STUDY OF SOLUBILIZATION OF SOME CEPHALOSPORIN ANTIBIOTICS IN SELF-ORGANIZING AOT SYSTEMS
Abstract and keywords
Abstract:
Self-organizing systems based on surfactants are widely used to deliver drugs and biologically active substances, peptides, and proteins. The advantages of transdermal drug delivery include protection of the gastrointestinal tract from irritation and painless administration. Cephalosporins are a group of antibiotics traditionally taken orally or by injection. However, their low oral bioavailability and painful injection therapy limit their effectiveness in some clinical situations. Therefore, to improve cephalosporin therapy, we developed and studied transport systems (microemulsions and liquid crystals) based on the anionic surfactant AOT, isopropyl myristate, lecithin, and bidistilled water. Cefazolin, cefuroxime, and ceftazidime were used as active components. Using the HLB additivity method we previously developed, we determined the optimal ratio of surfactants and cosurfactants, enabling the production of stable systems. The use of a lecithin-AOT mixture to create microemulsions containing cephalosporins allowed for the stabilization of larger microemulsions, increasing the amount of solubilized drug. It was found that, at a certain ratio of components, a hexagonal liquid crystal mesophase with a phase transition temperature of 45-55°C is formed. UV spectroscopy revealed that all antibiotics used are optically active and have absorption maxima at a wavelength of 278-280 nm (cefuroxime), cefazolin at 270-272 nm, and ceftazidime at 258-260 nm, and can be detected in solution using optical methods. Furthermore, the refractive indices of aqueous solutions of the drugs were determined. Using dynamic light scattering, the droplet size of microemulsions containing cefazolin was determined. It was shown that the droplet size increases with the addition of the drug, but the transdermal system remains stable. The obtained data can be used in studying the release of drugs from the developed microemulsions and liquid crystals.

Keywords:
MICROEMULSIONS, LIQUID CRYSTALS, CEPHALOSPORIN ANTIBIOTICS, DRUG DELIVERY, UV SPECTRA
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