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

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.

Keywords: Boronates; Cancer; Field flow fractionation; Hyaluronic acid; Responsive release; Targeted drug delivery.

MeSH terms

  • Animals
  • Drug Delivery Systems
  • Hyaluronic Acid / therapeutic use
  • Male
  • Mice
  • Mice, SCID
  • Micelles
  • Neoplasms* / drug therapy
  • Prodrugs* / pharmacology


  • Micelles
  • Prodrugs
  • Hyaluronic Acid