Thiolated chitosan: Development and in vivo evaluation of an oral delivery system for leuprolide

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 80, Issue 1, 2012, Pages 95-102

  Iqbal, Javed ^a   Shahnaz, Gul ^a   Perera, Glen ^a   Hintzen, Fabian ^a   Sarti, Federica ^a   Bernkop Schnürch, Andreas ^a  

^a UNIVERSITY OF INNSBRUCK   (Austria)

Author keywords

Chitosan TGA; Leuprolide; Oral drug delivery; Thiomers; Tight junctions

Indexed keywords

CHITOSAN; GLUTATHIONE; LEUPRORELIN; SODIUM CHLORIDE; THIOGLYCOLIC ACID;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG PENETRATION; DRUG SCREENING; DRUG TRANSPORT; GEL; IN VIVO STUDY; INTESTINE MUCOSA; MALE; NONHUMAN; ORAL DRUG ADMINISTRATION; RAT; SPRAGUE DAWLEY RAT;

ADMINISTRATION, ORAL; ANIMALS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; CHITOSAN; DRUG DELIVERY SYSTEMS; GELS; GLUTATHIONE; INTESTINAL MUCOSA; INTESTINE, SMALL; LEUPROLIDE; MALE; PERMEABILITY; RATS; RATS, SPRAGUE-DAWLEY; RHEOLOGY; SWINE; THIOGLYCOLATES;

EID: 83955165899     PISSN: 09396411     EISSN: 18733441     Source Type: Journal    
DOI: 10.1016/j.ejpb.2011.09.010     Document Type: Article

References (25)

