Prolonged release of tegafur from S/O/W multiple emulsion

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery Systems

Background:

• Developing effective drug delivery systems for prolonged and sustained therapeutic effects is crucial.
• Conventional formulations often face challenges in achieving long-term drug release profiles.
• Albumin microspheres offer potential for controlled drug release applications.

Purpose of the Study:

• To develop and evaluate an albumin microsphere-in-oil-in-water (S/O/W) emulsion for sustained drug release.
• To compare the in vitro and in vivo sustained release performance of S/O/W emulsions with control formulations.
• To assess the potential of S/O/W emulsions for delivering model drugs like tegafur.

Main Methods:

• Preparation of S/O/W emulsions incorporating albumin microspheres loaded with tegafur.
• Characterization of albumin microsphere size (3 microns) and drug entrapment ratio (~25%).
• In vitro and in vivo release studies comparing S/O/W emulsions with water-in-oil (W/O) emulsions and microsphere systems.

Main Results:

• S/O/W emulsions exhibited a fourfold greater t75 in in vitro release tests.
• In vivo studies showed more than twofold increase in mean residence time for tegafur from S/O/W emulsions compared to W/O emulsions or microspheres.
• S/O/W emulsions also demonstrated improved mean residence time for 5-fluorouracil (5-FU).

Conclusions:

• Albumin microsphere-in-oil-in-water (S/O/W) emulsions show significant promise for sustained and prolonged drug release.
• The S/O/W emulsion system offers enhanced drug retention and release kinetics compared to traditional formulations.
• This formulation strategy could be valuable for optimizing the delivery of various therapeutic agents, including tegafur and 5-FU.