A novel suspension formulation enhances intestinal absorption of macromolecules via transient and reversible transport mechanisms

Pharmaceutical Research

Volumn 31, Issue 8, 2014, Pages 2010-2021

  Tuvia, Shmuel ^a   Pelled, Dori ^a   Marom, Karen ^a   Salama, Paul ^a   Levin Arama, Maya ^a   Karmeli, Irina ^a   Idelson, Gregory H ^a   Landau, Isaac ^a   Mamluk, Roni ^a  

^a NONE   (Israel)

Author keywords

absorption enhancer; intestinal permeability; oral drug delivery; sodium caprylate; tight junction

Indexed keywords

ENTERIC COATED TABLET; MACROMOLECULE; OCTREOTIDE;

ANIMAL; CHEMISTRY; DRUG EFFECTS; ENTERIC COATED TABLET; FEMALE; INTESTINE ABSORPTION; MACACA FASCICULARIS; MACROMOLECULE; MALE; MEDICINAL CHEMISTRY; METABOLISM; PHARMACOLOGY; PHYSIOLOGY; PROCEDURES; RAT; SPRAGUE DAWLEY RAT; TRANSPORT AT THE CELLULAR LEVEL;

ANIMALS; BIOLOGICAL TRANSPORT; CHEMISTRY, PHARMACEUTICAL; FEMALE; INTESTINAL ABSORPTION; MACACA FASCICULARIS; MACROMOLECULAR SUBSTANCES; MALE; OCTREOTIDE; RATS; RATS, SPRAGUE-DAWLEY; TABLETS, ENTERIC-COATED;

EID: 84893944910     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-014-1303-9     Document Type: Article

References (38)

