Multifunctional matrices for oral peptide delivery

Critical Reviews in Therapeutic Drug Carrier Systems

Volumn 18, Issue 5, 2001, Pages 459-501

  Bernkop Schnurch A ^a   Walker, G ^a  

^a UNIVERSITY OF VIENNA   (Austria)

Author keywords

Enzyme inhibition; Mucoadhesive polymers; Multifunctional matrices; Oral peptide delivery; Permeation enhancement

Indexed keywords

ALGINIC ACID; BROMELAIN; BUFFER; BUSERELIN; CARBOMER; CARBOXYMETHYLCELLULOSE; CELLULOSE DERIVATIVE; CHITOSAN; CHYMOSTATIN; CYCLOSPORIN A; CYSTEINE; DESMOPRESSIN; DETERGENT; EDETIC ACID; ENZYME; INSULIN; MERCAPTAMINE; MUCOLYTIC AGENT; PAPAIN; PEPTIDE; PHLOGENZYM; POLYACRYLIC ACID; POLYCARBOPHIL; POLYMER; THIOGLYCOLIC ACID; THIOL; THIOL DERIVATIVE; TRITON X 100; UNINDEXED DRUG; WOBENZYM;

ADHESION; CELL TRANSPORT; COVALENT BOND; DELAYED RELEASE FORMULATION; DIFFUSION; DRUG BIOAVAILABILITY; DRUG DEGRADATION; DRUG DELIVERY SYSTEM; ENDOCYTOSIS; ENZYME INHIBITION; HUMAN; MEMBRANE; MEMBRANE TRANSPORT; MUCUS; NONHUMAN; REVIEW; SUSTAINED RELEASE PREPARATION;

EID: 0035206421     PISSN: 07434863     EISSN: None     Source Type: Journal    
DOI: 10.1615/critrevtherdrugcarriersyst.v18.i5.20     Document Type: Review

References (187)

