| abstract |
The invention belongs to the field of antibacterial drugs, and specifically relates to a preparation method and application of organic acid-modified polymyxin, and also includes the preparation and application of organic acid-modified polymyxin nanoparticles. The structure of the organic acid-modified polymyxin of the present invention is shown in Formula I, wherein R 1 , R 2 , and X are as described in the claims and description. The organic acid-modified polymyxin connects the organic acid molecule to the hydroxyl group of the polymyxin through a covalent bond to form a stable compound, and due to the difference in the hydrophobicity and saturation of the organic acid, the difference in the ester bond Different positions and quantities make the compound release the prototype drug differently; at the same time, the present invention prepares nanoparticles of polymyxins modified with organic acids, which prolong the half-life of polymyxins in vivo and reduce the toxicity of drugs . |