The lung as a route for systemic delivery of therapeutic proteins and peptides

Remigius U. Agu1, Michael Ikechukwu Ugwoke2, Michoel Armand1, Renaat Kinget1, Norbert Verbeke1
1Laboratorium voor Farmacotechnologie en Biofarmacie, KU Leuven, Leuven, Belgium
2Octoplus Pharmaceutical Development, Leiden, The Netherlands

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Wearley LL: Recent progress in protein and peptide delivery by non-invasive routes. Crit Rev Ther Drug Carrier Syst. 1991, 8: 1331-1394.

Wilson CG, Washington N: Physiological Pharmaceutics. England: John Wiley;. 1989

Banga AK: Therapeutic Peptides and Proteins: Formulation, Processing and Delivery Systems. Lancaster: Technomic;. 1995

Weibel ER: Morphometry of the Human Lung. Berlin: Springer Verlag;. 1963

Chrystyn H: Is total particle dose more important than particle distribution. Respir Med. 1997, 91(suppl): 17-19.

Gupta S, Moussy F, Dalby RN, Meikka SI, Bruley DF: Pulmonary delivery of human protein C and factor IX. In: Textbook of Advances in Experimental Medicine and Biology or Oxygen Transport to Tissue, vol 411. Edited by Nemoto EM, LaManna J. New York: Plenum Press;. 1997, 429-435.

Engel T, Heinig JH, Malling HJ, Scharling B, Nikander K, Madsen F: Clinical comparison of inhaled busesonide delivered either via pressurized metered dose inhaler or Turbuhaler®. Allergy. 1989, 44: 220-225.

Nielsen KG, Skov M, Klug B, Ifversen M, Bisgaard H: Flow-dependent effect of formoterol dry powder inhaled from the Aerolizer®. Eur Respir J. 1997, 10: 2105-2109.

Niven RW: Delivery of biotherapeutics by inhalation aerosol. Crit Rev Ther Drug Carrier Syst. 1995, 12: 151-231.

Sayani AP, Chien YW: Systemic delivery of peptides and proteins across absorptive mucosae. Crit Rev Ther Drug Carrier Syst. 1996, 13: 85-184.

Zhou XH: Overcoming enzymatic and absorption barriers to non-parenterally administered protein and peptide drugs. J Contr Rel. 1994, 29: 239-252.

Liu FY, Kildsig DO, Mitra AK: Pulmonary biotransformation of insulin in rat and rabbit. Life Sci. 1992, 51: 1683-1689.

Shen Z, Zhang Q, Wei S, Nagai T: Proteolytic enzymes as a limitation for pulmonary absorption of insulin: in vitro and in vivo investigations. Int J Pharm. 1999, 192: 115-121.

Fukuda F, Tsuji T, Fujita T, Yamamoto A, Muranishi S: Susceptibility of insulin to proteolysis in rat lung homogenates and its protection from proteolysis by various protease inhibitors. Biol Pharm Bull. 1995, 18: 891-894.

Wigley FM, Londono JH, Wood SH, Shipp JC, Waldman RH: Insulin across respiratory mucosa by aerosol delivery. Diabetes. 1971, 20: 552-556.

Colthorpe P, Farr SJ, Taylor G, Smith IJ, Wyatt D: The pharmacokinetics of pulmonary-delivered insulin: a comparison of intratracheal and aerosol administration to the rabbit. Pharm Res. 1992, 9: 764-768.

Okumura k, Iwaka S, Tsuguchika Y, Toshimitsu S, Komada F: Intratracheal delivery of insulin absorption from solution and aerosol by rat lung. Int J Pharm. 1992, 88: 63-73.

Sakr FM: A new approach for insulin delivery via the pulmonary route: design and pharmacokinetics in non-diabetics rabbits. Int J Pharm. 1992, 86: 1-7.

Jendle JH, Karlberg BE, Arborelius M: An exploration of intrapulmonary insulin administration in anaesthetized and mechanically ventilated pigs. Scand J Clin Lab Invest. 1996, 56: 251-258.

Gansslen M: About inhalation of insulin [abstract; in German]. Klin Wochenschr. 1925, 4: 71-

Jendle JH, Karlberg BE: Intrapulmonary administration of insulin to healthy volunteers. J Intern Med. 1996, 240: 93-98.

