Novel hydrofluoroalkane suspension formulations for respiratory drug delivery

Expert Opinion on Drug Delivery

Volumn 2, Issue 4, 2005, Pages 625-638

  Rogueda, Philippe ^a  

^a ASTRAZENECA   (United Kingdom)

Author keywords

Drug delivery to the lung; Formulations; HFA; Inhalation; Non aqueous; pMDI; Suspension

Indexed keywords

1,1,2 TRICHLORO 1,2,2 TRIFLUOROETHANE; BECLOMETASONE DIPROPIONATE; BETAMETHASONE VALERATE; CHLOROFLUOROCARBON; CROMOGLYCATE DISODIUM; DANAZOL; DEXAMETHASONE; DICHLOROMETHANE; FLUORINATED HYDROCARBON; FLUTICASONE; FLUTICASONE PROPIONATE PLUS SALMETEROL; FORMOTEROL FUMARATE; HYDROCORTISONE; HYDROCORTISONE ACETATE; INSULIN; IPRATROPIUM BROMIDE; LACTOSE; NANOPARTICLE; PERFLUORODECALIN; PERFLUOROOCTYL BROMIDE; PERFLUOROPENTANE; PREDNISONE; RESPIRATORY TRACT AGENT; SALBUTAMOL; SALBUTAMOL SULFATE; SOLVENT; STEROID; TRIFLUOROACETIC ACID;

ATOMIC FORCE MICROSCOPY; CHEMICAL BOND; CHEMICAL STRUCTURE; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG RESEARCH; DRUG SOLUBILITY; DRUG STABILITY; MATHEMATICAL COMPUTING; METERED DOSE INHALER; MICROEMULSION; MOLECULAR INTERACTION; PARTICULATE MATTER; PHARMACEUTICAL ENGINEERING; POROSITY; PREDICTION; REVIEW; SURFACE PROPERTY; SURFACE TENSION; SUSPENSION;

ALKANES; CHEMISTRY, PHARMACEUTICAL; DRUG DELIVERY SYSTEMS; EMULSIONS; LUNG; METERED DOSE INHALERS; NANOSTRUCTURES; SOLUBILITY; SUSPENSIONS;

EID: 22844444449     PISSN: 17425247     EISSN: None     Source Type: Journal    
DOI: 10.1517/17425247.2.4.625     Document Type: Review

References (101)

