Formulation and physiological factors influencing CNS delivery upon intranasal administration

Critical Reviews in Therapeutic Drug Carrier Systems

Volumn 23, Issue 4, 2006, Pages 319-347

  Vyas, Tushar K ^a   Tiwari, Sandip B ^a   Amiji, Mansoor M ^a  

^a NORTHEASTERN UNIVERSITY   (United States)

Author keywords

Blood brain barrier; Central nervous system; Intranasal administration

Indexed keywords

2 HYDROXYPROPYL BETA CYCLODEXTRIN; CARBAMAZEPINE; CARBOMER; CHITOSAN; CLONAZEPAM; DESMOPRESSIN; DIAZEPAM; DIETHYLENE GLYCOL MONOETHYL ETHER; HUMECTANT; HYDROXYPROPYLCELLULOSE; INSULIN; LABRASOL; LIDOCAINE; LIPOSOME; MACROGOL; METHYLCELLULOSE; MICROSPHERE; NICOTINE; NIMODIPINE; NOSE DROPS; NOSE SPRAY; PENTAZOCINE; POLYACRYLIC ACID; RESIN; SALCATONIN; SOMATOMEDIN; SUMATRIPTAN; UNINDEXED DRUG; VASOACTIVE INTESTINAL POLYPEPTIDE; ZOLMITRIPTAN;

AQUEOUS SOLUTION; BLOOD BRAIN BARRIER; DISSOLUTION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG DISTRIBUTION; DRUG DOSAGE FORM; DRUG FORMULATION; DRUG SOLUBILITY; DRUG TRANSPORT; EMULSION; ENZYME ACTIVITY; GEL; GELATION; HUMAN; LIPOPHILICITY; MOLECULAR WEIGHT; MUCOCILIARY CLEARANCE; NONHUMAN; OLFACTORY NERVE; OSMOLARITY; PARTICLE SIZE; PH MEASUREMENT; PHYSICAL CHEMISTRY; REVIEW; SOLUBILIZATION; TRIGEMINAL NERVE;

EID: 34047157527     PISSN: 07434863     EISSN: None     Source Type: Journal    
DOI: 10.1615/CritRevTherDrugCarrierSyst.v23.i4.20     Document Type: Review

References (101)