Laube BL, Georgopoulos A, Adams GK: Preliminary study of the efficiency of insulin aerosol delivered by oral inhalation in diabetic patients. JAMA. 1993, 269: 2106-2109.

Laube BL, Benedict GW, Dobs AS: The lung as an alternative route of delivery for insulin in controlling postprandial glucose levels in patients with diabetes. Chest. 1998, 114: 1734-1739.

Laube BL, Benedict GW, Dobs AS: Time to peak insulin level, relative bioavailability, and effect of site of deposition of nebulized insulin in patients with noninsulin-dependent diabetes mellitus. J Aerosol Med. 1998, 11: 153-173.

Pfützner A, Heise T, Steiner S, Heinemann L, Rave K: Inhaled technosphere: insulin shows a low variability in metabolic action in type 2 diabetic patients [abstract]. Diabetes. 2000, 49 (suppl): A121-

Rave KM, Heise T, Pfützner A, Steiner S, Heinemann L: Results of a dose-response study with a new insulin inhaler formulation [abstract]. Diabetes. 2000, 49(suppl): A75-

Elliot RB, Edgar BW, Pitcher CC, Quested C, McMaster J: Parenteral absorption of insulin from the lung in diabetic children. Aust Paediatr J. 1987, 23: 293-297.

Gelfand AG, Schwartz SL, Horton M, Law CG, Pun EF: Pharmacological reproducibility of inhaled human insulin pre-meal dosing in patients with type 2 diabetes mellitus (NIDDM) [abstract]. Diabetes. 1998, 47(suppl): A99-

Skyler JS, Gelfand RA, Kourides IA: Treatment of type 1 diabetes mellitus with inhaled human insulin: a 3-month, multicenter trial [abstract]. Diabetes. 1998, 47(suppl): A61-

Cefalu WT, Gelfand RA, Kourides I: Treatment of type 2 diabetes mellitus with inhaled human insulin: a 3-month, multicenter trial [abstract]. Diabetes. 1998, 47(suppl): A61-

Cappelleri JC, Gerber RA, Bell-farrow AD, English JS, Agramonte RF, Kourides IA: Improved patient satisfaction with inhaled insulin in subjects with type 2 diabetes mellitus: results from a multicenter randomized controlled trial [abstract]. Diabetes. 2000, 49(suppl): A100-

Gerber RA, Cappelleri JC, Bell-farrow AD, English JS, Agramonte RF, Gelfand RA: Improved patient satisfaction with inhaled insulin in subjects with type 1 diabetes mellitus after one year: results from a multicenter extension trial [abstract]. Diabetes. 2000, 49(suppl): A108-

Cefalu WT, Balagtas CC, Landschulz WH, Gelfand RA: Sustained efficacy and pulmonary safety of inhaled insulin during two years of outpatient therapy [abstract]. Diabetes. 2000, 49 (suppl): A101-

Farr S, McElduff A, Ward E, Okumu F, Mather L, Gonda I, Rubsamen R: A comparison of the pharmacokinetics and pharmacodynamics of inhaled insulin administered as different strength solutions to healthy volunteers [abstract]. Diabetes. 1998, 47(suppl): A61-

Farr S, McElduff A, Ward E, Okikawa J, Lloyd P, Schuster J, Mather L, Gonda I: The mode of inhalation influences the pharmacokinetics and pharmacodynamics of pulmonary delivered insulin in healthy fasted volunteers [abstract]. Pharm Res. 1997, 14(suppl): S136-

Kipnes M, Otulana B, Clauson P, Fischer J, Farr S, Hatorp V, Schwartz S: A comparison of the pharmacodynamic effects of inhaled insulin versus subcutaneous insulin in type 1 diabetic patients [abstract]. Diabetes. 1999, 48(suppl): A95-

Brunner GA, Balent B, Sendlhofer G, Ellmerer M, Schaupp L, Jendle JH, Kristensen A, Okikawa J, Pieber TR: Pharmacokinetics and pharmcodynamics of inhaled versus subcutaneous insulin in subjects with type 1 diabetes: a glucose clamp study [abstract]. Diabetes. 2000, 49(suppl): A76-

Weiss SR, Berger S, Cheng S, Kourides I, Landschulz WH, Gelfand R: Adjunctive therapy with inhaled human insulin in type 2 diabetic patients failing oral agents: a multicenter phase II trial [abstract]. Diabetes. 1999, 48(suppl): A12-

Patton JS, Trinchero P, Platz RM: Bioavailability of pulmonary delivered peptides and proteins: α-interferon, calcitonins and parathyroid hormone. J Contr Rel. 1994, 28: 79-85.

