Advanced spray-dried design, physicochemical characterization, and aerosol dispersion performance of vancomycin and clarithromycin multifunctional controlled release particles for targeted respiratory delivery as dry powder inhalation aerosols

International Journal of Pharmaceutics

Volumn 455, Issue 1-2, 2013, Pages 374-392

  Park, Chun Woong ^a,b   Li, Xiaojian ^a   Vogt, Frederick G ^c   Hayes, Don ^d   Zwischenberger, Joseph B ^e   Park, Eun Seok ^f   Mansour, Heidi M ^a,g,h  

^a University of Kentucky   (United States)

^b Chungbuk National University   (South Korea)

^c GLAXOSMITHKLINE   (United States)

^d THE OHIO STATE UNIVERSITY COLLEGE OF MEDICINE   (United States)

^e UNIVERSITY OF KENTUCKY   (United States)

^f Sungkyunkwan University   (South Korea)

^g UNIVERSITY OF KENTUCKY   (United States)

^h UNIVERSITY OF ARIZONA   (United States)

Author keywords

Aerosol performance enhancer; Antibiotic; Controlled release lung delivery; Dipalmitoylphosphatidylcholine (DPPC); Particle engineering design; Solid state

Indexed keywords

CLARITHROMYCIN; DIPALMITOYLPHOSPHATIDYLCHOLINE; LUNG SURFACTANT; METHANOL; PHOSPHOLIPID; VANCOMYCIN;

AEROSOL; ARTICLE; CONFOCAL MICROSCOPY; CONTROLLED RELEASE FORMULATION; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DRUG DELIVERY SYSTEM; DRY POWDER INHALER; EXPERIMENTAL DESIGN; GRAVIMETRY; LASER DIFFRACTION; MICROSCOPY; PHOSPHOLIPID BILAYER; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; RAMAN SPECTROMETRY; SCANNING ELECTRON MICROSCOPY; SOLID STATE; SPRAY DRYING; TITRIMETRY; X RAY POWDER DIFFRACTION;

AEROSOL PERFORMANCE ENHANCER; ANTIBIOTIC; CONTROLLED RELEASE LUNG DELIVERY; DIPALMITOYLPHOSPHATIDYLCHOLINE (DPPC); PARTICLE ENGINEERING DESIGN; SOLID-STATE;

1,2-DIPALMITOYLPHOSPHATIDYLCHOLINE; AEROSOLS; ANTI-BACTERIAL AGENTS; CLARITHROMYCIN; DELAYED-ACTION PREPARATIONS; DESICCATION; DRUG COMPOUNDING; DRY POWDER INHALERS; VANCOMYCIN;

EID: 84884124961     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2013.06.047     Document Type: Article

References (71)

