- Record: found
- Abstract: found
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Oral delivery of proteins and peptides: Challenges, status quo and future perspectives
review-article
Quangang Zhu
a
,
† ,
Zhongjian Chen
a
,
† ,
Pijush Kumar Paul
a
,
c
,
† ,
Yi Lu
a
,
b ,
Wei Wu
a
,
b
,
∗ ,
Jianping Qi
a
,
b
,
∗
29 April 2021
Proteins,
Peptides,
Oral delivery,
Permeation enhancer,
Enzyme inhibitor,
Stability,
Clinical,
ASBT, apical sodium-dependent bile acid transporter,
BSA, bovine serum albumin,
CAGR, compound annual growth,
CaP, calcium phosphate,
CD, Crohn's disease,
COPD, chronic obstructive pulmonary disease,
CPP, cell penetrating peptide,
DCs, dendritic cells,
DDVAP, desmopressin acetate,
DTPA, diethylene triamine pentaacetic acid,
EDTA, ethylene diamine tetraacetic acid,
EPD, empirical phase diagrams,
EPR, electron paramagnetic resonance,
FA, folic acid,
FcRn, Fc receptor,
FDA, U.S. Food and Drug Administration,
GALT, gut-associated lymphoid tissue,
GI, gastrointestinal,
GIPET, gastrointestinal permeation enhancement technology,
GLP-1, glucagon-like peptide 1,
GRAS, generally recognized as safe,
HBsAg, hepatitis B surface antigen,
HPMCP, hydroxypropyl methylcellulose phthalate,
IBD, inflammatory bowel disease,
ILs, ionic liquids,
LBNs, lipid-based nanoparticles,
LMWP, low molecular weight protamine,
MCT-1, monocarborxylate transporter 1,
MSNs, mesoporous silica nanoparticles,
NAC, N-acetyl-l-cysteine,
NLCs, nanostructured lipid carriers,
PAA, polyacrylic acid,
PBPK, physiologically based pharmacokinetics,
PCA, principal component analysis,
PCL, polycarprolacton,
PGA, poly-γ-glutamic acid,
pHPMA, N-(2-hydroxypropyl)methacrylamide,
pI, isoelectric point,
PLA, poly(latic acid),
PLGA, poly(lactic-co-glycolic acid),
PPs, proteins and peptides,
PVA, poly vinyl alcohol,
RGD, Arg-Gly-Asp,
RTILs, room temperature ionic liquids,
SAR, structure–activity relationship,
sc, subcutaneous,
sCT, salmon calcitonin,
SDC, sodium deoxycholate,
SGF, simulated gastric fluids,
SGC, sodium glycocholate,
STC, sodium taurocholate,
SIF, simulated intestinal fluids,
SLNs, solid lipid nanoparticles,
SNAC, sodium N-[8-(2-hydroxybenzoyl)amino]caprylate,
SNEDDS, self-nanoemulsifying drug delivery systems,
TAT, trans-activating transcriptional peptide,
Tf, transferrin,
TfR, transferrin receptors,
TMC, N-trimethyl chitosan,
UC, ulcerative colitis,
UEA1, ulex europaeus agglutinin 1,
VB12, vitamin B12,
WGA, wheat germ agglutinin
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Abstract
Proteins and peptides (PPs) have gradually become more attractive therapeutic molecules than small molecular drugs due to their high selectivity and efficacy, but fewer side effects. Owing to the poor stability and limited permeability through gastrointestinal (GI) tract and epithelia, the therapeutic PPs are usually administered by parenteral route. Given the big demand for oral administration in clinical use, a variety of researches focused on developing new technologies to overcome GI barriers of PPs, such as enteric coating, enzyme inhibitors, permeation enhancers, nanoparticles, as well as intestinal microdevices. Some new technologies have been developed under clinical trials and even on the market. This review summarizes the history, the physiological barriers and the overcoming approaches, current clinical and preclinical technologies, and future prospects of oral delivery of PPs.
