Isoliquiritigenin Containing PH Sensitive Micelles for Enhanced Anti-Colitis Activity

Area of Science:

• Pharmacology
• Drug Delivery Systems
• Materials Science

Background:

• Isoliquiritigenin (ISL) possesses diverse pharmacological activities.
• Poor water solubility of ISL limits its bioavailability and therapeutic efficacy.
• Developing advanced drug delivery systems is crucial for improving ISL's application.

Purpose of the Study:

• To formulate Isoliquiritigenin pH-sensitive micelles (ISL-M) for enhanced drug delivery.
• To evaluate the physicochemical properties, stability, and in vitro release of ISL-M.
• To assess the in vivo pharmacokinetics and anti-colitis efficacy of ISL-M.

Main Methods:

• ISL-M were prepared using the thin film hydration method.
• Characterization included micellar size, PDI, zeta potential, drug loading, and encapsulation efficiency.
• In vitro release studies, stability tests, pharmacokinetic analysis in rats, and anti-inflammatory evaluations were conducted.

Main Results:

• ISL-M exhibited favorable characteristics: size (151.15 nm), PDI (0.092), zeta potential (-31.32 mV), EE% (93.97%), and DL% (8.42%).
• ISL-M demonstrated pH-sensitive release and significantly increased cumulative release rates compared to unformulated ISL.
• Pharmacokinetic studies showed a 2.94-fold increase in AUC(0-t) and a 4.06-fold increase in Cmax for ISL-M compared to ISL.

Conclusions:

• ISL-M formulation effectively improves the bioavailability of Isoliquiritigenin.
• The developed micelles show promising pH-sensitive release and enhanced anti-inflammatory activity.
• ISL-M represent a viable strategy for increasing ISL's therapeutic potential, particularly for colitis treatment.