PEGylated Gambogic Acid Nanoparticles Enable Efficient Renal-Targeted Treatment of Acute Kidney Injury

Nano Lett. 2023 Jun 28;23(12):5641-5647. doi: 10.1021/acs.nanolett.3c01235. Epub 2023 Jun 9.


Acute kidney injury (AKI) is a common clinical syndrome lacking effective pharmacotherapy. Gambogic acid (GA), as an active ingredient of herbal medicines, exhibits antioxidant and anti-inflammatory effects that benefit the treatment of AKI, but its poor aqueous solubility limits effective renal delivery. We, for the first time, developed GA-based nanoparticles (GA-NPs) with preferential renal uptake for AKI treatment. By PEGylating with NH2-PEG5000-NOTA, hydrophobic GA was self-assembled into ∼4.5 nm nanoparticles, which showed the enhanced renal accumulation in AKI models from PET images. Importantly, the in vitro cell assays and in vivo tests of the two AKI models have confirmed the obvious nephroprotective effects and biosafety of GA-NPs. Therefore, this work indicates that GA-NPs can be a promising therapeutic candidate for the management of AKI.

Keywords: Acute kidney injury treatment; Gambogic acid; Nanoparticles; PET imaging; Renal targeting.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute Kidney Injury* / drug therapy
  • Drug Carriers / chemistry
  • Humans
  • Nanoparticles* / chemistry
  • Nanoparticles* / therapeutic use
  • Polyethylene Glycols / chemistry
  • Polyethylene Glycols / therapeutic use


  • Drug Carriers
  • gambogic acid
  • Polyethylene Glycols