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Inhibition of non‐enzymatic glycation processes is an essential aspect of treating type 2 diabetes and related complications. In this study, piperine's preventative, simultaneous and curative effect in glucose‐induced albumin glycation was examined by analyzing the structural and functional markers of albumin. The protective and antioxidant influence of piperine on erythrocytes was assessed by examining cellular membrane modifications with antioxidant status. Albumin glycation was performed in three different experimental sets of 21 days at 37°C in dark conditions‐using different piperine concentrations (250, 500, and 1,000 μM) and time of addition of glucose (30 mM)/piperine (1,000 μM) in a respective solution at 10th day. Piperine with glycated albumin leads to decreased fructosamine, carbonyl group, and protein‐bound glucose. It had protected free amino groups, thiol group, and reduced beta‐amyloid, protein aggregates formation. The presence of piperine with glycated albumin prevented erythrocytes hemolysis, membrane modifications, and maintained the antioxidant status. Piperine showed the antiglycation effects in a dose‐dependent manner, additionally, its pre‐treatment exhibited maximum attenuation by manifesting its primarily preventive role. Practical applications Piperine is a natural alkaloid compound found in pepper, has been reported to possess anti‐cancer, anti‐microbial, and anti‐inflammatory properties. The present study evaluated the antiglycation potential of piperine in albumin's glycation and it displayed preventive action, protected erythrocytes from oxidative damage induced by glycated albumin. We concluded that the daily intake of piperine can be adequate to prevent glycation‐induced diabetic complications development in hyperglycemic conditions.