Department of Cardio-Thoracic and Respiratory Science, University of Campania "Luigi Vanvitelli", 80138 Napoli, Italy.
Laboratory for Polymers and Biomaterials, Fondazione Istituto Italiano di Tecnologia, 16163 Genova, Italy.
Mater Sci Eng C Mater Biol Appl. 2021 Dec;131:112475. doi: 10.1016/j.msec.2021.112475. Epub 2021 Oct 12.
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.
基于透明质酸（HA）的前药，具有双响应（酸 pH 或氧化）的含儿茶酚药物的硼酸酯，用于治疗 SCID 小鼠中的异种移植人前列腺肿瘤（LNCaP）。HA 前药仅在肿瘤中（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，在后者中几乎没有（实际上是抗炎）后果。槲皮素-HA 前药以剂量依赖性方式显著减缓肿瘤生长，其功效（高达 4 倍）比等效剂量的游离槲皮素高得多。简而言之，硼酸化 HA 似乎是一种非常有前途的靶向化疗平台。
