Transport evaluation of alendronate across Caco-2 cell monolayers. 2009

F Karamustafa, and N Celebi, and Z Değim, and N Unal
Department of Pharmaceutical Technology, Gazi University, Faculty of Pharmacy, Etiler, Ankara, Turkey.

The transport of alendronate through Caco-2 monolayers in the absence and presence of absorption enhancers (sodium taurocholate-STC and dimethyl-beta-cyclodextrin-DM-beta-CD) was studied. The viability of Caco-2 cells was determined by MTT assay. The effects of the experiment period and serum existence in Dubelco's Modified Eagle's Medium (DMEM) on cell viability were examined. The least toxic concentrations of alendronate, STC and DM-beta-CD were found as 0.2% (w/v), 5 mM and 0.3% (w/v), respectively. Transport experiments were performed with these concentrations in DMEM supplemented with serum for an 8 h period. DM-beta-CD increased the transport of alendronate through Caco-2 monolayers significantly. No significance was observed with STC. Cell integrity was determined by measuring the electrical resistance values at the end of the transport experiments and found to be decreased to a greater extent with DM-beta-CD. These results indicate that DM-beta-CD is a promising agent for improving the transport of alendronate.

UI MeSH Term Description Entries
D002463 Cell Membrane Permeability A quality of cell membranes which permits the passage of solvents and solutes into and out of cells. Permeability, Cell Membrane
D002470 Cell Survival The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability. Cell Viability,Cell Viabilities,Survival, Cell,Viabilities, Cell,Viability, Cell
D005079 Excipients Usually inert substances added to a prescription in order to provide suitable consistency to the dosage form. These include binders, matrix, base or diluent in pills, tablets, creams, salves, etc. Excipient,Stabilizing Agent,Stabilizing Agents,Suspending Agent,Suspending Agents,Agent, Stabilizing,Agent, Suspending,Agents, Stabilizing,Agents, Suspending
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000042 Absorption The physical or physiological processes by which substances, tissue, cells, etc. take up or take in other substances or energy.
D001693 Biological Transport, Active The movement of materials across cell membranes and epithelial layers against an electrochemical gradient, requiring the expenditure of metabolic energy. Active Transport,Uphill Transport,Active Biological Transport,Biologic Transport, Active,Transport, Active Biological,Active Biologic Transport,Transport, Active,Transport, Active Biologic,Transport, Uphill
D013656 Taurocholic Acid The product of conjugation of cholic acid with taurine. Its sodium salt is the chief ingredient of the bile of carnivorous animals. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as a cholagogue and cholerectic. Cholyltaurine,Taurine Cholate,Taurocholate,Sodium Taurocholate,Taurocholate Sodium,Taurocholic Acid, (5 alpha)-Isomer,Taurocholic Acid, (7 beta)-Isomer,Taurocholic Acid, Monolithium Salt,Taurocholic Acid, Monosodium Salt,Taurocholate, Sodium
D013778 Tetrazolium Salts Quaternary salts derived from tetrazoles. They are used in tests to distinguish between reducing sugars and simple aldehydes, for detection of dehydrogenase in tissues, cells, and bacteria, for determination of corticosteroids, and in color photography. (From Mall's Dictionary of Chemistry, 5th ed, p455) Tetrazolium Salt,Salt, Tetrazolium,Salts, Tetrazolium
D013844 Thiazoles Heterocyclic compounds where the ring system is composed of three CARBON atoms, a SULFUR and NITROGEN atoms. Thiazole
D017097 Electric Impedance The resistance to the flow of either alternating or direct electrical current. Bioelectrical Impedance,Electric Resistance,Impedance,Ohmic Resistance,Biolectric Impedance,Electrical Impedance,Electrical Resistance,Impedance, Bioelectrical,Impedance, Biolectric,Impedance, Electric,Impedance, Electrical,Ohmic Resistances,Resistance, Electric,Resistance, Electrical,Resistance, Ohmic,Resistances, Ohmic

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