Fighting type 2 diabetes: Formulation strategies for peptide-based therapeutics  

作　　者：Carlos Bendicho-Lavilla Iria Seoane-Viano Francisco J.OteroEspinar Asteria Luzardo-Alvarez 

机构地区：[1]Department of Pharmacology,Pharmacy and Pharmaceutical Technology,Faculty of Pharmacy,University of Santiago de Compostela(USC),Santiago de Compostela 15782,Spain [2]Paraquasil Group,Health Research Institute of Santiago de Compostela(IDIS),Santiago de Compostela 15706,Spain [3]Department of Pharmacology,Pharmacy and Pharmaceutical Technology,School of Sciences,Campus de Lugo,University of Santiago de Compostela,Lugo 27002,Spain

出　　处：《Acta Pharmaceutica Sinica B》2022年第2期621-636,共16页药学学报（英文版）

基　　金：funded by Xunta de Galicia grant number GRC2013/015 and GPC2017/015(Spain)。

摘　　要：Diabetes mellitus is a major health problem with increasing prevalence at a global level.The discovery of insulin in the early 1900 s represented a major breakthrough in diabetes management,with further milestones being subsequently achieved with the identification of glucagon-like peptide-1(GLP-1)and the introduction of GLP-1 receptor agonists(GLP-1 RAs)in clinical practice.Moreover,the subcutaneous delivery of biotherapeutics is a well-established route of administration generally preferred over the intravenous route due to better patient compliance and prolonged drug absorption.However,current subcutaneous formulations of GLP-1 RAs present pharmacokinetic problems that lead to adverse reactions and treatment discontinuation.In this review,we discuss the current challenges of subcutaneous administration of peptide-based therapeutics and provide an overview of the formulations available for the different routes of administration with improved bioavailability and reduced frequency of administration.

关 键 词：Type 2 diabetes mellitus Glucagon-like peptide-1 receptor agonists EXENATIDE Subcutaneous administration Amylin mimetics Drug delivery systems BIOTHERAPEUTICS Peptide delivery Controlled-release formulations Microparticles Nanoparticles 

分 类 号：R977.15[医药卫生—药品]