Oral Fcrn-Targeted Insulin: Challenges and Current Strategies Publisher



A Aghakhani AVA ; F Bahreini FARBOD ; Vn Uversky Vladimir N ; N Rezaei NIMA
Source: Journal of Drug Delivery Science and Technology Published:2025

Abstract

Diabetes mellitus afflicts more than 830 million people worldwide, yielding 79.2 million disability-adjusted life years (DALYs) in 2021. Exogenous insulin is administered subcutaneously in patients with type 1 and severe type 2 diabetes. Despite its efficacy, administration of parenteral insulin has several issues regarding side effects and patient adherence. Oral delivery, an attractive substitute for parenteral insulin, still faces many challenges. Not only should these drugs overcome the physiological barriers of the human body, but also their structure and material are of great importance. Biocompatibility, pH-responsiveness, low cytotoxicity, and high cellular viability are desirable characteristics. One particularly interesting oral delivery method is targeting neonatal Fc receptors (FcRn) of the gastrointestinal (GI) tract. This review briefly introduces possible insulin delivery routes, delves into oral insulin delivery systems, discusses their merits and challenges, and comprehensively investigates the mechanisms, effects, and challenges of oral FcRn-targeted anti-diabetes medications. © 2025 Elsevier B.V., All rights reserved.