Komada F, Iwakawa S, Yamamoto N, Sakakibara H, Okumura K: Intratracheal delivery of peptide and protein agents: absorption from solution and dry powder by rat lung. J Pharm Sci. 1994, 83: 863-867.

Folkesson HG, Hedin L, Westrom BR, Pierzynowski SG, Karlsson BW: Lung to blood passage of human growth hormone after intratracheal instillation: stimulation of growth in hypophysectomized rats. J Endocrinol. 1992, 134: 197-203.

Colthorpe P, Farr SJ, Smith IJ, Wyatt D, Taylor G: The influence of regional deposition on the pharmacokinetics of pulmonary-delivered human growth hormone in rabbits. Pharm Res. 1995, 12: 356-359.

Shao Z, Li Y, Mitra AK: Cyclodextrins as mucosal absorption promoters of insulin III: pulmonary route of delivery. Eur J Pharm Biopharm. 1994, 40: 283-288.

Shen Z, Cheny Y, Zhang Q: Lanthanides enhance pulmonary absorption of insulin. Biol Trace Element Res. 2000, 75: 215-225.

Heinemann L, Klappoth W, Rave K, Hompesch B, Linkeschowa R, Heis T: Intra-individual variability of metabolic effect of inhaled insulin together with an absorption enhancer. Diabetes Care. 2000, 23: 1343-1347.

Kobayashi S, Kondo S, Juni K: Study of pulmonary delivery of salmon calcitonin in rats: effects of protease inhibitors and absorption enhancers. Pharm Res. 1994, 11: 1239-1243.

Morita T, Yamamoto A, Takakura Y, Hashida M, Sekaki H: Improvement of pulmonary absorption of (ASU1,7)-Eel calci-tonin by various protease inhibitors in rats. Pharm Res. 1994, 11: 909-913.

Yamamoto A, Okumura S, Fukuda Y, Fukui M, Takahashi K, Muran-ishi S: Improvement of the pulmonary absorption of (ASU1,7)-Eel calcitonin by various absorption enhancers and their pulmonary toxicity in rats. J Pharm Sci. 1997, 86: 1144-1147.

Edwards DA, Hanes J, Caponetti G, Hrkach J, Ben-Jebria A, Eskew ML, Mintzes J, Deaver D, Lotan N, Langer R: Large porous particles for pulmonary drug delivery. Science. 1997, 276: 1868-1871.

Kawashima Y, Yamamoto H, Takeuchi H, Fujoka S, Hino T: Pulmonary delivery of insulin with nebulized DL-lactide/glycolide copolymer (PLGA) nanosphere to prolong hypoglycemic effect. J Contr Rel. 1999, 62: 279-287.

Liu F, Shao Z, Kildsig DO, Mitra AK: Pulmonary delivery of free and liposomal insulin. Pharm Res. 1993, 10: 228-232.

Li Y, Mitra AK: Effect of phospholipid chain length, concentration, charge, and vesicle size on pulmonary insulin absorption. Pharm Res. 1996, 13: 76-79.

Smith PL, Yeulet SE, Citerone DR, Drake F, Cook K, Wall DA, Marcello J: SK&F 110679: comparison of absorption following oral or respiratory administration. J Contr Rel. 1994, 28: 67-77.

Ajei A, Garren J: Pulmonary delivery of peptide drugs: effect of particle size on bioavailability of leuprolide acetate in healthy voluteers. Pharm Res. 1990, 7: 565-569.

Adjei A, Johnson E, Doyle R, Sims K: Formulations of a non-apeptide: in vitro and in vivo studies [abstract]. J Pharm Sci. 1987, 76(suppl): PS47-

Adjei A, Hui J, Finley R, Lin T, Lancaster J, Fort F: Pulmonary bioavailability of leuprolide acetate following multiple dosing to beagle dogs: some pharmacokinetic and clinical issues. Int J Pharm. 1994, 107: 57-66.