1. Illum L. Transport of drugs from the nasal cavity to the central nervous system. Eur J Pharm Sci. 2000;11(1):1-18.
2. Vyas TK, Shahiwala A, Marathe S, Misra A. Intranasal drug delivery for brain targeting. Curr Drug Deliv. 2005;2(2):165-75.
3. Loscher W, Potschka H. Role of drug efflux transporters in the brain for drug disposition and treatment of brain diseases. Prog Neurobiol. 2005;76(1):22-76.
4. Misra A, Ganesh S, Shahiwala A, Shah SP. Drug delivery to the central nervous system: a review. J Pharm Pharm Sci. 2003;6(2):252-73.
5. Illum L. Nasal drug delivery: new developments and strategies. Drug Discov Today. 2002;7(23):1184-9.
6. Liu X, Chen C. Strategies to optimize brain penetration in drug discovery. Curr Opin Drug Discov Devel. 2005;8(4):505-12.
7. Sommerville KW. Bioequivalence in development of antiepileptic drugs. Epilepsy Res. 2006;68(1):82-5.
8. Illum L, Watts P, Fisher AN, Hinchcliffe M, Norbury H, Jabbal-Gill I, et al. Intranasal delivery of morphine. J Pharmacol Exp Ther. 2002;301(1):391-400.
9. Dahlof CG. Non-oral formulations of triptans and their use in acute migraine. Curr Pain Headache Rep. 2005;9(3):206-12.
10. Rapoport AM, Bigal ME, Tepper SJ, Sheftell FD. Intranasal medications for the treatment of migraine and cluster headache. CNS Drugs. 2004;18(10):671-85.
11. Brewster ME, Anderson W, Bodor N. Brain, blood, and cerebrospinal fluid distribution of a zidovudine chemical delivery system in rabbits. J Pharm Sci. 1991;80(9):843-6.
12. Brewster ME, Anderson WR, Webb AI, Pablo LM, Meinsma D, Moreno D, Derendorf H, Bodor N, Pop E. Evaluation of a brain-targeting zidovudine chemical delivery system in dogs. Antimicrob Agents Chemother. 1997;41(1):122-8.
13. Benowitz NL. Pharmacology of nicotine: addiction and therapeutics. Annu Rev Pharmacol Toxicol. 1996;36:597-613.
14. Zhang QZ, Jiang XG, Wu CH. Distribution of nimodipine in brain following intranasal administration in rats. Acta Pharmacol Sin. 2004;25(4):522-7.
15. Zhang YJ, Ma CH, Lu WL, Zhang X, Wang XL, Sun JN, Zhang Q. Permeation-enhancing effects of chitosan formulations on recombinant hirudin-2 by nasal delivery in vitro and in vivo. Acta Pharmacol Sin. 2005;26(11):1402-8.
16. Graff CL, Pollack GM. Nasal drug administration: potential for targeted central nervous system delivery. J Pharm Sci. 2005;94(6):1187-95.
17. Eppstein DA, Longenecker JP. Alternative delivery systems for peptides and proteins as drugs. Crit Rev Ther Drug Carrier Syst. 1988;5(2):99-139.
18. Illum L. Is nose-to-brain transport of drugs in man a reality? J Pharm Pharmacol. 2004;56(1):3-17.
19. Illum L. Nasal drug delivery - possibilities, problems and solutions. J Control Release. 2003;87(1-3):187-98.
20. Davis SS, Illum L. Absorption enhancers for nasal drug delivery. Clin Pharmacokinet. 2003;42(13):1107-28.
21. Almeida AJ, Alpar HO. Nasal delivery of vaccines. J Drug Target. 1996;3(6):455-67.
22. Alpar HO, Somavarapu S, Atuah KN, Bramwell VW. Biodegradable mucoadhesive particulates for nasal and pulmonary antigen and DNA delivery. Adv Drug Deliv Rev. 2005;57(3):411-30.
23. Fisher RS, Ho J. Potential new methods for antiepileptic drug delivery. CNS Drugs. 2002;16(9):579-93.
24. Li L, Nandi I, Kim KH. Development of an ethyl laurate-based microemulsion for rapid-onset intranasal delivery of diazepam. Int J Pharm. 2002;237(1-2):77-85.
25. Vyas TK, Babbar AK, Sharma RK, Misra A. Intranasal mucoadhesive microemulsions of zolmitriptan: preliminary studies on brain-targeting. J Drug Target. 2005;13(5):317-24.
26. Agarwal V, Mishra B. Recent trends in drug delivery systems: intranasal drug delivery. Indian J Exp Biol. 1999;37(1):6-16.
27. Aurora J. Development of nasal delivery systems: Ann Review Drug Deliv Tech. 2003;2(7).
28. Jones NS, Quraishi S, Mason JD. The nasal delivery of systemic drugs. Int J Clin Pract. 1997-;51(5):308-11.
29. Wermeling DP, Miller JL, Rudy AC. Systematic intranasal drug delivery: concepts and applications. Drug Deliv Tech. 2002;2(1).
