Sun Pengchao, Zhang Nan, Tang Yafang, Yang Yanan, Zhou Jie, Zhao Yongxing
School of Pharmaceutical Science, Zhengzhou University Zhengzhou Henan 450001 P. R China
Key Laboratory of Targeting Therapy and Diagnosis for Critical Diseases, Henan Province Zhengzhou Henan 450001 P. R China.
RSC Adv. 2018 Jul 23;8(46):26300-26308. doi: 10.1039/c8ra04589e. eCollection 2018 Jul 19.
Because of the remarkable features, including biocompatibility and biodegradability, DNA origami nanostructures have drawn much attention as ideal carriers for drug delivery. However, the cellular uptake of DNA origami nanostructures was a passive targeting process, resulting in limited therapeutic effect. To address this problem, we anchored the aptamer C2NP (Apt) on rectangular DNA origami nanostructures (RE) to enhance the tumor targeting properties and anticancer effects of doxorubicin (DOX). Apt was anchored onto RE with low or high density (RE-4Apt, RE-16Apt), followed by incubation with DOX to obtain DOX@RE-4Apt and DOX@RE-16Apt. The results showed that DOX@RE-4Apt and DOX@RE-16Apt exhibited excellent biocompatibility and targeting ability, as well as a synergic biological effect with chemotherapy on cancer therapy. More importantly, after conjugation with RE, the bioactivity of Apt was significantly increased. These results revealed that Apt anchored DNA nanostructures not only are potential carriers for precise therapy, but also supply a strategy to enhance the bioactivity of aptamers.
由于具有生物相容性和可生物降解性等显著特性，DNA折纸纳米结构作为药物递送的理想载体备受关注。然而，DNA折纸纳米结构的细胞摄取是一个被动靶向过程，导致治疗效果有限。为了解决这个问题，我们将适配体C2NP（Apt）锚定在矩形DNA折纸纳米结构（RE）上，以增强阿霉素（DOX）的肿瘤靶向特性和抗癌效果。将Apt以低密度或高密度锚定到RE上（RE-4Apt、RE-16Apt），然后与DOX孵育以获得DOX@RE-4Apt和DOX@RE-16Apt。结果表明，DOX@RE-4Apt和DOX@RE-16Apt表现出优异的生物相容性和靶向能力，以及与化疗对癌症治疗的协同生物学效应。更重要的是，与RE缀合后，Apt的生物活性显著提高。这些结果表明，Apt锚定的DNA纳米结构不仅是精确治疗的潜在载体，还提供了一种增强适配体生物活性的策略。
