Drug delivery to the nasal cavity: In vitro and in vivo assessment

Critical Reviews in Therapeutic Drug Carrier Systems

Volumn 21, Issue 1, 2004, Pages 21-66

  Newman, Stephen P ^a   Pitcairn, Gary R ^a   Dalby, Richard N ^b  

^a PHARMACEUTICAL PROFILES LTD   (United Kingdom)

^b UNIVERSITY OF MARYLAND SCHOOL OF PHARMACY   (United States)

Author keywords

Aerosol deposition; Gamma scintigraphy; Nasal cavity; Nasal spray; Pet imaging

Indexed keywords

AEROSOL; DRUG DELIVERY SYSTEM; DRUG FORMULATION; FOOD AND DRUG ADMINISTRATION; IN VITRO STUDY; IN VIVO STUDY; NOSE CAVITY; PARTICLE SIZE; POSITRON EMISSION TOMOGRAPHY; REVIEW; CLINICAL TRIAL; COMPUTER ASSISTED EMISSION TOMOGRAPHY; HISTOLOGY; HUMAN; INTRANASAL DRUG ADMINISTRATION; METABOLISM; METHODOLOGY; NEBULIZER; PHARMACOKINETICS; PHARMACOLOGY; SCINTISCANNING;

DRUG;

ADMINISTRATION, INTRANASAL; AEROSOLS; CLINICAL TRIALS; DRUG DELIVERY SYSTEMS; HUMANS; NASAL CAVITY; NEBULIZERS AND VAPORIZERS; PARTICLE SIZE; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS; PHARMACOLOGY; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 3042617896     PISSN: 07434863     EISSN: None     Source Type: Journal    
DOI: 10.1615/critrevtherdrugcarriersyst.v21.20     Document Type: Review

References (119)