30. Schipper NG, Verhoef JC, Merkus FW. The nasal mucociliary clearance: relevance to nasal drug delivery. Pharm Res. 1991;8(7):807-14.
31. Dhanda DS, Frey WH, II, Leopald D, Kompella UB. Approaches for drug deposition in the human olfactory epithelium. Drug Deliv Tech. 2005;5(4).
32. Hoang VD, Uchenna AR, Mark J, Renaat K, Norbert V. Characterization of human nasal primary culture systems to investigate peptide metabolism. Int J Pharm. 2002;238(1-2):247-56.
33. Al-Ghananeem AM, Traboulsi AA, Ditteert LW, Hussain AA. Targeted brain delivery of 17-β-estradiol via nasally administered water soluble prodrugs. AAPS Pharm Sci Tech 2002;3(1):E5
34. Hussain AA, Al-Bayatti AA, Dakkuri A, Okachi MA, Hussain AA. Testosterone 17-β-N,N-dimethylglycinate hydrochloride. A prodrug with potential for nasal delivery of testosterone. J Pharm Sci, 2002;91(3):785-89.
35. Lee VH, Yamamoto A, Kompella UB. Mucosal penetration enhancers for facilitation of peptide and protein drug absorption. Crit Rev Ther Drug Carrier Syst. 1991;8(2):91-192.
36. Shao Z, Krishnamoorthy R, Mitra AK. Cyclodextrins as nasal absorption promoters of insulin: mechanistic evaluations. Pharm Res. 1992;9(9):1157-63.
37. Tengamnuay P, Mitra AK. Bile salt-fatty acid mixed micelles as nasal absorption promoters of peptides. II. In vivo nasal absorption of insulin in rats and effects of mixed micelles on the morphological integrity of the nasal mucosa. Pharm Res. 1990;7(4):370-5.
38. Frey WH, II. Bypassing the blood-brain barrier to deliver therapeutic agents to the brain and spinal cord. Drug Deliv Tech. 2002;2(5).
39. Agarwal V, Mishra B. Recent trends in drug delivery systems: intranasal drug delivery. Indian J Exp Biol. 1999;37(1):6-16.
40. Thorne RG, Frey WH, II. Delivery of neurotrophic factors to the central nervous system: pharmacokinetic considerations. Clin Pharmacokinet. 2001;40(12):907-46.
41. Thorne RG, Pronk GJ, Padmanabhan V, Frey WH, II. Delivery of insulin-like growth factor-I to the rat brain and spinal cord along olfactory and trigeminal pathways following intranasal administration. Neuroscience. 2004;127(2):481-96.
42. Gizurarson S, Thorvaldsson T, Sigurdsson P, Gunnarsson E. Selective delivery of insulin into the brain: intraolfactory absorption. Int J Pharm. 1996;140(1):77-83.
43. Gizurarson S, Thorvaldsson T, Sigurdsson P, Gunnarsson E. Selective delivery of insulin into the brain: intraolfactory absorption. Int J Pharm. 1997;146(1):135-41.
44. Vidgren MT, Kublik H. Nasal delivery systems and their effect on deposition and absorption. Adv Drug Deliv Rev. 1998;29(1-2):157-77.
45. Newman SP, Moren F, Clarke SW. Deposition pattern from a nasal pump spray. Rhinology. 1987;25(2):77-82.
46. Newman SP, Moren F, Clarke SW. Deposition pattern of nasal sprays in man. Rhinology. 1988;26(2):111-20.
47. Turker S, Onur E, Ozer Y. Nasal route and drug delivery systems. Pharm World Sci. 2004;26(3):137-42.
48. Arora P, Sharma S, Garg S. Permeability issues in nasal drug delivery. Drug Discov Today. 2002;7(18):967-75.
49. Huang CH, Kimura R, Bawarshi-Nassar R, Hussain A. Mechanism of nasal absorption of drugs. II: Absorption of L-tyrosine and the effect of structural modification on its absorption. J Pharm Sci. 1985;74(12):1298-1301.
50. Bodor N, Buchwald P. Brain-targeted drug delivery: experiences to date. Am J Drug Deliv. 2003;1(1) :13-26.
51. Tirucherai GS, Yang C, Mitra AK. Prodrugs in nasal drug delivery. Expert Opin Biol Ther. 2001;1(1):49-66.
52. Doelker E. Crystalline modifications and polymorphism changes during drug manufacture. Ann Pharm Fr. 2002;60(3):161-76.
53. Morissette SL, Almarsson O, Peterson ML, Remenar JF, Read MJ, Lemmo AV, Ellis S, Cima MJ, Gardner CR. High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids. Adv Drug Deliv Rev. 2004;56(3):275-300.
54. Raw AS, Furness MS, Gill DS, Adams RC, Holcombe FO, Jr., Yu LX. Regulatory considerations of pharmaceutical solid polymorphism in Abbreviated New Drug Applications (ANDAs). Adv Drug Deliv Rev. 2004;56(3):397-414.
