| Cytotoxicity evaluation of enzyme inhibitors and absorption enhancers in Caco-2 cells for oral delivery of salmon calcitonin. | |
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MedLine Citation:
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PMID: 14999743 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The usefulness of enzyme inhibitors and absorption enhancers with least mucosal cell cytotoxicity was evaluated on Caco-2 cell monolayers. The temporal cytotoxicity of several protease inhibitors at 500 microg/mL (e.g., turkey and chicken ovomucoids, aprotinin, and Protease Inhibitor Cocktail) and absorption enhancers [e.g., cholate (3%), glycocholate (3%), glycosursodeoxycholate (3%), ethylenediaminetetraacetic acid (EDTA, 0.1%), hydroxypropyl-beta-cyclodextrin (HP-beta-CD, 5%), hydroxypropyl-gamma-cylcodextrin (HP-gamma-CD, 5%), gamma-cylcodextrin (gamma-CD, 5%), tetradecyl-beta-D-maltoside (0.25%), octylglucoside (0.25%), citric acid (10%), glycyrrhetinic acid (0.34 mM), and Tween-80 (0.1%)] was measured by monitoring their effect on Caco-2 cell viability. Cell viability was measured by mannitol permeability measurements, transepithelial electrical resistance (TEER) measurements, DNA-propidium iodide staining assay, and WST-1 assay (tetrazolium salt based assay). Sodium dodecyl sulfate (0.1%), a potent surfactant, was used as a positive control. Chicken and turkey ovomucoids were nontoxic to cells as evaluated by all the methods used. Aprotinin decreased the TEER, whereas plasma membrane damage was seen with Protease Inhibitor Cocktail after a 24-h period. With respect to the absorption enhancers, the toxicity increased directly as a result of an increase in the time of incubation. The enhancers EDTA and HP-beta-CD can be used safely for a short period of time, whereas glycosursodeoxycholate, glycyrrhetinic acid, octylglucoside, HP-gamma-CD, and gamma-CD can be used for a longer period. |
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Authors:
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Rakhi B Shah; Anitha Palamakula; Mansoor A Khan |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of pharmaceutical sciences Volume: 93 ISSN: 0022-3549 ISO Abbreviation: J Pharm Sci Publication Date: 2004 Apr |
Date Detail:
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Created Date: 2004-03-04 Completed Date: 2004-11-09 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 2985195R Medline TA: J Pharm Sci Country: United States |
Other Details:
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Languages: eng Pagination: 1070-82 Citation Subset: IM |
Copyright Information:
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Copyright 2004 Wiley-Liss, Inc. and the American Pharmacists Association. |
Affiliation:
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School of Pharmacy, Texas Tech University Health Sciences Center, 1300 Coulter, Amarillo, Texas 79106, USA. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Absorption
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drug effects Caco-2 Cells Calcitonin / administration & dosage* Cell Survival / drug effects Coloring Agents DNA / chemistry Dose-Response Relationship, Drug Electric Conductivity Enzyme Inhibitors / toxicity* Excipients / toxicity* Formazans / chemistry Humans Mannitol / chemistry Nuclear Envelope / drug effects Oxidoreductases / chemistry Propidium Tetrazolium Salts Thymidine / metabolism |
| Chemical | |
Reg. No./Substance:
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0/2-(4-iodophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium; 0/Coloring Agents; 0/Enzyme Inhibitors; 0/Excipients; 0/Formazans; 0/Tetrazolium Salts; 36015-30-2/Propidium; 47931-85-1/salmon calcitonin; 50-89-5/Thymidine; 69-65-8/Mannitol; 9007-12-9/Calcitonin; 9007-49-2/DNA; EC 1.-/Oxidoreductases |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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