Effects of physicochemical properties and other factors on systemic nasal drug delivery

Advanced Drug Delivery Reviews

Volumn 29, Issue 1-2, 1998, Pages 89-116

  Behl, C R ^a   Pimplaskar, H K ^a   Sileno, A P ^a   DeMeireles, J ^a   Romeo, V D ^a  

^a Nastech Pharmaceutical Company Inc   (United States)

Author keywords

Absorption factors; Intranasal drug delivery; Nasal delivery; Nasal gels; Nasal powders; Nasal solutions; Physical chemical properties

Indexed keywords

ABSORPTION; GELS; PHARMACOKINETICS; POWDERS;

INTRANASAL DRUG DELIVERY; NASAL GELS; NASAL POWDERS; PHYSICOCHEMICAL PROPERTIES;

CONTROLLED DRUG DELIVERY;

DRUG;

DRUG ABSORPTION; DRUG DELIVERY SYSTEM; DRUG FORMULATION; HUMAN; INTRANASAL DRUG ADMINISTRATION; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; REVIEW;

EID: 0032484574     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0169-409X(97)00063-X     Document Type: Review

References (188)

1. Hussain A.A., Hirai S., Bawarshi R. Nasal absorption of propranolol in rats. J. Pharm. Sci. 68:1979;1196.
2. Y.W. Chien, Industrial Seminar on Intranasal Drug Administration for Systemic Medications, Rutgers University, New Brunswick, NJ, 1984.
3. Y.W. Chien (Ed.), Transnasal Systemic Medications, Elsevier Science, New York, 1985.
4. Y.W. Chien, K.S.E. Su, S.F. Chang, Nasal Systemic Drug Delivery, Marcel Dekker, New York, 1989.
5. Smith R.W. Jr., Dickson L.C., Bryan J.B., Lowrie W.D. Nasal administration of ACTH: observations of effectiveness measured by blood eosinopenic response. J. Clin. Endocrinol. 12:1952;958.
6. Tonndorf J., Hyde R.W., Chinn H.I., Lett J.E. Absorption from nasal mucous membrane: systemic effect of hyoscine following intranasal administration. Ann. Otol. Rhinol. Laryngol. 62:1953;630.
7. The Pink Sheet, F-D-C Reports, 57 (1995) 10.
8. Eriksen J., Jensen N., Jensen M., Bjarno H., Frills P., Brewster D. The systemic availability of buprenorphine administered by nasal spray. J. Pharm. Pharmacol. 41:1989;803-805.
9. Secher C., Kirkegaard J., Borum P., Mansson A., Osterhammel P., Mygind N. Significance of H1 and H2 receptors in the human nose: rationale for the topical use of combined antihistamine preparations. Allergy Clin. Immunol. 70:1982;211-218.
10. Schaffer N., Seidmon E.E. The intranasal use of prophenpyridamine maleate and chlorprophepyr idamine maleate in allergic rhinitis. Ann. Allergy. 10:1952;194.
11. Schols-Hendriks M., Lohman J., Janknegt R., Korten J., Merkus F. Absorption of clonazepam after intranasal and buccal administration. Br. J. Clin. Pharmacol. 39:1995;449-451.
12. Dyke C.V., Barash P.G., Jatlow P.I., Byck R. Cocaine: plasma concentration after intranasal application in man. Science. 195:1977;859.
13. Romeo V.D., Sileno A., Wenig D.N. Intranasal cyanocobalamin. J. Am. Med. Assoc. 268:1992;1268-1269.
14. Gordon G., Ambruso D., Robinson W., Githens J. Intranasal administration of deferoxamine to iron overloaded patients. Am. J. Med. Sci. 297:1989;280-284.
15. Gaffey M., Gwaltney J., Sastre A., Dressler W., Sorrentino J., Hayden F. Intranasally and orally administered antihistamine treatment of experimental rhinovirus colds. Am. Rev. Resp. Dis. 136:1987;556-560.
16. V.D. Romeo, A. Sileno, H.K. Pimplaskar, J. deMeireles, W.J. Gries, C.R. Behl, Intranasal absorption of doxylamine succinate in healthy volunteers. In Preparation, 1996.
17. Aelling W., Rosenthaler J. Venoconstrictor effects of dihydroergotamine after intranasal and intramuscular administration. Eur. J. Clin. Pharmacol. 30:1986;581-584.
18. Rigg L., Milanes B., Villanueva B., Yen S. Efficacy of intravaginal and intranasal administration of micronized estradiol-17 beta. J. Clin. Endocrinol. Metab. 45:1977;1261-1264.
19. Dirksen H., Groth S., Mygind N. The bronchodilating effect of fenoterol after intranasal administration. Eur. J. Respir. Dis. 64:1983;116-118.
20. Rubinstein A. Intranasal administration of gentamicin in human subjects. Antimicrob. Agents Chemother. 23:1983;778-779.