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Author and article information
proteins,peptides,oral delivery,permeation enhancer,enzyme inhibitor,stability,clinical,asbt, apical sodium-dependent bile acid transporter,bsa, bovine serum albumin,cagr, compound annual growth,cap, calcium phosphate,cd, crohn's disease,copd, chronic obstructive pulmonary disease,cpp, cell penetrating peptide,dcs, dendritic cells,ddvap, desmopressin acetate,dtpa, diethylene triamine pentaacetic acid,edta, ethylene diamine tetraacetic acid,epd, empirical phase diagrams,epr, electron paramagnetic resonance,fa, folic acid,fcrn, fc receptor,fda, u.s. food and drug administration,galt, gut-associated lymphoid tissue,gi, gastrointestinal,gipet, gastrointestinal permeation enhancement technology,glp-1, glucagon-like peptide 1,gras, generally recognized as safe,hbsag, hepatitis b surface antigen,hpmcp, hydroxypropyl methylcellulose phthalate,ibd, inflammatory bowel disease,ils, ionic liquids,lbns, lipid-based nanoparticles,lmwp, low molecular weight protamine,mct-1, monocarborxylate transporter 1,msns, mesoporous silica nanoparticles,nac, n-acetyl-l-cysteine,nlcs, nanostructured lipid carriers,paa, polyacrylic acid,pbpk, physiologically based pharmacokinetics,pca, principal component analysis,pcl, polycarprolacton,pga, poly-γ-glutamic acid,phpma, n-(2-hydroxypropyl)methacrylamide,pi, isoelectric point,pla, poly(latic acid),plga, poly(lactic-co-glycolic acid),pps, proteins and peptides,pva, poly vinyl alcohol,rgd, arg-gly-asp,rtils, room temperature ionic liquids,sar, structure–activity relationship,sc, subcutaneous,sct, salmon calcitonin,sdc, sodium deoxycholate,sgf, simulated gastric fluids,sgc, sodium glycocholate,stc, sodium taurocholate,sif, simulated intestinal fluids,slns, solid lipid nanoparticles,snac, sodium n-[8-(2-hydroxybenzoyl)amino]caprylate,snedds, self-nanoemulsifying drug delivery systems,tat, trans-activating transcriptional peptide,tf, transferrin,tfr, transferrin receptors,tmc, n-trimethyl chitosan,uc, ulcerative colitis,uea1, ulex europaeus agglutinin 1,vb12, vitamin b12,wga, wheat germ agglutinin
proteins, peptides, oral delivery, permeation enhancer, enzyme inhibitor, stability, clinical, asbt, apical sodium-dependent bile acid transporter, bsa, bovine serum albumin, cagr, compound annual growth, cap, calcium phosphate, cd, crohn's disease, copd, chronic obstructive pulmonary disease, cpp, cell penetrating peptide, dcs, dendritic cells, ddvap, desmopressin acetate, dtpa, diethylene triamine pentaacetic acid, edta, ethylene diamine tetraacetic acid, epd, empirical phase diagrams, epr, electron paramagnetic resonance, fa, folic acid, fcrn, fc receptor, fda, u.s. food and drug administration, galt, gut-associated lymphoid tissue, gi, gastrointestinal, gipet, gastrointestinal permeation enhancement technology, glp-1, glucagon-like peptide 1, gras, generally recognized as safe, hbsag, hepatitis b surface antigen, hpmcp, hydroxypropyl methylcellulose phthalate, ibd, inflammatory bowel disease, ils, ionic liquids, lbns, lipid-based nanoparticles, lmwp, low molecular weight protamine, mct-1, monocarborxylate transporter 1, msns, mesoporous silica nanoparticles, nac, n-acetyl-l-cysteine, nlcs, nanostructured lipid carriers, paa, polyacrylic acid, pbpk, physiologically based pharmacokinetics, pca, principal component analysis, pcl, polycarprolacton, pga, poly-γ-glutamic acid, phpma, n-(2-hydroxypropyl)methacrylamide, pi, isoelectric point, pla, poly(latic acid), plga, poly(lactic-co-glycolic acid), pps, proteins and peptides, pva, poly vinyl alcohol, rgd, arg-gly-asp, rtils, room temperature ionic liquids, sar, structure–activity relationship, sc, subcutaneous, sct, salmon calcitonin, sdc, sodium deoxycholate, sgf, simulated gastric fluids, sgc, sodium glycocholate, stc, sodium taurocholate, sif, simulated intestinal fluids, slns, solid lipid nanoparticles, snac, sodium n-[8-(2-hydroxybenzoyl)amino]caprylate, snedds, self-nanoemulsifying drug delivery systems, tat, trans-activating transcriptional peptide, tf, transferrin, tfr, transferrin receptors, tmc, n-trimethyl chitosan, uc, ulcerative colitis, uea1, ulex europaeus agglutinin 1, vb12, vitamin b12, wga, wheat germ agglutinin