1. 2006. <601> Aerosols, Nasal Sprays, Metered-Dose Inhalers, and Dry Powder Inhalers Monograph, USP 29-NF 24 The United States Pharmacopoeia and The National Formulary: The Official Compendia of Standards. The United States Pharmacopeial Convention, Inc., Rockville, MD, pp. 2617-2636.
2. Acerbi, D., Brambilla, G., Kottakis, I., 2007. Advances in asthma and COPD management: delivering CFC-free inhaled therapy using Modulite® technology. Pulm. Pharmacol. Ther. 20, 290-303. (Pubitemid 46242202)
3. Adi, H., Young, P.M., Chan, H.-K., Agus, H., Traini, D., 2010a. Co-spray-dried mannitol-ciprofloxacin dry powder inhaler formulation for cystic fibrosis and chronic obstructive pulmonary disease. Eur. J. Pharm. Sci. 40, 239-247.
4. Adi, H., Young, P.M., Chan, H.K., Salama, R., Traini, D., 2010b. Controlled release antibiotics for dry powder lung delivery. Drug. Dev. Ind. Pharm. 36, 119-126.
5. Alves, G.P., Santana, M.H.A., 2004. Phospholipid dry powders produced by spray drying processing: structural, thermodynamic and physical properties. Powder Technol. 145, 139-148. (Pubitemid 39208838)
6. Ameri, M., Maa, Y.-F., 2006. Spray drying of biopharmaceuticals: stability and process considerations. Dry. Technol. 24, 763-768. (Pubitemid 43820928)
7. Arifin, D.Y., Lee, L.Y., Wang, C.-H., 2006. Mathematical modeling and simulation of drug release from microspheres: implications to drug delivery systems. Adv. Drug Deliver. Rev. 58, 1274-1325.
8. Batts, D.H., Martin, D., Holmes, R., Silva, J., Fekety, F.R., 1980. Treatment of antibiotic-associated Clostridium difficile diarrhea with oral vancomycin. J. Pediatr. 97, 151-153. (Pubitemid 10033788)
9. Carvalho, T.C., Carbalho, S.R., McConville, J.T., 2011. Formulations for pulmonary administration of anticancer agents to treat lung malignancies. J. Aerosol Med. Pulm. Drug Deliv. 24, 61-80.
10. Clark, A.R., Wolff, R.K., Eldon, M.A., Dwivedi, S.K., Anthony, W., 2006. The Application of Pulmonary Inhalation Technology to Drug Discovery, Annual Reports in Medicinal Chemistry. Academic Press, pp. 383-393.
11. Costa, P., Sousa Lobo, J.M., 2001. Modeling and comparison of dissolution profiles. Eur. J. Pharm. Sci. 13, 123-133. (Pubitemid 32288781)
12. Cruz, L.i., Soares, L.U., Costa, T.D., Mezzalira, G., da Silveira, N.P., Guterres, S.v.S., Pohlmann, A.R., 2006. Diffusion and mathematical modeling of release profiles from nanocarriers. International Journal of Pharmaceutics 313, 198-205.
13. Ei-Arini, S.K., Leuenberger, H., 1995. Modelling of drug release from polymer matrices: effect of drug loading. International Journal of Pharmaceutics 121, 141-148.
14. Finlay, W., 2008. The ARLA Respiratory Deposition Calculator, Retrieved 2010 from http://www.mece.ualberta.ca/arla/impactor mmad calculator.html
15. Forbes, B., Asgharian, B., Dailey, L.A., Ferguson, D., Gerde, P., Gumbleton, M., Gustavsson, L., Hardy, C., Hassall, D., Jones, R., Lock, R., Maas, J., McGovern, T., Pitcairn, G.R., Somers, G., Wolff, R.K., 2011. Challenges in inhaled product development and opportunities for open innovation. Adv. Drug Deliver. Rev. 63, 69-87.
16. Furuta, I., Kitahashi, T., Kuroda, T., Nishio, H., Oka, C., Morishima, Y., 2000. Rapid serum vancomycin assay by high-performance liquid chromatography using a semipermeable surface packing material column. Clin. Chim. Acta 301, 31-39.
17. Ganguly, S., Moolchandani, V., Roche, J.A., Shapiro, P.S., Somaraju, S., Eddington, N.D., Dalby, R.N., 2008. Phospholipid-induced in vivo particle migration to enhance pulmonary deposition. J. Aerosol Med. Pulm. Drug Deliv. 23, 181-187.
18. Garcia-Contreras, L., Hickey, A.J., 2002. Pharmaceutical and biotechnological aerosols for cystic fibrosis therapy. Adv. Drug Deliver. Rev. 54, 1491-1504. (Pubitemid 35375772)
