Influence of polymeric microcarriers on the in vivo intranasal uptake of an anti-migraine drug for brain targeting

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 83, Issue 2, 2013, Pages 174-183

  Gavini, Elisabetta ^a   Rassu, Giovanna ^a   Ferraro, Luca ^b   Beggiato, Sarah ^b   Alhalaweh, Amjad ^c   Velaga, Sitaram ^c   Marchetti, Nicola ^b   Bandiera, Pasquale ^a   Giunchedi, Paolo ^a   Dalpiaz, Alessandro ^b  

^a UNIVERSITY OF SASSARI   (Italy)

^b UNIVERSITY OF FERRARA   (Italy)

^c LULEÅ UNIVERSITY OF TECHNOLOGY   (Sweden)

Author keywords

Brain targeting; Chitosan; In vivo studies; Microspheres; Nasal administration; Zolmitriptan

Indexed keywords

CHITOSAN DERIVATIVE; CHITOSAN GLUTAMATE; DRUG CARRIER; HYDROXYPROPYLMETHYLCELLULOSE; MICROSPHERE; POLYMER; UNCLASSIFIED DRUG; ZOLMITRIPTAN; ADHESIVE AGENT; CHITOSAN; GLUTAMIC ACID; OXAZOLIDINONE DERIVATIVE; POWDER; TRYPTAMINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AQUEOUS SOLUTION; AREA UNDER THE CURVE; ARTICLE; BRAIN; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CEREBROSPINAL FLUID LEVEL; DRUG DOSAGE FORM COMPARISON; DRUG HALF LIFE; DRUG PENETRATION; DRUG UPTAKE; EX VIVO STUDY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; INTERMETHOD COMPARISON; MALE; MOLECULAR WEIGHT; MUCOADHESION; NONHUMAN; NOSE MUCOSA; POWDER; RAT; SCANNING ELECTRON MICROSCOPY; SUSPENSION; ADMINISTRATION AND DOSAGE; ANIMAL; CHEMISTRY; DRUG EFFECTS; INTRANASAL DRUG ADMINISTRATION; INTRAVENOUS DRUG ADMINISTRATION; MEDICINAL CHEMISTRY; MIGRAINE DISORDERS; PERMEABILITY; PROCEDURES; SWINE;

ADHESIVES; ADMINISTRATION, INTRANASAL; ADMINISTRATION, INTRAVENOUS; ANIMALS; AREA UNDER CURVE; BRAIN; CHEMISTRY, PHARMACEUTICAL; CHITOSAN; DRUG CARRIERS; GLUTAMIC ACID; HYPROMELLOSE DERIVATIVES; MIGRAINE DISORDERS; NASAL MUCOSA; OXAZOLIDINONES; PERMEABILITY; POLYMERS; POWDERS; SWINE; TRYPTAMINES;

EID: 84873710809     PISSN: 09396411     EISSN: 18733441     Source Type: Journal    
DOI: 10.1016/j.ejpb.2012.10.010     Document Type: Article

References (54)