21. Pontiroli A., Albertto M., Calderara A., Pajetta E., Pozza G. Nasal administration of glucagon and human calcitonin to healthy subjects: a comparison of powders and spray solutions and of different enhancing agents. Eur. J. Clin. Pharmacol. 37:1989;427-430.
22. Donnez J., Pochet M., Braun F., Sandow J., Roux F. Administration of nasal buserelin as compared with subcutaneous buserelin implant for endometriosis. Fertil. Steril. 52:1989;27-30.
23. Kllingmuller D., Schweikert H. Maintenance of spermatogenesis by intranasal administration of gonadotropin-releasing hormone in patients with hypothalamic hypogonadism. J. Clin. Endocrinol. Metab. 61:1985;868-872.
24. Laursen T., Ovesen O., Grandjean B., Jensen S., Otto J., Jorgensen L., Illum P., Christiansen J. Nasal absorption of growth hormone in normal subjects: studies with four different formulations. Ann. Pharmacother. 28:1994;845-848.
25. Ghigo E., Arvat E., Gianotti L., Imbimbo B., Lenarets V., Deghenghi R., Camanni F. Growth hormone releasing activity of hexarelin, a new synthetic hexapeptide after intravenous, intranasal, and oral administration in man. J. Clin. Endocrinol. Metab. 78:1993;693-698.
26. Merigan T.C., Reed S.E., Hall T.S., Tyrrell D.A.J. Inhibition of respiratory virus infection by locally applied interferon. Lancet. 1:1973;563.
27. Frauman A.G., Jeruns G., Louis W.J. Effects on intranasal insulin in non-obese type II diabetes. Diabet. Res. Clin. Pract. 3:1987;197-202.
28. Kaila T., Suonpaa J., Grenman R., Iisalo E. Vasomotor rhinitis and the systemic absorption of ipratropium bromide. Rhinology. 28:1990;83-89.
29. Adjei A., Sundberg D., Miller J., Chun A. Bioavailability of leuprolide acetate following nasal and inhalation delivery to rats and healthy humans. Pharm. Res. 9:1992;244-249.
30. Fink G., Gennser G., Liedholm P., Thorell J., Mulder J. Comparison of plasma levels of luteinizing hormone releasing hormone in man after intravenous or intranasal administration. J. Endocrinol. 63:1974;351.
31. V.D. Romeo, A. Sileno, H.K. Pimplaskar, J. deMeireles, W.J. Gries, C.R. Behl, Intranasal absorption of Meclizine HCl in healthy volunteers. In Preparation, 1996.
32. Citron M., Reynolds J., Kalra J., Kay B., Nathan K., Jaffe N., Miller F. Pharmacokinetic comparison of intranasal, oral, and intramuscular metoclopramide in healthy volunteers. Cancer Treat. Rep. 71:1987;317-319.
33. Fukuta O., Braham R., Yanase H., Atsumi N., Kurosu K. The sedative effects of intranasal midazolam administration in the dental treatment of patients with mental disabilities. Part I. The effect of 0.2 mg/kg dose. J. Clin. Pediatr. Dent. 17:1993;231-237.
34. Doebbeling B., Reagan D., Pfaller M., Houston A., Hollis R., Wenzel R. Long term efficacy of intranasal mupirocin ointment. Arch. Intern. Med. 154:1994;1505-1508.
35. Sghirlanzoni A., Pareyson D., Benvenuti C., Cei G., Cosi V., Lombardi M., Nicora M., Ricciardi R., Cornelio F. Efficacy of intranasal administration of neostigmine in myasthenic patients. J. Neurol. 239:1992;165-169.
36. Johansson C., Olsson P., Bende M., Carlsson T., Gunnarsson P. Absolute bioavailability of nicotine applied to different nasal regions. Eur. J. Clin. Pharmacol. 41:1991;585-588.
37. Landau A., Eberhardt R., Frishman W. Intranasal delivery of cardiovascular agents: an innovative approach to cardiovascular pharmacotherapy. Am. Heart. J. 127:1994;1594-1599.
38. Hill A.B., Bowley C.J., Nahrwold M.L., Knight P.R., Tait A.R., Taylor M.D., Kirsch M.M., Denlinger J.K. Intranasal administration of nitroglycerin. Anesthesiology. 51:1979;S67.
39. Anand Kumar T.C., Shah R., Chitlange S., Hazari K., Gopalkrishnan K., Vadigoppula A., Vernekar V., Borkar D., Puri C. Effects of intranasal administration of norethisterone on folliculogenesis, cervical mucus, vaginal cytology, endometrial morphology and reproductive profile in women. Contraception. 44:1991;245-267.
40. Kissel T., Drewe J., Bantle S., Rummelt A., Belinger C. Tolerability and absorption enhancement of intranasally administered octreotide by sodium taurodihydroxyfusidate in healthy subjects. Pharm. Res. 9:1992;52-57.
