Oral delivery system for peptides and proteins: I. Approaches to improve oral bioavailability;Administração oral de peptídios e proteínas: I. Estratégias gerais para aumento da biodisponibilidade oral

Revista Brasileira de Ciencias Farmaceuticas/Brazilian Journal of Pharmaceutical Sciences

Volumn 38, Issue 2, 2002, Pages 125-140

  Silva, Catarina ^a   Ribeiro, António ^b   Ferreira, Domingos ^c   Veiga, Francisco ^a  

^a UNIVERSITY OF COIMBRA   (Portugal)

^b Inst Sup de Cie da Saude do Norte   (Portugal)

^c UNIVERSITY OF PORTO   (Portugal)

Author keywords

Absorption enhancer; Formulation; Microencapsulation; Peptide drugs; Protease inhibitors

Indexed keywords

AMINOPEPTIDASE P; AMINOPEPTIDASE W; CARBOXYPEPTIDASE A; CARBOXYPEPTIDASE B; CHYMOTRYPSIN; CYTOSOL AMINOPEPTIDASE; DIPEPTIDYL CARBOXYPEPTIDASE; DIPEPTIDYL PEPTIDASE; ELASTASE; GAMMA GLUTAMYLTRANSFERASE; GLUTAMYL AMINOPEPTIDASE; MICROSOMAL AMINOPEPTIDASE; PEPTIDE; POLYPEPTIDE; PROLINE CARBOXYPEPTIDASE; PROTEINASE; PROTEINASE INHIBITOR; TRYPSIN; UNCLASSIFIED DRUG;

CHEMICAL MODIFICATION; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG DISPOSITION; DRUG FORMULATION; DRUG METABOLISM; DRUG PENETRATION; DRUG STABILITY; ENZYMATIC DEGRADATION; MICROENCAPSULATION; REVIEW;

EID: 0036557792     PISSN: 15169332     EISSN: None     Source Type: Journal    
DOI: 10.1590/s1516-93322002000200002     Document Type: Review

References (77)

