title: Multifunctional Delivery Systems for Advanced oral Uptake of Peptide/Protein Drugs.
abstract: In recent years, advances in biotechnology and protein engineering have enabled the production of large quantities of proteins and peptides as important therapeutic agents. Various researchers have used biocompatible functional polymers to prepare oral dosage forms of proteins and peptides for chronic use and for easier administration to enhance patient compliance. However, there is a need to enhance their safety and effectiveness further. Most macromolecules undergo severe denaturation at low pH and enzymatic degradation in the gastrointestinal tract. The macromolecules' large molecular size and low lipophilicity cause low permeation through the intestinal membrane. The major strategies that have been used to overcome these challenges (in oral drug carrier systems) can be classified as follows: enteric coating or encapsulation with pH-sensitive polymers or mucoadhesive polymers, co-administration of protease inhibitors, incorporation of absorption enhancers, modification of the physicochemical properties of the macromolecules, and site-specific delivery to the colon. This review attempts to summarize the various advanced oral delivery carriers, including nanoparticles, lipid carriers, such as liposomes, nano-aggregates using amphiphilic polymers, complex coacervation of oppositely charged polyelectrolytes, and inorganic porous particles. The particles were formulated and/or surface modified with functional polysaccharides or synthetic polymers to improve oral bioavailability of proteins and peptides. We also discuss formulation strategies to overcome barriers, therapeutic efficacies in vivo, and potential benefits and issues for successful oral dosage forms of the proteins and peptides.
authors.forename: Jin Woo
authors.initials: JW
authors.lastname: Park
authors.forename: Sun Jin
authors.initials: SJ
authors.lastname: Kim
authors.forename: Dong Sup
authors.initials: DS
authors.lastname: Kwag
authors.forename: Sol
authors.initials: S
authors.lastname: Kim
authors.forename: Jeyoung
authors.initials: J
authors.lastname: Park
authors.forename: Yu Seok
authors.initials: YS
authors.lastname: Youn
authors.affiliation: Department of Pharmaceutics and Pharmaceutical Chemistry, The University of Utah, 30S 2000 E, Room 2972, Salt Lake City, UT 84112, USA. you.bae@utah.edu.
authors.forename: You Han
authors.initials: YH
authors.lastname: Bae
authors.forename: Eun Seong
authors.initials: ES
authors.lastname: Lee
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems; D006801:Humans; D010455:Peptides / Q000008:administration & dosage*; D004364:Pharmaceutical Preparations / Q000008:administration & dosage*; D011506:Proteins / Q000008:administration & dosage*
chemical_list: D004337:Drug Carriers; D010455:Peptides; D004364:Pharmaceutical Preparations; D011506:Proteins