1. PITTROFF M, JANNICK P: Solkane 227a pharma and solkane 134a pharma for use in medical sprays. Solvay Fluor. Newsletter (2004) 5.
2. NAGEL MW, WIERSEMAN KJ, BATES L, MITCHELL JP: Performance of large and small volume valve holding chambers with a new combination long-term bronchodilator/anti-inflammatory formulation delivered by pressurized metered dose inhaler. J. Aero. Med. (2002) 15(4):427-433.
3. DALBY RN, BYRON PR: Comparison of output particle size distributions form pressurised aerosols formulated as solutions or suspensions. Pharm. Res. (1988) 5(1)36-39.
4. ZEIDLER M, CORREN J: Hydrofluoroalkane formulations of inhaled corticosteroids for the treatment of asthma. Treat. Respir. Med. (2004) 3(1):35-44.
5. WEERS JG, CLARK AR, CHALLONER P: High dose inhaled powder delivery: challenges and techniques. Proceedings of the 9th Respiratory Drug Delivery meeting. Palm Springs, CA, USA (2004).
6. KOTSOKECHAGIA T, SMITH A, MILLER N, RADSPINNER D: The relationship between fine particle mass and drug concentration for high powder loading pressurised metered dose inhalers. Proceedings of 13th meeting of the Aerosol Society: Drug Delivery to the Lungs XIII. London, UK (2002).
7. HARTMAN MS, GILL H, KENNEDY AA, TARARA T, WEERS J: The efficiency and stability of a novel lipid based budesonide metered dose inhaler formulation utilizing HFA. Proceedings of the Annual Meeting of the American Association of Pharmaceutical Scientists. Salt Lake City, UT, USA (2003).
8. TARARA TE, HARTMAN MS, GILL H, KENNEDY AA, WEERS JG: Characterization of suspension based metered dose inhaler formulations composed of spray dried budesonide microcrystals dispersed in HFA 134a. Pharm. Res. (2004) 21(9):1607-1614.
9. CHAN HK, GONDA I: Development of a systematic theory of suspension inhalation aerosols. II. Aggregates of monodisperse particles nebulized in polydisperse droplets. Int. J. Pharm. (1988) 41:147-157.
10. VANBEVER R, MINTZES JD, WANG J et al.: Formulation and physical characterisation of large porous particles for inhalation. Pharm. Res. (1999) 16(11):1735-1742.
11. DELLAMARY LA, TARARA TE, SMITH DJ et al.: Hollow porous particles in metered dose inhalers. Pharm. Res. (2000) 17(2):168-174.
12. LEHMLER HJ, BUMMER PM, JAY M: Liquid ventilation - a new way to deliver drugs to diseased lungs. Chemtech. (199) 29(10):7-12.
13. COURRIER HM, BUTZ N, VANDAMME TF: Pulmonary drug delivery systems: recent developments and prospects. Crit. Rev. Therapeutic Drug Carrier Syst. (2002) 19(4&5):425-498.
14. JOHNSON KA: Interfacial phenomena and phase behaviour in metered does inhaler formulations. In: Lung Biology in Health and Disease (Volume 94). Inhalation Aerosols: Physical and Biological Basis for Therapy. AJ Hickey (Ed.), Marcel Dekker, New York (1996):385-415.
15. ISRAELACHVILI J: Intermolecular & surface forces. Academic Press (1997).
16. SIDHU BK, WASHINGTON C, DAVIS SS, PUREWAL TS: Electrophoretic properties of lactose and salbutamol sulfate suspensions in halogenated solvents. Langmuir (1993) 9:839-843.
17. WYATT DA, VINCENT B: Electrical effects in non-aqueous systems. J. Biopharm. Sci. (1992) 3(1/2):27-31.
18. FOWKES FM, JINNAI H, MOSTAFA MA, ANDERSON FW, MOORE RJ: Mechanism of electric charging of particles in non-aqueous liquids. ACS Symposium Series (1982) 200:307-324.
19. ROGUEDA P: Electrostatic Stabilisation of HFA pMDIs. Annual meeting of the American Association of Pharmaceutical Scientists. Denver, CO, USA (2001).
20. ROGUEDA P: Particle interactions in HFA formulations: experiment, theory, and practice. Proceedings of the 8th Respiratory Drug Delivery Meeting. Tucson, AZ, USA (2002).
21. ROGUEDA PG: HPFP, a model propellant for pMDIs. Drug Dev. Ind. Pharm. (2003) 29(1):29-50.
