Ultrafast charge-conversional nanocarrier for tumor-acidity-activated targeted drug elivery†,Biomaterials Science

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Ultrafast charge-conversional nanocarrier for tumor-acidity-activated targeted drug elivery†
Biomaterials Science ( IF 5.8 ) Pub Date : 2017-11-29 00:00:00 , DOI: 10.1039/c7bm01025g
Jing Liu _{1,

2,

3,

4} , Shoaib Iqbal _{1,

2,

3,

4} , Xiao-Jiao Du _{4,

5,

6,

7,

8} , Youyong Yuan _{4,

5,

6,

7,

8} , Xianzhu Yang _{4,

5,

6,

7,

8} , Hong-Jun Li _{4,

5,

6,

7,

8} , Jun Wang _{1,

2,

3,

4,

5}

Affiliation

Nanocarriers with tumor-acidity-activated charge-conversional ability are of particular interest for targeted drug delivery in the field of precision nanomedicine. Nevertheless, the key challenge of this strategy is the slowness of reversing the surface charge at the tumor tissue. As a proof-of-concept, we synthesized the amphiphilic triblock polymer poly(ethylene glycol)-block-poly(2-carboxyethylacrylate)-block-poly(2-azepaneethylmethacrylate) (PEG-b-PCEA-b-PAEMA) to prepare the cisplatin-loaded nanocarrier UCC-NP/Pt. The PAEMA block at the physiological pH values was hydrophobic, which formed the core of UCC-NP/Pt. In contrast, at the tumor acidity, the tertiary amine groups of PAEMA block rapidly protonated, resulting in the ultrafast charge conversion of UCC-NP/Pt within 10 s. Such ultrafast charge-conversional effect more efficiently enhanced tumor cell internalization of nanocarriers, thus achieving targeted drug delivery, which in turn exhibited superior anticancer efficacy even in the cisplatin-resistant cells. This approach provides new avenues for tumor-acidity-activated targeted drug delivery.

中文翻译：

超快速电荷转换纳米载体，用于肿瘤酸性激活的靶向药物递送†

具有肿瘤酸度激活的电荷转化能力的纳米载体在精密纳米医学领域中对于靶向药物递送特别感兴趣。然而，该策略的主要挑战是逆转肿瘤组织表面电荷的缓慢性。作为验证的概念，我们合成了两亲性三嵌段聚合物，聚（乙二醇） -嵌段-聚（2-羧乙酯） -嵌段-聚（2- azepaneethylmethacrylate）（PEG- b -PCEA- b-PAEMA）制备顺铂负载的纳米载体UCC-NP / Pt。生理pH值下的PAEMA嵌段是疏水的，形成了UCC-NP / Pt的核心。相反，在肿瘤酸性下，PAEMA的叔胺基团迅速质子化，从而导致UCC-NP / Pt的超快速电荷转化在10 s内。这种超快的电荷转换效应可以更有效地增强纳米载体在肿瘤细胞中的内在化，从而实现靶向药物的输送，从而即使在顺铂耐药细胞中也表现出优异的抗癌功效。该方法为肿瘤酸度激活的靶向药物输送提供了新途径。

更新日期：2017-11-29

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