Pulmonary pharmacokinetics of levofloxacin in rats after aerosolization of immediate-release chitosan or sustained-release PLGA microspheres

European Journal of Pharmaceutical Sciences

Volumn 93, Issue , 2016, Pages 184-191

  Gaspar, Marisa C ^a,b,c   Grégoire, Nicolas ^c,d   Sousa, João J S ^a,b   Pais, Alberto A C C ^e   Lamarche, Isabelle ^c,d   Gobin, Patrice ^c,f   Olivier, Jean Christophe ^c,d   Marchand, Sandrine ^c,d,f   Couet, William ^c,d,f  

^a UNIVERSITY OF COIMBRA   (Portugal)

^b UNIVERSITY OF COIMBRA   (Portugal)

^c INSERM   (France)

^d UNIVERSITÉ DE POITIERS   (France)

^e UNIVERSITY OF COIMBRA   (Portugal)

^f POITIERS UNIVERSITY HOSPITAL   (France)

Author keywords

Chitosan; Levofloxacin; Microsphere; PLGA; Pulmonary delivery; Pulmonary pharmacokinetics; Sustained release

Indexed keywords

CHITOSAN; CIPROFLOXACIN; LEVOFLOXACIN; MICROSPHERE; POLYGLACTIN; AEROSOL; ANTIINFECTIVE AGENT; DELAYED RELEASE FORMULATION; LACTIC ACID; POLYGLYCOLIC ACID; POLYLACTIC ACID-POLYGLYCOLIC ACID COPOLYMER;

AEROSOL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; COMPARATIVE STUDY; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DIFFUSION; DRUG FORMULATION; DRUG PENETRATION; DRUG RELEASE; DRUG SOLUTION; DRY POWDER; EPITHELIAL LINING FLUID; IMMEDIATE RELEASE FORMULATION; IN VITRO STUDY; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; SUSTAINED RELEASE FORMULATION; TIME TO MAXIMUM PLASMA CONCENTRATION; VOLUME OF DISTRIBUTION; ADMINISTRATION AND DOSAGE; ANIMAL; BLOOD; CHEMISTRY; DELAYED RELEASE FORMULATION; INHALATIONAL DRUG ADMINISTRATION; PHARMACOKINETICS; SPRAGUE DAWLEY RAT;

ADMINISTRATION, INHALATION; AEROSOLS; ANIMALS; ANTI-BACTERIAL AGENTS; CHITOSAN; DELAYED-ACTION PREPARATIONS; LACTIC ACID; LEVOFLOXACIN; MALE; MICROSPHERES; POLYGLYCOLIC ACID; RATS, SPRAGUE-DAWLEY;

EID: 84983350474     PISSN: 09280987     EISSN: 18790720     Source Type: Journal    
DOI: 10.1016/j.ejps.2016.08.024     Document Type: Article

References (34)