22. JONES SA, MARTIN GP, FORBES B, BROAN MB: The influence of electrostatic stabilisation within apolar suspension formulations. 31st Annual Meeting & Exposition of the Controlled Release Society. Honolulu, HI, USA (2004).
23. GUPTA A, MYRDAL PB: Novel method for the determination of solubility in aerosol propellants. J. Pharm. Sci. (2004) 93(10):2411-2419.
24. WILLIAMS III RO, ROGERS TL, LIU J: Study of solubility of steroids in hydrofluoroalkane propellants. Drug Dev. Ind. Pharm. (1999) 25(12):1227-1234.
25. GLOVER W, KWOK P, CHAN HK: Electrostatic charges in metered dose inhalers. Proceedings of the 9th Respiratory Drug Delivery meeting. Palm Springs, CA, USA (2004).
26. GLOVER W. CHAN HK: Electrostatic charge characterization of pharmaceutical aerosols using electrical low-pressure impaction (ELPI). J. Aero. Sci. (2004) 35(6):755-764.
27. ORBAN JC, PEART J: Simultaneous electrostatic charge characterization and particle size analysis of metered dose inhalers (pMDIs) using the electrical low pressure impactor. Proceedings of the 9th Respiratory Drug Delivery meeting. Palm Springs, CA, USA (2004).
28. ASHAYER R, LUCKHAM PF, MANIMAARAN S, ROGUEDA P: Investigation of the molecular interactions in a pMDI formulation by atomic force microscopy. Euro. J. Pharm. Sci. (2004) 21:533-543.
29. MILLER NC: The effects of water in inhalation suspension aerosol formulations. Proceedings of the 1st Respiratory Drug Delivery meeting. Boca Raton, FL, USA (1990).
30. BERRY J, KLINE LC, SHERWOOD JK et al.: Influence of the size of micronised active pharmaceutical ingredient on the aerodynamic particles size and stability of a metered does inhaler. Drug Dev. Ind. Pharm. (2004) 30(7):705-714.
31. MALBREL CA, SOMASUNDARAN P: Water-induced dispersion flocculation of colloidal suspensions in nonpolar media. J. Coll. Int. Sci. (1989) 133(2):404-408.
32. GRIFFITHS P, PAUL A, ROGUEDA P: Using polymers to control the stability of non-aqueous suspensions. Proceedings of the SCI/RSC Colloid Groups Meeting on 'Advances in Non-Aqueous Colloids'. London, UK (2004).
33. ROBERTS CJ: What can we learn from atomic force microscopy adhesion measurements with single drug particles? Eur. J. Pharm. Sci. (2004) 24:153-157.
34. HOOTON JC, GERMAN CS, ALLEN S et al.: Characterisation of particle interactions by atomic force microscopy: Effect of contact area. Pharm. Res. (2003) 20(3):508-514.
35. ROGUEDA P, GROSVENOR M, LUCKHAM P, MANIMAARAN S: Quantification of the interactions between micronised formoterol and a selection of surfaces found in a pressurised metered dose inhaler (pMDI). Proceedings of the Annual meeting of the American Association of Pharmaceutical Scientists. Salt Lake City, UT, USA (2003).
36. ROGUEDA P, GROSVENOR M, LUCKHAM P, MANIMAARAN S: Evaluation of the effectiveness of stabilisers in reducing cohesive and adhesive forces between formoterol particles in pressurised metered dose inhalers (pMDIs). Proceedings of the Annual Meeting of the American Association of Pharmaceutical Scientists. Salt Lake City, UT, USA (2003).
37. TRAINI D, ROGUEDA PGA, PRICE R: Interactions of model drugs in HFAs and crystals dissolution: an AFM in situ investigation using functionalised AFM probes. Proceedings of the 11th International Conference on Surface and Colloid Science. Iguassu Falls, Brazil (2003).
38. TRAINI D, ROGUEDA P, YOUNG PM, PRICE R: Surface energy and interparticle forces correlations in model pMDI formulations. Pharm. Res. (2005) 22(5):816-825.
39. CLINE D, DALBY R: Predicting the quality of powders for inhalation from surface energy and area. Pharm. Res. (2002) 19(9):1274-1277.
