Solubility Enhancement of Ebastine by Formulating Microemulsion Using D-Optimal Mixture Design: Optimization and...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Ebastine, a BCS class II drug, exhibits poor aqueous solubility, limiting its therapeutic efficacy.
• Allergic rhinitis and chronic idiopathic urticaria are common conditions treated with ebastine.

Purpose of the Study:

• To enhance the aqueous solubility and dissolution rate of ebastine.
• To formulate and optimize a microemulsion system for ebastine delivery.

Main Methods:

• A microemulsion system was formulated using oleic acid, Transcutol® HP, and Tween®80.
• Phase titration and custom mixture design with D-optimality were employed for formulation development and optimization.
• The optimized formulation was characterized for physical properties and in vitro drug release.

Main Results:

• The optimized microemulsion formulation showed high cumulative drug release (82.9%–90.6% dissolution, 83.3%–100% diffusion).
• In vitro release kinetics indicated mixed-order release (dissolution) and anomalous diffusion (dissolution studies) or zero-order release (diffusion studies).

Conclusions:

• Microemulsion formulation is a promising strategy for improving the solubility and dissolution rate of ebastine.
• This approach can enhance the bioavailability of BCS class II drugs.