41. Dalton M., Bromham D., Osborne J., Dalton K. Nasal absorption of progesterone in women. Br. J. Obstet. Gynecol. 94:1987;84-88.
42. Hussain A.A., Foster T., Hirai S., Kashihara T., Batenhorst R., Jone M. Nasal absorption of propranolol in humans. J. Pharm. Sci. 69:1980;1240-1243.
43. Jackson R.T. Prostaglandin E1 as nasal constrictor in normal human volunteers. Curr. Ther. Res. 12:1970;711.
44. Haynes G., Brahen N., Hill H. Plasma sufentanil concentration after intranasal administration to pediatric outpatients. Can. J. Anesth. 40:1993;286-288.
45. Larochelle P., Souich P., Bolte E., Lelorier J., Goyer R. Tixocortol pivalate, a corticosteroid with no systemic glucorticoid effect after oral intrarectal, and intranasal application. Clin. Pharmacol. Ther. 33:1983;343-350.
46. Ouilligan J.J. Jr., Francis T. Jr. Serological response to intranasal administration of inactive influenza virus in children. J. Clin. Invest. 26:1947;1079.
47. Beare A.S., Hopson D., Reed S.E., Tyrrell D.A.J. A comparison of live and killed influenza virus vaccines. Lancet. 2:1968;418.
48. Wigley F.M., Fruchtman M.H., Waldman R.H. Aerosol immunization of humans with inactivated with para-influenza type 2 vaccine. N. Engl. J. Med. 283:1970;1250.
49. McCrumb F.R. Jr., Kress S., Saunders E., Snyder M.J., Schluederberg A.E. Studies with live attenuated measles-virus vaccine. I. Clinical and immunological responses in institutionalized children. Am. J. Dis. Child. 101:1961;689.
50. Ogra P.L., Karzon D.T. Poliovirus antibody response in serum and nasal secretions following intranasal inoculation with inactivated poliovaccine. J. Immunol. 102:1969;15.
51. Blumgart H.L. The antidiuretic effect of pituitary extract applied intranasally in a case of diabetes insipidus. Arch. Intern. Med. 29:1982;508.
52. Dashe A.M., Kleeman C.R., Czaczkes J.W., Rubinoff H., Spears I. Synthetic vasopressin nasal spray in treatment of diabetes insipidus. J. Am. Med. Assoc. 190:1964;1069.
53. N. Cauna, Blood and nerve supply of the nasal lining, in: D.F. Proctor, I.B. Andersen (Eds.), Chapter in The Nose: Upper Airway Physiology and the Atmospheric Environment, Elsevier Biomedical Press, Amsterdam, 1982, pp. 45-69.
54. A. Kolliker, Handbuch der Gewebelehre des Menschen, Wilhem Engelmann, Leipzig, 1852.
55. O. Kohlrausch, Ueber das Schwellgewebe an den Muscheln der Nasenschleimhout, Arch. Anat. Physiol., (1853) 149-150.
56. Zuckerkandl E. Das Schwellgewebe der Nasenschleimhaut und dessen Beziehung zum Respiration-sspalt. Wien. Med. Wochenschr. 38:1884;1121-1125.
57. Burnham H.H. An anatomical investigation of blood vessels of the lateral nasal wall. J. Laryngol. 50:1935;569-595.
58. Swindle P.F. The architecture of the blood vascular networks in the erectile and secretory lining of the nasal passages. Ann. Otol. Rhinol. Laryngol. 144:1935;913-932.
59. Mygind N. Scanning electron microscopy of the human nasal mucosa. Rhinology. 13:1975;57-75.
60. Watanabe K., Watanabe I., Saito Y., Mizuhira V. Characteristics of capillary permeability in nasal mucosa. Ann. Otol. 89:1980;377-382.
61. Geurkink N. Post graduate course. Nasal anatomy, physiology, and function. J. Allergy Clin. Immunol. 72:1983;123-128.
62. Brofeldt S., Secher C., Mygind N. Biophysical characteristics of nasal secretions. A preliminary report. Eur. J. Respir. Dis. 64:1983;436-440.
63. Bende M. Studies of blood flow in the human nasal mucosa. Eur. J. Respir. Dis. 64:1983;400-402.
64. Bisgaard H., Krogsgaard O., Mygind N. Measurement of secretion in nasal lavage. Clin. Sci. 73:1987;217-222.
65. Dawes J.D.K., Prichard M. Studies of the vascular arrangement of the nose. J. Anat. 87:1953;311-322.
66. Cauna N., Hinderer K.H. Fine structure of blood vessels of the human nasal respiratory mucosa. Ann. Otol. Rhinol. Laryngol. 78:1969;865-885.
67. Fisher A., Brown K., Davis S., Parr G., Smith D.A. The effect of molecular size on the nasal absorption of water-soluble compounds in the albino rat. J. Pharm. Pharmacol. 39:1987;357-362.
68. Maitani Y., Machida Y., Nagai T. Influence of molecular weight and charge on nasal absorption of dextran and DEAE-dextran in rabbits. Int. J. Pharm. 40:1989;23-27.
