Highlights

• This patent developed a PLGA-based sustained-release microsphere formulation loaded with S-propargyl-cysteine, prepared via the emulsion–solvent evaporation method, forming either W/O/W or W/O/S microspheres.
• The formulation achieved a drug loading of up to 12.72% and encapsulation efficiency of 78.15%, with sustained release lasting up to 30 days.
• It can effectively regulate hydrogen sulfide production, thereby enhancing treatment efficacy for cardiovascular diseases and rheumatoid arthritis while reducing cellular toxicity.

Summary

This invention patent developed a sustained-release microsphere formulation loaded with S-propargyl-cysteine (SPRC) and its preparation method. The formulation uses biodegradable poly(lactic-co-glycolic acid) (PLGA) as the carrier. It is prepared using the emulsion–solvent evaporation method, forming two possible types: water-in-oil-in-water (W/O/W) and water-in-oil-in-solid (W/O/S).

Experimental results showed that the microspheres exhibited excellent drug-loading performance (up to 12.72%) and high encapsulation efficiency (up to 78.15%), and were capable of sustained drug release for up to 30 days.

In addition, in vitro release studies indicated that the formulation can effectively regulate the in vivo hydrogen sulfide (H₂S) generation rate. This controlled-release feature significantly enhances the therapeutic effect for cardiovascular diseases and rheumatoid arthritis, while also reducing the potential cytotoxicity of hydrogen sulfide. The preparation process is simple and reliable, showing promising clinical application potential.

朱依谆, 胜吕纶贵子, 朱依纯, “Microsphere Formulation Loaded with S-Propargyl-Cysteine and Its Preparation Method,” China Patent CN115634204A, Jan. 24, 2023.