ABSTRACTThis review highlights recent advances in the bioanalysis of cephalosporins using liquid chromatographic methods, focusing on green sample preparation (GSP) techniques. Cephalosporins, a class of β‐lactam antibiotics, are critical in combating bacterial infections but present challenges related to drug resistance and toxicity. This article evaluates various sample preparation methods, including solid‐phase extraction, solid‐phase microextraction, and protein precipitation, which have been employed in the extraction and quantification of cephalosporins from biological matrices. Special attention is given to the optimization of critical parameters, such as pH, extraction solvents, and purification techniques to maximize analytes’ recovery and sensitivity. Emerging trends in GSP, such as the use of molecularly imprinted polymers and miniaturized processing devices, are also discussed. The review underscores the growing importance of integrating environmentally friendly approaches in cephalosporin bioanalysis, paving the way for future innovations in bioanalytical research.