1. A.M. Rapoport, M.E. Bigal, S.J. Tepper, and F.D. Sheftell Intranasal medications for the treatment of migraine and cluster headache CNS Drugs 18 2004 671 685
2. W.H. Frey II Bypassing the blood-brain barrier to delivery therapeutic agents to the brain and spinal cord Drug Del. Technol. 2 2002 46 49
3. R.G. Thorne, L.R. Hanson, T.M. Ross, D. Tung, and W.H. Frey II Delivery of interferon-β to the monkey nervous system following intranasal administration Neuroscience 152 2008 785 797
4. D.A. Wolf, L.R. Hanson, E.L. Aronovich, Z. Nan, W.C. Low, W.H. Frey II, and R.S. McIvor Lysosomal enzyme can bypass the blood-brain barrier and reach the CNS following intranasal administration Mol. Genet. Metab. 106 2012 131 134
5. A. Rapoport, and P. Winner Nasal delivery of antimigraine drugs: clinical rationale and evidence base Headache 46 2006 192 201
6. C.G.H. Dahlöf, M. Linde, and E. Kerekes Zolmitriptan nasal spray provides fast relief of migraine symptoms and is preferred by patients: a Swedish study of preference in clinical practice J. Headache Pain. 5 2004 237 242
7. R. Yates, K. Nairn, R. Dixon, and E. Seaber Preliminary studies of the pharmacokinetics and tolerability of zolmitriptan nasal spray in healthy volunteers J. Clin. Pharmacol. 42 2002 1237 1243
8. M.E. Bigal, C.A. Bordini, A.L. Antoniazzi, and J.G. Speciali The triptan formulations: a critical evaluation Arq. Neuro-Psiquiatr. 61 2003 313 320
9. P.J. Goadsby, and R. Yates Zolmitriptan intranasal: a review of the pharmacokinetics and clinical efficacy Headache 46 2006 138 149
10. S. Horvát, A. Fehér, H. Wolburg, P. Sipos, S. Veszelka, A. Tóth, L. Kis, A. Kurunczi, G. Balogh, L. Kürti, I. Ers, P. Szabó-Révész, and M.A. Deli Sodium hyaluronate as a mucoadhesive component in nasal formulation enhances delivery of molecules to brain tissue Eur. J. Pharm. Biopharm. 72 2009 252 259
11. A. Mistry, S. Stolnik, and L. Illum Nanoparticles for direct nose-to-brain delivery of drugs Int. J. Pharm. 379 2009 146 157
12. T.K. Vyas, A.K. Babbar, R.K. Sharma, and A. Misra Intranasal mucoadhesive microemulsions of zolmitriptan: preliminary studies on brain-targeting J. Drug Target. 13 2005 317 324
13. C. Yu, P. Gu, W. Zhang, C. Cai, H. He, and X. Tang Evaluation of submicron emulsion as vehicles for rapid-onset intranasal delivery and improvement in brain targeting of zolmitriptan Drug Deliv. 18 2011 578 585
14. C. Yu, P. Gu, W. Zhang, N. Qi, C. Cai, H. He, and X. Tang Preparation and evaluation of zolmitriptan submicron emulsion for rapid and effective nasal absorption in beagle dogs Drug Dev. Ind. Pharm. 37 2011 1509 1516
15. R. Jain, S. Nabar, P. Dandekar, and V. Patravale Micellar nanocarriers: potential nose-to-brain delivery of zolmitriptan as novel migraine therapy Pharm. Res. 27 2010 655 664
16. H. Kublik, and M.T. Vidgren Nasal delivery systems and their effect on deposition and absorption Adv. Drug Del. Rev. 29 1998 157 177
17. E. Marttin, S.G. Romeijn, J.C. Verhoef, and F.W.H.M. Merkus Nasal absorption of dihydroergotamine from liquid and powder formulations in rabbits J. Pharm. Sci. 86 1997 802 807
18. W. Wang Instability, stabilization, and formulation of liquid protein pharmaceuticals Int. J. Pharm. 185 1999 129 188
19. D.S. Dhanda, W.H. Frey II, D. Leopold, and U.B. Kompella Approaches for drug deposition in the human olfactory epithelium Drug Del. Technol. 5 2005 64 72
20. H.R. Costantino, L. Illum, G. Brandt, P.H. Johnson, and S.C. Quay Intranasal delivery: physicochemical and therapeutic aspects international Int. J. Pharm. 337 2007 1 24
