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Glycosylation is a useful synthetic technique to increase the bioavailability of medicinal peptides

Jaylin Hey

Glycosylation of peptides is a promising technique for enhancing peptide medication absorption through biological membranes and altering their physicochemical properties. This review discusses several glycoconjugate synthesis methods as well as recent advances in the creation of glycosylated peptide therapies. Furthermore, the effects of glycosylation on overcoming current obstacles to peptide transport in the mouth and brain are discussed. Peptides offer high activity, target specificity, low toxicity, and limited non-specific and drug–drug interactions, making them viable therapeutic candidates for a variety of illnesses. There have been numerous attempts to improve the pharmacological characteristics of peptide medicines and transport them efficiently to target areas, notably via non-parenteral methods. However, peptides' weak physicochemical qualities prevent them from being delivered effectively. More importantly, biological obstacles such as fluctuating pH across the Gastrointestinal Tract (GIT), the presence of proteases, and physical barriers can make oral peptide distribution difficult. The phospholipid bilayer in biological membranes, for example, prevents peptide medicines from penetrating fully into intestinal cells. In addition, insufficient absorption and quick breakdown by proteolytic enzymes are further roadblocks that contribute to the low oral bioavailability of peptides (less than 1-2%