The invention discloses a preparation method and application of
bioactive lipid and lipid nanoparticles thereof. The
bioactive lipid molecule is formed by bonding long-chain
fatty acid (LCFA) with different chain lengths with two functional small molecules, namely
phenylboronic acid pinacol ester (PBAP) and Tempol (Tpl) respectively, so that two types of lipid molecules, namely PBAP-LCFA and Tpl-LCFA, with anti-inflammatory activity are constructed. The lipids are used as functional components, and the anti-inflammatory lipid nanoparticles with good
biocompatibility, including PLP, TLP and TPLP, can be prepared through a film dispersion method. The lipidoid and the lipid nanoparticles are simple and convenient in preparation process, controllable in
structure and function and easy for large-scale production, and have treatment potential in various acute and chronic inflammatory diseases. In an
animal model, the lipid nanoparticles have remarkable curative effects on acute
peritonitis, acute
lung injury,
acute hepatic failure,
asthma and other diseases. Besides, the
lipid bilayer structure of the TPLP can efficiently entrap hydrophilic / hydrophobic drugs, can synergistically deliver treatment drugs while exerting the anti-inflammatory effect of the TPLP, and realizes a synergistic
combined treatment strategy for chronic
lung inflammation and other diseases.