69. McMartin C., Hutchinson L.E.F., Hyde R., Peters G.E. Analysis of structural requirements for the absorption of drugs and macromolecules from the nasal cavity. J. Pharm. Sci. 76:1987;535-540.
70. Donovan M., Flynn G., Amidon G. Absorption of polyethylene glycols 600 through 2000: the molecular weight dependence of gastrointestinal and nasal absorption. Pharm. Res. 7:1990;863-868.
71. Donovan M.D., Flynn G., Amidon G. The molecular weight dependence of nasal absorption: the effect of absorption enhancers. Pharm. Res. 7:1990;808-814.
72. Fisher A., Illum L., Davis S., Schacht E. Di-iodo-L-tyrosine labelled dextrans as molecular size markers of nasal absorption in the rat. J. Pharm. Pharmacol. 44:1992;550-554.
73. Yamamoto A., Morita T., Hashida M., Sezaki H. Effect of absorption promoters on the nasal absorption of drugs with various molecular weights. Int. J. Pharm. 93:1993;91-99.
74. Huang C., Kimura R., Nassar R., Hussain A.A. Mecahnism of nasal absorption of drugs II: absorption of L-tyrosine and the effect of structural modifications on its absorption. J. Pharm. Sci. 74:1985;1298-1301.
75. Huang C., Kimura R., Nassar R., Hussain A.A. Mechanism of nasal absorption of drugs I: physicochemical parameters influencing the rate of in-situ nasal absorption of drugs in rats. J. Pharm. Sci. 74:1985;608-611.
76. Ohwaki K., Ando H., Watanabe S., Miyake Y. Effects of dose, pH, and osmolarity on nasal absorption of secretin in rats. J. Pharm. Sci. 74:1985;550-552.
77. Ohwaki K., Ando H., Kakimoto F., Useugi K., Watanabe S., Miyake S., Kayano M. Effects of dose, pH, osmolarity on nasal absorption of secretin in rats: histological aspects of the nasal mucosa in relation to the absorption variation due to the effects of pH and osmolarity. J. Pharm. Sci. 76:1987;695-698.
78. Ohwaki T., Ishii M., Aoki S., Tatsushi K., Kayano M. Effect of dose, pH and osmolarity on nasal absorption of secretin in rats III: in vivo membrane permeation test and determination of apparent partition coefficient of secretin. Chem. Pharm. Bull. 37:1989;3359-3362.
79. Corbo D.C., Liu J.C., Chien Y.W. Drug absorption through mucosal membranes. Effect of mucosal route and penetrant hydrophilicity. Pharm. Res. 6:1989;848-852.
80. Corbo D.C., Liu J.C., Chien Y.W. Characterization of the barrier properties of mucosal membrane. J. Pharm. Sci. 79:1990;202-206.
81. Gonda I., Gipps E. Model of disposition of drugs administered into the human nasal cavity. Pharm. Res. 7:1990;69-75.
82. Illum L. The nasal delivery of peptides and proteins. Trends Biotechnol. 9:1991;284-289.
83. Vora J., Christensen G., Reginato M., Maciz R., Guchoco C., Oh C. Influence of formulation variables on plasma growth hormone levels following intranasal administration of growth hormone releasing peptide in anesthetized rats. J. Control. Release. 24:1993;193-200.
84. Sakane T., Akizuki M., Yamashita S., Sezaki H., Nada T. Direct drug transport from the rat nasal cavity to the cerebrospinal fluid: the relation to the dissociation of the drug. J. Pharm. Pharmacol. 46:1993;378-379.
85. Shao Z., Park G., Krishnamurthy R., Mitra A. The physicochemical properties, plasma enzymatic hydrolysis and nasal absorption of acyclovir and its 2′-ester prodrugs. Pharm. Res. 11:1994;237-242.
86. Hirai S., Yashika T., Matsuzawa T., Mima H. Absorption of drugs from the nasal mucosa of rat. Int. J. Pharm. 7:1981;317-325.
87. Hogben C.A., Tocco D.J., Brodie B.B., Schanker L.S. On the mechanism of intestinal absorption of drugs. J. Pharmacol. Exp. Ther. 125:1959;275-282.
88. Schanker L.S. Absorption of drugs from the rat colon. J. Pharmacol. Exp. Ther. 126:1959;283-290.
89. Kakemi K., Arita T., Muranishi S. Absorption and excretion of drugs. XXV. On the mechanism of rectal absorption of sulfonamides. Chem. Pharm. Bull. 13:1965;861-869.
90. Narukar M.N., Mitra A.K. Synthesis, physicochemical properties, and cytotoxicity of a series of 5′-ester prodrugs of 5-iodo-2′-deoxyuridine. Pharm. Res. 5:1988;734-737.
