Abstract
Tiotropium, a longer acting anticholinergic bronchodilator, has been widely used for treatment of chronic obstructive pulmonary disease (COPD). To improve the therapeutic effect of tiotropium, we developed various inhalation microparticular formulations of tiotropium using starch, hyaluronate, bovine serum albumin (BSA), and poly(lactide-co-glycolide) (PLGA). All formulations showed ~90 % inhalation efficiency in the lung epithelium of BALB/c mice after initial administration. Interestingly, when compared to other formulations using starch, hyaluronate, and BSA, the inhalation formulation of tiotropium using PLGA showed longer drug residence (up to 7 days) in in vivo lung epithelium. We believe that this microparticle system is expected to improve the treatment efficacy for the patients with COPD by maintaining drug therapeutic effect during the extended period after initial inhalation.
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References
Barnes PJ (2004) Mediators of chronic obstructive pulmonary disease. Pharmacol Rev 56:515–548
Bivas-Benita M, Zwier R, Junginger HE, Borchard G (2005) Non-invasive pulmonary aerosol delivery in mice by the endotracheal route. Eur J Pharm Biopharm 61:214–218
Disse B, Speck GA, Rominger KL, Witek TJ Jr, Hammer R (1999) Tiotropium (Spiriva): mechanistical considerations and clinical profile in obstructive lung disease. Life Sci 64:457–464
Halbert RJ, Natoli JL, Gano A, Badamgarav E, Buist AS, Mannino DM (2006) Global burden of COPD: systematic review and meta-analysis. Eur Respir J 28:523–532
Knoell DL (2007) Anticholinergic medications for COPD. P&T 32:150–159
Koumis T, Samuel S (2005) Tiotropium bromide: a new long-acting bronchodilator for the treatment of chronic obstructive pulmonary disease. Clin Ther 27:377–392
Lee ES, Na K, Bae YH (2005) Doxorubicin loaded pH-sensitive polymeric micelles for reversal of resistant MCF-7 tumor. J Control Release 103:405–418
Lopez AD, Murray CC (1998) The global burden of disease, 1990–2020. Nat Med 4:1241–1243
Mahoney BP, Raghunand N, Baggett B, Gillies RJ (2003) Tumor acidity, ion trapping and chemotherapeutics. I. Acid pH affects the distribution of chemotherapeutic agents in vitro. Biochem Pharmacol 66:1207–1218
Mundargi RC, Babu VR, Rangaswamy V, Patel P, Aminabhavi TM (2008) Nano/micro-technologies for delivering macromolecular therapeutics using poly(d,l-lactide-co-glycolide) and its derivatives. J Control Release 125:193–209
Pauwels RA, Rabe KF (2004) Burden and clinical features of chronic obstructive pulmonary disease (COPD). Lancet 364:613–620
Wang J, Jiang Y, Wang Y, Li H, Fawcett JP, Gu J (2007) Highly sensitive assay for tiotropium, a quaternary ammonium, in human plasma by high-performance liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom 21:1755–1758
Yoo NY, Youn YS, Oh NM, Oh KT, Lee DK, Cha KH, Oh YT, Lee ES (2011) Antioxidant encapsulated porous poly(lactide-co-glycolide) microparticles for developing long acting inhalation system. Colloids Surf B 88:419–424
Acknowledgments
This work was financially supported by the GRRC Program of Gyeonggi Province [GRRC 2012-B01, Development of industrial nano-/micro-sized biomaterials for high performance drug release control].
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Oh, N.M., Oh, K.T., Youn, Y.S. et al. Development of tiotropium inhalation formulations for the treatment of chronic obstructive pulmonary disease. Journal of Pharmaceutical Investigation 43, 71–74 (2013). https://doi.org/10.1007/s40005-013-0054-7
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DOI: https://doi.org/10.1007/s40005-013-0054-7