Transport of leuprolide across rat intestine, rabbit intestine and Caco-2 cell monolayer

International Journal of Pharmaceutics

Volumn 278, Issue 2, 2004, Pages 415-422

  Guo, J ^a   Ping, Q ^a   Jiang, G ^b   Dong, J ^a   Qi, S ^a   Feng, L ^a   Li, Z ^c   Li, C ^c  

^a CHINA PHARMACEUTICAL UNIVERSITY   (China)

^b BD Technologies   (United States)

^c NANJING NORMAL UNIVERSITY   (China)

Author keywords

Caco 2 cell; Chitosan; Everted gut sac technique; Leuprolide; Transport; Trypsin inhibitor

Indexed keywords

ALGINIC ACID; CHITOSAN; CHYMOTRYPSIN A; EDETIC ACID; LEUPRORELIN; PROTEINASE; TRYPSIN INHIBITOR;

ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CELL INTERACTION; CELL LINE; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DIFFUSION; DRUG EFFECT; DRUG TRANSPORT; ENZYME ACTIVITY; ENZYME DEGRADATION; HUMAN; HUMAN CELL; INTESTINE MUCOSA PERMEABILITY; MALE; NONHUMAN; PRIORITY JOURNAL; RABBIT; RAT; SPECIES; TECHNIQUE; TIGHT JUNCTION;

ALGINATES; ANIMALS; BIOLOGICAL TRANSPORT; CACO-2 CELLS; CHITIN; CHITOSAN; DRUG CARRIERS; EDETIC ACID; GLUCURONIC ACID; HEXURONIC ACIDS; HUMANS; JEJUNUM; LEUPROLIDE; MALE; PERMEABILITY; PHARMACEUTIC AIDS; RABBITS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, LHRH; SPECIES SPECIFICITY; TRYPSIN INHIBITORS;

EID: 2942579920     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2004.03.031     Document Type: Article

References (18)

1. Adjei A., Sundberg D., Miller J., Chun A. Bioavailability of leuprolide acetate following nasal and inhalation delivery to rats and healthy humans. Pharm. Res. 9:1992;244-248
2. Adjei A., Love S., Johnson E., Diaz U., Greer J., Haviv F., Bush E. Effect of formulation adjuvants on gastrointestinal absorption of leuprolide acetate. J. Drug Target. 1:1993;251-258
3. Barthe L., Woodley J., Houin G. Gastrointestinal absorption of drugs: methods and studies. Fundam. Clin. Pharmacol. 13:1999;154-168
4. + co-transport system in the Caco-2 human colon carcinoma cell line. Biochem. J. 299:1994;253-260
5. De Boer A., Noach A., Roosemalen M., Kurosaki Y., Breimer D. Effect of apical and/or basolateral application of EDTA on the permeability of hydrophilic compounds in a human intestinal epithelial cell line. Pharm. Res. 8:1991;S215
6. Fu lu M., Lee D., Rao G.S. Percutaneous absorption enhancement of leuprolide. Pharm. Res. 9:1992;1575-1579
7. Fu lu, M., Reiland, T., 1994. Compositions and method for the sublingual or buccal administration of therapeutic agents. US Patent 5,284,657.
8. Gan L., Hsyu P., Pritchard J., Thakker D. Mechanism of intestinal absorption of ranitidine and ondansetron: transport across Caco-2 cell monolayers. Pharm. Res. 10:1993;1722-1725
9. Haviv F., Fitzpatrick T.D., Nichols C.J., Swenson R.E., Bush E.N., Diaz G., Nguyen A., Nellans H.N., Hoffman D.J., Ghanbari H., Johnson E.S., Love S., Cybulski V., Greer J. Stabilization of the N-terminal residues of LHRH agonists and the effect on pharmacokinetics. J. Med. Chem. 35:1992;3890-3894
10. Hidalgo I.J., Borchardt R.T. Transport of a large neutral amino acid (phenylalanine) in a human intestinal epithelial cell line: Caco-2. Biochim. Biophys. Acta. 1028:1990;25-30
11. Kas H. Chitosan: properties, preparations and application to microparticulate systems. J. Microencap. 14:1997;689-711
12. Kotze A.F., Lueβen H.L., De B.J., Boer A.G., Verhoef J.C., Junginger H. Comparison of the effect of different chitosan salts and N-trimethylchitosan chloride on the permeability of intestinal epithelial cells (Caco-2). J. Control Relat. 51:1998;35-46
13. Milovic V., Faust D., Turchanowa L., Stein J., Caspary W.F. Permeability characteristics of polyamines across intestinal epithelium using the Caco-2 monolayer system: comparison between transepithelial flux and mitogen-stimulated uptake into epithelial cells. Nutrition. 17:2001;462-466
14. Noach A.B.J., Kurosaki Y., Blom-Roosemalen M.C.M., de Boer A.G., Breimer D.D. Cell-polarity dependent effect of chelation on the paracellular permeability of confluent Caco-2 cell monolayers. Int. J. Pharm. 90:1993;229-237
15. Qiu Y., Johnson H.W., Reiland T., Fu lu M. Sublingual absorption of leuprolide: comparison between human and animal models. Int. J. Pharm. 179:1999;27-36
16. Rowland R.N., Woodley J.F. The uptake of distearyphosphatidylcholine/ choolesterol liposomes by rat intestinal sac in vitro. Biochim. Biophys. Acta. 673:1981;399-406
17. Yamada K., Murakami M., Yamamoto A., Takada K., Muranishi S. Type hepatic uptake of liposomes in the rat. J. Pharm. Pharmacol. 44:1992;711-721
18. Zheng Y., Fu Lu M., Qiu Y., Reiland T. Enzymatic degradation of leuprolide in rat intestinal mucosal homogenates. Pharm. Dev. Technol. 4:1999;539-544