1. ADSON, A., RAUB, T. J., BURTON, P. S., BARSUHN, C. L., HILGERS, A. R. Quantitative approaches to delineate paracellular diffusion in cultured epithelial cell monolayers. J. Pharm. Sci., Washington, v. 83, p. 1529-1536, 1994.
2. AL ACHI, A., GREENWOOD, R. Erythrocytes as oral delivery systems for human insulin. Drug Dev. Ind. Pharm., New York, v. 24, p. 67-72, 1998.
3. ALLEMANN, E., LEROUX, J. C., GURNY, R. Polymeric nano- and microparticles for the oral delivery of peptides and peptidomimetics. Adv. Drug Deliv. Rev., Amsterdam, v. 34, p. 171-189, 1998.
4. ALPAR, H. O., EYLES, J. E., WILLIAMSON, E. D. Oral and nasal immunization with microencapsulated clinically relevant proteins. STP Pharma. Sci., Paris, v. 8, p. 31-39, 1998.
5. ANDERBERG, E. K., LINDMARK, T., ARTURSSON, P. Sodium caprate elicits dilatations in human intestinal tight junctions. Pharm. Res., Stuttgart, v. 10, p. 857-864, 1993.
6. ARTURSSON, P. Cell cultures as models for intestinal peptide transport. STP Pharma. Sci., Paris, v. 3, p. 5-10, 1993.
7. ARTURSSON, P., LINDMARK, T., DAVIS, S. S., ILLUM, L. Effect of chitosan on the permeability of monolayers of intestinal epithelial cells (Caco-2). Pharm. Res., Stuttgart, v. 11, p. 1358-1361, 1994.
8. BAI, J. P., CHANG, L. L., GUO, J. H. Effects of polyacrylic polymers on the lumenal proteolysis of peptide drugs in the colon. J. Pharm. Sci., Washington, v. 84, p. 1291-1294, 1995.
9. BERNKOP SCHNURCH, A., FRAGNER, R. Investigations into difusion behaviour of polypeptides in native intestinal mucus with regard to their peroral administration. Pharm. Sci., v. 2, p. 361, 1996.
10. BERNKOP-SCHNURCH, A. The use of inhibitory agents to overcome the enzymatic barrier to perorally administered therapeutic peptides and proteins. J. Control Release, Amsterdam, v. 52, p. 1-16, 1998.
11. BERNKOP-SCHNURCH, A., VALENTA, C., DAEE, S. M. Peroral polypeptide delivery. A comparative in vitro study of mucolytic agents. Arzneimittelforschung, Aulendorf, v. 49, p. 799-803, 1999.
12. BORCHARD, G., LUEBEN, H. L., DE BOER, A. G., VERHOEF, J. C., LEHR, C.-M., JUNGINGER, H. E. The potencial of mucoadhesive polymers in enhancing intestinal peptide drug absorption. III: Effects of chitosan-glutamate and carbomer on epithelial tight junctions in vitro. J. Controlled Release, Amsterdam, v. 39, p. 131-138, 1996.
13. BUNDGAARD, H. The utility of the prodrug approach to improve peptide absorption. J. Controlled Release, Amsterdam, v. 21, p. 63-72, 1992.
14. BURKE, P. A. Controlled release protein therapeutics: Effects of process and formulation on stability. In: WISE, D. L., ed. Handbook of pharmaceutical controlled release technology. New York: Marcel-Dekker, 2000. p. 661-692.
15. CARINO, G. P., MATHIOWITZ, E. Oral insulin delivery. Adv. Drug Deliv. Rev., Amsterdam, v. 35, p. 249-257, 1999.
16. CHEN, H., LANGER, R. Oral particulate delivery: status and future trends. Adv. Drug Deliv. Rev., Amsterdam, v. 34, p. 339-350, 1998.
17. CHEN, T. Formulation concerns of protein drugs. Drug Dev. Ind. Pharm., New York, v. 18, p. 1311-1354, 1992.
18. CHICKERING, D. E., JACOB, P., MATHIOWITZ, E. A tensile technique to evalute the interaction of bioadhesive microspheres with intestinal mucosa. Proc. Int. Symp. Control Release Bioact. Mater., v. 19, p. 88-89, 1992.
19. CHICKERING, D. E., MATHIOWITZ, E. Bioadhesive microspheres: I. A novel electrobalance-based method to study adhesive interactions between individual microspheres and intestinal mucosa. J. Controlled Release, Amsterdam, v. 34, p. 251-261, 1995.
20. COUVREUR, P., DUBERNET, C., PUISIEUX, F. Controlled drug delivery with nanoparticles: current possibilities and future trends. Eur J. Pharm. Biopharm., Stuttgart, v. 41, p. 2-13, 1995.
21. DESAI, M. P., LABHASETWAR, V., AMIDON, G. L., LEVY, R. J. Gastrointestinal uptake of biodegradable microparticles: effect of particle size. Pharm. Res., Stuttgart, v. 13, p. 1838-1844, 1996.
