Enhanced cell penetration of acid-degradable particles functionalized with cell-penetrating peptides
Enhanced cell penetration of acid-degradable particles functionalized with cell-penetrating peptides
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DOI：
10.1021/bc700414j
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发表时间：
2008-04-01
影响因子：
4.7
通讯作者：
Frechet, Jean M. J.
中科院分区：
文献类型：
--
作者：
Cohen, Jessica L.;Almutairi, Adah;Frechet, Jean M. J.
蛋白质和DNA等生物制药已经证明了它们在预防和治疗疾病方面的潜力。这种治疗剂的成功取决于它们是否有能力跨越体内的复杂障碍，完好无损地到达目标。为了获得这些治疗剂的全部益处，需要一种能够将货物运送到所有类型的吞噬和非吞噬细胞的运输工具。本文介绍了一种能够穿透细胞和亚细胞触发释放封装有效载荷的微粒运载工具的合成和评价。合成了聚精氨酸细胞穿透肽(CPP)功能化的pH敏感型聚丙烯酰胺颗粒。将CPP掺入微粒中，可使培养中的非吞噬细胞有效摄取。此外，在本研究使用的浓度下，CPP修饰的颗粒没有显示出细胞毒性作用。结果表明，这些颗粒可能为成功地将治疗剂输送到各种类型的细胞提供了一种载体。
Biopharmaceuticals, such as proteins and DNA, have demonstrated their potential to prevent and cure diseases. The success of such therapeutic agents hinges upon their ability to cross complex barriers in the body and reach their target intact. In order to reap the full benefits of these therapeutic agents, a delivery vehicle capable of delivering cargo to all cell types, both phagocytic and non-phagocytic, is needed. This article presents the synthesis and evaluation of a microparticle delivery vehicle capable of cell penetration and sub-cellular triggered release of an encapsulated payload. pH-sensitive polyacrylamide particles functionalized with a polyarginine cell-penetrating peptide (CPP) were synthesized. The incorporation of a CPP into the microparticles led to efficient uptake by non-phagocytic cells in culture. In addition, the CPP-modified particles showed no cytotoxic effects at concentrations used in this study. The results suggest that these particles may provide a vehicle for the successful delivery of therapeutic agents to various cell types.