1. Systemic delivery of peptides and proteins across absorptive mucosae
2. Transdermal iontophoresis. Part II. Peptide and protein delivery
3. Bacterial chemotactic oligopeptides and the intestinal mucosal barrier
4. The use of inhibitory agents to overcome the enzymatic barrier to perorally administered therapeutic peptides and proteins
5. Enhancement of the intestinal absorption of peptides and non-peptides
6. Polymeric nano- and microparticles for the oral delivery of peptides and peptidomimetics
7. Application of surface-coated liposomes for oral delivery of peptide: Effects of coating the liposome's surface on the GI transit of insulin
8. "Targeted delivery" in the gastrointestinal tract
9. Mucoadhesive polymers in peroral peptide drug delivery. VI. Carbomer and chitosan improve the intestinal absorption of the peptide drug buserelin in vivo
10. Design and in vivo evaluation of an oral delivery system for insulin
11. N-trimethylated chitosan chloride (TMC) improves the intestinal permeation of the peptide drug buserelin in vitro (Caco-2 cells) and in vivo (rats)
12. Mucusmodelle zur untersuchung von intestinalen absorptionsmechanismen
13. Small intestinal mucin: Polymerization and the "link glycopeptide"
14. An estimate of turnover time of intestinal mucus gel layer in the rat in situ loop
15. Intestinal mucins in health and disease
16. Diffusion coefficient in native mucus gel of rat small intestine
17. The hydrophobic barrier properties of gastrointestinal mucus
18. Diffusion of drugs in native and purified gastrointestinal mucus
19. Investigations into the diffusion behaviour of polypeptides in native intestinal mucus with regard to their peroral administration
20. A study of macromolecular diffusion through native porcine mucus
21. Peroral administration of enzymes: Strategies to improve the galenic of dosage forms for trypsin and bromelain
22. Evidence of mucoadhesion by chain interpenetration at a poly(acrylic acid)/mucin interface using ATR-FTIR spectroscopy
23. A rheological assessment of the nature of interactions between mucoadhesive polymers and a homogenised mucus gel
24. Development and in vitro evaluation of systems to protect peptide drugs from aminopeptidase N
25. Chitosans as absorption enhancers of poorly absorbable drugs. 3. Influence of mucus on absorption enhancement
26. Developmental changes in distribution of the mucous gel layer and intestinal permeability in rat small intestine
27. Peroral polypeptide delivery: A comparative in vitro study of mucolytic agents
28. Novel bioadhesive chitosan-EDTA conjugate protects leucine enkephalin from degradation by aminopeptidase N
29. Treatment of patients with lung abscess by local administration of papain
30. Use of the proteolytic enzyme papain in the treatment of cervical osteochondrosis
31. Retardation of hydrogen ion diffusion by gastric mucus constituents: Effect of proteolysis
32. Measurment of sputum viscosity in a cone-plate viscometer
33. The roles of enteric bacterial sialidase sialate O-acetyl esterase and glycosulfatase in the degradation of human colonic mucin
34. Polymer-inhibitor conjugates: A promising strategy to overcome the enzymatic barrier to perorally administered (poly)peptide drugs?
35. Prodrugs of peptides obtained by derivatisation of the C-terminal peptide bond in order to effect protection against degradation by carboxypeptidases
36. Coumarinic acid-based cyclic prodrugs of opoid peptides that exhibit metabolic stability to peptidases and excellent cellular permeability
37. Effect of various protease inhibitors on the intestinal absorption and degradation of insulin in rat
38. Oral absorption of peptides: Influence of pH and inhibitors on the intestinal hydrolysis of Leu-enkephalin and analogues
39. Pepsin
40. Enzymatic barriers for GI peptide and protein delivery
41. Structure specificity of mucosal-cell transport and metabolism of amino acids peptide drugs: Implications for oral peptide delivery
42. Transepithelial transport of insulin. I. Insulin degradation by insulin-degrading enzyme in the small intestinal epithelium
43. Subcellular distribution of proteolytic activities degrading bioactive peptides and analogues in mucosal cells of the small intestine and colon
44. Intestinal transport of macromolecules
45. Lysosomal enzymes
46. Transport of β-lactoglobulin across rabbit ileum in vivo
47. Proteases and proteolysis in the lysosome
48. Structural basis of substrate specificity in the serine proteases
49. On the size of the active site in proteases. I. Papain
50. Activity of pancreatic endopeptidases toward luteinizing hormone releasing hormones
51. Mapping the S' subsites of serine proteases using acyl transfer to mixtures of peptide nucleophiles
52. Role of the S' subsites in serine protease catalysis. Active-site mapping of rat chmyotrypsin α-lytic protease and cercarial protease from Schistosoma mansoni
53. Substrate specificity of aminopeptidase P from Escherichia coli: Comparison with membrane-bound forms from rat and bovine lung
54. N-domain selectivity of angiotensin I-converting enzyme as assessed by structure-function studies of its highly selective substrate N-acetyl-serl-aspartyl-lysyl-proline
55. Non-pancreatic hydrolysis of N-benzoyl-p-amino benzoic acid (PABA-peptide) in the human small intestine
56. Susceptibility of ebiratide to proteolysis in rat intestinal fluid and homogenates and its protection by various protease inhibitors
57. Insulin and proinsulin proteolysis in mucosal homogenates of the albino rabbit: Implications in peptide delivery from nonoral routes
58. Metabolism and transport of the pentapeptide metkephamid by brush-border membrane vesicles of rat intestine
59. Feedback regulation of human pancreatic secretion
60. Significance of microflora in proteolysis in the colon
61. Permeability and absorption of leuprolide from various intestinal regions in rabbits and rats
62. Degradation of proteins by guinea pig intestinal enzymes
