Abstract

Growing demand for insulin and glucagon-like peptide-1 receptor agonists (GLP-1 RA) is observed, considering the progressive nature of diabetes and the potential therapeutic role of peptides in its treatment. However, chronic parenteral administration is responsible for pain and rashes at the site of injection. Oral delivery of insulin and GLP-1 RA promises better patient compliance owing to their ease of administration and reduction in chances of peripheral hypoglycaemia and weight gain. The review article discusses the potential of lipid carriers in combination with different strategies such as absorption enhancers, PEGylation, lipidisation, etc. The lipid nanocarriers improve the membrane permeability and oral bioavailability of high molecular weight peptides. Additionally, the clinical status of different nanocarriers for anti-diabetic peptides is discussed. Previous research on nanocarriers showed significant hypoglycaemic activity and safety in animal studies; however, extrapolation of the same in human subjects is not validated. With the rising global burden of diabetes, the lipid nanocarriers show the potential to revolutionise treatment with oral delivery of insulin and GLP-1 RA.

摘要

考虑到糖尿病的进展性和肽在其治疗中的潜在治疗作用，观察到对胰岛素和胰高血糖素样肽-1 受体激动剂 (GLP-1 RA) 的需求不断增长。然而，长期肠胃外给药会导致注射部位的疼痛和皮疹。胰岛素和 GLP-1 RA 的口服给药由于易于给药和减少外周低血糖和体重增加的机会而有望提高患者的依从性。这篇综述文章讨论了脂质载体与吸收促进剂、聚乙二醇化、脂质化等不同策略相结合的潜力。脂质纳米载体提高了高分子量肽的膜通透性和口服生物利用度。此外，讨论了抗糖尿病肽的不同纳米载体的临床状况。先前对纳米载体的研究在动物研究中显示出显着的降血糖活性和安全性；然而，在人类受试者中的外推尚未得到验证。随着全球糖尿病负担的增加，脂质纳米载体显示出通过口服胰岛素和 GLP-1 RA 来彻底改变治疗的潜力。