The effect of formulation excipients on protein stability and aerosol performance of spray-dried powders of a recombinant humanized anti-IgE monoclonal antibody

Pharmaceutical Research

Volumn 16, Issue 3, 1999, Pages 350-358

  Andya, James D ^a   Maa, Yuh Fun ^b   Costantino, Henry R ^c   Nguyen, Phuong Anh ^a   Dasovich, Nancy ^a   Sweeney, Theresa D ^a   Hsu, Chung C ^a   Shire, Steven J ^a  

^a GENENTECH INC   (United States)

^b Powderject Technologies   (United States)

^c ALKERMES INC   (United States)

Author keywords

Aggregation; Fine particle fraction; Glycation; Protein formulation; Protein stability; Spray drying

Indexed keywords

DIMER; DRUG CARRIER; EXCIPIENT; IMMUNOGLOBULIN E ANTIBODY; LACTOSE; MANNITOL; MONOCLONAL ANTIBODY; PROTEIN; TREHALOSE;

AEROSOL; AFFINITY CHROMATOGRAPHY; ARTICLE; CONCENTRATION (PARAMETERS); CRYSTALLIZATION; DISULFIDE BOND; DRUG EFFECT; DRUG FORMULATION; DRUG STABILITY; DRUG STORAGE; DRY POWDER; GEL PERMEATION CHROMATOGRAPHY; ISOELECTRIC FOCUSING; POLYACRYLAMIDE GEL ELECTROPHORESIS; PRIORITY JOURNAL; PROTEIN AGGREGATION; PROTEIN CONFORMATION; PROTEIN CONTENT; PROTEIN GLYCOSYLATION; PROTEIN STABILITY; X RAY POWDER DIFFRACTION;

EID: 0032962882     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1018805232453     Document Type: Article

References (32)