91. Ghosh M.K., Mitra A.K. Effects of 5′-ester modification on the physicochemical properties and plasma protein binding of 5-iodo-2′-deoxyuridine. Pharm. Res. 6:1991;771-775.
92. Ghosh M.K., Mitra A.K. Enhanced delivery of 5-iodo-2′-deoxyuridine to the brain parenchyma. Pharm. Res. 9:1992;1173-1176.
93. Beauchamp L.M., Orr G.F., de Miranda P., Burnette T., Krenistsky T.A. Amino acid ester prodrugs of acyclovir. Antiviral Chem. Chemother. 3:1992;157-164.
94. Hofstee B.H. Specificity of esterase. II. Behavior of pancreatic esterase I and II toward a homologous series of n-fatty acid esters. J. Biol. Chem. 199:1952;365-371.
95. Stott W.T., McKenna M.J. Hydrolysis of several glycol ether acetate and acrylate esters by nasal mucosal carboxylesterase in vitro. Fundam. Appl. Toxicol. 5:1985;399-404.
96. Sarkar M. Drug metabolism in the nasal mucosa. Pharm. Res. 9:1992;1-9.
97. Shao Z., Mitra A.K. Bile salt-fatty acid mixed micelles as nasal absorption promoters III. Effects on nasal transport and enzymatic degradation of acyclovir prodrugs. Pharm. Res. 11:1994;243-250.
98. Bogdanffy M.S. Biotransformation enzymes in the rodent nasal mucosa: the value of a histochemical approach. Environ. Health Perspect. 85:1990;177-186.
99. Bogdanffy M.S., Kee C.R., Hinchman C.A., Trela B.A. Metabolism of dibasic esters by rat nasal mucosal carboxylesterase. Drug Metab. Dispos. 19:1991;124-129.
100. Bogdanffy M.S., Randall H.W., Morgan K.T. Biochemical quantitation and histochemical localization of carboxylesterase in the nasal passages of the Fisher-344 rat and B6CF1 mouse. Toxicol. Appl. Pharmacol. 88:1987;183-194.
101. Olson M.J., Martin J.L., LaRosa A.C., Brady A.N., Pohl L.R. Immunohistochemical localization of carboxylesterase in the nasal mucosa of rats. J. Histochem. Cytochem. 41:1993;307-311.
102. Shao Z., Hoffman A., Mitra A. Biodegradation characteristics of acyclovir 2-ester prodrugs by respiratory carboxylesterases: implications in prodrug design for intranasal and pulmonary drug delivery. Int. J. Pharm. 112:1994;181-190.
103. H.D. Kao, Ph.D. Thesis. Enhancement of Delivery of L-Dopa by the Administration of Its Prodrugs Via the Nasal Route. University of Kentucky, Lexington, Kentucky, 1995.
104. K.S.E. Su, K. Campanale, Nasal Drug Delivery Systems Requirements, Development, and Evaluations, in: Transnasal Systemic Medications, Elsevier Science, New York, 1985, pp. 139-159.
105. Eppstein D., Longenecker J. Alternative delivery systems for peptides and proteins as drugs. Crit. Rev. Ther. Drug. Carr. Syst. 5:1988;99-139.
106. Lee V., Yamamoto A., Kompella U. Mucosal penetration enhancers for facilitation of peptide and protein drug absorption. Crit. Rev. Ther. Drug. Carr. Syst. 8:1991;91-192.
107. Chien Y.W., Su K.S.E. Intranasal drug delivery for systemic medications. Crit. Rev. Ther. Drug. Carr. Syst. 4:1987;67-194.
108. Resta O., Barbaro M., Carnimeo N. A comparison of sodium cromoglycate nasal solution and powder in the treatment of allergic rhinitis. Br. J. Clin. Pract. 46:1992;94-98.
109. Harris A., Hedner P., Vilhardt H. Nasal administration of desmopressin by spray and drops. J. Pharm. Pharmacol. 39:1987;932-934.
110. Harris A., Svensson E., Wagner Z., Lethagen S., Nilsson I. Effect of viscosity on particle size deposition and clearance of nasal delivery system containing desmopressin. J. Pharm. Sci. 77:1988;405-408.
111. Harris A., Ohlin M., Lethagen S., Nilsson I. Effects of concentration and volume on nasal bioavailability and biological response to desmopressin. J. Pharm. Sci. 77:1988;337-339.
112. Harris A., Ohlin M., Svensson E., Lethagen S., Nilsson I. Effect of viscosity on pharmacokinetics and biological response to intranasal desmopressin. J. Pharm. Sci. 78:1989;470-471.
113. David G., Puri C., Anand Kumar T. Bioavailability of progesterone enhanced by intranasal spray. Experientia. 37:1981;533-535.
114. Pillion D., Atchison J., Garbiulo C., Want R., Wang P., Meezan E. Insulin delivery in nose drops, new formulations containing alkylglycosides. Endocrinology. 135:1994;2386-2391.