1. Anderson, J.M., Shive, M.S., Biodegradation and biocompatibility of PLA and PLGA microspheres. Adv. Drug Deliv. Rev. 28:1 (1997), 5–24, 10.1016/S0169-409X(97)00048-3.
2. Beal, S.L., Ways to fit a PK model with some data below the quantification limit. J. Pharmacokinet. Pharmacodyn. 28:5 (2001), 481–504.
3. Brillault, J., De Castro, W.V., Couet, W., Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model. Antimicrob. Agents Chemother. 54:1 (2010), 543–545, 10.1128/aac.00733-09.
4. Bulitta, J.B., Bingölbali, A., Shin, B.S., Landersdorfer, C.B., Development of a new pre- and post-processing tool (SADAPT-TRAN) for nonlinear mixed-effects modeling in S-ADAPT. AAPS J. 13:2 (2011), 201–211, 10.1208/s12248-011-9257-x.
5. Díez, S., Tros de Ilarduya, C., Versatility of biodegradable poly(D,L-lactic-co-glycolic acid) microspheres for plasmid DNA delivery. Eur. J. Pharm. Biopharm. 63:2 (2006), 188–197, 10.1016/j.ejpb.2006.03.007.
6. Doan, T.V.P., Olivier, J.C., Preparation of rifampicin-loaded PLGA microspheres for lung delivery as aerosol by premix membrane homogenization. Int. J. Pharm. 382:1–2 (2009), 61–66, 10.1016/j.ijpharm.2009.08.008.
7. Doan, T.V., Couet, W., Olivier, J.C., Formulation and in vitro characterization of inhalable rifampicin-loaded PLGA microspheres for sustained lung delivery. Int. J. Pharm. 414:1–2 (2011), 112–117, 10.1016/j.ijpharm.2011.05.007.
8. Doan, T.V.P., Grégoire, N., Lamarche, I., Gobin, P., Marchand, S., Couet, W., et al. A preclinical pharmacokinetic modeling approach to the biopharmaceutical characterization of immediate and microsphere-based sustained release pulmonary formulations of rifampicin. Eur. J. Pharm. Sci. 48:1–2 (2013), 223–230, 10.1016/j.ejps.2012.10.024.
9. EMA, Quinsair - Summary of Product Characteristics. 2015, European Medicines Agency, Science Medicines Health (http://ec.europa.eu/health/documents/community-register/2015/20150326130815/anx_130815_en.pdf. Accessed 26 October 2015).
10. Feng, T., Tian, H., Xu, C., Lin, L., Xie, Z., Lam, M.H.-W., et al. Synergistic co-delivery of doxorubicin and paclitaxel by porous PLGA microspheres for pulmonary inhalation treatment. Eur. J. Pharm. Biopharm. 88:3 (2014), 1086–1093, 10.1016/j.ejpb.2014.09.012.
11. Foundation, C.F., Drug Development Pipeline. 2015 Accessed 27 October 2015.
12. Gagnadoux, F., Pape, A.L., Lemarie, E., Lerondel, S., Valo, I., Leblond, V., et al. Aerosol delivery of chemotherapy in an orthotopic model of lung cancer. Eur Respir J. 26:4 (2005), 657–661.
13. Gaspar, M.C., Couet, W., Olivier, J.C., Pais, A.A.C.C., Sousa, J.J.S., Pseudomonas aeruginosa infection in cystic fibrosis lung disease and new perspectives of treatment: a review. Eur. J. Clin. Microbiol. Infect. Dis. 32:10 (2013), 1231–1252, 10.1007/s10096-013-1876-y.
14. Gaspar, M.C., Sousa, J.J.S., Pais, A.A.C.C., Cardoso, O., Murtinho, D., Serra, M.E.S., et al. Optimization of levofloxacin-loaded crosslinked chitosan microspheres for inhaled aerosol therapy. Eur. J. Pharm. Biopharm. 96 (2015), 65–75, 10.1016/j.ejpb.2015.07.010.
15. Geller, D.E., Aerosol antibiotics in cystic fibrosis. Respir. Care 54:5 (2009), 658–670.
16. Geller, D.E., Flume, P.A., Staab, D., Fischer, R., Loutit, J.S., Conrad, D.J., Levofloxacin inhalation solution (MP-376) in patients with cystic fibrosis with Pseudomonas aeruginosa. Am. J. Respir. Crit. Care Med. 183:11 (2011), 1510–1516, 10.1164/rccm.201008-1293OC.
17. Gontijo, A.V.L., Brillault, J., Grégoire, N., Lamarche, I., Gobin, P., Couet, W., et al. Biopharmaceutical characterization of nebulized antimicrobial agents in rats: 1. Ciprofloxacin, moxifloxacin, and grepafloxacin. Antimicrob. Agents Chemother. 58:7 (2014), 3942–3949, 10.1128/aac.02818-14.
18. Govender, T., Stolnik, S., Garnett, M.C., Illum, L., Davis, S.S., PLGA nanoparticles prepared by nanoprecipitation: drug loading and release studies of a water soluble drug. Journal of Controlled Release. 57:2 (1999), 171–185, 10.1016/S0168-3659(98)00116–3.
19. Hirota, K., Kawamoto, T., Nakajima, T., Makino, K., Terada, H., Distribution and deposition of respirable PLGA microspheres in lung alveoli. Colloids Surf. B: Biointerfaces 105 (2013), 92–97, 10.1016/j.colsurfb.2012.12.027.
