2results about How to "Improve brain targeting" patented technology

The invention belongs to the technical field of biological medicine, and discloses a brain-targeted nano drug delivery system, a preparation method and application. According to the invention, dipentaerythritol-polycaprolactone-histidine (DPE-PCL-HIS) is used as a basic drug carrier, and drug curcumin (Cur) molecules are entrapped in a physical embedding manner; and modifying bovine serum albumin (BSA) grafted with a bifunctional intermediate connection compound 4-(N-maleimide methyl) cyclohexane-1-carboxylic acid 3-sulfo-N-hydroxysuccinimide ester sodium salt (Sulfo-SMCC) on a precoating layer, and finally connecting an apolipoprotein E mimic peptide as a brain-targeting ligand, so as to construct the brain-targeting bionic protein crown nano drug delivery system, wherein the bovine serum albumin (BSA) is grafted with the bifunctional intermediate connection compound 4-(N-maleimide methyl) cyclohexane-1-carboxylic acid 3-sulfo-N-hydroxysuccinimide ester sodium salt (Sulfo-SMCC). According to the prepared brain-targeted nano drug delivery system, apolipoprotein E mimic peptide [RLLRKRLK (PEG2000) RLGWC] is used as a ligand and enters the brain under the transendocytosis action of the apolipoprotein E mimic peptide [RLLRKRLK (PEG2000) RLGWC] and a blood-brain barrier (BBB) surface receptor, the blood-brain barrier permeability of a drug is increased, the brain targeting property and bioavailability of drug-loaded nanoparticles are improved, and the brain-targeted nano drug delivery system has wide application prospects in the aspect of treating brain diseases.

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.