115. Thamsborg G., Storm T., Sykulski R., Brinch E., Nielsen H., Sorensen O. Effect of different doses of nasal salmon calcitonin on bone mass. Calcif. Tissue. Int. 48:1991;302-307.
116. Chiang R., Barnes R., Shoupe D., Lobo R. Dose related changes in LH bioactivity with intranasal GnRH agonist administration. Contraception. 32:1985;347-357.
117. Kotani A., Hayashi M., Awazu S. Selection of volume indicator for the study of the nasal drug absorption. Chem. Pharm. Bull. 31:1983;1097-1100.
118. Hardy J., Lee S., Wilson C. Intranasal drug delivery by spray and drops. J. Pharm. Pharmacol. 37:1984;294-297.
119. Batts A., Marriott C., Martin G., Bond S. The effect of some preservatives used in nasal preparations on mucociliary clearance. J. Pharm. Pharmacol. 41:1989;156-159.
120. Schipper N., Romeijn S., Verhoef J., Merkus F. Nasal insulin delivery with dimethyl beta cyclodextrin as an absorption enhancer in rabbits: powder more effective than liquid formulations. Pharm. Res. 10:1993;682-686.
121. Illum L., Farraj N., Davis S. Chitosan as a novel nasal delivery system for peptide drugs. Pharm. Res. 11:1994;1186-1189.
122. Kararli T., Needham T., Schoenhard G., Baron D., Schmidt R., Katz B., Belonio B. Enhancement of nasal delivery of a renin inhibitor in the rat using emulsion formulations. Pharm. Res. 9:1992;1024-1028.
123. Deitmer T., Scheffler R. The effect of different preparations of nasal decongestants on ciliary beat frequency in-vitro. Rhinology. 31:1993;151-153.
124. Gopinath P., Gopinath G., Anand Kumar T. Target site of intranasally sprayed substances and their transport across the nasal mucosa: a new insight into the intranasal route of drug delivery. Curr. Ther. Res. 23:1978;596-607.
125. Davis S., Hardy J., Newmann S., Wilding I. Gamma scintigraphy in the evaluation of pharmaceutical dosage forms. Eur. J. Nuclear Med. 19:1992;971-986.
126. Illum L., Farraj N., Critchley H., Davis S. Nasal administration of gentamicin using a novel microsphere delivery system. Int. J. Pharm. 46:1988;261-265.
127. Bjork E., Edman P. Characterization of degradable starch microspheres as a nasal delivery system for drugs. Int. J. Pharm. 62:1990;187-192.
128. Edman P., Bjork E., Ryden L. Microspheres as a nasal delivery system for peptide drugs. J. Control. Release. 21:1992;165-172.
129. Ting T., Gonda I., Gipps E. Microparticles of PVA for nasal delivery I. Generation by spray drying and spray desolvation. Pharm. Res. 9:1992;1330-1335.
130. Holmberg K., Bjork E., Bake B., Edman P. Influence of degradable starch microspheres on the human nasal mucosa. Rhinology. 31:1992;74-77.
131. Vyas S., Talwar N., Karajgi J., Jain N. An erythrocyte based bioadhesive system for nasal delivery of propranolol. J. Control. Release. 23:1993;231-237.
132. Illum L., Farraj N., Fisher A., Gill I., Miglietta M., Benedetti L. Hyaluronic acid ester microspheres as a nasal delivery system for insulin. J. Control. Release. 29:1994;133-141.
133. Critchley H., Davis S., Farraj N., Illum L. Nasal absorption of desmopressin in rats and sheep. Effect of bioadhesive microsphere delivery system. J. Pharm. Pharmacol. 46:1994;651-656.
134. Newman S., Moren F., Clarke S. Deposition pattern from a nasal pump spray. Rhinology. 25:1987;77-82.
135. Der Yu C., Jones R., Wright J., Henesian M. Characterization of dose delivery and spray pattern of a metered dose flunisolide nasal spray. Drug. Dev. Ind. Pharm. 9:1983;473-483.
136. Der Yu C., Jones R., Henesian M. Cascade impactor method for the droplet size characterization of metered-dose nasal spray. J. Pharm. Sci. 73:1984;344-347.
137. L. Illum, Microsphere as a potential controlled release nasal drug delivery system, in: S.S. Davis, L. Illum, E. Tomlinson (Eds.), Delivery Systems for Peptide Drugs, Plenum Press, New York, 1986, pp. 205-210.
138. Illum L., Jorgensen H., Bisgaard H., Krogsgaard O., Rossing N. Bioadhesive microspheres as a potential nasal drug delivery system. Int. J. Pharm. 39:1987;189-199.
139. Illum L., Faraj N., Davis S., Johansen B., O'Hagan D. Investigation of the nasal absorption of biosynthetic human growth hormone in sheep: use of a bioadhesive microsphere delivery system. Int. J. Pharm. 63:1990;207-211.
