Synergistic Effect of Acetazolamide-(2-hydroxy)propyl β-Cyclodextrin in Timolol Liposomes for Decreasing and...

Area of Science:

• Ophthalmology
• Pharmaceutics
• Drug Delivery

Background:

• Glaucoma treatment often requires multiple medications.
• Conventional drug delivery methods for glaucoma face challenges in efficacy and duration.
• Liposomal formulations offer potential for improved drug delivery and sustained release.

Purpose of the Study:

• To design and characterize a co-loaded liposomal formulation (CLL) for glaucoma treatment.
• To incorporate timolol maleate (TM) and acetazolamide (Acz) into a single liposomal system.
• To evaluate the in vitro and in vivo performance of the CLL for enhanced glaucoma therapy.

Main Methods:

• Preparation and characterization of co-loaded liposomes containing TM and Acz-HPβCD complexes.
• Optimization of liposomal formulation using design of experiment methodology.
• In vitro drug release and permeation studies.
• In vivo studies to assess intraocular pressure (IOP) reduction.

Main Results:

• HPβCD enhanced acetazolamide solubility.
• Optimized liposomal formulation (CLL) demonstrated improved physicochemical properties and encapsulation efficiency.
• CLL exhibited superior in vitro drug release and permeation compared to single-drug formulations and standard solutions.
• CLL significantly reduced and prolonged IOP in vivo.

Conclusions:

• Co-loading timolol maleate and acetazolamide into liposomes is a viable strategy for glaucoma treatment.
• The developed CLL formulation shows enhanced efficacy due to synergistic drug effects and permeation enhancement.
• This co-loading approach holds significant potential for improving glaucoma therapy outcomes.