1. Mahato RI, Narang AS, Thoma L, Miller DD. Emerging trends in oral delivery of peptide and protein drugs. Crit Rev Ther Drug Carrier Syst. 2003;20:153-214.
2. Song H, Johns R, Griesgraber GW, Wagner CR, Zimmerman CL. Disposition and oral bioavailability in rats of an antiviral and antitumor amino acid phosphoramidate prodrug of AZT-monophosphate. Pharm Res. 2003;20:448-51.
3. Maher S, Brayden D. Overcoming poor permeability: translating permeation enhancers for oral peptide delivery. Drug Discov Today Technol. 2012;9:e113-9.
4. Hayashiand M, Tomita M. Mechanistic analysis for drug permeation through intestinal membrane. Drug Metab Pharmacokinet. 2007;22:67-77.
5. Salama NN, Eddington ND, Fasano A. Tight junction modulation and its relationship to drug delivery. Adv Drug Deliv Rev. 2006;58:15-28.
6. Tsukita S, Furuse M, Itoh M. Multifunctional strands in tight junctions. Nat Rev Mol Cell Biol. 2001;2:285-93.
7. Ulluwishewa D, Anderson RC, McNabb WC, Moughan PJ, Wells JM, Roy NC. Regulation of tight junction permeability by intestinal bacteria and dietary components. J Nutr. 2011;141:769-76.
8. Kwan KC. Oral bioavailability and first-pass effects. Drug Metab Dispos. 1997;25:1329-36.
9. Kosińska A, Andlauer W. Modulation of tight junction integrity by food components. Food Res Int. 2013;54:951-60.
10. Maher S, Leonard TW, Jacobsen J, Brayden DJ. Safety and efficacy of sodium caprate in promoting oral drug absorption: from in vitro to the clinic. Adv Drug Deliv Rev. 2009;61:1427-49.
11. Sawada T, Ogawa T, Tomita M, Hayashi M, Awazu S. Role of paracellular pathway in nonelectrolyte permeation across rat colon epithelium enhanced by sodium caprate and sodium caprylate. Pharm Res. 1991;8:1365-71.
12. Sharma P, Varma MV, Chawla HP, Panchagnula R. Absorption enhancement, mechanistic and toxicity studies of medium chain fatty acids, cyclodextrins and bile salts as peroral absorption enhancers. Farmaco. 2005;60:884-93.
13. Willmann S, Schmitt W, Keldenich J, Dressman JB. A physiologic model for simulating gastrointestinal flow and drug absorption in rats. Pharm Res. 2003;20:1766-71.
14. Cano-Cebrian MJ, 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;2:9-22.
15. Weckbecker G, Lewis I, Albert R, Schmid HA, Hoyer D, Bruns C. Opportunities in somatostatin research: biological, chemical and therapeutic aspects. Nat Rev Drug Discov. 2003;2:999-1017.
16. Uchidaand M, Shimizu K. 13C-acetic acid is more sensitive than 13C-octanoic acid for evaluating gastric emptying of liquid enteral nutrient formula by breath test in conscious rats. Biol Pharm Bull. 2007;30:487-9.
17. Salama P, Mamluk R, Marom K, Weinstein I, Tzabari M. Pharmaceutical compositions and related methods of delivery, US 2012/0093886 A1, 2012.
18. Tuvia S, Atsmon J, Teichman SL, Katz S, Salama P, Pelled D, et al. Oral octreotide absorption in human subjects: comparable pharmacokinetics to parenteral octreotide and effective growth hormone suppression. J Clin Endocrinol Metab. 2012;97:2362-9.
19. Bevan JS. Clinical review: the antitumoral effects of somatostatin analog therapy in acromegaly. J Clin Endocrinol Metab. 2005;90:1856-63.
20. Fricker G, Drewe J, Vonderscher J, Kissel T, Beglinger C. Enteral absorption of octreotide. Br J Pharmacol. 1992;105:783-6.
21. Chen C, Wang P, Su Q, Wang S, Wang F. Myosin light chain kinase mediates intestinal barrier disruption following burn injury. PloS One. 2012;7:e34946.
22. Shen L, Weber CR, Raleigh DR, Yu D, Turner JR. Tight junction pore and leak pathways: a dynamic duo. Annu Rev Physiol. 2011;73:283-309.
23. Lindmark T, Soderholm JD, Olaison G, Alvan G, Ocklind G, Artursson P. Mechanism of absorption enhancement in humans after rectal administration of ampicillin in suppositories containing sodium caprate. Pharm Res. 1997;14:930-5.
24. Anderberg EK, Lindmark T, Artursson P. Sodium caprate elicits dilatations in human intestinal tight junctions and enhances drug absorption by the paracellular route. Pharm Res. 1993;10:857-64.
25. Suzukiand T, Hara H. Difructose anhydride III and sodium caprate activate paracellular transport via different intracellular events in Caco-2 cells. Life Sci. 2006;79:401-10.
26. Kimura Y, Hosoda Y, Yamaguchi M, Nagano H, Shima M, Adachi S, et al. Effects of medium-chain fatty acids on intracellular calcium levels and the cytoskeleton in human intestinal (Caco-2) cell monolayers. Biosci Biotechnol Biochem. 2001;65:743-51.
27. Kurasawa M, Kuroda S, Kida N, Murata M, Oba A, Yamamoto T, et al. Regulation of tight junction permeability by sodium caprate in human keratinocytes and reconstructed epidermis. Biochem Biophys Res Commun. 2009;381:171-5.
28. Mehvarand R, Shepard TL. Molecular-weight-dependent pharmacokinetics of fluorescein-labeled dextrans in rats. J Pharm Sci. 1992;81:908-12.
29. Swindle MM, Makin A, Herron AJ, Clubb Jr FJ, Frazier KS. Swine as models in biomedical research and toxicology testing. Vet Pathol. 2012;49:344-56.
30. Turner JR. Intestinal mucosal barrier function in health and disease. Nat Rev Immunol. 2009;9:799-809.
31. Su L, Shen L, Clayburgh DR, Nalle SC, Sullivan EA, Meddings JB, et al. Targeted epithelial tight junction dysfunction causes immune activation and contributes to development of experimental colitis. Gastroenterology. 2009;136:551-63.
32. Laukoetter MG, Nava P, Lee WY, Severson EA, Capaldo CT, Babbin BA, et al. JAM-A regulates permeability and inflammation in the intestine in vivo. J Exp Med. 2007;204:3067-76.
33. Drewe J, Fricker G, Vonderscher J, Beglinger C. Enteral absorption of octreotide: absorption enhancement by polyoxyethylene-24-cholesterol ether. Br J Pharmacol. 1993;108:298-303.
34. Fricker G, Drewe J. Enteral absorption of octreotide: modulation of intestinal permeability by distinct carbohydrates. J Pharmacol Exp Ther. 1995;274:826-32.
35. Fricker G, Fahr A, Beglinger C, Kissel T, Reiter G, Drewe J. Permeation enhancement of octreotide by specific bile salts in rats and human subjects: in vitro, in vivo correlations. Br J Pharmacol. 1996;117:217-23.
36. Michael S, Thole M, Dillmann R, Fahr A, Drewe J, Fricker G. Improvement of intestinal peptide absorption by a synthetic bile acid derivative, cholylsarcosine. Eur J Pharm Sci Off J Eur Fed Pharm Sci. 2000;10:133-40.
37. Thanou M, Verhoef JC, Marbach P, Junginger HE. Intestinal absorption of octreotide: N-trimethyl chitosan chloride (TMC) ameliorates the permeability and absorption properties of the somatostatin analogue in vitro and in vivo. J Pharm Sci. 2000;89:951-7.
38. Melmed S. Acromegaly pathogenesis and treatment. J Clin Invest. 2009;119:3189-202.