Development and in vivo bioavailability study of an oral fondaparinux delivery system

European Journal of Pharmaceutical Sciences

Volumn 41, Issue 3-4, 2010, Pages 489-497

  Vetter, A ^a   Perera, G ^a   Leithner, K ^a   Klima, G ^b   Bernkop Schnurch A ^a  

^a UNIVERSITY OF INNSBRUCK   (Austria)

^b INNSBRUCK MEDICAL UNIVERSITY   (Austria)

Author keywords

Cytotoxicity; Fondaparinux; In vivo study; Permeation; Thiomers

Indexed keywords

DECANOIC ACID; FONDAPARINUX; GLUTATHIONE; POLYCARBOPHIL;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CYTOTOXICITY; DRUG ABSORPTION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; DRUG DESIGN; DRUG PENETRATION; DRUG RELEASE; DRUG SCREENING; DRUG TARGETING; DRUG UPTAKE; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; INTESTINE MUCOSA PERMEABILITY; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PRIORITY JOURNAL; RAT; SINGLE DRUG DOSE; SMALL INTESTINE; TABLET FORMULATION;

ADMINISTRATION, ORAL; ANIMALS; ANTICOAGULANTS; BIOLOGICAL AVAILABILITY; CACO-2 CELLS; CELL SURVIVAL; GELS; HUMANS; INTESTINE, SMALL; MALE; POLYSACCHARIDES; RATS; RATS, SPRAGUE-DAWLEY; VAGINAL CREAMS, FOAMS, AND JELLIES;

EID: 77957284759     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2010.08.001     Document Type: Article

References (31)