1. 1. L. G. Presta, S. J. Lahr, R. L. Schields, J. P. Porter,C. M. Gorman, B. M. Fendly, and P. M. Jardieu. Humanization of an antibody directed against IgE. J. Immunol. 151:2623-2632 (1993).
2. 2. J. Liu, P. Lester, S. Builder, and S. J. Shire. Characterization of complex formation by humanized anti-IgE monoclonal antibody and monoclonal human IgE. Biochemistry 34:10474-10482 (1995).
3. 3. J. V. Fahy, H. E. Fleming, H. H. Wong, J. T. Liu, J. Q. Su, J. Reimann, R. B. Fick Jr., and D. W. Cockcroft. The effect of an anti-IgE monoclonal antibody on the early-and late-phase responses to allergen inhalation in asthmatic subjects. Am. J. Resp. Critical Care Med. 155:1828-1834 (1997).
4. 4. L. P. Boulet, K. R. Chapman, J. Cote, S. Kalra, R. Bhagat, V. A. Swystun, M. Laviolette, L. D. Cleland, F. Deschesnes, J. Q. Su, A. DeVault, R. B. Fick Jr., and D. W. Cockcroft. Inhibitory effects of an anti-IgE antibody E25 on allergen-induced early asthmatic response. Am. J. Resp. Critical Care Med. 155:1835-1840 (1997).
5. 5. R. W. Niven. Delivery of biotherapeutics by inhalation aerosols. Pharm. Technol. 17(7):72-82 (1993).
6. 6. J. Broadhead, S. K. Rouan Edmond, and C. T. Rhodes. The spray drying of pharmaceuticals. Drug Dev. Ind. Pharm. 18:1169-1206 (1992).
7. 7. J. Broadhead, S. K. Rouan Edmond, I. Hau, and C. T. Rhodes. The effect of process and formulation variables on the properties of spray-dried β-galactosidase. J. Pharm. Pharmacol. 46:458-467 (1994).
8. 8. M. Mumenthaler, C. C. Hsu, and R. Pearlman. Feasibility study on spray-drying protein pharmaceuticals. Recombinant human growth hormone and tissue-type plasminogen activator. Pharm. Res. 11:12-20 (1994).
9. 9. H-K. Chan, A. R. Clark, I. Gonda, M. Mumenthaler, and C. C. Hsu. Spray-dried powders and powder blends of recombinant human deoxyribonuclease (rhDNase) for aerosol delivery. Pharm. Res. 14:431-437 (1997).
10. 10. Y-F. Maa, H. R. Costantino, P-A. Nguyen, and C. C. Hsu. The effect of operating and formulation variables on the morphology of spray-dried protein particles. Pharm. Dev. Technol. 2:213-223 (1997).
11. 11. J. L. Cleland, M. F. Powell, and S. J. Shire. The development of stable protein formulations. A close look at protein aggregation, deamidation, and oxidation. Critical Rev. Ther. Drug Carrier Sys. 10:307-377 (1993).
12. 12. A. R. Clark, N. Dasovich, I. Gonda, and H-K. Chan. The balance between biochemical and physical stability for inhalation protein powders. rhDNase as an example. In R. N Darby, P. R. Byron, and S. J. Farr (eds.), Respiratory Drug Delivery V, Interpharm Press, Buffalo Grove, 1996, pp. 167-174.
13. 13. J. F. Young. Humidity control in the laboratory using salt solutions. A review. J. Appl. Chem. 17:241-245 (1967).
14. 14. R. A. Gray, A. Stern, T. A. Bewley, D. McRorie, P. Voelker, J. Liu, and S. J. Shire. Determination of protein concentration by improved optical methods. Pharm. Res. 11:76 (1994).
15. 15. J. Liu, J. Ruppel, and S. J. Shire. Interaction of human IgE with soluble forms of IgE high affinity receptors. Pharm. Res. 14:1388-1393 (1997).
16. 16. Y-F. Maa, P-A. Nguyen, J. D. Andya, N. Dasovich, S. J. Shire, and C. C. Hsu. Effect of spray drying and subsequent processing on residual moisture content and physical/biochemical stability of protein inhalation powders. Pharm. Res. 15:768-775 (1998).
17. 17. A. Saleki-Gerhardt and G. Zografi. Non-isothermal and isothermal crystallization of sucrose from the amorphous state. Pharm. Res. 11:1166-1173 (1994).
18. 18. L. M. Crowe, D. S. Reid, and J. H. Crowe. Is trehalose special for preserving dry biomaterials? Biophysical J. 71:2087-2093 (1996).
19. 19. F. Franks, B. Aldous, and T. Auffret. Using water-soluble glasses as a strategy for bioproduct stabilization. Gen. Eng. News 15:20 (1995).
20. 20. J. F. Carpenter, M. J. Pikal, B. S. Chang, and T. W. Randolph. Rational design of stable lyophilized protein formulations. Some practical advice. Pharm. Res. 14:969-975 (1997).
21. 21. D. B. Volkin and C. R. Middaugh. The effect of temperature on protein structure. In T. J. Ahern, and M. C. Manning (Eds.), Stability of Protein Pharmaceuticals, Part A Chemical and Physical Pathways of Protein Degradation, Plenum Press, New York, 1993, pp. 215-247.
22. 22. H. R. Costantino, R. Langer, and A. M. Klibanov. Solid-phase aggregation of proteins under pharmaceutically relevant conditions. J. Pharm. Sci. 83:1662-1669 (1994).
23. 23. M. J. Pikal. Freeze-drying of proteins. Process, formulation, and stability. In J. L. Cleland, and R. Langer (Eds.), Formulation and Delivery of Proteins and Peptides. American Chemical Society, Washington, DC, 1994, pp. 120-133.
24. 24. L. N. Bell, M. J. Hageman, and L. M. Muraoka. Thermally induced denaturation of lyophilized bovine somatotropin and lysozyme as impacted by moisture and excipients. J. Pharm. Sci. 84:707-712 (1995).
25. 25. H. R. Costantino, K. G. Carrasquillo, R. A. Cordero, M. Mumenthaler, C. C. Hsu, and K. Griebenow. The effect of excipients on the stability and structure of lyophilized recombinant human growth hormone (rhGH). J. Pharm. Sci., in press, 1998.
26. 26. H. R. Costantino, J. D. Andya, P-A. Nguyen, N. Dasovich, T. D. Sweeney, S. J. Shire, C. C. Hsu and Y-F. Maa. The effect of mannitol crystallization on the stability and aerosol performance of a spray-dried pharmaceutical protein, recombinant humanized anti-IgE monoclonal antibody. J. Pharm. Sci., 18:1406-1411 (1998).
27. 27. J. F. Carpenter, and J. H. Crowe. An infrared spectroscopic study of the interactions of carbohydrates with dried proteins. Biochemistry 28: 3916-3922 (1989).
28. 28. S. J. Prestrelski, K. A. Pikal, and T. Arakawa. Optimization of lyophilization conditions for recombinant human interleukin-2 by dried-state conformational analysis using fourier-transform infrared spectroscopy. Pharm Res. 12:1250-1259 (1995).
29. 29. H. R. Costantino, J. D. Andya, S. J. Shire, and C. C. Hsu. Fourier-transform infrared spectroscopic analysis of the secondary structure of recombinant humanized immunoglobulin G. Pharm. Sci. 3:121-128 (1997).
30. 30. H. R. Costantino, J. G. Curley, and C. C. Hsu. Determining the water sorption monolayer of lyophilized pharmaceutical proteins. J. Pharm. Sci. 86:1390-1393 (1997).
31. 31. A. J. Furth. Methods for assaying nonenzymatic glycosylation. Anal. Biochem. 175:347-360 (1988).
32. 32. F. J. Shen, J. D. Andya, S. J. Shire, and R. J. Harris. The detection of lactosylated sites. Protein Sci. 6(Suppl. 2):152 (1997).