55. Chien YW SK, Chang S. Nasal systemic drug delivery. New York NY: Marcel Dekker Inc., 1989.
56. Matsuyama T, Morita T, Horikiri Y, Yamahara H, Yoshino H. Enhancement of nasal absorption of large molecular weight compounds by combination of mucolytic agent and nonionic surfactant. J Control Release. 2006;110(2):347-52.
57. Shin BS, Jung JH, Lee KC, Yoo SD. Nasal absorption and pharmacokinetic disposition of salmon calcitonin modified with low molecular weight polyethylene glycol. Chem Pharm Bull (Tokyo). 2004;52(8):957-60.
58. Yu S, Zhao Y, Wu F, Zhang X, Lu W, Zhang H, Zhang Q. Nasal insulin delivery in the chitosan solution: in vitro and in vivo studies. Int J Pharm. 2004;281(1-2):11-23.
59. Jansson B, Hagerstrom H, Fransen N, Edsman K, Bjork E. The influence of gellan gum on the transfer of fluorescein dextran across rat nasal epithelium in vivo. Eur J Pharm Biopharm. 2005;59(3):557-64.
60. Suzuki Y, Makino Y. Mucosal drug delivery using cellulose derivatives as a functional polymer. J Control Release. 1999;62(1-2):101-7.
61. Pitha J, Irie T, Sklar PB, Nye JS. Drug solubilizers to aid pharmacologists: amorphous cyclodextrin derivatives. Life Sci. 1988;43(6):493-502.
62. Shimpi S, Chauhan B, Shimpi P. Cyclodextrins: application in different routes of drug administration. Acta Pharm. 2005;55(2):139-56.
63. Waterman KC, Adami RC, Alsante KM, Hong J, Landis MS, Lombardo F. Stabilization of pharmaceuticals to oxidative degradation. Pharm Dev Technol. 2002;7(1):1-32.
64. Ohtake K, Maeno T, Ueda H, Natsume H, Morimoto Y. Poly-L-arginine predominantly increases the paracellular permeability of hydrophilic macromolecules across rabbit nasal epithelium in vitro. Pharm Res. 2003;20(2):153-60.
65. Lebe E, Baka M, Yavasoglu A, Aktug H, Ates U, Uyanikgil Y. Effects of preservatives in nasal formulations on the mucosal integrity: an electron microscopic study. Pharmacology. 2004;72(2):113-20.
66. Marple B, Roland P, Benninger M. Safety review of benzalkonium chloride used as a preservative in intranasal solutions: an overview of conflicting data and opinions. Otolaryngol Head Neck Surg. 2004;130(1):131-41.
67. Szabadka H. Clinical observations with Paxirasol nasal spray. Ther Hung. 1992;40(1):31-6.
68. Corbo DC, Liu JC, Chien YW. Drug absorption through mucosal membranes: effect of mucosal route and penetrant hydrophilicity. Pharm Res. 1989;6(10):848-52.
69. Mustafa F, Yang T, Khan MA, Ahsan F. Chain length-dependent effects of alkylmaltosides on nasal absorption of enoxaparin. J Pharm Sci. 2004;93(3):675-83.
70. Dale O, Hoffer C, Sheffels P, Kharasch ED. Disposition of nasal, intravenous, and oral methadone in healthy volunteers. Clin Pharmacol Ther. 2002;72(5):536-45.
71. Sachdeva MS, Fulzele SV, Dayal PP. Factors that affect droplet size distribution from nasal sprays using polymeric gel vehicles. Drug Deliv Tech. 2005;5(7), http://www.drugdeliverytech.com/cgi-bin/articles.cgi?idArticle=401
72. http://www.drugdeliverytech.com/cgi-bin/issues.cgi?idIssue=37 (Accessed April 05, 2006)
73. Chilvers MA, O'Callaghan C. Local mucociliary defense mechanisms. Paediatr Respir Rev. 2000;1(1):27-34.
74. Schipper NG, Verhoef JC, Merkus FW. The nasal mucociliary clearance: relevance to nasal drug delivery. Pharm Res. 1991;8(7):807-14.
75. Hoang VD, Uchenna AR, Mark J, Renaat K, Norbert V. Characterization of human nasal primary culture systems to investigate peptide metabolism. Int J Pharm. 2002;238(1-2):247-56.
76. Minn A, Leclerc S, Heydel JM, Minn AL, Denizcot C, Cattarelli M, Netter P, Gradinaru D. Drug transport into the mammalian brain: the nasal pathway and its specific metabolic barrier. J Drug Target. 2002;10(4):285-96.
77. Sarkar MA. Drug metabolism in the nasal mucosa. Pharm Res. 1992;9(1):1-9.
78. Tafaghodi M, Abolghasem Sajadi Tabassi S, Jaafari MR, Zakavi SR, Momen-Nejad M. Evaluation of the clearance characteristics of various microspheres in the human nose by gamma-scintigraphy. Int J Pharm. 2004;280(1-2):125-35.
