This invention relates to an
enzyme-responsive brain-targeting sustained-release formulation based on dialkylimidazolium biomimetic lipids, its preparation method, and its application, belonging to the field of
drug delivery. First, dialkylimidazolium biomimetic lipids are covalently coupled with
natural phospholipids to form a dialkylimidazolium conjugate. Then, this dialkylimidazolium conjugate is self-assembled with dialkylimidazolium biomimetic lipids,
natural phospholipids,
cholesterol, and a therapeutic
drug to form a
drug-loaded lipid
nanoparticle delivery system. This
drug delivery system can effectively cross the blood-brain barrier to achieve brain-targeted delivery of the loaded drug. In the
glioma microenvironment, this
drug delivery system can gradually hydrolyze the dialkylimidazolium conjugate through an
enzyme-responsive mechanism to achieve sustained release of the loaded drug, providing a new strategy for improving the
brain targeting and
efficacy of different types of anti-
glioma drugs, such as small
nucleic acid drugs,
peptide drugs, and
small molecule drugs.