63. Degradation and aggregation of human calcitonin in vitro
64. Contribution of the microflora to proteolysis in the human large intestine
65. Targeting of peptide and protein drugs to specific sites in the oral route
66. Comparison of distribution of brush-border exo- and endopeptidases in rat and rabbit intestine
67. An effect of calcium ions on the activity heat stability and structure of trypsin
68. Effect of diet on the trypsin and chymotrypsin output in the stools of patient with an ileostomy
69. Determination of immunoreactive trypsin pancreatic elastase and chymotrypsin in extracts of human feces and ileostomy drainage
70. Intestinal peptide transport systems and oral drug delivery availability
71. Expression cloning of a mammalian proton-coupled oligopeptide transporter
72. +/peptide cotransporter: Cloning functional expression and chromosomal localization
73. +/peptide cotransporter mediating absorption of β-lactam antibiotics in the intestine and kidney
74. Regulation of the PepT1 peptide transporter in the rat small intestine in response to 5-fluorouracil-induced injury
75. Peptide transporter in the rat small intestine: Ultrastructural localization and the effect of starvation and administration of amino acids
76. +/peptide transporter PepT1
77. Endocytosis in absorptive cells of cultured human small-intestine tissue: Horseradish peroxidase lactoperoxidase and ferritin as markers
78. Small intestinal adsorption of horseradish peroxidase: A cytochemical study
79. Membrane-bound and fluid-phase macromolecules enter separate prelysosomal compartments in adsorptive cells of suckling rat ileum
80. Mechanism of insulin absorption by the intestinal mucosa: A morpho-cytochemical study
81. Adsorptive-mediated endocytosis of a dynorphin-like analgesic peptide E-2078 into the blood brain barrier
82. Transport mechanism of a new behaviourally highly potent andreno-corticotropic hormone (ACTH) analogue ebirate through the blood-brain barrier
83. Adsorptive-mediated transcytosis of a synthetic basic peptide 001-C8 in Caco-2 cells
84. Intestinal absorption of a fluoresence-derivatised cationic peptide 001-C8-NBD via adsorptive-mediated transcytosis
85. Partition coefficients and their uses
86. Epithelial transport of drugs in cell culture. I. A model for studying the passive diffusion of drugs over intestinal absorptive (Caco-2) cells
87. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells
88. The influence of peptide structure on transport across Caco-2 cells
89. Desolvation energy: A major determinant of absorption but not clearance of peptides in rats
90. Effect of restricted conformational flexibility on the permeation of model hexapeptides across Caco-2 cell monolayers
91. Barrier function of the epithelium
92. Structural basis for physiological regulation of paracellular pathways in intestinal epithelia
93. Passive movement of water and sodium across the human small intestinal mucosa
94. Permeability characteristics of the human small intestine
95. Effect of changing intestinal flow rate on measurement of intestinal permeability
96. Filtration diffusion and molecular sieving through porous cellulose membranes
97. An improved everted gut sac as a simple and accurate technique to measure paracellular transport across the small intestine
98. Absorption enhancers
99. The relationship between rat intestinal permeability and hydrophilic probe size
100. Effect of size and charge on the passive diffusion of peptides across Caco-2 cell monolayers via the paracellular pathway
101. Paracellular drug transport across the intestinal epithelia: Influence of charge and induced water flux
102. A simple rheological method for the in vitro assessment of mucin-polymer bioadhesive bond strength
103. Synthesis and characterisation of mucoadhesive thiolated polymers
104. The effect of polycarbophil on the gastric emptying of pellets
105. GI transit of potential bioadhesive formulations in man: A scintigraphic study
106. Mucosal drug delivery using cellulose derivatives as a functional polymer
107. Mucoadhesive DL-lactide/glycolide copolymer nanospheres coated with chitosan to improve oral delivery of elcatonin
108. Mucoadhesive liposomes coated with chitosan or carbopol for oral administration of peptide drugs
109. Mucoadhesive polymers as platforms for peroral peptide delivery and absorption: Synthesis and evaluation of different chitosan-EDTA conjugates
110. Oral peptide drug delivery: Polymer-inhibitor conjugates protecting insulin from enzymatic degradation in vitro
111. Effects of the mucoadhesive polymer polycarbophil on the intestinal absorption of a peptide drug in the rat
112. Mucoadhesive polymers in peroral peptide drug delivery. II. Carbomer and polycarbophil are potent inhibitors of the intestinal proteolytic enzyme trypsin
113. Polycarbophil-cysteine conjugates as platforms for oral (poly)peptide delivery systems
114. In vitro evaluation of the permeation-enhancing effect of thiolated polycarbophil
115. Factors affecting in vitro gastric mucoadhesion. II. Physical properties of polymers
116. An in vitro investigation of mucosa-adhesive materials for use in controlled drug delivery
117. Chitosan and its derivatives: Potential excipients for peroral peptide delivery systems
118. Chitosan: A unique polysaccharide for drug delivery
119. Toxicity of chitosan
120. Chitosan and its use as a pharmaceutical excipient
121. Enteral absorption of insulin in rats from mucoadhesive chitosan-coated liposomes
122. From sticky stuff to sweet receptors: Achievements limits and novel approaches to bioadhesion
123. Polymers with thiol groups: A new generation of mucoadhesive polymers?
124. Thiolated polymers: Development and in vitro evaluation of chitosan-thioglycolic acid conjugates
125. Improvement in the mucoadhesive properties of alginate by the covalent attachment of cysteine
126. Development of controlled drug release systems based on polymer-cysteine conjugates
127. Synthese und in vitro evaluierung von chitosan-cystein konjugaten