79. Hardy JG, Lee SW, Wilson CG. Intranasal drug delivery by spray and drops. J Pharm Pharmacol. 1985;37(5):294-7.
80. Ikechukwu Ugwoke M, Kaufmann G, Verbeke N, Kinget R. Intranasal bioavailability of apomorphine from carboxymethylcellulose-based drug delivery systems. Int J Pharm. 2000;202(1-2):125-31.
81. Bertram U, Bodmeier R. In situ gelling, bioadhesive nasal inserts for extended drug delivery: in vitro characterization of a new nasal dosage form. Eur J Pharm Sci. 2006;27(1):62-71.
82. Joshi HM, Bhumkar DR, Joshi K, Pokharkar V, Sastry M. Gold nanoparticles as carriers for efficient transmucosal insulin delivery. Langmuir. 20063;22(1):300-5.
83. 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(1):109-19.
84. Bagger M, Bechgaard E. A microdialysis model to examine nasal drug delivery and olfactory absorption in rats using lidocaine hydrochloride as a model drug. Int J Pharm. 2004;269(2):311-22.
85. Dufes C, Olivier JC, Gaillard F, Gaillard A, Couet W, Muller JM. Brain delivery of vasoactive intestinal peptide (VIP) following nasal administration to rats. Int J Pharm. 2003;255(1-2):87-97.
86. Sankar C, Rani M, Srivastava AK, Mishra B. Chitosan based pentazocine microspheres for intranasal systemic delivery: development and biopharmaceutical evaluation. Pharmazie. 2001;56(3):223-6.
87. Gavini E, Hegge AB, Rassu G, Sanna V, Testa C, Preisino G, Karlsen J, Giunchedi P. Nasal administration of carbamazepine using chitosan microspheres: in vitro/in vivo studies. Int J Pharm. 2006;307(1):9-15.
88. Wang J, Tabata Y, Morimoto K. Aminated gelatin microspheres as a nasal delivery system for peptide drugs: Evaluation of in vitro release and in vivo insulin absorption in rats. J Control Release. 2006 Mar 27; [Epub ahead of print]
89. Terada N, Arakaki R, Okada Y, Kitahara M, Kaneko Y, Omori K, Nishimura K. Efficacy of intranasal desmopressin in the treatment of nocturia due to nocturnal polyuria. Hinyokika Kiyo. 2005;51(3):151-4.
90. Jung BH, Chung BC, Chung SJ, Lee MH, Shim CK. Prolonged delivery of nicotine in rats via nasal administration of proliposomes. J Control Release. 2000;66(1):73-9.
91. Zhang QZ, Jiang XG, Wu CH. Distribution of nimodipine in brain following intranasal administration in rats. Acta Pharmacol Sin. 2004;25(4):522-7.
92. Suman JD. Nasal drug delivery. Expert Opin Biol Ther. 2003;3(3):519-23.
93. Krauland AH, Guggi D, Bernkop-Schnurch A. Thiolated chitosan microparticles: A vehicle for nasal peptide drug delivery. Int J Pharm. 2006;307(2):270-7.
94. Varshosaz J, Sadrai H, Alinagari R. Nasal delivery of insulin using chitosan microspheres. J Microencapsul. 2004;21(7):761-74.
95. Lerner EN, van Zanten EH, Stewart GR. Enhanced delivery of octreotide to the brain via transnasal iontophoretic administration. J Drug Target. 2004;12(5):273-80.
96. Gavini E, Rassu G, Sanna V, Cossu M, Giunchedi P. Mucoadhesive microspheres for nasal administration of an antiemetic drug, metoclopramide: in-vitro/ex-vivo studies. J Pharm Pharmacol. 2005;57(3):287-94.
97. Bertram U, Bodmeier R. In situ gelling, bioadhesive nasal inserts for extended drug delivery: in vitro characterization of a new nasal dosage form. Eur J Pharm Sci. 2006 Jan;27(1):62-71. Epub 2005 Oct 4.
98. Cerchiara T, Luppi B, Chidichimo G, Bigucci F, Zecchi V. Chitosan and poly(methyl vinyl ether-co-maleic anhydride) microparticles as nasal sustained delivery systems. Eur J Pharm Biopharm. 2005;61(3):195-200.
99. Chavanpatil MD, Vavia PR. Nasal drug delivery of sumatriptan succinate. Pharmazie. 2005;60(5):347-9.
100. Vyas TK, Babbar AK, Sharma RK, Singh S, Misra A. Preliminary brain-targeting studies on intranasal mucoadhesive microemulsions of sumatriptan. AAPS Pharm Sci Tech. 2006;7(1):E8.
101. Vyas TK, Babbar AK, Sharma RK, Singh S, Misra A. Intranasal mucoadhesive microemulsions of clonazepam: preliminary studies on brain targeting. J Pharm Sci. 2006;95(3):570-80.