Folate-chitosan Coated Quercetin Liposomes for Targeted Cancer Therapy

Area of Science:

• Nanotechnology in Drug Delivery
• Cancer Therapeutics
• Pharmacology

Background:

• Quercetin shows potential anti-tumor effects but faces limitations in clinical use due to poor targeting and inherent defects.
• Developing targeted delivery systems is crucial to enhance quercetin's efficacy against tumors.

Purpose of the Study:

• To prepare and characterize active targeting folate-chitosan modified quercetin liposomes (FA-CS-QUE-Lip).
• To evaluate the in vitro and in vivo anti-tumor activity of FA-CS-QUE-Lip.

Main Methods:

• Optimal quercetin liposomes (QUE-LP) formulated using Box-Behnken Design.
• FA-CS-QUE-LP prepared by conjugating folic acid chitosan complex (FA-CS) with QUE-LP.
• In vitro release, cytotoxicity (MTT assay on HepG2 cells), and in vivo pharmacokinetic/pharmacodynamic studies in mice.

Main Results:

• FA-CS-QUE-LP showed optimal characteristics: 261.6 nm size, 22.3 mV zeta potential, 98.63% encapsulation efficiency, and sustained release.
• FA-CS-QUE-LP demonstrated significantly higher inhibition rates against HepG2 cells compared to quercetin solution.
• In vivo studies showed altered quercetin pharmacokinetics and significant tumor growth inhibition (30.26% weight, 37.35% volume) in S180 tumor-bearing mice.

Conclusions:

• FA-CS-QUE-LP effectively inhibits HepG2 cells and exhibits anti-tumor activity in vivo.
• This targeted liposomal formulation improves quercetin's pharmacokinetic profile and offers a promising strategy for cancer treatment.