Vincenzo Quagliariello , Arianna Gennari , Som Akshay Jain , Francesco Rosso , Rosario Vincenzo Iaffaioli , Alfonso Barbarisi , Manlio Barbarisi , Nicola Tirelli
{"title":"Double-responsive hyaluronic acid-based prodrugs for efficient tumour targeting","authors":"Vincenzo Quagliariello , Arianna Gennari , Som Akshay Jain , Francesco Rosso , Rosario Vincenzo Iaffaioli , Alfonso Barbarisi , Manlio Barbarisi , Nicola Tirelli","doi":"10.1016/j.msec.2021.112475","DOIUrl":null,"url":null,"abstract":"<div><p>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.</p></div>","PeriodicalId":18212,"journal":{"name":"Materials science & engineering. C, Materials for biological applications","volume":null,"pages":null},"PeriodicalIF":8.1000,"publicationDate":"2021-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0928493121006159/pdfft?md5=6c6310230d5c4577ead76049f7bd87b9&pid=1-s2.0-S0928493121006159-main.pdf","citationCount":"7","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Materials science & engineering. C, Materials for biological applications","FirstCategoryId":"5","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0928493121006159","RegionNum":1,"RegionCategory":"工程技术","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"MATERIALS SCIENCE, BIOMATERIALS","Score":null,"Total":0}
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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