Рegylated antimicrobials

Abstract

Recently, bacterial strains resistant to the antibiotic enrofloxacin appeared which indicates the development of antibiotic resistance. Enrofloxacin is poorly soluble in water. This physical property creates difficulties in obtaining optimal doses of the dissolved form and limits the bioavailability of the substance. It is hygroscopic and has a bitter taste, which reduces the possibility of oral use. In addition, enrofloxacin can cause a cytotoxic effect on the body. Therefore, the search for new compounds and forms of the antibiotic enrofloxacin with improved characteristics is topical. PEGylation is one of the most successful ways to improve drug delivery. PEG is biodegradable and biocompatible, as it does not form toxic metabolites, and is commercially available. The development of a model compound of enrofloxacin with a PEG-400 polymer (PEGylation of the antibiotic enrofloxacin) by covalent connection showed improved antibacterial activity, which is associated with the ability of PEG to affect the permeability of membranes, ensuring the absorption of the active substance by cells. PEGylation of the antibiotic enrofloxacin increases the size and molecular weight of conjugated biomolecules, increases their water solubility and protection against enzymatic degradation, reduces hepatotoxicity and nephrotoxicity, limits immunogenic and antigenic reactions, does not affect hematopoiesis and hemostasis. Consequently, The PEGylation of the antibiotic enrofloxacin helps to increase the therapeutic effect providing good solubility, increasing the accumulation of the active substance in the pathological area, and reducing the toxic effect on the body.