Development and in vivo evaluation of an oral insulin-PEG delivery system

European Journal of Pharmaceutical Sciences

Volumn 22, Issue 4, 2004, Pages 315-323

  Calceti, P ^a   Salmaso, S ^a   Walker, G ^b   Bernkop Schnurch A ^c  

^a UNIVERSITY OF PADOVA   (Italy)

^b UNIVERSITY OF MUNICH   (Germany)

^c UNIVERSITY OF INNSBRUCK   (Austria)

Author keywords

Insulin; Mucoadhesive tablets; Oral delivery; PEGylation; Thiolated polymers; Thiomers

Indexed keywords

BOVINE INSULIN; CARBONIC ACID; CYSTEINE; DRUG CARRIER; ELASTASE; GLUCOSE; INSULIN DERIVATIVE; MACROGOL; PEPSIN A; POLYACRYLIC ACID; POLYMER; PROTEIN; PROTEINASE;

ADHESION; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONJUGATE; CONTROLLED STUDY; DEPROTECTION REACTION; DIABETES MELLITUS; DRUG ACTIVITY; DRUG DEGRADATION; DRUG DELIVERY SYSTEM; DRUG PENETRATION; DRUG SCREENING; DRUG STABILITY; GLUCOSE BLOOD LEVEL; GUINEA PIG; IN VITRO STUDY; IN VIVO STUDY; INTESTINE ABSORPTION; INTESTINE MUCOSA; MALE; MOLECULAR WEIGHT; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN DEGRADATION; SUSTAINED RELEASE FORMULATION; TABLET FORMULATION;

ADMINISTRATION, ORAL; ANIMALS; BIOTRANSFORMATION; CATTLE; DIABETES MELLITUS, EXPERIMENTAL; DIABETES MELLITUS, TYPE 1; DRUG CARRIERS; DRUG STABILITY; FLUORESCEIN-5-ISOTHIOCYANATE; INJECTIONS, SUBCUTANEOUS; INSULIN; MICE; MICE, INBRED BALB C; MICE, INBRED NOD; POLYETHYLENE GLYCOLS;

EID: 2942534489     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2004.03.015     Document Type: Article

References (35)