1. Qurashi MS, Jones NS, Mason JDT. The nasal delivery of drugs. Clin Otolaryngol 1997; 22:389-301.
2. Mygind N, Weeke B. Allergic and Vasomotor Rhinitis: Clinical Aspects. Copenhagen: Munksgaard, 1985.
3. Homer JJ, Aggarwal R, Cordoza A. Delivery of topical nasal drugs: clinical implications for rhinosinusitis therapy research. Am J Drug Deliv 2003; 1:125-131.
4. Chien YW, Chang SF. Historic development of transnasal systemic medications. In: Chien YW, editor. Transnasal Systemic Medications. Amsterdam: Elsevier, 1985.
5. Harris AS. Clinical opportunities provided by the nasal administration of peptides. J Drug Targeting 1993; 1:101-116.
6. Davis SS, Illum L. Nasal delivery of drugs, vaccines and DNA-a novel concept. Eur Pharm Contractor 2000: August; 54-58.
7. Illum L. Is nose-to-brain transport of drugs in man a reality? J Pharm Pharmacol 2004; 35:3-17.
8. Illum L. Nasal drug delivery-possibilities, problems and solutions. J Control Release 2003; 87:187-198.
9. Yates R, Dixon R. Preliminary studies of the pharmacokinetics and tolerability of zolmitriptan nasal spray in healthy volunteers. J Clin Pharmacol 2002; 42:1237-1243.
10. Illum L. Nasal drug delivery: new developments and strategies. Drug Discovery Today 2002; 7:1184-1189.
11. Jabbal-Gill I. Nasal vaccines. Drug Deliv Syst Sci 2001; 3:89-94.
12. Vajdy M, O'Hagan DT. Microparticles for intranasal immunization. Adv Drug Deliv Rev 2001; 51:127-141.
13. Glück R. Intranasal immunization against influenza. J Aerosol Med 2002; 15:221-228.
14. Cheng Y-H, Watts P, Hinchcliffe M, Hotchkiss R, Nankervis R, Faraj NF, Smith A, Davis SS, Illum L. Development of a novel nasal formulation comprising an optimal pulsatile and sustained plasma profile for smoking cessation. J Control Release 2002; 79:243-254.
15. O'Hagan DT, Rappouli R. Novel delivery systems for intranasal immunisation with inactivated influenza vaccine. Drug Deliv Syst Sci 2001, 2:41-44.
16. Southall J, Ellis C. Developments in nasal drug delivery. Innovat Pharm Technol 2000, October:110-115.
17. Petri W, Schmiedel R, Sandow J. Development of a metered-dose nebulizer for intranasal peptide administration. In: Chien YW, editor. Transnasal Systemic Medications. Amsterdam: Elsevier Science Publishers, 1985.
18. Bommer R. Advances in nasal drug delivery technology. Pharm Tech Eur 1999; September:26-33.
19. Bruna P, Burel S, Carlotti P, Despris-Gnis F, Guiffray JL, Williams G. A comparative study of two single dose powder aerosol devices for delivery to the nasal airways. Proceedings of Drug Delivery to the Lungs X Conference. London: The Aerosol Society, 1999, 48-51.
20. Devalia JL, Prime D, Richards DH. Effect of variable inspiratory flow rate on the performance of the budesonide Rhinocort Turbuhaler. Clin Drug Invest 2001; 21:195-201.
21. Davies N, Coffee RA, Humphrey MJ, Billotte A, Shepherd M. Evaluation of hydroelectrohydrodynamics to deliver charged droplets to the nasal cavity. In: Dalby RN, Byron PR, Peart J, Farr SF, editors. Respiratory Drug Delivery VIII. Raleigh: Davis Horwood, 2002.
22. Proctor DF. The upper airway. In: Proctor DF, Andersen I, editors. The Nose. Amsterdam: Elsevier, 1982.
23. Proctor DF. The upper airway I. Nasal physiology and defence of the lungs. Am Rev Respir Dis 1977; 115:97-129.
24. Mygind N. Upper airway: structure, function and therapy. In: Morén F, Dolovich MB, Newhouse MT, Newman SP, editors. Aerosols in Medicine: Principles, Diagnosis and Therapy. Amsterdam: Elsevier, 1993.
25. Heyder J, Gebhardt J, Rudolf G, Schiller CF, Stahlhofen W. Deposition of particles in the human respiratory tract in the size range 0.005 to 15 μm. J Aerosol Sci 1986; 17:811-825.
26. Task Group on Lung Dynamics. Deposition and retention models for internal dosimetry of the human respiratory tract. Health Phys 1966; 12:173-207.
27. Proctor DF. The mucociliary system. In: Proctor DF, Andersen I, editors. The Nose. Amsterdam: Elsevier, 1982.
