Highlights

• This patent successfully developed Leonurine nanoliposomes using thin-film hydration combined with active loading techniques, significantly improving the encapsulation efficiency and drug loading capacity of this poorly soluble drug.
• The nanoliposomes are spherical with diameters of 80–200 nm, capable of sustained in vitro release for 8–24 hours.
• The formulation enhances Leonurine’s bioavailability, features a simple and reproducible preparation process, and provides an efficient new delivery system for treating cardiovascular and neurological conditions, as well as gynecological disorders.

Summary

This invention patent describes the development of Leonurine-loaded nanoliposomes designed to address the challenges of poor water and lipid solubility and low bioavailability of Leonurine. The formulation is prepared using the thin-film hydration method to create blank liposomes, followed by active drug loading using either an ammonium sulfate gradient or pH gradient method, which significantly improves encapsulation efficiency (30%–90%) and drug loading (2%–20%).

The resulting nanoliposomes are uniformly spherical with particle sizes ranging from 80 to 200 nm, and they exhibit sustained in vitro drug release lasting 8–24 hours, indicating strong controlled-release properties. The preparation process is simple, reproducible, and suitable for large-scale manufacturing.

This liposomal formulation not only significantly improves the stability and bioavailability of Leonurine but also offers a novel drug delivery strategy for its application in neuroprotection, cardiovascular diseases, and gynecological indications.

朱依谆, 余越, “Endogenous Hydrogen Sulfide Sustained-Release Formulation: Preparation Method and Application,” China Patent CN114246845A, Mar. 29, 2022.