21. A. Dalpiaz, E. Gavini, G. Colombo, P. Russo, F. Bortolotti, L. Ferraro, S. Tanganelli, A. Scatturin, E. Menegatti, and P. Giunchedi Brain uptake of an antiischemic agent by nasal administration of microparticles J. Pharm. Sci. 97 2008 4889 4903
22. S.M. Wang, K. Inthavong, J. Wen, J.Y. Tu, and C.L. Xue Comparison of micron- and nanoparticle deposition patterns in a realistic human nasal cavity Respir. Physiol. Neurobiol. 166 2009 142 151
23. S.V. Dhuria, L.R. Hanson, and W.H. Frey II Intranasal delivery to the central nervous system: mechanisms and experimental considerations J. Pharm. Sci. 99 2010 1654 1673
24. R.J. Soane, M. Frier, A.C. Perkins, N.S. Jones, S.S. Davis, and L. Illum Evaluation of the clearance characteristics of bioadhesive systems in humans Int. J. Pharm. 178 1999 55 65
25. M.I. Ugwoke, R.U. Agu, N. Verbeke, and R. Kinget Nasal mucoadhesive drug delivery: background, applications, trends and future perspectives Adv. Drug Del. Rev. 57 2005 1640 1665
26. S.T. Charlton, S.S. Davis, and L. Illum Evaluation of bioadhesive polymers as delivery systems for nose to brain delivery: In vitro characterization studies J. Control. Release 118 2007 225 234
27. S.T. Charlton, N.S. Jones, S.S. Davis, and L. Illum Distribution and clearance of bioadhesive formulations from the olfactory region in man: effect of polymer type and nasal delivery device Eur. J. Pharm. Sci. 30 2007 295 302
28. S.T. Charlton, S.S. Davis, and L. Illum Nasal administration of an angiotensin antagonist in the rat model: effect of bioadhesive formulations on the distribution of drugs to the systemic and central nervous systems Int. J. Pharm. 338 2007 94 103
29. E. Gavini, G. Rassu, L. Ferraro, A. Generosi, J.V. Rau, A. Brunetti, P. Giunchedi, and A. Dalpiaz Influence of chitosan glutamate on the in vivo intranasal absorption of rokitamycin from microspheres J. Pharm. Sci. 100 2011 1488 1502
30. A. Alhalaweh, S. Andersson, and S.P. Velaga Preparation of zolmitriptan-chitosan microparticles by spray drying for nasal delivery Eur. J. Pharm. Sci. 38 2009 206 214
31. A. Alhalaweh, A. Vilinska, E. Gavini, G. Rassu, and S. Velaga Surface thermodynamics of mucoadhesive dry powder formulation of zolmitriptan AAPS PharmSciTech 12 2011 1186 1192
32. E. Gavini, G. Rassu, V. Sanna, M. Cossu, and P. Giunchedi Mucoadhesive microspheres for nasal administration of an antiemetic drug, metoclopramide: in vitro/ex vivo studies J. Pharm. Pharmacol. 57 2005 287 294
33. E. Gavini, G. Rassu, T. Haukvik, C. Lanni, M. Racchi, and P. Giunchedi Mucoadhesive microspheres for nasal administration of cyclodextrins J. Drug Target. 17 2009 168 179
34. M. Cossu, E. Gavini, G. Rassu, C. Juliano, P. Giunchedi, A New diffusion system for the evaluation of transmucosal permeation across synthetic or biological membranes, in: Proceedings of Innovation in Drug Delivery: from Biomaterials to Devices, Naples, Italy, 2007. p. 343.
35. E. Gavini, G. Spada, G. Rassu, G. Cerri, A. Brundu, M. Cossu, M. Sorrenti, and P. Giunchedi Development of solid nanoparticles based on hydroxypropyl-beta-cyclodextrin aimed for the colonic transmucosal delivery of diclofenac sodium J. Pharm. Pharmacol. 63 2011 472 482
36. E.M. Clement, and M. Franklin Simultaneous measurement of zolmitriptan and its major metabolites N-desmethyl zolmitriptan and zolmitriptan N-oxide in human plasma by high performance liquid chromatography with coulometric detection J. Chromatogr. B: Biomed. Sci. Appl. 766 2002 339 343