28. Wilson CG, Washington N. Nasal drug delivery. In: Wilson CG, Washington N, editors. Physiological Pharmaceutics: Biological Barriers to Drug Absorption. Chichester: Ellis Horwood, 1989.
29. Wermeling DP, Miller JL, Ridy AC. Systemic intranasal drug delivery: concepts and application. Drug Deliv Technol 2002; 2:56-61.
30. Proctor DF, Anderson I, Lundquist G. Clearance of inhaled particles from the human nose. Arch Intern Med 1973; 131:132-139.
31. Hounam RF. The removal of particles from the nasopharyngeal compartment of the respiratory tract by nose blowing and swabbing. Health Phys 1975; 28:743-753.
32. Schipper NGM, Verhoef JC, Merkus FWHM. The nasal mucociliary clearance: relevance to nasal drug delivery. Pharm Res 1991; 8:807-815.
33. Verhoef JC, Merkus FWHM. Nasal absorption enhancement: relevance to nasal drug delivery. In: de Boer AG, editor. Drug Absorption Enhancement: Concepts, Possibilities, Limitations and Trends. Zurich: Harwood Academic, 1994.
34. Merkus FWHM, Verhoef JC, Marttin E, Romeijn SG, van der Kuy PHM, Hermens WAJJ, Schipper NGM. Cyclodextrins in nasal drug delivery. Adv Drug Deliv Rev 1999; 36:41-57.
35. Illum L, Fisher AN, Jabbal-Gill I, Davis SS. Bioadhesive starch microspheres and absorption enhancing agents act synergistically to enhance the nasal absorption of polypeptides. Int J Pharm 2001; 222:109-119.
36. Davis SS, Illum L. Absorption enhancers for nasal drug delivery. Clin Pharmacokinet 2003; 42:1107-1128.
37. Haffejee N, du Plessis J, Muller DG, Schulz CM, Kotze AF, Goosen C. Intranasal toxicity of selected absorption enhancers. Pharmazie 2001; 56:882-888.
38. Illum L. Nasal drug delivery: new developments and strategies. Drug Discov Today 2002; 7:1184-1189.
39. Fisher AN, Illum L, Davis SS, Schacht EH. Di-iodo-L-tyrosone labeled dextrans as molecular size markers of nasal absorption. J Pharm Pharmacol 1992; 44:550-554.
40. Frey W. Bypassing the blood-barrier to deliver therapeutic agents to the brain and spinal cord. Drug Deliv Technol 2002, July/August:46-49.
41. Graff CL, Plooack GM. P-glycoprotein attenuates brain uptake of substrates after nasal installation. Pharm Res 2003; 20:1225-1230.
42. Illum L. Transport of drugs from the nasal cavity to the central nervous system. Eur J Pharm Sci 2000; 1:1-18.
43. Messerklinger W. Background and evolution of endoscopic sinus surgery. Ear Nose Throat J 1994; 73:449-450.
44. Adams WP, Singh GJP, Williams RL. Nasal inhalation aerosols and metered dose spray pumps: FDA bioequivalence issues. In: Dalby RN, Byron PR, Farr SJ, editors. Respiratory Drug Delivery VI. Buffalo Grove: Interpharm Press, 1998.
45. US FDA. Draft guidance for industry: bioavailability and bioequivalence studies for nasal aerosols and nasal sprays for local action. Washington DC: US Food and Drug Administration, 1999.
46. US FDA. Draft guidance for industry: bioavailability and bioequivalence studies for nasal aerosols and nasal sprays for local action. Washington DC: US Food and Drug Administration, 2003.
47. Pharmaceutical Previews, Chapter 601. Aerosols, metered dose inhalers and dry powder inhalers. Pharm Forum 1996; 22:3065-3095.
48. Hallworth GW. Particle size analysis of therapeutic aerosols. In: Morén F, Dolovich MB, Newhouse MT, Newman SP, editors. Aerosols in Medicine: Principles, Diagnosis and Therapy. Amsterdam: Elsevier, 1993.
49. Ranucci J. Dynamic plume-particle size analysis using laser diffraction. Pharm Tech 1992; 16:108-114.
50. Someraju S, Suman RD, Dalby RN, Stridick WF. Semi-automated spray pattern testing of nasal sprays. Pharm Tech 1997; 21:58-64.
51. Miszuk S, Gupta BM, Chen FC, Clawans C, Knapp JZ. Video characterization of flume patterns of inhalation aerosols. J Pharm Sci 1980; 69:713-717.
52. Dhand R, Malik SK, Balakrishnan M, Verma SR. High speed photographic analysis of aerosols produced by metered dose inhalers. J Pharm Pharmacol 1988; 40:429-430.