22. ELDRIDGE, J. H., HAMMOND, C. J., MEULBROEK, J. A., STAAS, J. K., GILLEY, R. M., TICE, T. R. Controlled vaccine in the gut-associated lymphoid tissues. I. Orally administered biodegradable microspheres target the payer's patches. J. Controlled Release, Amsterdam, v. 11, p. 205-214, 1990.
23. FIX, J. A. Oral controlled release technology for peptides: status and future prospects. Pharm. Res., Stuttgart, v. 13, p. 1760-1764, 1996a.
24. FIX, J. A. Strategies for delivery of peptides utilizing absorption-enhancing agents. J. Pharm. Sci., Washington, v. 85, p. 1282-1285, 1996b.
25. FLORENCE, A. T. The oral absorption of micro- and nanoparticulates: neither exceptional nor unusual. Pharm. Res., Stuttgart, v. 14, p. 259-266, 1997.
26. GEARY, R. S., SCHLAMEUS, H. W. Vancomycin and insulin used as models for oral delivery of peptides. J. Controlled Release, Amsterdam, v. 23, p. 65-74, 1993.
27. GOMBOTZ, W. R., WEE, S. F. Protein release from alginate matrices. Adv. Drug Deliv. Rev., Amsterdam, v. 31, p. 267-285, 1998.
28. HANDJANI-VILA, R. M., VANLERBERGHE, G. Les niosomes. In: BURI, P., PUISIEUX, F., DOELKER, E., BENOIT, J. P., eds. Formes pharmaceutiques nouvelles. Aspects technologique, biopharmaceutique & medical. Paris: Tecnique et documentation (Lavoisier), 1985. p. 561-575.
29. HAYAKAWA, E., LEE, V. H. L. Aminopeptidase activity in the jejunal and ileal Peyer's patches of the albino rabbit. Pharm. Res., Stuttgart, v. 9, p. 535-540, 1992.
30. HILGERS, A. R., CONRADI, R. A., BURTON, P. S. Caco-2 cell monolayers as a model for drug transport across the intestinal mucosa. Pharm. Res., Stuttgart, v. 7, p. 902-910, 1990.
31. HO, H. O., HSIAO, C. C., SHEU, M. T. Preparation of microemulsions using polyglycerol fatty acid esters as surfactant for the delivery of protein drugs. J. Pharm. Sci., Washington, v. 85, p. 138-143, 1996.
32. HOCHMAN, J., ARTURSSON, P. Mechanisms of absorption enhancement and tight junction regulation. J. Controlled Release, Amsterdam, v. 29, p. 253-267, 1994.
33. HOSNY, E. A., KHAN GHILZAI, N. M., AL NAJAR, T. A., ELMAZAR, M. M. Hypoglycemic effect of oral insulin in diabetic rabbits using pH-dependent coated capsules containing sodium salicylate without and with sodium cholate. Drug Dev. Ind. Pharm. New York, v. 24, p. 307-311, 1998.
34. IWANAGA, K., ONO, S., NARIOKA, K., MORIMOTO, K., KAKEMI, M., YAMASHITA, S., NANGO, M., OKU, N. Oral delivery of insulin by using surface coating liposomes: improvement of stability of insulin in GI tract. Int. J. Pharm., Amsterdam, v. 157, p. 73-80, 1997.
35. JULIANO, R. L. Microparticulate drug carriers: liposomes, microspheres, and cells. In: ROBINSON, J. R., LEE, V. H. L., eds. Controlled drug delivery. Fundamentals and applications. New York: Marcel-Dekker, 1987. p. 555-580.
36. KIMURA, T., SATO, K., SUGIMOTO, K., TAO, R., MURAKAMI, T., KUROSAKI, Y., NAKAYAMA, T. Oral administration of insulin as poly(vinyl alcohol)-gel spheres in diabetic rats. Biol. Pharm. Bull., Tokyo, v. 19, p. 897-900, 1996.
37. KOLAC, C., STREICHHAN, P., LEHR, C. M. Oral bioavailability of proteolytic enzymes. Eur. J. Pharm. Biopharm., Stuttgart, v. 42, p. 222-232, 1996.
38. LANGGUTH, P., BOHNER, V., HEIZMANN, J., MERKLE, H. P., WOLFFRAM, S., AMIDON, G. L., YAMASHITA, S. The challenge of proteolytic enzymes in intestinal peptide delivery. J. Controlled Release, Amsterdam, v. 46, p. 39-57, 1997.
39. LEE, V. H. L. Protease inhibitors and penetration enhancers as approaches to modify peptide absorption. J. Controlled Release, Amsterdam, v. 13, p. 213-223, 1990.
40. LEHR, C.-M. An estimate of turnover time of intestinal mucus gel layer in the rat in situ loop. Int. J. Pharm., Amsterdam, v. 70, p. 235-240, 1991.
41. LEHR, C.-M. Lectin-mediated drug delivery: the second generation of bioadhesives. J. Controlled Release, Amsterdam, v. 65, p. 19-29, 2000.