37. A. Dalpiaz, N. Marchetti, A. Cavazzini, L. Pasti, S. Velaga, E. Gavini, S. Beggiato, and L. Ferraro Quantitative determination of zolmitriptan in rat blood and cerebrospinal fluid by reversed phase HPLC-esi-ms/ms analysis: application to in vivo preclinical pharmacokinetic study J. Chromatogr. B 901 2012 72 78
38. A. Hubaux, and G. Vos Decision and detection limits for linear calibration curves Anal. Chem. 42 1970 849 855
39. M.P. van den Berg, S.G. Romeijn, J.C. Verhoef, and F.W. Merkus Serial cerebrospinal fluid sampling in a rat model to study drug uptake from the nasal cavity J. Neurosci. Methods 116 2002 99 107
40. J.L. Meek, and N.H. Neff Is cerebrospinal fluid the major avenue for the removal of 5-hydroxyindoleacetic acid from the brain? Neuropharmacology 12 1973 497 499
41. H. Davson, K. Welch, and M.B. Segal The secretion of the cerebrospinal fluid H. Davson, K. Welch, M.B. Segal, Anonymous Physiology and Pathophysiology of the Cerebrospinal Fluid 1987 Churchill Livingstone London, England 189 246
42. C. Sacchetti, M. Artusi, P. Santi, and P. Colombo Caffeine microparticles for nasal administration obtained by spray drying Int. J. Pharm. 242 2002 335 339
43. E. Gavini, G. Rassu, C. Muzzarelli, M. Cossu, and P. Giunchedi Spray-dried microspheres based on methylpyrrolidinone chitosan as new carrier for nasal administration of metoclopramide Eur. J. Pharm. Biopharm. 68 2008 245 252
44. B. Luppi, F. Bigucci, T. Cerchiara, and V. Zecchi Chitosan-based hydrogels for nasal drug delivery: from inserts to nanoparticles Expert Opin. Drug Deliv. 7 2010 811 828
45. P. Sinswat, and P. Tengamnuay Enhancing effect of chitosan on nasal absorption of salmon calcitonin in rats: comparison with hydroxypropyl- and dimethyl-beta-cyclodextrins Int. J. Pharm. 257 2003 15 22
46. L. Na, S. Mao, J. Wang, and W. Sun Comparison of different absorption enhancers on the intranasal absorption of isosorbide dinitrate in rats Int. J. Pharm. 397 2010 59 66
47. G. Borchard, H.L. Lueßen, G.A. De Boer, J. Coos Verhoef, C.M. Lehr, and H.E. Junginger The potential of mucoadhesive polymers in enhancing intestinal peptide drug absorption. III. Effects of chitosan glutamate and carbomer on epithelial tight junctions in vitro J. Control. Release 39 1996 131 138
48. M.A. Deli Potential use of tight junction modulators to reversibly open membranous barriers and improve drug delivery Biochim. Biophys. Acta 1788 2009 892 910
49. D. Mei, S.R. Mao, W. Sun, Y.J. Wang, and T. Kissel Effect of chitosan structure properties and molecular weight on the intranasal absorption of tetramethylpyrazine phosphate in rats Eur. J. Pharm. Biopharm. 70 2008 874 881
50. E. Hagesaether Permeation modulating properties of natural polymers-effect of molecular weight and mucus Int. J. Pharm. 409 2011 150 155
51. E.J. Seaber, R.W. Peck, D.A. Smith, J. Allanson, N.R. Hefting, J.J. van Lier, F.A.E. Sollie, J. Wermer, and J.H.G. Jonkman The absolute bioavailability and effect on food on the pharmacokinetics of zolmitriptan in healthy volunteers Br. J. Clin. Pharmacol. 46 1998 433 439
52. B.R. Charlesworth, A.J. Dowson, A. Purdy, W.J. Becker, S. Boes-Hansen, and M. Farkkila Speed of onset and efficacy of zolmitriptan nasal spray in the acute treatment of migraine: a double-blind, placebo controlled, dose-ranging study versus zolmitriptan tablet CNS Drugs 17 2003 653 667
53. S.T. Lim, B. Forbes, D.J. Berry, G.P. Martin, and M.B. Brown In vivo evaluation of novel hyaluronan/chitosan microparticulate delivery systems for the nasal delivery of gentamicin in rabbits Int. J. Pharm. 231 2002 73 82
54. L. Illum Nasal drug delivery-possibilities, problems and solutions J. Control. Release 87 2003 187 198