140. Benedetti L.M., Topp E.M., Stella V.J. Microspheres of hyaluronic acid esters. Fabrication methods and in vitro hydrocortisone release. J. Control. Release. 13:1987;351-355.
141. Bjork E., Edman P. Degradable starch microspheres as a nasal delivery system for insulin. Int. J. Pharm. 47:1988;233-238.
142. Ryden L., Edman P. Effect of polymers and microspheres on the nasal absorption of insulin in rats. Int. J. Pharm. 83:1992;1-10.
143. Bjork E., Bjurstrom S., Edman P. Morphological examination of rabbit nasal mucosa after nasal administration of degradable starch microspheres. Int. J. Pharm. 75:1991;73-80.
144. Vyas S.P., Bhatnagar S., Gogoi P.J., Jain N.K. Preparation and characterization of HSA propranolol microspheres for nasal administration. Int. J. Pharm. 69:1991;5-12.
145. Rao R.V.R., Buri P. A novel in situ method to test polymers and coated microparticles for bioadhesion. Int. J. Pharm. 52:1989;265-270.
146. Claus M.L., Bouwastra J.A., Tukker J.J., Junginger H.E. Intestinal transit of bioadhesive microspheres in an in situ loop in the rat - a comparative study with copolymers and blends based on poly (acrylic) acid. J. Control. Release. 13:1990;51-62.
147. Farraj N.F., Johansen B.R., Davis S.S., Illum L. Nasal administration of insulin using bioadhesive microspheres as a delivery system. J. Control. Release. 13:1990;253-261.
148. Morimoto K., Yamaguchi H., Iwakura Y., Morisaka K., Ohashi Y., Nakai Y. Effects of viscous hyaluronate-sodium solutions on the nasal absorption of vasopressin and an analogue. Pharm. Res. 8:1991;471-474.
149. Saettone M.F., Chetoni P., Torracca M.T., Burgalassi S., Giannaccini B. Evaluation of mucoadhesive properties and in vivo activity of ophthalmic vehicles based on hyaluronic acid. Int. J. Pharm. 51:1989;203-212.
150. A.A. Hussain, R. Bawarshi-Nassar, C.H. Huang, Physicochemical consideration in intranasal drug administration in transnasal systemic medications, in: Y.W. Chien (Ed.), Elsevier Science, New York, 1985, pp. 121-137.
151. Brannon M.D., Herron J.M., Reidenberg P., Affrime M.B. Lack of hypothalamic-pituitary-adrenal axis suppression with once-daily or twice-daily beclomethasone dipropionate aqueous nasal spray administered to patients with allergic rhinitis. Clin. Ther. 17:1995;637-647.
152. Clement P., Roovers M.H., Francillon C., Dodion P. Dose ranging, placebo controlled study of cetrizine nasal spray in adults with perennial allergic rhinitis. Allergy. 49:1994;668-672.
153. Streisand B., Zhang J., Niu S., McJames S., Natte R. Buccal absorption of fentanyl is pH dependent in dogs. Anesthesiology. 82:1995;759-764.
154. Fabricant N.D. Significance of the pH of nasal secretions in situ. Arch. Otolaryngol. 34:1941;150-153.
155. Fabricant N.D. Effect of progressively buffered solutions of ephedrine on nasal mucosa. J. Am. Med. Assoc. 151:1953;21-24.
156. Fabricant N.D. The pH of the throat, nose and ear. Eye Ear Nose Throat Monthly. 43:1964;60-64.
157. Fabricant N.D. Relation of the pH of nasal secretions in situ to the activity of lysozyme. Arch. Otolaryngol. 41:1945;53-55.
158. Mayer K. The relationship of lysozyme to avidin. Science. 99:1944;391.
159. Thompson R. Lysozyme and its relation to antibacterial properties of various tissues and secretions. Arch. Pathol. 30:1940;1096.
160. Jackson R.T., Turner J.S. Some observations on nasal pH. Arch. Otolaryngol. 84:1966;446-450.
161. N. Cuna, Blood and nerve supply of the nasal lining, in: D.F. Proctor, I. Anderson (Eds.), The Nose: Upper Airway Physiology and Atmospheric Environment, Elsevier Science, New York, 1982, pp. 45-66.
162. P.G. Gervasi, V. Longo, F. Ursino, G. Pnattoni, Drug metabolizing enzymes in the respiratory mucosa of humans. Comparison with rats, in: Proceedings of the 6th International Conference on the Biochemistry and Biophysics of Cytochrome P450, Taylor and Francis, London, 1989, pp. 198-199.
163. J.P. Schreider, Comparative anatomy and function of the nasal passages, in: C.S. Barrow (Ed.), Toxicology of the Nasal Passages, Hemisphere, Washington, DC, 1986, pp. 1-23.
