Treating acute cystitis with biodegradable micelle-encapsulated quercetin

Int J Nanomedicine. 2012:7:2239-47. doi: 10.2147/IJN.S29416. Epub 2012 May 8.

Abstract

Intravesical application of an anti-inflammatory drug is an efficient strategy for acute cystitis therapy. Quercetin (QU) is a potent anti-inflammatory agent; however, its poor water solubility restricts its clinical application. In an attempt to improve water solubility of QU, biodegradable monomethoxy poly(ethylene glycol)-poly(ɛ-caprolactone) (MPEG-PCL) micelles were used to encapsulate QU by self-assembly methods, creating QU/MPEG-PCL micelles. These QU/MPEG-PCL micelles with DL of 7% had a mean particle size of <34 nm, and could release QU for an extended period in vitro. The in vivo study indicated that intravesical application of MPEG-PCL micelles did not induce any toxicity to the bladder, and could efficiently deliver cargo to the bladder. Moreover, the therapeutic efficiency of intravesical administration of QU/MPEG-PCL micelles on acute cystitis was evaluated in vivo. Results indicated that QU/MPEG-PCL micelle treatment efficiently reduced the edema and inflammatory cell infiltration of the bladder in an Escherichia coli-induced acute cystitis model. These data suggested that MPEG-PCL micelle was a candidate intravesical drug carrier, and QU/MPEG-PCL micelles may have potential application in acute cystitis therapy.

Keywords: MPEG-PCL; nanomedicine; self-assembly.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute Disease
  • Analysis of Variance
  • Animals
  • Cystitis / drug therapy*
  • Cystitis / metabolism
  • Disease Models, Animal
  • Female
  • Histocytochemistry
  • Mice
  • Mice, Inbred BALB C
  • Micelles*
  • Nanocapsules / administration & dosage*
  • Nanocapsules / chemistry
  • Nanocapsules / toxicity
  • Organ Size / drug effects
  • Particle Size
  • Polyesters / chemistry
  • Polyethylene Glycols / chemistry
  • Quercetin / chemistry
  • Quercetin / pharmacokinetics
  • Quercetin / pharmacology*
  • Tissue Distribution
  • Urinary Bladder / drug effects
  • Urinary Bladder / metabolism

Substances

  • Micelles
  • Nanocapsules
  • Polyesters
  • methoxy poly(ethylene glycol-co-epsilon-caprolactone)
  • Polyethylene Glycols
  • Quercetin