1. A. Adjei, S. Love, E. Johnson, U. Diaz, J. Greer, F. Haviv, and E. Bush Effect of formulation adjuvants on gastrointestinal absorption of leuprolide acetate J. Drug Target. 1 1993 251 258
2. M.F Lu, T, Reiland, Compositions and Method for the Sublingual or Buccal Administration of Therapeutic Agents, US Patent 5284,657, 1994.
3. F. Haviv, T.D. Fitzpatrick, C.J. Nichols, R.E. Swenson, E.N. Bush, G. Diaz, A. Nguyen, H.N. Nellans, D.J. Hoffman, H. Ghanbari, E.S. Johnson, S. Love, V. Cybulski, and J. Greer Stabilization of the N-terminal residues of LHRH agonists and the effect on pharmacokinetics J. Med. Chem. 35 1992 3890 3894
4. Y. Zheng, M.F. Lu, Y. Qiu, and L.T. Reiland Enzymatic degradation of leuprolide in rat intestinal mucosal homogenates Pharm. Dev. Technol. 4 1999 539 544 (Pubitemid 29536074)
5. A. Adjei, D. Sundberg, J. Miller, and A. Chun Bioavailability of leuprolide acetate following nasal and inhalation delivery to rats and healthy humans Pharm. Res. 9 1992 244 248
6. G. Guo, Q. Ping, G. Jiang, J. Dong, S. Qi, L. Feng, Z. Li, and C. Li Transport of leuprolide across rat intestine, rabbit intestine and Caco-2 cell monolayer Int. J. Pharm. 278 2004 415 422 (Pubitemid 38759513)
7. A. Bernkop-Schnürch, V. Schwarz, and S. Steininger Polymers with thiol groups: a new generation of mucoadhesive polymers? Pharm. Res. 16 1999 876 881 (Pubitemid 29284199)
8. M.D. Hornof, C.E. Kast, and A. Bernkop-Schnurch In vitro evaluation of the viscoelastic behavior of chitosan-thioglycolic acid conjugates Eur. J. Pharm. Biopharm. 55 2003 85 190
9. A. Bernkop-Schnürch Thiomers: a new generation of mucoadhesive polymers Adv. Drug Deliv. Rev. 57 2004 1569 1582
10. A. Bernkop-Schnürch, C.E. Kast, and D. Guggi Permeation enhancing polymers in oral delivery of hydrophilic macromolecules: thiomer/GSH systems J. Control. Release 93 2003 95 103 (Pubitemid 37421352)
11. A.E. Clausen, C.E. Kast, and A. Bernkop-Schnürch The role of glutathione in the permeation enhancing effect of thiolated polymers Pharm. Res. 19 2002 602 608 (Pubitemid 34553666)
12. C.E. Kast, and A. Bernkop-Schnürch Thiolated polymers - thiomers: development and in vitro evaluation of chitosan-thioglycolic acid conjugates Biomaterials 22 2001 2345 2352 (Pubitemid 32666227)
13. J. Hombach, T.F. Palmberger, and A. Bernkop-Schnürch Development and in vitro evaluation of a mucoadhesive vaginal delivery system for nystatin J. Pharm. Sci. 98 2008 555 564
14. A.E. Clausen, and A. Bernkop-Schnürch In vitro evaluation of the permeation-enhancing effect of thiolated polycarbophil J. Pharm. Sci. 89 2000 1253 1261
15. F. Föger, H. Hoyer, K. Kafedjiiski, M. Thaurer, and A. Bernkop-Schnürch In vivo comparison of various polymeric and low molecular mass inhibitors of intestinal P-glycoprotein Biomaterials 27 2006 5855 5860 (Pubitemid 44287029)
16. A. Vettrer, R. Martein, and A. Bernkop-Schnürch Thiolated polycarbophil as an adjuvant for permeation enhancement in nasal delivery of antisense oligonucleotides Pharm. Technol. 99 2010 1427 1439
17. Z.D. Sofianos, T. Karsila, N. Kostomitsopoulos, V. Balafas, J. Matsoukas, T. Tselios, and C. Tamvakopoulos In vivo evaluation and in vitro metabolism of leuprolide in mice - mass spectrometry-based biomarker measurement for efficacy and toxicity J. Mass. Spectrom. 43 2008 1381 1392
18. R. Fernandez-Urrusuna, D. Romani, P. Calvo, J.L. Vila-Jato, and M.J. Alonso Development of a freeze dried formulation of insulin-loaded chitosan nanoparticles intended for nasal administration STP Pharma. Sci. 5 1999 429 436
19. A. Bernkop-Schnürch, M. Hornof, and T. Zoidl Thiolated polymers-thiomers: synthesis and in vitro evaluation of chitosan-2-iminothiolane conjugates Int. J. Pharm. 260 2003 229 237 (Pubitemid 36773920)
20. C.E. Kast, C. Valenta, M. Leopold, and A. Bernkop-Schnürch Design and in vitro evaluation of a novel bioadhesive vaginal drug delivery system for clotrimazole J. Control. Release 81 2002 347 354 (Pubitemid 34607154)
21. W.C. Barrett, J.P. DeGnore, S. Konig, H.M. Fales, Y.F. Keng, Z.Y. Zhang, M.B. Yim, and P.B. Chock Regulation of PTP1B via glutathionylation of the active site cysteine 215 Biochemistry 38 1999 6699 6705
22. A. Bernkop-Schnürch, D. Guggi, and Y. Pinter Thiolated chitosans: development and in vivo evaluation of a mucoadhesive permeation-enhancing oral drug delivery system J. Control. Release 94 2004 177 186 (Pubitemid 37542387)
23. D. Guggi, N. Langoth, M. Hoffer, M. Wirth, and A. Bernkop-Schnürch Comparative evaluation of cytotoxicity of a glucosamine-TBA conjugate and chitosan-TBA conjugate Int. J. Pharm. 278 2004 353 360 (Pubitemid 38759508)
24. A. Bernkop-Schnürch, M.D. Hornof, C.E. Kast, and N. Langoth Thiolated polymers: stability of thiol moities under different storage conditions Sci. Pharm. 70 2002 331 339 (Pubitemid 36024994)
25. G.L. Plosker, and R.N. Brogden Leuprorelin: a review of its pharmacology and therapeutic use in prostatic cancer, endometriosis and other sex hormone-related disorders Drugs 48 1994 930 967