164. Hall L.J., Jackson R.T. Effects of alpha and beta adrenergic agonists on nasal blood flow. Ann. Otol. Rhinol. Laryngol. 77:1968;1120-1130.
165. Malm L. Responses of resistance and capacitance vessels in feline nasal mucosa to vasoactive agents. Acta Otolaryngol. (Stockh.). 78:1974;90-97.
166. Anggard A., Edwall L. The effects of sympathetic nerve stimulation on the tracer disappearance rate and local blood content in the nasal mucosa of the cat. Acta. Otolaryngol. (Stockh.). 77:1974;131-135.
167. Richerson H.B., Seeboham P.M. Nasal airway response to exercise. J. Allergy. 41:1968;269-284.
168. Bende M. The effect of topical decongestant in blood flow in normal and infected nasal mucosa. Acta. Otol. 96:1983;523-527.
169. Olson P., Bende M. Influence of environmental temperature on human nasal mucosa. Ann. Otol. Rhinol. Laryngol. 94:1985;153-157.
170. Paulsson B., Bende M., Ohlin P. Nasal mucosal blood flow at rest and during exercise. Acta Otolaryngol. (Stockh.). 99:1985;140-144.
171. Anderson K., Bende M. Adrenoceptors in the control of human nasal mucosal blood flow. Ann. Otol. Rhinol. Laryngol. 93:1984;179-182.
172. Bende M., Flysberg K., Larsson I., Ohlin P., Olson P. A method for determination of blood flow with 133-xenon in human nasal mucosa. Acta Otolaryngol. (Stockh.). 96:1983;277-280.
173. Lung M., Wang J. Nasal blood flow and airway resistance canine study. Ann. Otol. Rhinol. Laryngol. 94:1985;198-201.
174. McLean J.A., Mathews K.P., Ciarkowski A.A., Briayton P.R., Solomon W.R. The effects of topical saline and isoproterenol on nasal airway resistance. J. Allergy Clin. Immunol. 58:1976;563-574.
175. Borum P., Mygind N. Inhibition of immediate allergic reaction in the nose by beta-2-adrenostimulant fenoterol. J. Allergy Clin. Immunol. 66:1980;25-32.
176. Schumacher M.J. Effect of a beta-adrenergic agonist, fenoterol, on nasal sensitivity to allergen. J. Allergy Clin. Immunol. 66:1980;33-38.
177. Dahl A.R. The inhibition of rat nasal cytochrome P450-dependent mono-oxygenase by essence heliotropin (Piperonal). Drug Metab. Dispos. 10:1982;553-558.
178. Dahl A.R., Hadley W.M. Formaldehyde production promoted by rat nasal cytochrome P450-dependent mono-oxygenase with nasal decongestant, essences, solvents, air pollutants, nicotine, and cocaine as substrates. Toxicol. Appl. Pharmacol. 67:1983;200-206.
179. Hadley W.M., Dahl A.R. Cytochrome P450-dependent mono-oxygenase activity in rat nasal epithelial membranes. Toxicol. Lett. 10:1982;417-418.
180. Dahl A.R., Hadley W.M., Hahn F.F., Benson J.M., McClellan R.O. Cytochrome P450-dependent mono-oxygenase in olfactory epithelial of dogs: possible role in tumorigenicity. Science. 216:1982;57-59.
181. Hadley W.M., Dahl A.R. Cytochrome P450-dependent mono-oxygenase activity in nasal membranes of six species. Drug Metab. Dispos. 11:1983;275-279.
182. Longo V., Pacifici G.M., Panattoni G., Ursino F., Gervasi P.G. Metabolism of diethylnitrosamine by microsomes of human respiratory nasal mucosa and liver. Biochem. Pharmacol. 38:1989;1867-1869.
183. Schorn K., Kochstraßer K. Das Isoenzymmuster der Laktatdehydrogenase im Nasensekret. Laryngol. Rhinol. 55:1976;961-966.
184. Werner E., Meyer P. Lokalisation von kohlenhydraten und einigen oxydoreduktasen in der regio respiratoria der normalen nasenschleimhaut des menschen. Acta Histochem. Bd. 33:1969;S179.
185. Werner E., Myer P. Localisation von lipiden und hydrolasen in der regio respiratoria der normalen nasenschleimhaut des menschen. Acta Histochem. Bd. 35:1970;S61.
186. Smith E.L., Hill R.L., Borman A. Activity of insulin degraded by leucine aminopeptidase. Biochem. Biophys. Acta. 29:1958;207-214.
187. Brittebo E.G., Rafter J.J. Steroid metabolism by rat nasal mucosa: studies on progesterone and testosterone. Steroid. Biochem. 20:1984;1147.
188. D.F. Proctor, Nasal physiology in intranasal drug administration, in: Y.W. Chien (Ed.), Transnasal Systemic Medications, Elsevier Sciences, New York, 1985, pp. 101-106.