40. PHILLIPS EM, BYRON PR, DALBY RN: Axial ratio measurements for early detection of crystal growth in suspension type metered dose inhalers. Pharm. Res. (1993) 10(3):454-456.
41. DALBY RN, PHILLIPS EM, BYRON PR: Determination of drug solubility in aerosol propellants. Pharm. Res. (1991) 8(9):1206-1209.
42. VERVAET C, BYRON PR: Drug surfactant propellant interactions in HFA formulations. Int. J. Pharm. (1999) 186:13-30.
43. BYRON PR, MILLER NC, BLONDINO FE, VISICH JE, WARD GH: Some aspects of alternative propellant solvency. Proceedings of the 4th Respiratory Drug Delivery meeting. Buffalo Grove, IL, USA (1994).
44. DUMANLI I, LAROSA D, ZHU Y, ADJEI AL: An investigation of the solubility of recombinant human insulin in tetrafluorethane propellant and aqueous media. Proceedings of the 9th Respiratory Drug Delivery meeting. Palm Springs, FL, USA (2004).
45. ROGUEDA PG, LUCKHAM PF, STEPHENS JS: Inhalation particles interactions in fluorinated liquids. Proceedings of Particles 2002. Orlando, USA (2002).
46. YOUNG P, PRICE R, LEWIS D, EDGE S, TRAINI D: Under pressure: predicting pressurized metered dose inhaler interactions using the atomic force microscope. J. Coll. Int. Sci. (2003) 262:298-302.
47. TRAINI D, ROGUEDA P, PRICE R, YOUNG PM: Assessing the Degree of Drug Adhesion to Different pMDI Canister Walls by Surface Energy and AFM Measurements. Proceedings of the 9th Respiratory Drug Delivery meeting. Palm Springs, USA (2004) RDDIX.
48. WILLIAMS III RO, REPKA M, LIU J: Influence of propellant composition on drug delivery from a pressurized metered dose inhaler. Drug Dev. Ind. Pharm. (1998) 24(8):763-770.
49. MILLER NC, SCHULTZ RK, SCHACTNER WJ: Through life dose uniformity in pressurized metered dose inhalers. Proceedings of the Annual Meeting of the American Association of Pharmaceutical Scientists. Las Vegas, NV, USA (1990).
50. MILLER NC, SCHULTZ RK: Interparticle interaction in nonpolar liquid media an its influence on dose reproducibility. J. Biopharm. Sci. (1992) 3(1/2):19-25.
51. GOVIND N, PRICE A, BRINDLEY A, SPARY S, COLTHORPE P: Correlation of two methods for assessing pMDI suspension stability. Proceedings of the 7th Respiratory Drug Delivery meeting. Tarpon Springs, FL, USA (2000).
52. BERRY J, KLINE LC, HART JL, SEQUEIRA J: Influence of the storage orientation on the aerodynamic particle size of a suspension metered dose inhaler containing propellant HFA 227. Drug Dev. Ind. Pharm. (2003) 29(6):631-639.
53. MICHAEL Y, SNOWDEN MJ, CHOWDHRY BZ, ASHURST IC, DAVIES-CUTTING CJ, RILEY T: Characterisation of the aggregation behaviour in salmeterol and fluticasone propionate inhalation aerosol system. Int. J. Pharm. (2001) 221:165-174.
54. NELSON HS, CHAPMAN KR, PYKE SD, JOHNSON M, PRITCHARD JN. Enhanced synergy between fluticasone propionate and salmeterol inhaled from a single inhaler versus separate inhalers. J. Allergy Clin. Immunol. (2003) 112(1):29-36.
55. STEIN SW, STEFELY JS: Reinventing metered dose inhalers: from poorly efficient CFC MDIs to highly efficient HFA MDIs. www.drugdeliverytech.com (2003).
56. ROGUEDA P: Pushing the boundaries: searching for novel HFA suspension formulations. Proceedings of the 9th Respiratory Drug Delivery meeting. Palm Springs, FL, USA (2004).
57. BLONDINO FE, BYRON PR. Surfactant dissolution and water solubilisation in chlorine free liquefied gas propellants. Drug Dev. Ind. Pharm. (1998) 24(10):935-945.
58. BYRON PR, MILLER NC, BLONDINO FE, WISICH JE, WARD GH: Some aspects of alternative propellant solvency. Proceedings of the 4th Respiratory Drug Delivery meeting. Buffalo Grove, IL, USA (1994).
59. DICKINSON PA, SEVILLE PC, McHALER H, PERKINS NC, TAYLOR G: An investigation of the solubility of various compounds in the hydrodluoroalkane propellants and possible model liquid propellants. J. Aero. Med. (2000) 13(3):179-186.