1. Ashada H., Douen T., Mizokoshi Y., Fujita T., Murakami M., Yamamoto A., Muranishi S. Absorption characteristics of chemically modified insulin derivatives with various fatty acids in the small and large intestine. J. Pharm. Sci. 84:1995;682-687
2. Baudys M., Uchio T., Hovgaard L., Zhu E.F., Avramaoglou T., Jozefowics M., Rihova B., Park J.Y., Lee H.K., Kim S.W. Glycosilated insulins. J. Control. Release. 36:1995;151-157
3. Bernkop-Schnürch A. The use of inhibitory agents to overcome the enzymatic barrier to perorally administered therapeutic peptides and proteins. J. Control. Release. 52:1998;1-16
4. Bernkop-Schnürch A., Thaler S. Polycarbophil-cysteine conjugates as platforms for oral (poly)peptide delivery systems. J. Pharm. Sci. 89:2000;901-909
5. Bernkop-Schnürch A., Schwarz V., Steininger S. Polymers with thiol groups: a new generation of mucoadhesive polymers? Pharm. Res. 16:1999;876-881
6. Blundell T.L., Cutfield J.F., Cutfield S.M., Dodson E.J., Dodson G.G., Hodgkin D.C., Mercola D.A. Three-dimensional atomic structure of insulin and its relationship to activity. Diabetes. 21:1972;492-505
7. Caliceti P., Veronese F.M. Improvement of the physico-chemical and biopharmaceutical properties of insulin by poly(ethylene glycol) conjugation. STP Pharma Sci. 9:1999;107-113
8. Caliceti P., Veronese F.M. Pharmacokinetic and biodistribution properties of poly(ethylene glicol)-protein conjugates. Adv. Drug Deliv. Rev. 55:2003;1261-1277
9. Clausen A.E., Bernkop-Schnürch A. Thiolated Carboxymethylcellulose: in vitro evaluation of its permeation enhancing effect on peptide drugs. Eur. J. Parm. Biopharm. 51:2001;25-32
10. Clausen A.E., Kast C.E., Bernkop-Schnürch A. The role of glutathione in the permeation enhancing effect of thiolated polymers. Pharm. Res. 19:2002;602-608
11. Cleland J.L., Daugherty A., Mrsny R. Emerging protein delivery methods. Curr. Opin. Biotechnol. 12:2001;212-219
12. Damagè C., Vrankx H., Balsschmidt P., Couvreur P. Poly(alkyl cianoacrylate) nanospheres for oral administration of insulin. J. Pharm. Sci. 86:1997;1403-1409
13. Drews J. Strategic trends in drug industry. Drug Discovery Today. 8:2003;411-420
14. Gordon-Still J. Development of oral insulin: progress and current status. Diabetes Metab. Res. Rev. 18:2002;S29-S37
15. Habeeb A.F.S.A. Determination of free amino groups in proteins by trinitrobenzensulfonic acid. Anal. Biochem. 14:1966;328-336
16. Haupt S., Rubinstein A. The colon as a possible target for orally administered peptide and protein drugs. Crit. Rev. Ther. Drug Deliv. Syst. 19:2002;499-551
17. Hinds K.D., Kim S.W. Effects of PEG conjugation on insulin properties. Adv. Drug Deliv. Rev. 54:2002;505-530
18. Knauff M.J., Bell D.P., Hirtzer P., Luo Z.P., Young J.D., Kartre N.V. Relationship of effective molecular size to systemic clearance in rats of recombinant interleukin-2 chemically modified with water soluble polymers. J. Biol. Chem. 263:1988;15064-15070
19. Lee H.J. Protein drug oral delivery: the recent progress. Arch. Pharm. Res. 25:2002;572-584
20. Leitner V., Walker G.F., Bernkop-Schnürch A. Thiolated polymers: evidence for the formation of disulphide bonds with mucus glycoproteins. Eur. J. Pharm. Biopharm. 56:2003;207-214
21. Lowman A.M., Morishita M., Kajita M., Nagai T., Peppas N.A. Oral delivery of insulin using pH-responsive complexation gels. J. Pharm. Sci. 88:1999;933-937
22. Luessen H.L., Verhoef J.C., Borchard G., Lehr C.M., de Boer A.G., Junginger H.E. Mucoadhesive polymers in peroral peptide drug delivery. II. Carbomer and polycarbophil are potent inhibitors of the intestinal proteolytic enzyme trypsin. Pharm Res. 12:1995;1293-1298
23. Markussen J., Halstrom J., Wiberg F.C., Schaffer L. Immobilized insulin for high capacity affinity chromatography of insulin receptors. J. Biol. Chem. 266:1991;18814-18818
24. Marschütz M.K., Caliceti P., Bernkop-Schnörch A. Design and in vivo evaluation of an oral delivery system for insulin. Pharm. Res. 17:2000;1468-1474
25. Marschütz M.K., Bernkop-Schnürch A. Thiolated polymers: advance in mucoadhesion by use of in situ crosslinking poly(acrylic acid)-cysteine conjugates. Eur. J. Pharm. Sci. 15:2002;387-394
26. Ray N.K., Sharma C.P. Oral insulin - a perspective. J. Biomater. Appl. 17:2003;183-196
27. Sastry S.V., Nyshadham J.R., Fix J.A. Recent technological advances in oral drug delivery - a review. PSTT. 3:2000;138-145
28. Shein W.C. Oral peptide and protein delivery: unfulfilled promises? Drug Discovery Today. 8:2003;607-608
29. Sims G.E.C., Snape T.J. A method for estimation of poly(ethylene glycol) in plasma protein fractions. Anal. Biochem. 107:1980;60-63
30. Still J.G. Development of oral insulin: progress and current status. Diabetes Met. Res. Rev. 18:2002;S29-S37
31. Veronese F.M. Peptide and protein PEGylation: a review of problems and solutions. Biomaterials. 22:2001;405-417
32. Veronese F.M., Largajolli R., Boccù E., Benassi C.A., Schiavon O. Surface modification of protein: activation of monomethoxy-polyethylene-glycols by phenylchloroformates and modification of ribonuclease and superoxide dismutase. Appl. Biochem. Biotechnol. 11:1985;141-152
33. Veronese F.M., Monfardini C., Caliceti P., Schiavon O., Scrawen M.D., Beer D. Improvment of pharmacokinetic, immunological and stability properties of asparaginase by conjugation to linear and branched monomethoxypoly(ethylene glycol). J. Control. Release. 40:1996;199-209
34. Wissenschaftliche Tabellen Geigy, eighth ed., Basel, 1977.
35. Yeh, P.Y., Bentley, M.D., Clark, I.L., Kim, G., Smith, P.L., 2000. Intestinal transport of PEGylated small drug molecule, In: Proceedings of the 27th International Symposium on Contr. Rel. Bioact. Mater., Paris, France, pp. 59-60.