Formulation of Self-Emulsifying Microemulsion for Acemetacin Using D-Optimal Design: Enteric-Coated Capsule for...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Acemetacin (ACM) exhibits poor aqueous solubility and oral bioavailability.
• Gastrointestinal complications are a concern with conventional ACM formulations.
• Novel drug delivery systems are needed to improve ACM's therapeutic efficacy and safety.

Purpose of the Study:

• To formulate and optimize a self-emulsifying microemulsion drug delivery system (SEME) for acemetacin (ACM).
• To enhance ACM's aqueous solubility and oral bioavailability.
• To reduce ACM-induced gastrointestinal complications.

Main Methods:

• Component screening and pseudo-ternary phase diagrams were used to select optimal ratios.
• D-optimal design was employed to optimize the ACM-SEME formulation.
• Physicochemical characterization included particle size, zeta potential, and in vitro release studies. In vivo antinociceptive activity and ex vivo permeation studies were conducted.

Main Results:

• The optimized ACM-SEME formulation exhibited desirable physicochemical properties, including small globule size and high transmittance.
• In vivo studies demonstrated significant antinociceptive activity of ACM-SEME compared to controls.
• Ex vivo permeation studies confirmed enhanced intestinal permeation of ACM from the SEME system.

Conclusions:

• The developed ACM-SEME system significantly improved physicochemical properties and release behavior.
• ACM-SEME demonstrated superior therapeutic performance and enhanced permeation potential.
• This SEME platform offers a promising, safer, and more effective oral delivery strategy for acemetacin.