Overexpression of proteins in the body can cause severe diseases and other physiological disturbances. The development of protein blockers and local delivery systems would offer opportunities for addressing the health problems caused by protein overexpression. Nucleic acid aptamers are an emerging class of ligands with the potential to block proteins effectively; however, little effort has been made in developing polymer systems for local aptamer delivery. In this work, polymer microneedles capable of delivering DNA aptamers locally to inhibit the function of vascular endothelial growth factor (VEGF) were developed and studied. The presence of anti-VEGF aptamer in the polymer matrix did not change the apparent mechanical strength of the microneedles. Once in contact with a physiological solution, the polymer microneedles quickly dissolved, generating a high concentration of anti-VEGF aptamer in the surrounding local microenvironment. Aptamer delivery by way of dissolving polymer microneedles in a tissue phantom reduced VEGF-mediated endothelial cell tube formation. Thus, aptamer-loaded polymer microneedles hold great potential as a therapeutic tool for the treatment of human diseases resulting from protein overexpression.

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聚合物微针介导的局部适体传递，以阻断血管内皮生长因子的功能

体内蛋白质的过度表达会导致严重的疾病和其他生理失调。蛋白质阻滞剂和局部递送系统的发展将为解决由蛋白质过表达引起的健康问题提供机会。核酸适体是一类新兴的配体，具有有效阻断蛋白质的潜力。然而，在开发用于局部适体递送的聚合物系统方面所做的努力很少。在这项工作中，开发并研究了能够局部递送DNA适体以抑制血管内皮生长因子（VEGF）功能的聚合物微针。聚合物基质中抗VEGF适体的存在不会改变微针的表观机械强度。一旦与生理溶液接触，聚合物微针就会迅速溶解，在周围的局部微环境中产生高浓度的抗VEGF适体。通过将聚合物微针溶解在组织体模中，适体递送减少了VEGF介导的内皮细胞管的形成。因此，负载适体的聚合物微针具有巨大的潜力，可以作为治疗因蛋白质过表达而引起的人类疾病的治疗工具。