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

Authors :
Quagliariello, Vincenzo
Gennari, Arianna
Jain, Som Akshay
Rosso, Francesco
Iaffaioli, Rosario Vincenzo
Barbarisi, Alfonso
Barbarisi, Manlio
Tirelli, Nicola
Source :
Materials Science & Engineering: C. Dec2021, Vol. 131, pN.PAG-N.PAG. 1p.
Publication Year :
2021

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. Hyaluronic acid-based prodrugs bearing side-chain boronic esters show excellent tumour accumulation (targeting) and acid pH- or reactive oxygen species (ROS)-responsive release of polyphenolic drugs such as quercetin. The chemotherapeutic performance of the latter in xenografted mice is dramatically improved upon conjugation with HA. [Display omitted] • Boronate-linked payloads can be released from hyaluronic acid upon acidification or oxidation. • Boronate-based hyaluronic acid prodrugs accumulate in tumours up to 40–50% of the injected doses. • Boronate-based hyaluronic acid prodrugs efficiently treat human prostate tumours in SCID mice. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
09284931
Volume :
131
Database :
Academic Search Index
Journal :
Materials Science & Engineering: C
Publication Type :
Academic Journal
Accession number :
153847628
Full Text :
https://doi.org/10.1016/j.msec.2021.112475