20. Hoppentocht, M., Hagedoorn, P., Frijlink, H.W., de Boer, A.H., Developments and strategies for inhaled antibiotic drugs in tuberculosis therapy: a critical evaluation. Eur. J. Pharm. Biopharm. 86:1 (2014), 23–30, 10.1016/j.ejpb.2013.10.019.
21. Hurtado, F.K., Weber, B., Derendorf, H., Hochhaus, G., Dalla, C.T., Population pharmacokinetic modeling of the unbound levofloxacin concentrations in rat plasma and prostate tissue measured by microdialysis. Antimicrob. Agents Chemother. 58:2 (2014), 678–686, 10.1128/aac.01884-13.
22. King, P., Lomovskaya, O., Griffith, D.C., Burns, J.L., Dudley, M.N., In vitro pharmacodynamics of levofloxacin and other aerosolized antibiotics under multiple conditions relevant to chronic pulmonary infection in cystic fibrosis. Antimicrob. Agents Chemother. 54:1 (2010), 143–148, 10.1128/aac.00248-09.
23. Kirkby, S., Novak, K., McCoy, K., Aztreonam (for inhalation solution) for the treatment of chronic lung infections in patients with cystic fibrosis: an evidence-based review. Core Evidence 6 (2011), 59–66.
24. Koeppe, M.O., Cristofoletti, R., Fernandes, E.F., Storpirtis, S., Junginger, H.E., Kopp, S., et al. Biowaiver monographs for immediate release solid oral dosage forms: levofloxacin. J. Pharm. Sci. 100:5 (2011), 1628–1636.
25. Marchand, S., Gobin, P., Brillault, J., Baptista, S., Adier, C., Olivier, J.-C., et al. Aerosol therapy with colistin methanesulfonate: a biopharmaceutical issue illustrated in rats. Antimicrob. Agents Chemother. 54:9 (2010), 3702–3707, 10.1128/aac.00411-10.
26. Ramazani, F., Chen, W., Van Nostrum, C.F., Storm, G., Kiessling, F., Lammers, T., et al. Formulation and characterization of microspheres loaded with imatinib for sustained delivery. Int. J. Pharm. 482:1–2 (2015), 123–130, 10.1016/j.ijpharm.2015.01.043.
27. Saelim, N., Suksawaeng, K., Chupan, J., Techatanawat, I., Biopharmaceutics classification system (BCS)-based biowaiver for immediate release solid oral dosage forms of moxifloxacin hydrochloride (moxiflox GPO) manufactured by the government pharmaceutical organization (GPO). Asian Journal of Pharmaceutical Sciences., 2015, 10.1016/j.ajps.2015.11.016.
28. Sah, E., Sah, H., Recent trends in preparation of poly(lactide-co-glycolide) nanoparticles by mixing polymeric organic solution with antisolvent. J. Nanomater., 2015, 2015, 22, 10.1155/2015/794601.
29. Sawicki, G.S., Signorovitch, J.E., Zhang, J., Latremouille-Viau, D., von Wartburg, M., Wu, E.Q., et al. Reduced mortality in cystic fibrosis patients treated with tobramycin inhalation solution. Pediatr. Pulmonol. 47:1 (2012), 44–52, 10.1002/ppul.21521.
30. Seral, C., Barcia-Macay, M., Mingeot-Leclercq, M.P., Tulkens, P.M., Van Bambeke, F., Comparative activity of quinolones (ciprofloxacin, levofloxacin, moxifloxacin and garenoxacin) against extracellular and intracellular infection by Listeria monocytogenes and Staphylococcus aureus in J774 macrophages. J. Antimicrob. Chemother. 55:4 (2005), 511–517, 10.1093/jac/dki059.
31. Shen, J., Burgess, D.J., Accelerated in vitro release testing methods for extended release parenteral dosage forms. J. Pharm. Pharmacol. 64:7 (2012), 986–996, 10.1111/j.2042-7158.2012.01482.x.
32. Stockmann, C., Sherwin, C.M.T., Ampofo, K., Spigarelli, M.G., Development of levofloxacin inhalation solution to treat Pseudomonas aeruginosa in patients with cystic fibrosis. Ther. Adv. Respir. Dis. 8:1 (2014), 13–21, 10.1177/1753465813508445.
33. Traini, D., Young, P.M., Delivery of antibiotics to the respiratory tract: an update. Expert Opinion on Drug Delivery. 6:9 (2009), 897–905, 10.1517/17425240903110710.
34. Zimmermann, E.S., Laureano, J.V., dos Santos, C.N., Schmidt, S., Lagishetty, C.V., de Castro, W.V., et al. A simultaneous semi-mechanistic population analysis of levofloxacin in plasma, lung and prostrate to describe the influence of efflux transporters on drug distribution following intravenous and intratracheal administration. Antimicrob. Agents Chemother., 2015, 10.1128/aac.02317-15.