1. Anderberg E.K., Lindmark T., Artursson P. Sodium caprate elicits dilatations in human intestinal tight junctions and enhances drug absorption by the paracellular route. Pharm. Res. 1993, 10(6):857-864.
2. Asada H., Douen T., Waki M., Adachi S., Fujita T., Yamamoto A., Muranishi S. Absorption characteristics of chemically modified-insulin derivatives with various fatty acids in the small and large intestine. J. Pharm. Sci. 1995, 84:682-687.
3. Baluom M., Friedman M., Assaf P., Abdullah I.H.Y., Rubinstein A. Synchronized release of sulpiride and sodium decanoate from HPMC matrices: a rational approach to enhance sulpiride absorption in the rat intestine. Pharm. Res. 2000, 17(9):1071-1076.
4. Bernkop-Schnürch A., Krajicek M.E. Mucoadhesive polymers as platforms for oral peptide delivery and absorption: synthesis and evaluation of different chitosan-EDTA conjugates. J. Control. Release 1997, 50:215-223.
5. Bernkop-Schnürch A., Schwarz V., Steininger S. Polymers with thiol groups: a new generation of mucoadhesive polymers?. Pharm. Res. 1999, 16(6):876-881.
6. Bernkop-Schnürch A., Kast C.E., Guggi D. Permeation enhancing polymers in oral delivery of hydrophilic macromolecules: thiomer/GSH systems. J. Control. Release 2003, 93:95-103.
7. Blumenkrantz N., Asboe-Hansen G. New method for quantitative determination of uronic acids. Anal. Chem. 1973, 54:484-489.
8. Bounameaux H. The novel anticoagulants: entering a new era. Swiss Med. WKLY 2009, 139(5-6):60-64.
9. Cano-Cebrián M.J., Zornoza T., Granero L., Polache A. Intestinal absorption enhancement via the paracellular route by fatty acids, chitosans and others: a target for drug delivery. Curr. Drug Deliv. 2005, 2(1):9-22.
10. Chao A.C., Nguyen J.V., Broughall M., Griffin A., Fix J.A., Daddona P.E. In vitro and in vivo evaluation of effects of sodium caprate on enteral peptide absorption and on mucosal morphology. Int. J. Pharm. 1999, 191(1):15-24.
11. Charite, Berlin, 2010. Zentralinstitute für Laboratoriumsmedizin und Pathobiochemie.
12. Clausen A.E., Bernkop-Schnürch A. In vitro evaluation of the permeation enhancing effect of thiolated polycarbophil. J. Pharm. Sci. 2000, 89:1253-1261.
13. Ellman G.L. A colorimetric method for determining low concentrations of mercaptans. Arch. Biochem. Biophys. 1958, 74(2):443-450.
14. Grabovac V., Schmitz T., Föger F., Bernkop-Schnürch A. Papain: an effective permeation enhancer for orally administered low molecular weight heparin. Pharm. Res. 2007, 24(5):1001-1006.
15. Gum J.R., Hicks J.W., Toribara N.W., Rothe E.-M., Lagace R.E., Kim Y.S. The human MUC2 intestinal mucin has cysteine-rich subdomains located both upstream and downstream of its central repetitive region. J. Biol. Chem. 1992, 267:21375-21383.
16. Habeeb A.F. A sensitive method for localization of disulfide containing peptides in column effluents. Anal. Biochem. 1973, 56(1):60-65.
17. Kast C.E., Guggi D., Langoth N., Bernkop-Schnürch A. Development and in vivo evaluation of an oral delivery system for low molecular weight heparin based on thiolated polycarbophil. Pharm. Res. 2003, 20(6):931-936.
18. Kim S.K., Lee D.Y., Lee E., Lee Y.K., Kim C.Y., Moon H.T., Byun Y. Absorption study of deoxycholic acid-heparin conjugate as a new form of oral anti-coagulant. J. Control. Release 2007, 120(1-2):4-10.
19. Leitner V.M., Guggi D., Bernkop-Schnürch A. Thiomers in noninvasive polypeptide delivery: in vitro and in vivo characterization of a polycarbophil-cysteine/glutathione gelformulation for human growth hormone. J. Pharm. Sci. 2004, 93(7):1682-1691.
20. Leitner V.M., Walker G.F., Bernkop-Schnürch A. Thiolated polymers: Evidence fort he formation of disulphide bonds with mucus glycoproteins. Eur. J. Pharm. Biopharm. 2003, 56:207-214.
21. Lindmark T., Kimura Y., Artursson P. Absorption enhancement through intracellular regulation of tight junction permeability by medium chain fatty acids in Caco-2 cells. J. Pharmacol. Exp. Ther. 1998, 284(1):362-369.
22. Luessen H.L., Rentel C.O., Kotzé A.F., Lehr C.-M., de Boer A.G., Verhoef J.C., Junginger H.E. Mucoadhesive polymers in peroral peptide drug delivery. IV. Polycarbophil and chitosan are potent enhancers of peptide transport across intestinal mucosae in vitro. J. Control. Release 1997, 45:15-23.
23. Lutz K.L., Siahaan T.J. Molecular structure of the apical junction complex and its contribution to the paracellular barrier. J. Pharm. Sci. 1997, 86(9):977-984.
24. Maher S., Kennelly R., Bzik V.A., Baird A.W., Wang X., Winter D., Brayden D.J. Evaluation of intestinal absorption enhancement and local mucosal toxicity of two promoters. I. Studies in isolated rat and human colonic mucosae. Eur. J. Pharm. Sci. 2009, 38(4):291-300.
25. Masuda Y., Yoshikawa H., Takada K., Muranishi S. The mode of enhanced enteral absorption of macromolecules by lipid-surfactant mixed micelles I. J. Pharmacobio-Dyn. 1986, 9:793-798.
26. Motlekar N.A., Srivenugopal K.S., Wachtel M.S., Youan B.B. Oral delivery of low-molecular-weight heparin using sodium decanoate as absorption enhancer reaches therapeutic levels. J. Drug Target 2005, 13(10):573-583.
27. Motlekar N.A., Srivenugopal K.S., Wachtel M.S., Youan B.B. Evaluation of the oral bioavailability of low molecular weight heparin formulated with glycyrrhetinic acid as permeation enhancer. Drug Dev. Res. 2006, 67(2):166-174.
28. Muranishi S. Absorption enhancers. Crit. Rev. Ther. Drug. Carrier Syst. 1990, 7(1):1-33.
29. Riley R.G., Green K.L., Smart J.D., Tsibouklis J., Davis J.A., Hampson F., Dettmar P.W., Wilber W.R. The gastrointestinal transit profile of 14C-labelled poly(acrylic acids): an in vivo study. Biomaterials 2001, 22(13):1861-1867.
30. Schmitz T., Leitner V.M., Bernkop-Schnürch A. Oral heparin delivery: design and evaluation of a stomach-targeted mucoadhesive delivery system. J. Pharm. Sci. 2004, 94(5):966-973.
31. Tomita M., Sawada T., Ogawa T., Ouchi H., Hayashi M., Awazu S. Differences in the enhancing effects of sodium caprate on colonic and jejunal drug absorption. Pharm. Res. 1992, 9(5):648-653.