19. Gasparini, G., Kosvintsev, S.R., Stillwell, M.T., Holdich, R.G., 2008. Preparation and characterization of PLGA particles for subcutaneous controlled drug release by membrane emulsification. Colloids Surf. B: Biointerfaces 61, 199-207.
20. Groneberg, D.A., Paul, H., Welte, T., 2006. Novel strategies of aerosolic pharmacotherapy. Exp. Toxicol. Pathol. 57, 49-53. (Pubitemid 43766078)
21. Hadinoto, K., Phanapavudhikul, P., Kewu, Z., Tan, R.B.H., 2007. Dry powder aerosol delivery of large hollow nanoparticulate aggregates as prospective carriers of nanoparticulate drugs: effects of phospholipids. Int. J. Pharm. 333, 187-198. (Pubitemid 46283279)
22. Hardy, D.J., Guay, D.R.P., Jones, R.N., 1992. Clarithromycin, a unique macrolide: a pharmacokinetic, microbiological, and clinical overview. Diagn. Microbiol. Infect. Dis. 15, 39-53.
23. Hayes, D.J., Murphy, B.S., Mullett, T.W., Feola, D.J., 2009. Aerosolized vancomycin for the treatment of MRSA after lung transplantation. Respirology 15, 182-186.
24. Hickey, A.J., Mansour, H.M., 2008. Formulation challenges of powders for the delivery of small molecular weight molecules as aerosols. In: Rathbone, M.J., Hadgraft, J., Roberts, M.S., Lane, M.E. (Eds.), Modified-Release Drug Delivery Technology, vol. 2, 2nd ed. Informa Healthcare, New York, pp. 573-602 (Chapter 43).
25. Hickey, A.J., Mansour, H.M., 2009. Delivery of drugs by the pulmonary route. In: Florence, A.T., Siepmann, J. (Eds.), Modern Pharmaceutics., 5th ed. Taylor and Francis, Inc., New York, pp. 191-219 (Chapter 5).
26. Hickey, A.J., Mansour, H.M., Telko, M.J., Xu, Z., Smyth, H.D., Mulder, T., McLean, R., Langridge, J., Papadopoulos, D., 2007a. Physical characterization of component particles included in dry powder inhalers. I. Strategy review and static characteristics. J. Pharm. Sci. 96, 1282-1301. (Pubitemid 46804582)
27. Hickey, A.J., Mansour, H.M., Telko, M.J., Xu, Z., Smyth, H.D., Mulder, T., McLean, R., Langridge, J., Papadopoulos, D., 2007b. Physical characterization of component particles included in dry powder inhalers. II. Dynamic characteristics. J. Pharm. Sci. 96, 1302-1319. (Pubitemid 46804583)
28. Hrvacic, B., Bosnjak, B., Bosnar, M., Ferencic, Z., Glojnaric, I., Haber, V.E., 2009. Clarithromycin suppresses airway hyperresponsiveness and inflammation in mouse models of asthma. Eur. J. Pharmacol. 616, 236-243.
29. Hwang, S.M., Kim, D.D., Chung, S.J., Shim, C.K., 2008. Delivery of ofloxacin to the lung and alveolar macrophages via hyaluronan microspheres for the treatment of tuberculosis. J. Control. Release 129, 100-106.
30. Johnson, K.A., 1997. Preparation of peptide and protein powders for inhalation. Adv. Drug Deliver. Rev. 26, 3-15. (Pubitemid 27288480)
31. Kikuchi, H., Yamauchi, H., Hirota, S., 1991. A spray drying method for mass production of liposomes. Chem. Pharm. Bull. 39, 1522-1527.
32. Le Brun, P.P.H., de Boer, A.H., Mannes, G.P.M., de Fraîture, D.M.I., Brimicombe, R.W., Touw, D.J., Vinks, A.A., Frijlink, H.W., Heijerman, H.G.M., 2002. Dry powder inhalation of antibiotics in cystic fibrosis therapy: Part 2. Inhalation of a novel colistin dry powder formulation: a feasibility study in healthy volunteers and patients. Eur. J. Pharm. Biopharm. 54, 25-32. (Pubitemid 34663853)
33. Li, X., Mansour, H.M., 2011. Physicochemical Characterization and Water Vapor Absorption of Organic Solution Advanced Spray Dried Trehalose Microparticles and Nanoparticles for Targeted Dry Powder Pulmonary Inhalation Delivery. AAPS PharmSciTech: Special Theme: Advances in Pharmaceutical Excipients Research and Use: Novel Materials, Functionalities and Testing, 12., pp. 1420-1430.
34. Mabrey, S., Sturtevant, J.M., 1976. Investigation of phase-transitions of lipids and lipid mixtures by high sensitivity differential scanning calorimetry. Proc. Am. Assoc. Cancer Res. 73, 3862-3866.
