Melittin as a Permeability Enhancer II: In Vitro Investigations in Human Mucus Secreting Intestinal Monolayers and Rat Colonic Mucosae

• Published in: Pharmaceutical research Vol. 24; no. 7; pp. 1346 - 1356
• Main Authors: Maher, Sam, Feighery, Linda, Brayden, David J., McClean, Siobhán
• Format: Journal Article
• Language: English
• Published: New York, NY Springer 01.07.2007; Springer Nature B.V
• Subjects: Animals; Bioavailability; Biochemistry; Biological and medical sciences; Caco-2 Cells; Calcium-binding protein; Calcium-Calmodulin-Dependent Protein Kinases - antagonists & inhibitors; Calcium-Calmodulin-Dependent Protein Kinases - metabolism; Calmodulin; Calmodulin - metabolism; Cell Survival - drug effects; Cellular biology; Colon; Colon - drug effects; Colon - metabolism; Cytotoxicity; Diffusion Chambers, Culture; Dose-Response Relationship, Drug; Drug delivery; Drug Stability; Electric Impedance; Electrical resistivity; General pharmacology; Hemolysis - drug effects; HT29 Cells; Human subjects; Humans; In Vitro Techniques; Intestinal Absorption - drug effects; Intestinal Mucosa - drug effects; Intestinal Mucosa - metabolism; Intestine; Ions; Large intestine; Male; Mannitol; Mannitol - metabolism; Medical sciences; Melitten - chemistry; Melitten - pharmacology; Membrane Potentials - drug effects; Mucosa; Mucus; Mucus - metabolism; Peptides; Permeability; Permeability - drug effects; Pharmaceutical technology. Pharmaceutical industry; Pharmacology; Pharmacology. Drug treatments; Protein Kinase Inhibitors - pharmacology; Rats; Rats, Sprague-Dawley; Rodents; Sheep; Short-circuit current; Small intestine; Sulfonamides - pharmacology; Transmission electron microscopy; Tritium; Human; Stomach; Pharmaceutical technology; gastrointestinal permeability models; Peptides; Rat; melittin; Rodentia; Gut; Oral administration; oral peptide delivery; Mucus; Permeability; Gastrointestinal; In vitro; Vertebrata; Mammalia; Animal; ussing chambers; Absorption enhancer; Colon
• ISSN: 0724-8741; 1573-904X
• DOI: 10.1007/s11095-007-9246-z

Melittin has shown potential as a non-cytotoxic absorption enhancer in Caco-2 monolayers. Our objectives were to assess in vitro efficacy and cytotoxicity of melittin in two intestinal permeability models and investigate the potential mechanism by which melittin might enhance gastrointestinal absorp...