Abstract Inflammation represents a real micromilieu of many diseases as well as the actual application environment of nanocarriers. However, few studies have focused on the influence of the inflammatory environment on the effects of nanoparticle delivery. Herein, a novel inflammation self-adaptive nanocarrier is designed and fabricated by attaching the ascorbyl palmitate (AP) onto the surface of gene-entrapped polymeric nanocomplexes through the formation of phenylboronate bond. In vitro and in vivo studies demonstrate that the introduction of AP enhances considerably the accumulation of entrapped gene in inflammation and facilitates the intracellular uptake of gene-loading nanoparticles. Meanwhile, the gene transfection efficiency of DNA and in vivo gene therapy of nanocomplexes under an inflammation stimulus is significantly enhanced. Hence, our delicate design concept opens up a new pathway to develop an inflammation self-adaptive drug delivery system for precise drug/gene delivery and therapy.

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一种用于高效基因治疗的炎症自适应纳米载体

摘要 炎症代表了许多疾病的真实微环境以及纳米载体的实际应用环境。然而，很少有研究关注炎症环境对纳米颗粒递送效果的影响。在此，通过形成苯基硼酸酯键将抗坏血酸棕榈酸酯 (AP) 连接到基因包埋的聚合物纳米复合物的表面，设计并制造了一种新型炎症自适应纳米载体。体外和体内研究表明，AP 的引入显着增强了炎症中捕获基因的积累，并促进了基因加载纳米颗粒的细胞内摄取。同时，DNA的基因转染效率和纳米复合物在炎症刺激下的体内基因治疗效率显着提高。因此，