Quercetin-containing self-assemble proliposome preparation and evaluation

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Quercetin, a flavonoid, exhibits limited oral bioavailability due to poor absorption.
• Developing effective oral delivery systems is crucial for maximizing quercetin's therapeutic potential.
• Self-assembling proliposomes offer a promising approach to improve drug solubility and absorption.

Purpose of the Study:

• To develop a simple, liquid self-assembling proliposome formulation for quercetin oral delivery.
• To investigate the effect of Cremophor RH40 concentration on proliposome characteristics and performance.
• To evaluate the in vitro and in vivo efficacy of the developed quercetin proliposome system.

Main Methods:

• Preparation of liquid self-assembling proliposomes by dissolving phospholipids, surfactants, and quercetin in ethanol.
• Characterization of proliposomes, including particle size, polydispersity index, and drug entrapment efficiency.
• In vitro drug release studies and in situ intestinal absorption and pharmacokinetic studies in vivo.

Main Results:

• Liquid self-assembling proliposomes were successfully prepared in a single step without special equipment.
• Increasing Cremophor RH40 concentration decreased particle size and polydispersity index but slightly reduced drug entrapment efficiency.
• Proliposomes demonstrated prolonged in vitro quercetin release, enhanced in vivo bioavailability, and good stability at room temperature.

Conclusions:

• Liquid self-assembling proliposomes are a viable and efficient system for oral quercetin delivery.
• Optimizing Cremophor RH40 concentration below 26% is recommended for high drug entrapment and reduced irritation.
• The enhanced bioavailability highlights the potential of this proliposome formulation for improving quercetin's therapeutic outcomes.