Formulation and evaluation of celastrol-loaded liposomes

Area of Science:

• Pharmacology
• Drug Delivery Systems
• Nanotechnology

Background:

• Celastrol is a potent antineoplastic agent with poor water solubility, limiting its oral bioavailability.
• Developing effective oral drug delivery systems is crucial for maximizing celastrol's therapeutic potential.

Purpose of the Study:

• To evaluate liposomes as an oral drug delivery system for celastrol.
• To assess the impact of liposomes on celastrol's intestinal absorption and antineoplastic activity.

Main Methods:

• Liposomes were prepared using the ethanol-injection method with phospholipid, cholesterol, and Tween-80.
• Characterization included encapsulation efficiency, particle size, and zeta potential analysis.
• Intestinal absorption was assessed using a four-site perfusion rat model.
• Antineoplastic effect was evaluated in C57BL/6 mice.

Main Results:

• Optimized liposomes achieved high encapsulation efficiency (98.06 ± 0.94%) and a stable particle size (89.6 ± 7.3 nm).
• Celastrol-loaded liposomes demonstrated significantly improved effective permeability compared to the free drug in rat intestinal segments (p < 0.05).
• Liposomal celastrol effectively inhibited tumor growth in mice.

Conclusions:

• Liposomes represent a viable oral drug delivery system for celastrol.
• This formulation enhances celastrol's intestinal absorption and anticancer efficacy.
• Liposomal delivery offers a promising strategy for improving celastrol's therapeutic application.