Effect of PEGylation on the Drug Release Performance and Hemocompatibility of Photoresponsive Drug-Loading Platform
Effect of PEGylation on the Drug Release Performance and Hemocompatibility of Photoresponsive Drug-Loading Platform
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DOI：
10.3390/ijms23126686
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发表时间：
2022-06-15
影响因子：
5.6
通讯作者：
Akagi, Yuki
中科院分区：
文献类型：
--
作者：
Mizuno, Hayato L.;Anraku, Yasutaka;Sakuma, Ichiro;Akagi, Yuki
冠状动脉狭窄一直是最常见的心脏病之一，它大大增加了心脏病发作等致命疾病的风险。使用药物涂层球囊（DCB）的血管成形术是最安全和最有前途的治疗方法之一。为了最大限度地降低介入治疗期间此类DCB的血栓形成风险，需要采用不同的方法，确保血流下的高血液相容性。在这里，我们报告了一种通过将聚乙二醇（PEG）结合到位于球囊表面的官能团上来改善光响应平台的血液相容性的方法。在这项研究中，乳胶微珠被用作球囊模型，以便在显微镜下精确观察其表面。这些珠用各种长度和接枝密度的PEG聚合物修饰，沿着Cy 5-光可交联（PC）接头缀合物以模拟待加载到平台上的药物。结果表明，PEG长度和接枝密度是影响其血液相容性、载药量和释药效率的关键因素。因此，尽管有必要进一步研究以优化血液相容性、载药量和释放效率之间的权衡，但可以安全地得出结论，DCB表面的聚乙二醇化是增强和维持高血液相容性的有效方法，以最大限度地降低血管成形术期间血栓形成的风险。
Coronary stenosis has been one of the most common heart diseases that drastically increases the risk of fatal disorders such as heart attack. Angioplasty using drug coated balloons (DCB) has been one of the most safe and promising treatments. To minimize the risk of thrombosis of such DCBs during intervention, a different approach that can secure high hemocompatibility under blood flow is necessary. Here we report a method of improving the photoresponsive platform’s hemocompatibility by conjugating polyethylene glycol (PEG), onto the functional groups located at the balloon surface. In this study, latex microbeads were used as models for balloons to enable precise observation of its surface under microscopy. These beads were decorated with PEG polymers of a variety of lengths and grafting densities, along with the Cy5-Photoclevable (PC) linker conjugate to mimic drugs to be loaded onto the platform. Results showed that PEG length and grafting density are both critical factors that alter not only its hemocompatibility, but also the drug load and release efficiency of such platform. Thus, although further investigation is necessary to optimize the tradeoff between hemocompatibility, drug load, and release efficiency, it is safe to conclude that PEGylation of DCB surface is an effective method of enhancing and maintaining high hemocompatibility to minimize the risk of thrombosis during angioplasty.
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