53. Hallworth GW, Padfield JM. A comparison of the regional deposition in a model nose of a drug discharged from metered aerosol and metered pump nasal delivery systems. J Allergy Clin Immunol 1986; 77:348-353.
54. Mygind N, Vesterhauge S. Aerosol distribution in the nose. Rhinology 1978; 16:79-88.
55. Durand M, Rusch P, Granjon D, Chantrel G, Prades JM, Dubois F, Esteve D, Pouget J-F, Martin C. Preliminary study of the deposition of aerosol in the maxillary sinuses using a plastinated model. J Aerosol Med 2001; 14:83-93.
56. Miyabe S, Koizuka I, Tanaka K, Otani Y, Hatsutori K. Distribution of the fluticasone propionate aerosol particles in the nasal cavity during aerosol therapy. Sei Marianna Ika Daikagu Zasshi 1999; 27:503-509.
57. Homer JJ, Raine CH. An endoscopic photographic comparison of nasal drug delivery by aqueous spray. Clin Otolaryngol 1998; 23:560-563.
58. Homer JJ, Maughan J, Burniston M. A quantitative analysis of the intranasal delivery of topical nasal drugs to the middle meatus: spray versus drop administration. J Laryngol Otol 2002; 116:10-13.
59. Johansson CJ, Olsson P, Bende M, Carlsson T, Gunnarson PO. Absolute bioavailability of nicotine applied to different nasal regions. Eur J Clin Pharmacol 1991; 41:585-588.
60. Daley-Yates PT, Baker RC. Systemic bioavailability of fluticasone propionate administered as nasal drops and aqueous nasal spray formulations. Br J Clin Pharmacol 2001; 51:103-105.
61. Thorsson L, Borga O, Edsbacker S. Systemic availability of budesonide after nasal administration of three different formulations: pressurized aerosol, aqueous pump spray and powder. Br J Clin Pharmacol 1999; 47:619-624.
62. Davis SS, Hardy JG, Newman SP, Wilding IR. Gamma scintigraphy in the evaluation of pharmaceutical dosage forms. Eur J Nucl Med 1992; 19:971-986.
63. Newman SP. Scintigraphic assessment of therapeutic aerosols. Crit Rev Ther Drug Carrier Syst 1993; 10:65-109.
64. Smaldone GC. Radionuclide scanning, respiratory physiology and pharmacokinetics. J Aerosol Med 2001; 14:135-137.
65. Meseguer G, Gurny R, Buri P. In vivo evaluation of dosage forms: application of gamma scintigraphy to non-enteral routes of administration. J Drug Targeting 1994; 2:269-288.
66. Perkins AC, Frier M. Nuclear medicine imaging and drug delivery. Nucl Med Comm 2000; 21:415-416.
67. 99mTc. J Aerosol Med 1997; 10:92.
68. Lafont P, Bellon G, Mein-Tapponnier N, Meurisse G, Barbier Y. Alpha-1-antitrypsin labeling with technetium-99m for monitoring the deposition of alpha-1 antitrypsin in aerosol therapy. Nucl Med Biol 1998; 25:509-511.
69. Thorsson L, Newman SP, Weisz A, Trofast E, Morén F. Nasal distribution of budesonide inhaled via a powder inhaler. Rhinology 1993; 31:7-10.
70. Newman SP, Morén F, Clarke SW. The nasal distribution of metered dose inhalers. J Laryngol Otol 1987; 101:127-132.
71. Soane RJ, Hinchcliffe M, Davis SS, Illum L. Clearance characteristics of chitosan based formulations in the sheep nasal cavity. Int J Pharm 2001; 217:183-191.
72. Suman JD, Laube BL, Dalby RN. Comparison of nasal deposition and clearance by aerosol generated by a nebulizer and an aqueous spray pump. Pharm Res 1999; 16:1648-1652.
73. Fleming JS, Conway JH. Three-dimensional imaging of aerosol deposition. J Aerosol Med 2001; 14:147-153.
74. Sasajima T, Kinouchi H, Tomura N, Watarai J, Mizoi K. High uptake of 123I-metaiodobenzylguanidine (MIBG) related to olfactory neuroblastoma revealed by single photon emission CT. Am J Neuroradiol 2000; 21:717-720.
75. Jones T. New opportunities in molecular imaging using PET. Drug Inform J 1997; 31:991-995.
76. 11C-nicotine vapour in the human airway as visualized by positron emission tomography. Clin Pharmacol Ther 1995; 57:309-317.
77. Dolovich M, Hahmias C, Coates G. Unleashing the PET:3D imaging of the lung. In: Dalby RN, Byron PR, Farr SJ, Peart J, editors. Respiratory Drug Delivery VII. Raleigh: Serentec Press, 2000.
