Double-responsive hyaluronic acid-based prodrugs for efficient tumour targeting

IF 8.1 1区工程技术 Q1 MATERIALS SCIENCE, BIOMATERIALS Materials science & engineering. C, Materials for biological applications Pub Date : 2021-12-01 DOI:10.1016/j.msec.2021.112475

Vincenzo Quagliariello , Arianna Gennari , Som Akshay Jain , Francesco Rosso , Rosario Vincenzo Iaffaioli , Alfonso Barbarisi , Manlio Barbarisi , Nicola Tirelli

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引用次数: 7

Abstract

Hyaluronic acid (HA)-based prodrugs bearing double-responsive (acid pH or oxidation) boronates of catechol-containing drugs were used to treat xenografted human prostate tumours (LNCaP) in SCID mice. The HA prodrugs accumulated significantly only in tumours (impressively, up to 40% of the injected dose after 24 h) and in liver, with negligible – actually anti-inflammatory - consequences in the latter. A quercetin-HA prodrug significantly slowed down tumour growth, in a dose-dependent fashion and with a much higher efficacy (up to 4 times) than equivalent doses of free quercetin. In short, boronated HA appears to be a very promising platform for targeted chemotherapy.

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基于透明质酸的双反应前药有效靶向肿瘤

以透明质酸(HA)为基础的前药含有儿茶酚类药物的双响应(酸性pH或氧化)硼酸盐，用于治疗SCID小鼠的异种移植人前列腺肿瘤(LNCaP)。透明质酸前药仅在肿瘤(令人印象深刻的是，24小时后高达注射剂量的40%)和肝脏中显著积累，后者的效果可以忽略不计——实际上是抗炎作用。槲皮素- ha前药以剂量依赖的方式显著减缓肿瘤生长，其功效远高于同等剂量的游离槲皮素(高达4倍)。简而言之，硼化透明质酸似乎是一个非常有前途的靶向化疗平台。

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来源期刊

Materials science & engineering. C, Materials for biological applications MATERIALS SCIENCE, BIOMATERIALS-

CiteScore

12.60

自引率

0.00%

发文量

审稿时长

3.3 months

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