Application of quasi-emulsification and modified double emulsification techniques for formulation of tacrolimus...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Tacrolimus (TCM) is a crucial immunosuppressant macrolide antibiotic.
• Current formulations may have limitations, necessitating improved delivery systems.
• Microsponges offer a safe and effective platform for drug delivery with potentially reduced side effects.

Purpose of the Study:

• To develop a stable and sustained-release delivery system for tacrolimus (TCM).
• To formulate tacrolimus into ethyl cellulose and xanthan gum-based microsponges.
• To evaluate the physicochemical properties and in vitro drug release of the developed microsponges.

Main Methods:

• Ethyl cellulose (EC) and xanthan gum (XG)-facilitated microsponges were prepared using emulsification and modified double emulsification techniques.
• Various concentrations of drug and excipients were used.
• Micromeritics, drug-excipient compatibility, yield, drug content, entrapment efficiency, zeta potential, size distribution, and in vitro drug release were evaluated.

Main Results:

• The prepared microsponges exhibited excellent flow properties and adequate entrapment efficiency.
• In vitro dissolution studies showed a sustained drug release profile for up to 8 hours.
• Particle size ranged from 1.99-3.09 µm, and zeta potential ranged from -15.33 to -3.38 mV, indicating stable microparticles.

Conclusions:

• The developed emulsification technique and the combination of ethyl cellulose and xanthan gum are suitable for creating sustained-release tacrolimus microsponges.
• The formulation demonstrates potential for improved tacrolimus delivery.
• This study provides a foundation for further development of microsponge-based drug delivery systems.