78. Gould P. The rise and rise of medical imaging. Phys World 2003; August:29-31.
79. Aoki FY, Crawley JCW. Distribution and removal of human serum albumin-technetium 99m instilled intranasally. Br J Clin Pharmacol 1976; 3:869-878.
80. Lee SW, Hardy JG, Wilson CG, Smelt GJC. Nasal sprays and polyps. Nucl Med Comm 1984; 5:697-703.
81. Bond SW, Hardy JG, Wilson CG. Deposition and clearance of nasal sprays. In: Aiache JM, Hirtz J, editors. Proceedings of 2nd European Congress of Biopharmaceutics and Pharmacokinetics. Paris: Lavoisier, 1984, 93-98.
82. MacLean JA, Bacon JR, Mathews KP, Thrall JH, Banas JM, Hedden J, Bayne NK. Distribution and clearance of radioactive aerosol on the nasal mucosa. Rhinology 1984; 22:65-75.
83. Hardy JG, Lee SW, Wilson CG. Intranasal drug delivery by spray and drops. J Pharm Pharmacol 1985; 37:294-297.
84. Harris AS, Nilsson IM, Wagner ZG, Alkner U. Intranasal administration of peptides: nasal deposition, biological response and absorption of desmopressin. J Pharm Sci 1986; 75:1085-1088.
85. Illum L, Jorgensen H, Bisgaard H, Krogsgaard O, Rossing N. Bioadhesive microspheres as a potential nasal drug delivery system. Int J Pharm 1987; 189:189-197.
86. Newman SP, Morén F, Clarke SW. Deposition pattern of nasal sprays in man. Rhinology 1987; 26:111-120.
87. Morén F, Bjornek K, Klint T, Wagner ZG. A comparative distribution study of two procedures for administration of nose drops. Acta Otolaryngol 1988; 106:286-290.
88. Pennington AK, Ratcliffe JH, Wilson CG, Hardy JG. The influence of solution viscosity on nasal spray deposition and clearance. Int J Pharm 1988; 43:221-224.
89. Harris AS, Svensson E, Wagner ZG, Lethagen S, Nilsson IM. Effect of viscosity on particle size, deposition and clearance of nasal delivery systems containing desmopressin. J Pharm Sci 1988; 77:405-408.
90. Morén F, Newman SP. Aerosol particles and deposition in the airways. In: Mygind N, Pipkorn U, Dahl R, editors. Rhinitis and Asthma: Similarities and Differences. Copenhagen: Munksgaard, 1990.
91. Newman SP, Steed KP, Hardy JG, Wilding IR, Hooper G, Sparrow RA. The distribution of an intranasal insulin formulation in healthy volunteers. Effect of different administration techniques. J Pharm Pharmacol 1994; 46:657-660.
92. Newman SP, Steed KP, Hooper G, Brickwell J. Scintigraphic assessment of the oropharyngeal and nasal depositions of fusafungine from a pressurized inhaler and from a novel pump spray device. J Pharm Pharmacol 1995; 47:818-821.
93. Ridley D, Perkins AC, Washington N, Wilson CG, Wastie ML, O'Flynn P, Blattman A, Poncel G, Duchêne D. The effect of posture on nasal clearance of bioadhesive starch microspheres. STP Pharma Sci 1995; 5:442-446.
94. Sandefer EP, Goldberg A, Doll WJ, Page R, Digenis GA. Rhinoscintigraphy in the assessment of nasal delivery performance in man. Pharm Res 1995; 12 (Suppl):S-288.
95. Chang Y, Sandefer EP, Doll WJ, Page RC, Digenis GA. Rhinoscintigraphy to assess bioequivalence of nasal products for non-systemically absorbed drugs. Proceedings of AAPS meeting, Seattle, 1996, S-175.
96. Okuyama S. The first attempt at radioisotopic evaluation of the integrity of the nose-brain barrier. Life Sci 1997; 60:1881-1884.
97. Matsune S, Furuta S, Ohyama M, Sato T, Noikura T. Effective administration of aerosol particles into paranasal sinuses by conservative technique for treatment of sinusitis. Jibi Innkoh-ka Ten-Boh 1997; 40:201-205.
98. Berridge MS, Heald DL, Muswick GJ, Leisure GP, Voelker KW, Miraldi F. Biodistribution and kinetics of nasal C-11 triamcinolone acetonide. J Nucl Med 1998; 39:1972-1977.
99. Berridge MS, Lee Z, Leisure GP, Miraldi F, Heald DL. Nasal delivery and kinetics of fluticasone propionate using positron tomography. Pharm Sci 1998; 1:S-208-209.
100. Bergstrom M, Cass LMR, Valind S, Westerberg G, Lundberg E-L, Gray S, Bye A, Langstrom B. Deposition and disposition of [11C] zanamivir as an intranasal spray. Clin Pharmacokinet 1999; 36 (Suppl 1):33-39.
