Treating acute cystitis with biodegradable micelle-encapsulated quercetin

Area of Science:

• Biomaterials Science
• Pharmacology
• Urology

Background:

• Intravesical anti-inflammatory drug delivery is effective for acute cystitis.
• Quercetin (QU) possesses potent anti-inflammatory properties but suffers from poor water solubility, limiting its clinical use.
• Biodegradable monomethoxy poly(ethylene glycol)-poly(ɛ-caprolactone) (MPEG-PCL) micelles offer a potential solution for drug delivery challenges.

Purpose of the Study:

• To develop and characterize quercetin-loaded MPEG-PCL micelles (QU/MPEG-PCL) for improved water solubility and intravesical delivery.
• To evaluate the in vitro drug release profile of QU/MPEG-PCL micelles.
• To assess the in vivo safety, bladder targeting efficiency, and therapeutic efficacy of QU/MPEG-PCL micelles in an acute cystitis model.

Main Methods:

• Quercetin was encapsulated into biodegradable MPEG-PCL micelles via self-assembly.
• Micelle particle size, drug loading (DL), and in vitro quercetin release were analyzed.
• In vivo studies involved intravesical administration in an Escherichia coli-induced acute cystitis rat model to assess bladder toxicity, cargo delivery, and therapeutic effects.

Main Results:

• QU/MPEG-PCL micelles exhibited a mean particle size of <34 nm with a DL of 7% and demonstrated sustained quercetin release in vitro.
• Intravesical administration of MPEG-PCL micelles showed no significant bladder toxicity and efficient cargo delivery.
• Treatment with QU/MPEG-PCL micelles significantly reduced bladder edema and inflammatory cell infiltration in the acute cystitis model.

Conclusions:

• MPEG-PCL micelles are a promising biodegradable carrier for intravesical drug delivery.
• QU/MPEG-PCL micelles demonstrate potential for the effective treatment of acute cystitis by improving quercetin's therapeutic profile.