42. LEHR, C.-M., BOUWSTRA, J. A., SCHACHT, E. H., JUNGINGER, H. E. In vitro evaluation of mucoadhesive properties of chitosan and some other natural polymers. Int. J. Pharm., Amsterdam, v. 78, p. 43-48, 1992.
43. LENAERTS, V. Systems for the oral delivery of peptides Proc. Formulation of poorly-available drugs for oral administration. Paris, 1996. p. 59-65.
44. LIPKA, E., CRISON, J., AMIDON, G. L. Transmembrane transport of peptide type compounds: prospects for oral delivery. J. Controlled Release, Amsterdam, v. 39, p. 121-129, 1996.
45. LUEBEN, H. L., LEEUW, B. J., PÉRARD, D., LEHR, C.-M., DE BOER, A. G., VERHOEF, J. C., JUNGINGER, H. E. Mucoadhesive polymers in peroral peptide drug delivery. I. Influence of mucoadhesive excipients on the proteolytic activity of intestinal enzymes. Eur. J. Pharm. Sci., Amsterdam, v. 4, p. 117-128, 1996.
46. LUEBEN, H. L., LEHR, C.-M., RENTEL, C.-O., NOACH, A. B. J., DE BOER, A. G., VERHOEF, J. C., JUNGINGER, H. E. Bioadhesive polymers for the peroral delivery of peptide drugs. J. Control Release, Amsterdam, v. 29, p. 329-338, 1994.
47. LUEBEN, H. L., RENTEL, C.-O., KOTZE, A. F., LEHR, C.-M., DE BOER, A. G., VERHOEF, J. C., JUNGINGER, H. E. Mucoadhesive polymers in peroral peptide drug delivery. IV. Polycarbophil and chitosan are potent enhancers of peptide transport across intestinal mucosae in vitro. J. Controlled Release, Amsterdam, v. 45, p. 15-23, 1997.
48. MANNING, M. C., PATEL, K., BORCHARDT, R. T. Stability of protein pharmaceuticals. Pharm. Res., Stuttgart, v. 6, p. 903-918, 1989.
49. MATSUZAWA, A., MORISHITA, M., TAKAYAMA, K., NAGAI, T. Absorption of insulin using water-in-oil-in-water emulsion from an enteral loop in rats. Biol. Pharm. Bull., Tokyo, v. 18, p. 1718-1723, 1995.
50. MORISHITA, I., MORISHITA, M., TAKAYAMA, K., MACHIDA, Y., NAGAI, T. Hypoglycemic effect of novel oral microspheres of insulin with protease inhibitor in normal and diabetic rats. Int. J. Pharm., Amsterdam, v. 78, p. 9-16, 1992a.
51. MORISHITA, M., MORISHITA, I., TAKAYAMA, K., MACHIDA, Y., NAGAI, T. Novel oral microspheres of insulin with protease inhibitor protecting from enzymatic degradation. Int. J. Pharm., Amsterdam, v. 78, p. 1-7, 1992b.
52. OKADA, J., COHEN, S., LANGER, R. In vitro evaluation of polymerized liposomes as an oral drug delivery system. Pharm. Res., Stuttgart, v. 12, p. 576-582, 1995.
53. OKUMU, F. W., PAULETTI, G. M., VANDER VELDE, D. G., SIAHAAN, T. J., BORCHARDT, R. T. Effect of restrcited conformational flexibility on the permeation of model hexapeptides across Caco-2 cell monolayers. Pharm. Res., Stuttgart, v. 14, p. 169-175, 1997.
54. PAULETTI, G. M., GANGWAR, S., KNIPP, G. T., NERURKAR, M. M., OKUMU, F. W., TAMURA, K., SIAHAAN, T. J., BORCHARDT, R. T. Structural requirements for intestinal absorption of peptide drugs. J. Controlled Release, Amsterdam, v. 41, p. 3-17, 1996.
55. PAULETTI, G. M., OKUMU, F. W., BORCHARDT, R. T. Effect of size and charge on the passive diffusion of peptides across Caco-2 cell monolayers via the paracellular pathway. Pharm. Res., Stuttgart, v. 14, p. 164-168, 1997.
56. PUTNEY, S. D. Advances in protein drug delivery. Pharmaceutical News, v. 6, 1999.
57. ROUGE, N., DOELKER, E. Drug absorption sites in the gastrointestinal tract and dosage forms for site-specific delivery. Int. J. Pharm., Amsterdam, v. 136, p. 117-139, 1996.
58. RUBINSTEIN, A., TIROSH, B., BALUOM, M., NASSAR, T., FRIEDMAN, M., ET AL. Rationale for peptide drug delivery to the colon and the potential of polymeric carriers as effective tools. J. Controlled Release, Amsterdam, v. 46, p. 59-73, 1997.
59. SARCIAUX, J. M., ACAR, L., SADO, P. A. Using microemulsion formulations for oral drug delivery of therapeutic peptides. Int. J. Pharm., Amsterdam, v. 120, p. 127-136, 1995.
60. SCHILLING, R. J., MITRA, A. K. Intestinal mucosal transport of insulin. Int. J. Pharm., Amsterdam, v. 62, p. 53-64, 1990.
