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