60. GUPTA A, MYRDAL P: Evaluating solubility behaviour of compounds in HFA 134a propellant. Proceedings of the Annual Meeting of the American Association of Pharmaceutical Scientists. Baltimore, MD, USA (2004).
61. METRANGOLO P, PILATI T, RESNATI G, STEVENAZZI A: Halogen bonding driven self assembly of fluorocarbons and hydrocarbons. Curr. Op. Coll. Inter. Sci. (2003) 8:215-222.
62. STEFELY JS: Novel Excipients for inhalation drug delivery: expanding the capability of the MDI. Drug. Del. Tech. (2002) 2(6):6-69.
63. RIESS JG, KRAFFT MP: Fluorinated materials for in vivo oxygen transport (blood substitutes), diagnosis and drug delivery. Biomaterials (1998) 19:1529-1539.
64. KRAFFT MP: Fluorocarbons and fluorinated amphiphiles in drug delivery and biomedical research. Adv. Drug Del. Rev. (2001) 47:209-228.
65. GANDERTON D, LEWIS D, DAVIES R, MEAKIN B, CHURCH T: The formulation and evaluation of a CFC free budesonide pressurised metered dose inhaler. Resp. Med. (2003) (Supp. D):54-59.
66. SASO Y, KONDO S, SEKI T, MORIMOTO K: Formulation design and pharmaceutical evaluation of an HFA 227 based furosemide metered dose inhaler. J. Drug Del. Sci. Tech. (2004) 14(2):135-140.
67. PATEL N, FORBES B: The formulation of lipid: DNA complexes in pMDIs. King's College. Poster. J. Pharm. Pharmaco. (2003) 55(Supp.):S41.
68. PAUL A, GRIFFITHS PC, ROGUEDA P: Water induced phase separation in polymer/fluorinated liquid mixtures. Proceedings of the 11th International Conference on Surface and Colloid Science. Iguassu Falls, Brazil (2003).
69. SMYTH HD: The influence of formulation variables on the performance of alternative propellant driven metered dose inhalers. Adv. Drug Del. Rev. (2003) 55:807-828.
70. BRAMBILLA G, GANDERTON D, GARZIA R, LEWIS D, MEAKIN B, VENTURA P: Modulation of aerosol clouds produced by pressurised inhalation aerosols. Int. J. Pharm. (1999) 186:53-61.
71. STEIN SW, MYRDAL PB: A theoretical and experimental analysis of formulation and device parameters affecting solution MDI size distributions. J. Pharm. Sci. (2004) 93(8):2158-2175.
72. BEAUSANG EL, BURNS S, BUCKTON G: The engineering of powder surface energy to produce pMDI suspensions of improved stability. Proceedings of the Pharmaceutical Sciences World Congress. Kyoto, Japan (2004).
73. BEAUSANG EL, BURNS S, BUCKTON G: Surface modification of a model hydrophilic drug using insoluble surfactants and the resulting effect on suspension behaviour in HFA 134a. Proceedings of 14th meeting of the Aerosol Society: Drug Delivery to the Lungs XIV. London, UK (2003).
74. URICANU V, EASTMAN JR, VINCENT B: Stability in colloidal mixtures containing particles with a large disparity in size. J. Coll. Int. Sci. (2001) 233:1-11.
75. BLEIER A, MATIJEVIC E: Heterocoagulation. J. Chem. Soc. Faraday Trans. (1978) 74:1346-1359.
76. JONES R, EVANS R, WARREN S, TAYLOR G: Development of a novel suspension MDI formulation using a low energy dispersion system. Proceedings of the 8th Respiratory Drug Delivery meeting. Tucson, AZ, USA (2002).
77. JONES R, EVANS R, WARREN S, TAYLOR G: Development of a fluticasone propionate suspension pMDI formulation using a second particulate system. Proceedings of the 9th Respiratory Drug Delivery meeting. Palm Springs, CA, USA (2004).
78. FUEG LM, MULLER-WALZ R, NIEDERLAENDER C, VENTHOYE G: Flutiform HFA MDI: a stable fluticasone/Formoterol combination employing Skyedry formulation technology. Proceedings of the 9th Respiratory Drug Delivery Meeting. Palm Springs, CA, USA (2004).
79. STECKEL H, WHELE S: A novel formulation technique for metered dose inhaler (MDI) suspensions. Int. J. Pharm. (2004) 284:75-82.
