反应中获得了杯形和嘴形颗粒。微粒可以带有结晶药物，以使晶体同时存在于微孔和大空腔中的方式以及有效局部化疗所需的量。抗真菌药物伏立康唑，亲脂性和结晶，被用来证明这一点。我们认为微孔/空洞化 DEB 携带亲脂性化疗药物的能力尤为重要。DEB-TACE 很可能在未来几年成为介入肿瘤学的基石方法，