101
Views
6
CrossRef citations to date
0
Altmetric
Research Article

Protective Effect of Carbopol on Enzymatic Degradation of a Peptide-Like Substrate I: Effect of Various Concentrations and Grades of Carbopol and Other Reaction Variables on Trypsin Activity

, , &
Pages 89-96 | Received 06 Jun 2006, Accepted 05 Aug 2006, Published online: 07 Oct 2008

REFERENCES

  • Bernkop-Schnurch A., Gilge B. The use of inhibitory agents to overcome the enzymatic barrier to perorally administered therapeutic peptides and proteins. J. Control. Release. 1998; 52(1–2)1–16
  • Ohtani S., Shirasu K., Ogawara K., Higaki K., Kimura T. Evaluation of inhibitory activity of casein on proteases in rat intestine. Pharm. Res. 2003; 20(4)611–617
  • Foltz M., Meyer A., Theis S., Demuth H.U., Daniel H. A rapid in vitro screening for delivery of peptide-derived peptidase inhibitors as potential drug candidates via epithelial peptide transporters. J. Pharmacol. Exp. Ther. 2004; 310(2)695–702
  • Tolkatchev D., Vinogradova A., Ni F. Transforming bivalent ligands into retractable enzyme inhibitors through polypeptide-protein interactions. Bioorg. Med. Chem. Lett. 2005; 15(23)5120–5123
  • Krstic D., Krinulovic K., Vasic V. Inhibition of Na+/K(+)-ATPase and Mg(2+)-ATPase by metal ions and prevention and recovery of inhibited activities by chelators. J. Enzyme Inhib. Med. Chem. 2005; 20(5)469–476
  • Lorenzo M., Moldes D., Rodriguez Couto S., Sanroman M.A. Inhibition of laccase activity from Trametes versicolor by heavy metals and organic compounds. Chemosphere 2005; 60(8)1124–1128
  • Shah R.B., Palamakula A., Khan M.A. Cytotoxicity evaluation of enzyme inhibitors and absorption enhancers in Caco-2 cells for oral delivery of salmon calcitonin. J. Pharm. Sci. 2004; 93(4)1070–1082
  • Cascone M.G., Sim B., Downes S. Blends of synthetic and natural polymers as drug delivery systems for growth hormone. Biomaterials 1995; 16(7)569–574
  • Bernkop-Schnurch A., Walker G. Multifunctional matrices for oral peptide delivery. Crit. Rev. Ther. Drug Carrier Syst. 2001; 18(5)459–501
  • Guo J-H. Excipient update: Carbopol polymers for pharmaceutical drug delivery applications. Drug Delivery Technology. 2003; 32–36
  • Bulletin 4. Toxicology Studies. Noveon Inc., Cleveland, OH January, 2002; 1–22
  • 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. 1995; 12(9)1293–1298
  • Walker G.F., Ledger R., Tucker I.G. Carbomer inhibits tryptic proteolysis of luteinizing hormone-releasing hormone and N-alpha-benzoyl-L-arginine ethyl ester by binding the enzyme. Pharm. Res. 1999; 16(7)1074–1080
  • Wen J.Y., Ledger R., Butt A.G., McLeod B.J., Davies N.M., Tucker I.G. Inhibition of proteolysis in luminal extracts from the intestine of the brushtail possum. J. Pharm. Pharmacol. 2002; 54(10)1365–1372
  • Ameye D., Voorspoels J., Foreman P., Tsai J., Richardson P., Geresh S., Remon J.P. Trypsin inhibition, calcium and zinc ion binding of starch-g‐poly(acrylic acid) copolymers and starch/poly(acrylic acid) mixtures for peroral peptide drug delivery. J. Control. Release. 2001; 75(3)357–364
  • Foss A.C., Goto T., Morishita M., Peppas N.A. Development of acrylic-based copolymers for oral insulin delivery. Eur. J. Pharm. Biopharm. 2004; 57(2)163–169
  • Tamiya T., Okahashi N., Sakuma R., Aoyama T., Akahane T., Matsumoto J.J. Freeze denaturation of enzymes and its prevention with additives. Cryobiology 1985; 22(5)446–456
  • Bhatnagar B.S., Nehm S.J., Pikal M.J., Bogner R.H. Post-thaw aging affects activity of lactate dehydrogenase. J. Pharm. Sci. 2005; 94(6)1382–8
  • Bulletin 2. Product and Regulatory Guide. Noveon Inc., Cleveland, OH 2002; 1–9
  • Noveon Inc. Technical Data Sheet. Molecular Weight of Carbopol® and Pemulen® Polymers. Noveon Inc., Cleveland, OH 1999; 1–3
  • R.C. Rowe, P.J. Sheskey, P.J. WellerHandbook of Pharmaceutical Excipients 4th, . Pharmaceutical Press and the American Pharmaceutical Association, Washington, DC 2003
  • Patel M., Patel B., Patel R., Patel J., Bharadia P., Patel M. Carbopol: A versatile polymer. Drug Delivery Technology. 2006; 32–43
  • Morimoto K., Morisaka K., Kamada A. Enhancement of nasal absorption of insulin and calcitonin using polyacrylic acid gel. J. Pharm. Pharmacol. 1985; 37(2)134–136
  • Le Bourlais C.A., Chevanne F., Turlin B., Acar L., Zia H., Sado P.A., Needham T.E., Leverge R. Effect of cyclosporine A formulations on bovine corneal absorption: ex-vivo study. J. Microencapsul. 1997; 14(4)457–67
  • Morimoto K., Iwamoto T., Morisaka K. Possible mechanisms for the enhancement of rectal absorption of hydrophilic drugs and polypeptides by aqueous polyacrylic acid gel. J. Pharmacobiodyn. 1987; 10(2)85–91
  • Bulletin 3. Nomenclature and Chemistry. Noveon, Inc., Cleveland, OH 2002; 1–5
  • Copeland R.A. Enzymes: A Practical Introduction to Structure, Mechanism and Data Analysis 2nd. John Wiley and Sons, New York 2000
  • E.J. McNallyProtein Formulation and Delivery, . Marcel Dekker, Inc, Ridgefield, CT 2000
  • Ooya T., Eguchi M., Ozaki A., Yui N. Carboxyethylester-polyrotaxanes as a new calcium chelating polymer: synthesis, calcium binding and mechanism of trypsin inhibition. Int. J. Pharm. 2002; 242(1–2)47–54
  • Madsen F., Peppas N.A. Complexation graft copolymer networks: swelling properties, calcium binding and proteolytic enzyme inhibition. Biomaterials 1999; 20(18)1701–1708
  • Zhao H., Li J., Jiang L. Inhibition of HIV-1 TAR RNA-Tat peptide complexation using poly(acrylic acid). Biochem. Biophys. Res. Commun. 2004; 320(1)95–99

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.