101. Bryant ML, Brown P, Gurevich N, McDougall IR. Comparison of the clearance of radiolabeled nose drops and nasal spray as mucosally delivered vaccine. Nucl Med Comm 1999; 20:171-174.
102. Soane RJ, Frier M, Perkins AC, Jones NS, Davis SS, Illum L. Evaluation of the clearance characteristics of bioadhesive systems in humans. Int J Pharm 1999; 178:55-65.
103. Suman JD, Laube BL, Dalby RN. Nasal nebulizers versus aqueous nasal spray pumps: a comparison of deposition patterns in human volunteers. In: Dalby RN, Byron PR, Farr SJ, editors. Respiratory Drug Delivery VI. Buffalo Grove: Interpharm Press, 1998.
104. Washington N, McGlashan JA, Jackson SJ, Bush D, Pitt KG, Rawlins DA, Gill DA. The effect of nasal patency on the clearance of radiolabeled saline in healthy volunteers. Pharm Res 2000; 17:733-736.
105. Perkins AC, Carney AS, Soane RJ, Frier M, Davis SS, Illum L, Jones NS. A dual radionuclide study to assess the effect of the nasal cycle on nasal drug delivery. Nucl Med Comm 2000; 21:374.
106. 15O-water. J Aerosol Med 2001; 14:416.
107. Dewit O, Ball D, Hirst PH, Newman SP, Wray H, Ritchie S, Vousden M. Scintigraphic assessment of nasal deposition and clearance of an aqueous nasal spray administered to healthy volunteers whelst experiencing a common cold. Br J Clin Pharmacol 2001; 51:374P.
108. Suman JD, Laube BL, Lin T-C, Brouet G, Dalby RN. Are in vitro tests of nasal solutions predictive of in vivo behaviour. In: Dalby RN, Byron PR, Farr SJ, Peart J, editors. Respiratory Drug Delivery VII. Raleigh: Serentec Press, 2000.
109. Suman JD, Laube BL, Lin T-C, Brouet G, Dalby R. Validity of in vitro tests on aqueous spray pumps as surrogates for nasal deposition. Pharm Res 2002; 19:1-6.
110. Borum S, Becker B, Mygind N, Borum P. Comparison between the effect of ipratropium bromide as a pressurized aerosol and as an aqueous pump spray on methacholine-induced rhinorrhoea. Rhinology 1996; 34:198-200.
111. Nuutinen J, Pietiläinen T, Pietola M, Salminen M, Pirilä T, Rinne J, Seppä J, Suonpää J, Silvasti M, Vidgren P, Korhonen P. Aerosol versus powder form of beclomethasone dipropionate in the treatment of seasonal allergic rhinitis. A multicenter study. Proceedings of XVI European Congress of Allergology and Clinical Immunology, Madrid, 1995, 525-529.
112. Malmberg H, Holopainen E, Simola M, Böss I, Lindqvist N. A comparison between intranasal budesonide aerosol and budesonide dry powder in the treatment of hay fever symptoms. Rhinology 1991; 29:137-141.
113. Dowley AC, Homer JJ. The effect of inferior turbinate hypertrophy on nasal spray distribution in the middle meatus. Clin Otolaryngol 2001; 26:488-490.
114. Meyer R. US regulatory perspective on radiolabeled studies. Proceedings of International Society for Aerosols in Medicine conference, Baltimore, 2003.
115. Chen M-L, Shah V, Patnaik R, Adams W, Hussain A, Connor D, Mehta M, Malinowski H, Lazor J, Huang S-M, Hare D, Lesko L, Sporn D, Williams R. Bioavailability and bioequivalence: an FDA regulatory overview. Pharm Res 2002; 18:1645-1650.
116. Newman SP, Simpson M, Fisher T, Iqbal K. Demonstrating neglible lung deposition for a nasally administered drug formulation containing chitosan. In: Dalby RN, Byron PR, Farr SJ, Peart J, editors. Respiratory Drug Delivery IX, 2004, In Press.
117. Suman J. In search of suitable in vitro/in vivo correlates of intranasal deposition. Presentation to International Society for Aerosols in Medicine conference, Baltimore, 2003.
118. Vogel JS, Turteltaub KW, Finkel R, Nelson DE. Accelerator mass spectrometry-isotope quantification at attomole sensitivity. Anal Chem 1995; 67:A353-A359.
119. Venitz J, Byron PR. Bioequivalence requirements for multiphase nasal sprays-the future for inhalers? In: Dalby RN, Byron PR, Farr SJ, Peart J, editors. Respiratory Drug Delivery VII. Raleigh: Serentec Press, 2000.