Bennett DB, Tyson E, Nuremberg CA, Mah S, De Groot JS, Teitelbaum Z: Pulmonary delivery of detirelix by intratracheal instillation and aerosol inhalation in briefly anesthetized dog. Pharm Res. 1994, 11: 1048-1055.

Schreier H, McNicol KJ, Bennette DB, Teitelbaum Z, Derendorf H: Pharmacokinetics of detirelix following intratracheal instillation and aerosol inhalation in the unanesthethized awake sheep. Pharm Res. 1994, 11: 1056-1059.

Lizio R, Klenner T, Borchard G, Romeis P, Sarlikiotis AW, Reissmann T, Lehr C: Systemic delivery of the GnRH antagonist cetrorelix by intratracheal instillation in anesthetized rat. Eur J Pharm Sci. 2000, 9: 253-258.

Folkesson HG, Westrom BR, Karlsson BW: Permeability of the respiratory tract to different sized macromolecules after intratracheal instillation in young and adult rats. Acta Physiol Scand. 1990, 139: 347-354.

Folkesson HG, Westrom BR, Pierzynowski SG, Svendsen J, Karlsson BW: Lung to blood passage of albumin and a nonapeptide after intratracheal instillation in the young developing pig. Acta Physiol Scand. 1993, 147: 173-178.

Bot AI, Tarara TE, Smith DJ, Bot SR, Woods CM, Weers JG: Novel lipid-based hollow-porous microparticles as a platform for immunoglobulin delivery to the respiratory tract. Pharm Res. 2000, 17: 275-283.

Hänninen A, Harisson LC: γδ T cells as mediators of mucosal tolerance: the autoimmune diabetes model. Immunol Rev. 2000, 173: 109-119.

Harrison LC, Dempsey-Collier , Kramer DR, Takahashi K: Aerosol insulin induces regulatory CD8 γδ T cells that prevent murine insulin-dependent diabetes. J Exp Med. 1996, 184: 2167-2174.

Altrock BW, Fagin KD, Hockman HR, Fish EN, Goldstein L, Chang D, Duker K, Stebbing N: Antiviral and antitumor effects of human interferon analog, IFN-α Con1, assessed in hamsters. J Interferon Res. 1986, 6: 405-415.

Niven RW, Whitcomb KL, Woodwards M, Liu J, Jornacion C: Systemic absorption and activity of recombinant consensus interferons after intratracheal intillation and aerosol administration. Pharm Res. 1995, 12: 1889-1895.

Niven RW, Lott FD, Cribbs JM: Pulmonary absorption of recombinant methionyl human granulocyte colony stimulating factor (r-huG-CSF) after intratracheal instillation to the hamster. Pharm Res. 1993, 10: 1604-1610.

Niven RW, Lott FD, Ip AY, Cribbs JM: Pulmonary delivery of powders and solutions containing granulocyte colony-stimulating factor (r-huG-CSF) to the rabbit. Pharm Res. 1994, 11: 1101-1109.

Taljanski W, Pierzynowki SG, Lundin PD, Westrom BR, Eirefelt S, Podlesny J, Dahlback M, Siwinska-Golebiowska H, Karlsson BW: Pulmonary delivery of intratracheally instilled and aerosolized cyclosporin A to young and adult rats. Drug Metab Dis. 1997, 25: 917-920.

Niven RW, Whitcomb KL, Shaner LD, Ralph LD, Habberfield AD, Wilson JV: Pulmonary absorption of polyethylene glycolated recombinant human granulocyte colony stimulating factor (PEGr-huG-CSF). J Contr Rel. 1994, 32: 177-189.

Wolff RK: Safety of inhaled proteins for therapeutic use. J Aerosol Med. 1998, 11: 197-219.

Myers MA, Thomas DA, Straub L, Soucy DW, Niven RW, Kaltenback M, Hood CI: Pulmonary effect of chronic exposure to liposome aerosols in mice. Exp Lung Res. 1993, 19: 1-19.

Dokka S, Toledo D, Shi X, Castranova V, Rojanasakul Y: Oxygen radical-mediated pulmonary toxicity induced by some cationic liposomes. Pharm Res. 2000, 17: 521-525.