128. Thiolated carboxymethylcellulose: In vitro evaluation of its permeation enhancing effect on peptide drugs
129. Thiolated polymers: Synthesis and in vitro evaluation of polymer-cysteamine conjugates
130. Synthesis and evaluation of a modified mucoadhesive polymer protecting from α-chymotrypsinic degradation
131. Modified mucoadhesive polymers for peroral administration of mainly elastase degradable therapeutic (poly)peptides
132. Effects of polyacrylic polymers on the lumenal proteolysis of peptide drugs in the colon
133. Mucoadhesive polymers in peroral peptide drug delivery. I. Influence of mucoahesive excipients on the proteolytic activity of intestinal enzymes
134. Mucoadhesive polymers in peroral peptide drug delivery. V. Effect of poly(acrylates) on the enzymatic degradation of peptide drugs by intestinal brush border membrane vehicles
135. Carbomer and polycarbophil are potent inhibitors of the intestinal proteolytic enzyme trypsin
136. Carbomer inhibits tryptic proteolysis of luteinizing hormone-releasing hormone and N-α-benzoyl-L-arginine ethyl ester by binding the enzyme
137. Oral route of peptide and protein drug delivery
138. Subchronic oral toxicity study with regular and enzymatically depolymerized sodium carboxymethylcellulose in rats
139. The potential of mucoadhesive polymers in enhancing intestinal peptide drug absorption. III. Effects of chitosan-glutamate and carbomer on epithelial tight junctions in vitro
140. Chitosan as a novel nasal delivery system for peptide drugs
141. Comparison of absorption-enhancing effect between sodium caprate and disodium ethylenediaminetetraacetate in Caco-2 cells
142. Assembly and sealing of tight junctions: Possible participation of G-proteins, phospholipase C, protein kinase C, and calmodulin
143. Chitosans as absorption enhancers for poorly absorbable drugs. 2. Mechanism of absorption enhancement
144. Oxidant-induced disruption of intestinal epithelial barrier function: Role of tyrosine phosphorylation
145. Regulation of PTP1B via glutathionylation of the active site cysteine 215
146. Chitosans for enhanced delivery of therapeutic peptides across intestinal epithelia: In vitro evaluation in Caco-2 cell monolayers
147. Mucoadhesive polymers in peroral peptide drug delivery. IV. Polycarbophil and chitosan are potent enhancers of peptide transport across intestinal mucosae in vitro
148. Chitosan for enhanced intestinal permeability: Prospects for derivatives soluble in neutral and basic environments
149. Starch microspheres induce pulsatile delivery of drugs and peptides across the epithelial barrier by reversible separation of the tight junctions
150. Enhancement of paracellular drug transport with highly quarternized N-trimethyl chitosan chloride in natural environments: In vitro evaluation in intestinal epithelial cells (Caco-2)
151. Anionic mucoadhesive polymers as auxiliary agents for the peroral administration of (poly)peptide drugs: Influence of the gastric fluid
152. Epidermal growth factor-urogastrone, a polypeptide acquiring hormonal status
153. Gastric ulcer treatment with intravenous human epidermal growth factor: A double-blind controlled clinical study
154. Colloidal bismuth subcitrate inhibits peptic degradation of gastric mucus and epidermal growth factor in vitro
155. Effects of polyacrylic polymers on the degradation of insulin and peptide drugs by chymotrypsin and trypsin
156. Oral controlled release technology for peptides: Status and future prospects
157. Insulin stabilization and GI absorption
158. Development and in vitro evaluation of a peptide drug delivery system based on thiolated polycarbophil
159. Basic studies on bioadhesive delivery systems for peptide and protein drugs
160. 2EDTA and sodium glycocholate on intestinal absorption of insulin
161. Absorption of 1-deamino-8-arginine vasopressin from different regions of the gastrointestinal tract in rabbits
162. A new approach to the oral administration of insulin and other peptide drugs
163. Enhancement of jejunal and colonic absorption of fosfomycin by promotors in the rat
164. Enhancement of colonic drug absorption by the paracellular permeation route
165. Enhanced permeability of insulin across the rat intestinal membrane by various enhancers: Their intestinal mucosal toxicity and absorption-enhancing mechanism of n-lauryl-β-D-maltopyranoside
166. Biopharmaceutical approaches for developing and assessing oral peptide delivery strategies and systems: In vitro permeability and in vivo oral absorption of salmon calcitonin (sCT)
167. Coated dosage forms for colon-specific drug delivery
168. Targeted enternal delivery of insulin to rats
169. The effect of Eudragit RL-100 on the mechanical and mucoadhesion properties of polycarbophildosage forms
170. The rationale of peptide drug delivery to the colon and the potential of polymeric carriers as effective tools
171. Targeting drugs to the colon: Delivery systems for oral administration
172. Biodegradable axopolymer coating for oral delivery of peptide drugs
173. Hydrogels for site-specific oral delivery: Synthesis and characterisation
174. Hydrogels for specific drug delivery to the colon: In vitro and in vivo degradation
175. Novel pH-sensitive hydrogels with adjustable swelling kinetics
176. Chitosan capsules for colon-specific drug delivery: Improvement of insulin absorption from the rat colon
177. Colonic-specific delivery of peptide drugs and anti-inflammatory drugs using chitosan capsules
178. Synthesis of chitosan succinate and chitosan phthalate and their evaluation as suggested matrices in orally administered colon-specific drug delivery systems
179. Influence of glutaraldehyde on drug release and mucoadhesive properties of chitosan microspheres
180. Evaluation of the biological properties of soluble chitosan and chitosan microspheres
181. Controlled release of albumin from chitosan-alginate microcapsules
182. Design of microcapsulated chitosan microspheres for colonic drug delivery