61. SHAH, D., SHEN, W. C. Transcellular delivery of an insulin-transferrin conjugate in enterocyte-like Caco-2 cells. J. Pharm. Sci., Washington, v. 85, p. 1306-1311, 1996.
62. SHAO, Z., LI, Y., CHERMAK, T., MITRA, A. K. Cyclodextrins as mucosal absorption promoters of insulin. Part 2. Effects of beta-cyclodextrin derivatives on alpha-chymotryptic degradation and enteral absorption of insulin in rats. Pharm. Res., Stuttgart, v. 11, p. 1174-1179, 1994.
63. SHAO, Z., LI, Y., KRISHNAMOORTHY, R., CHERMAK, T., MITRA, A. K. Differential effects of anionic, cationic, nonionic, and physiologic surfactants on the dissociation, alpha-chymotryptic degradation, and enteral absorption of insulin hexamers. Pharm. Res., Stuttgart, v. 10, p. 243-251, 1993.
64. SRIAMORNSAK, P. Investigation of pectin as a carrier for oral delivery of proteins using calcium pectinate gel beads. Int. J. Pharm., Amsterdam, v. 169, p. 213-220, 1998.
65. SUZUKI, A., MORISHITA, M., KAJITA, M., TAKAYAMA, K., ISOWA, K., CHIBA, Y., TOKIWA, S., NAGAI, T. Enhanced colonic and rectal absorption of insulin using a multiple emulsion containing eicosapentaenoic acid and docosahexaenoic acid. J. Pharm. Sci., Washington, v. 87, p. 1196-1202, 1998.
66. TAKEUCHI, H., YAMAMOTO, H., NIWA, T., HINO, T., KAWASHIMA, Y. Enteral absorption of insulin in rats from mucoadhesive chitosan-coated liposomes. Pharm. Res., Stuttgart, v. 13, p. 896-901, 1996.
67. TOMITA, M., SHIGA, M., HAYASHI, M., AWAZU, S. Enhancement of colonic drug absorption by the paracellular permeation route. Pharm. Res., Stuttgart, v. 5, p. 341-346, 1988.
68. TOUITOU, E., ALHAIQUE, F., FISHER, P., MEMOLI, A., RICCIERI, F. M., SANTUCCI, E. Prevention of molecular self-association by sodium salicylate: Effect on insulin and 6-carboxyfluorescein. J. Pharm. Sci., Washington, v. 76, p. 791-793, 1987.
69. TOZAKI, H., KOMOIKE, J., TADA, C., MARUYAMA, T., TERABE, A., SUZUKI, T., YAMAMOTO, A., MURANISHI, S. Chitosan capsules for colon-specific drug delivery: improvement of insulin absorption from the rat colon. J. Pharm. Sci., Washington, v. 86, p. 1016-1021, 1997.
70. TOZAKI, H., NISHIOKA, J., KOMOIKE, J., OKADA, N., FUJITA, T., MURANISHI, S., KIM, S. I., TERASHIMA, H., YAMAMOTO, A. Enhanced absorption of insulin and (Asu(1,7))eel-calcitonin using novel azopolymer-coated pellets for colon-specific drug delivery. J. Pharm. Sci., Washington, v. 90, p. 89-97, 2001.
71. TRENKTROG, T., MULLER, B. W., SEIFERT, J. In vitro-investigation into the enhancement of intestinal peptide absorption by emulsion systems. Eur. J. Pharm. Biopharm., Stuttgart, v. 41, p. 284-290, 1995.
72. UCHIYAMA, T., SUGIYAMA, T., QUAN, Y. S., KOTANI, A., OKADA, N., FUJITA, T., MURANISHI, S., YAMAMOTO, A. Enhanced permeability of insulin across the rat intestinal membrane by various absorption enhancers: their intestinal mucosal toxicity and absorption-enhancing mechanism of n-lauryl-beta-D-maltopyranoside. J. Pharm. Pharmacol., London, v. 51, p. 1241-1250, 1999.
73. WATSON, C. J., ROWLAND, M., WARHURST, G. Functional modeling of tight junctions in intestinal cell monolayers using polyethylene glycol oligomers. Am. J. Physiol. Cell Physiol., v. 281, p. C388-C397, 2001.
74. XIA, C. Q., WANG, J., SHEN, W. C. Hypoglycemic effect of insulin-transferrin conjugate in streptozotocin-induced diabetic rats. J. Pharmacol. Exp. Ther., Baltimore, v. 295, p. 594-600, 2000.
75. YOSHIDA, H., LEHR, C.-M., KOK, W., JUNGINGER, H. E., VERHOEF, J. C., BOUWSTRA, J. A. Niossomes for oral delivery of peptide drugs. J. Controlled Release, Amsterdam, v. 21, p. 145-154, 1992.
76. ZHOU, X. H. Overcoming enzymatic and absorption barriers to nonparenterally administered protein and peptide drugs. J. Controlled Release, Amsterdam, v. 29, p. 239-252, 1994.
77. ZHOU, X. H., LI WAN PO, A. Peptide and protein drugs: I. Therapeutic applications, absorption and parenteral administration. Int. J. Pharm., Amsterdam, v. 75, p. 97-115, 1991.