Given the prevalence of diabetes and the increasing number of diabetics, it is essential to find more effective medicines to decrease the chronic complications of diabetes. Several studies have demonstrated that uncontrolled hyperglycemia and its complications are directly related to glycation of biomolecules. Thus, identifying natural inhibitors to stop extensive nonenzymatic glycation of biomolecules may play a crucial role in managing the consequences of diabetes. Currently, various natural and synthetic compounds with anti-glycation attributes have been reported. The use of natural compounds in herbs (medicinal and non-medicinal) may be of particular importance due to fewer side effects and wide range of therapeutic properties. Based on the extensive biological properties of biophenols including antioxidant, chelating, and free radical scavenging activities, herein, a biodegradable controlled release system was designed for their controlled delivery, as well as the possible association of chemical composition with the inhibitory function of glyco-induced aggregation were examined. Such results are applicable to formulation of small-molecule nutraceuticals for treatment of many conformational diseases such as diabetes, atherosclerosis, chronic kidney disease and Alzheimer's disease.