80. WILLIAMS III RO, ARRON MK, ALONSO MJ, REMUNAN-LOPEZ C: Investigation of a pMDI system containing chitosan microspheres and P134a. Int. J. Pharm. (1998) 174:209-222.
81. COLUMBANO A, BUCKTON G, WIKELEY P: Characterisation of surface modified salbutamol sulphate-alkylpolyglycoside micropartilces prepared by spray drying. Int. J. Pharm. (2003) 253:61-70.
82. REHMAN M, SHEKUNOVA BY, YORK P et al.: Optimisation of powders for pulmonary delivery using supercritical fluid technology. Euro. J. Pharm. Sci. (2004) 22(1):1-17.
83. EDWARDS DA, AHNES J, CAPONETTI G et al.: Large porous particles for pulmonary drug delivery. Science (1997) 276:1868-1871.
84. EDWARDS DA, BEN-JEBRIA A, LANGER R: Recent advances in pulmonary drug delivery using large, porous inhaled particles. J. Applied Physio. (1998) 84(2):379-385.
85. HIRST PH, PITCARIN GR, WEERS JG et al.: In vivo lung deposition of hollow porous particles from a pressurised metered dose inhaler. Pharm. Res. (2002) 19(3):258-264.
86. RABINOV BE: Nanosuspensions in drug delivery. Nat. Rev. (2004) 3:1-12.
87. YIM D, CIPOLLA D, BOYD B: Feasability of pulmonary delivery of nano-suspension formulations using the AERx System. Proceedings of the 15th International Congress of the International Society for Aerosols in Medicine. Perth, Australia (2005).
88. BIVAS-BENITA M, ROMEIJN S, JUNGINGER HE, BORCHARD G: PLGA-PEI naoparticles for gene delivery to pulmonary epithelium. Euro. J. Pharm. Biopharm. (2004) 58:1-6.
89. CRAMPTON M, KINNERSLEY R, AYRES J: Sub-micrometer particle production by pressurised metered dose inhalers. J. Aero. Med. (2004) 17(1):33-42.
90. JACOBS C, MULLER RH: Budesonide nanosuspension for pulmonary administration: Production and aerosolisation properties. Proceedings of the 28th Annual Meeting & Exposition of the Controlled Release of bioactive materials Society. San Diego, CA, USA (2001).
91. BORM PJA, KREYLING W. Toxicologial hazards of inhaled nanoparticles - potential implications for drug delivery. J. Nanosci. Nanotech. (2004) 4(5):521-531.
92. KEYLING WG, SEMMLE M, MOLLER W. Dosimetry and toxicology of ultrafine particles. J. Aero. Med. (2004) 17(2):140-152.
93. PATEL N, MARLOW M, LAWRENCE MJ: Formation of fluorinated non-ionic surfactant microemulsions in hydrofluorocarbon 134a (HFC 124a). J. Coll. Int. Sci. (2003) 258:345-353.
94. LATTES A, RICO-LATTES I: Microemulsions of perfluorinated and semi fluorinated compounds. Art. Cells Blood Subs. Immob. Biotech. (1994) 22(4):1007-1018.
95. WEERS JG, ARLAUSKAS RA, TARARA TE, PELURA TJ: Characterisation of fluorocarbon in water emulsions with added triglyceride. Langmuir (2004) 20:7430-7435.
96. STEYTLER DC, THORPE M, EASTOE J, DUPONT A, HEENAN RK: Microemulsion formation in 1,1,1,2 tetrafluoroethane (R134a). Langmuir (2003) 19:8715-8720.
97. LAI CL, O'REAR FA, HARWELL JH: Formation of fluorocarbon surfacrant reversed micelles in a halosolvent. J. Coll. Int. Sci. (1996) 183:166-175.
98. BUTZ N, PORTE C, COURRIER H, KRAFFT MP, VAN DAMME TF: Reverse water in fluorocarbon emulsions for use in pressurized metered dose inhalers containing hydrofluoroalkane propellants. Int. J. Pharm. (2002) 238:257-269.
99. SOMMERVILLE ML, HICKEY AJ: Aerosol generation by metered dose inhalers containing dimethyl ether/propane inverse microemulsions. AAPS Pharm. Sci. Tech. (2003) 4(4):E58.
100. RIESS JG, KRAFFT MP: Advanced fluorocarbon based systems for oxygen and drug delivery, and diagnosis. Art. Cells Blood Subs. Immob. Biotech. (1997) 25(1&2):43-52.
101. BYRON PR: Aerosol formulation, generation and delivery using metered systems. Proceedings of the 1st Respiratory Drug Delivery meeting. Boca Raton, FL, USA (1990).