Highlights

• This invention developed a mesoporous silica formulation loaded with S-propargyl-cysteine, achieving efficient drug loading and sustained release using mesoporous silica as the carrier, and significantly enhancing the slow-release capacity of H₂S in vivo.
• The formulation improves therapeutic efficacy for cardiovascular diseases and rheumatoid arthritis, while reducing cytotoxicity to normal cells.
• It features high drug-loading capacity, good biocompatibility, and a simple preparation process, indicating broad application potential.

Summary

This invention patent describes the development of a mesoporous silica-based nanomedicine formulation loaded with S-propargyl-cysteine (SPRC) and its preparation method, within the field of pharmaceutical technology. The formulation uses mesoporous silica with an ordered pore structure as the carrier, and SPRC is loaded through physical adsorption, forming a sustained-release drug delivery system.

This formulation significantly improves the release profile of SPRC, achieving a 41% cumulative release over 48 hours in vitro, and enables the slow, controlled release of hydrogen sulfide (H₂S) in vivo. Animal experiments showed that the formulation effectively increased plasma H₂S concentration and enhanced cystathionine γ-lyase (CSE) activity in rats with myocardial infarction, thereby reducing myocardial damage. It also demonstrated markedly lower toxicity to normal cells.

The preparation process is simple, offers high drug loading, and exhibits excellent biocompatibility and sustained-release characteristics, providing a novel nanomedicine strategy for the treatment of cardiovascular diseases and rheumatoid arthritis.

朱依谆, 余越, 谢莹, “Mesoporous Silica Formulation Loaded with S-Propargyl-Cysteine and Its Preparation Method,” China Patent CN110478320A, Sep. 14, 2021.