Highlights

• This patent utilizes the S/O/W double emulsion–solvent evaporation method to prepare Leonurine-PLGA sustained-release microspheres.
• These microspheres are the core technology, significantly enhancing drug loading capacity and encapsulation efficiency, enabling a 15–60 day sustained release in vitro.
• Animal experiments indicate that this formulation can effectively maintain plasma drug concentration, improve hyperlipidemia outcomes, and extend the dosing frequency from once daily to once every 14 days, thereby significantly enhancing treatment efficacy and patient compliance.

Summary

This invention patent developed a Leonurine sustained-release microsphere and investigated its role in the treatment of hyperlipidemia. The sustained-release microspheres use Leonurine as the active ingredient, poly(lactic-co-glycolic acid) (PLGA) as the carrier, and magnesium carbonate as the porogen. They are prepared using the solid-in-oil-in-water (S/O/W) double emulsion–solvent evaporation method.

This patented method significantly improves the drug loading capacity and encapsulation efficiency of the poorly soluble drug Leonurine, achieving in vitro sustained release for 15–60 days. Animal experiments have demonstrated that the microsphere formulation can significantly prolong the in vivo maintenance time of plasma drug concentration and effectively improve blood lipid profiles in hyperlipidemic model rats.

This invention offers an effective formulation strategy to solve the problems of low bioavailability and rapid elimination of Leonurine in the body. It demonstrates promising potential for clinical translation and application.

王晓琳, 朱依谆, 宋智玲, 唐桩, “Preparation Method and Application of Leonurine Sustained-Release Microspheres,” China Patent CN114224872B, Feb. 20, 2024.