Milk-derived exosomes as a promising vehicle for oral delivery of hydrophilic biomacromolecule drugs  

作　　者：Yuting Li Liyun Xing Lingling Wang Xi Liu Licheng Wu Mingjie Ni Zhou Zhou Lian Li Xiuxiu Liu Yuan Huang 

机构地区：[1]Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province,Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology,West China School of Pharmacy,Sichuan University,Chengdu 610041,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2023年第2期137-149,共13页亚洲药物制剂科学（英文）

基　　金：The authors gratefully acknowledge financial support from National Natural Science Foundation of China(81872818);National Key R&D Program of China(2021YFE0115200).

摘　　要：Exosomes,as promising vehicles,have been widely used in the research of oral drug delivery,but the generally low drug loading efficiency of exosomes seriously limits its application and transformation.In this study,we systematically investigated the effects of drug loading methods and physicochemical properties(lipophilicity and molecular weight)on drug loading efficiency of milk-derived exosomes to explore the most appropriate loading conditions.Our finding revealed that the drug loading efficiency of exosomes was closely related to the drug loading method,drug lipophilicity,drug molecular weight and exosome/drug proportions.Of note,we demonstrated the universality that hydrophilic biomacromolecule drugs were the most appropriate loading drugs for milk-derived exosomes,which was attributed to the efficient loading capacity and sustained release behavior.Furthermore,milk-derived exosomes could significantly improve the transepithelial transport and oral bioavailability of model hydrophilic biomacromolecule drugs(octreotide,exendin-4 and salmon calcitonin).Collectively,our results suggested that the encapsulation of hydrophilic biomacromolecule drugs might be the most promising direction for milk exosomes as oral drug delivery vehicles.

关 键 词：Milk-derived exosomes Loading efficiency Drug lipophilicity Molecular weight Drug release Oral delivery 

分 类 号：R943[医药卫生—药剂学]