35. Mansour, H., Wang, D.S., Chen, C.S., Zografi, G., 2001. Comparison of bilayer and monolayer properties of phospholipid systems containing dipalmitoylphosphatidylglycerol and dipalmitoylphosphatidylinositol. Langmuir 17, 6622-6632. (Pubitemid 35330647)
36. Mansour, H.M., Damodaran, S., Zografi, G., 2008. Characterization of the in situ structural and interfacial properties of the cationic hydrophobic heteropolypeptide, KL4, in lung surfactant bilayer and monolayer models at the air-water interface: implications for pulmonary surfactant delivery. Mol. Pharm. 5, 681-695.
37. Mansour, H.M., Hickey, A.J., 2007. Raman characterization and chemical imaging of biocolloidal self-assemblies, drug delivery systems, and pulmonary inhalation aerosols. A review. AAPS PharmSciTech 8 (Article 99 (E01-E16)).
38. Mansour, H.M., Rhee, Y.S., Park, C.W., DeLuca, P.P., 2011. Lipid nanoparticulate drug delivery and nanomedicine. In: Moghis, A. (Ed.), Lipids in Nanotechnology. American Oil Chemists Society (AOCS) Press, Urbana, Illinois, pp. 221-268.
39. Mansour, H.M., Rhee, Y.S., Wu, X., 2009. Nanomedicine in pulmonary delivery. Int. J. Nanomed. 4, 299-319.
40. Mansour, H.M., Sohn, M., Al-Ghananeem, A.P.P.D., 2010. Materials for pharmaceutical dosage forms: molecular pharmaceutics and controlled release drug delivery aspects. Invited paper. Int. J. Mol. Sci.: Special Issue: Mater. Sci. Nanotechnol. Sect.: Biodegradability of Materials 11, 3298-3322.
41. Mansour, H.M., Zografi, G., 2007a. The relationship between water vapor absorption and desorption by phospholipids and bilayer phase transitions. J. Pharm. Sci. 96, 377-396. (Pubitemid 46363568)
42. Mansour, H.M., Zografi, G., 2007b. Relationships between equilibrium spreading pressure and phase equilibria of phospholipid bilayers and monolayers at the air-water interface. Langmuir 23, 3809-3819. (Pubitemid 46581908)
43. Masters, K., 1991. Spray Drying Handbook. Longman Scientific & Technical, Wiley.
44. Maury, M., Murphy, K., Kumar, S., Maurer, A., Lee, G., 2005. Spray-drying of proteins: effects of sorbitol and trehalose on aggregation and FT-IR amide I spectrum of an immunoglobulin G. Eur. J. Pharm. Biopharm. 59, 251-261. (Pubitemid 40127582)
45. McCalden, T.A., 1990. Particulate systems for drug delivery to the lung. Adv. Drug Deliver. Rev. 5, 253-263. (Pubitemid 20333027)
46. Meenach, S.A., Vogt, F.G., Anderson, K.W., Hilt, J.Z., McGarry, R.C., Mansour, H.M., 2013. Design, physicochemical characterization, and optimization of organic solution advanced spray-dried inhalable DPPC and DPPC:DPPE-PEG microparticles and nanoparticles for targeted respiratory nanomedicine delivery as dry powder inhalation aerosols. Int. J. Nanomed. 8, 275-293.
47. Mizoe, T., Ozeki, T., Okada, H., 2007. Preparation of drug nanoparticle-containing microparticles using a 4-fluid nozzle spray drier for oral, pulmonary, and injection dosage forms. J. Control. Release 122, 10-15. (Pubitemid 47284548)
48. Morinaga, Y., Yanagihara, K., Miyashita, N., Seki, M., Izumikawa, K., Kakeya, H., Yamamoto, Y., Mukae, H., Yamada, Y., Kohno, S., Kamihira, S., 2009. Azithromycin, clarithromycin and telithromycin inhibit MUC5AC induction by Chlamydophila pneumoniae in airway epithelial cells. Pulm. Pharmacol. Ther. 22, 580-586.
49. O'Hara, P., Hickey, A.J., 2000. Respirable PLGA microspheres containing rifampicin for the treatment of tuberculosis: manufacture and characterization. Pharm. Res. 17, 955-961.
50. Park, C.W., Hayes, D.J., Mansour, H.M., 2011. Pulmonary inhalation aerosols for targeted antibiotics delivery. Eur. Pharm. Rev. 16, 32-36.
51. Park, C.W., Rhee, Y.S., Vogt, F., Hayes, D.J., Zwischenberger, J.B., DeLuca, P.P., Mansour, H.M., 2012. Advances in microscopy and complementary imaging techniques to assess the fate of drugs ex-vivo in respiratory drug delivery. Invited paper. Adv. Drug Deliver. Rev. 64, 344-356.
