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CRGDK-Functionalized PAMAM-Based Drug-Delivery System with High Permeability

机译：CRGDK功能化的普遍渗透性的药物输送系统，具有高渗透性

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The low tumor permeability of nanomedicines is a major challenge for their application in tumor therapy. Reducing the size of nanomedicines or integrating penetrating peptides has been demonstrated to be very helpful to improve the tumor permeability of nanomedicines. In this paper, poly(amidoamine) (PAMAM) functionalized with the penetrating peptide CRGDK was designed as a drug carrier with a diameter of ～5 nm. Paclitaxel (PTX) was used as a model drug and covalently linked to the carrier via a biocleavable ester bond. The CRGDK-functionalized drug-loaded nanoparticle exhibited a higher cellular uptake and a higher tumor accumulation and penetration than its nontargeted counterpart, which also endowed the functionalized nanomedicine with a higher antitumor efficiency than its nontargeted counterpart and the clinical Taxol formulation. The good performance of the peptide-bearing PAMAM-based nanomedicine indicates that our strategy is feasible to improve the tumor accumulation and penetration of nanomedicines.
机译：纳米胺的低肿瘤渗透性是它们在肿瘤治疗中的应用的主要挑战。已经证明了减少纳米海运金属碱或整合渗透肽的尺寸非常有助于改善纳米喂养尼的肿瘤渗透性。本文用渗透肽CRGDK官能化的聚（酰胺胺）（PAMAM）设计为具有直径为5nm的药物载体。紫杉醇（PTX）用作模型药物，并通过生物可去酯键与载体共价连接。 CRGDK官能化的药物负载的纳米粒子表现出比其非靶向对应物更高的细胞摄取和更高的肿瘤积累和渗透，这也赋予了官能化纳米胺，其抗肿瘤效率高于其非靶向对应物和临床紫杉醇制剂。含肽的帕姆姆的纳米美发内的良好性能表明我们的策略是可行的，可以改善纳米胺的肿瘤积累和渗透。

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