52. Paterson, D.L., 2006. Clinical experience with recently approved antibiotics. Curr. Opin. Pharmacol. 6, 486-490. (Pubitemid 44348532)
53. Rhee, Y.S., Mansour, H.M., 2011. Nanopharmaceuticals I: nanocarrier systems in drug delivery. Invited paper. Int. J. Nanotechnol.: Special Issue: Nanopharm. 8, 84-114.
54. Richter, K., 2004. Successful use of DPI systems in asthmatic patients-key parameters. Resp. Med. 98, S22-S27. (Pubitemid 40029139)
55. Salama, R., Traini, D., Chan, H.K., Young, P.M., 2009. Recent advances in controlled release pulmonary therapy. Curr. Drug Deliv. 6, 404-414.
56. Sethuraman, V.V., Hickey, A.J., 2002. Powder properties and their influence on dry powder inhaler delivery on an antitubercular drug. AAPS PharmSciTech 3 (article 1).
57. Siepmann, J., Peppas, N.A., 2001. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv. Drug Deliver. Rev. 48, 139-157. (Pubitemid 32434400)
58. Siepmann, J., Siepmann, F., 2008. Mathematical modeling of drug delivery. Int. J. Pharm. 364, 328-343.
59. Song, J.-H., 2008. What's new on the antimicrobial horizon? Int. J. Antimicrob. Agents 32, S207-S213.
60. Suarez, S., Hickey, A.J., 2000. Drug properties affecting aerosol behavior. Resp. Care 45, 652-666. (Pubitemid 30484805)
61. Sung, J.C., Padilla, D.J., Garcia-Contreras, L., VerBerkmoes, J.L., Durbin, D., Peloquin, C.A., Elbert, K.J., Hickey, A.J., Edwards, D.A., 2009. Formulation and pharmacokinetics of self-assembled rifampicin nanoparticle systems for pulmonary delivery. Pharm. Res. 26, 1847-1855.
62. USP, 1995. US Pharmacopeia 1995 Official Monographs/Clarithromycin, Rockville, p. 383.
63. Ventura, C.A., Tommasini, S., Crupi, E., Giannone, I., Cardile, V., Musumeci, T., Puglisi, G., 2008. Chitosan microspheres for intrapulmonary administration of moxi-floxacin: interaction with biomembrane models and in vitro permeation studies. Eur. J. Pharm. Biopharm. 68, 235-244.
64. Willis, L., Hayes, D.J., Mansour, H.M., 2012. Therapeutic liposomal dry powder inhalation aerosols for targeted lung delivery. Lung 190, 251-262.
65. Wu, X., Hayes, D.J., Zwischenberger, J.B., Kuhn, R.J., Mansour, H.M., 2013a. Design and physicochemical characterization of advanced spray-dried tacrolimus multifunctional particles for inhalation. Drug Des. Dev. Ther. 7, 59-72.
66. Wu, X., Li, X., Mansour, H.M., 2010. Surface analytical techniques in solid-state particle characterization: implications for predicting performance in dry powder inhalers. Invited paper. KONA Powder Part. J. 28, 3-19.
67. Wu, X., Mansour, H.M., 2011. Nanopharmaceuticals II: application of nanoparticles and nanocarrier systems in pharmaceutics and nanomedicine. Invited paper. Int. J. Nanotechnol.: Special Issue: Nanopharm. 8, 115-145.
68. Wu, X., Zhang, W., Hayes, D.J., Mansour, H.M., 2013b. Physicochemical characterization and aerosol dispersion performance of organic solution advanced spray-dried cyclosporine A multifunctional particles for dry powder inhalation aerosol delivery. Int. J. Nanomed. 8, 1-15.
69. Xu, Z., Mansour, H.M., Hickey, A.J., 2011. Particle interactions in dry powder inhaler unit processes. J. Adhes. Sci. Technol.: Special Issue on Adhesion Aspects in Pharmaceutical Sciences 25, 451-482.
70. Xu, Z., Mansour, H.M., Mulder, T., McLean, R., Langridge, J., Hickey, A.J., 2010. Heterogeneous particle deaggregation and its implication for therapeutic aerosol performance. J. Pharm. Sci. 99, 3442-3461.
71. Zijlstra, G.S., Hinrichs, W.L.J., Boer, A.H.D., Frijlink, H.W., 2004. The role of particle engineering in relation to formulation and de-agglomeration principle in the development of a dry powder formulation for inhalation of cetrorelix. Eur. J. Pharm. Sci. 23, 139-149.