Effect of pH and excipients on structure, dynamics, and long-term stability of a model IgG1 monoclonal antibody upon freeze-drying

Pharmaceutical Research

Volumn 30, Issue 4, 2013, Pages 968-984

  Park, Jihea ^a   Nagapudi, Karthik ^a   Vergara, Camille ^a   Ramachander, Ranjini ^a   Laurence, Jennifer S ^b   Krishnan, Sampathkumar ^a,c  

^a AMGEN INC   (United States)

^b UNIVERSITY OF KANSAS   (United States)

^c Hospira Inc   (United States)

Author keywords

IgG1 antibody lyophilization; protein formulation; protein structure; solid state NMR; solid state stability

Indexed keywords

EXCIPIENT; IMMUNOGLOBULIN G1; MANNITOL; MONOCLONAL ANTIBODY; SUCROSE;

ANALYSIS; ANTIBODY STRUCTURE; ARTICLE; CONTROLLED STUDY; CORRELATION ANALYSIS; COVALENT BOND; DRUG FORMULATION; DRUG MONITORING; DRUG STORAGE; DYNAMICS; FLUORESCENCE SPECTROSCOPY; FREEZE DRYING; GEL PERMEATION CHROMATOGRAPHY; GLASSY STATE; INFRARED SPECTROSCOPY; ION EXCHANGE CHROMATOGRAPHY; LIGHT OBSCURATION TECHNIQUE; MATERIAL STATE; MOLECULAR MODEL; PH; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEIN SECONDARY STRUCTURE; PROTEIN STABILITY; PROTEIN TERTIARY STRUCTURE; RAMAN SPECTROMETRY; RELAXATION TIME; SOLID STATE; TEMPERATURE;

ANTIBODIES, MONOCLONAL; DRUG STORAGE; EXCIPIENTS; FREEZE DRYING; IMMUNOGLOBULIN G; MANNITOL; NUCLEAR MAGNETIC RESONANCE, BIOMOLECULAR; PROTEIN STABILITY; PROTEIN STRUCTURE, SECONDARY; PROTEIN STRUCTURE, TERTIARY; SPECTROSCOPY, FOURIER TRANSFORM INFRARED; SUCROSE; TEMPERATURE;

EID: 84876481833     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-012-0933-z     Document Type: Article

References (47)

1. Carpenter JF, Pikal MJ, Chang BS, Randolph TW. Rational design of stable lyophilized protein formulations: some practical advice. Pharm Res. 1997;15(8):969-75.
2. Cleland JL, Lam X, Kendrick B, Yang J, Yang T, Overcashier D, et al. A specific molar ratio of stabilizer to protein is required for storage stability of a lyophilized monoclonal antibody. J Pharm Sci. 2001;90:310-21.
3. Pikal M, Rigsbee D, Roy M, Galreath D, Kovach K, Wang B, et al. Solid state chemistry of proteins: II. The correlation of storage stability of freeze-dried human growth hormone (hGH) with structure and dynamics in the glassy solid. J Pharm Sci. 2008;97(12):5106-21.
4. Abdul-Fattah AM, Truong-Le V, Yee L, Nguyen L, Kalonia D, Cicerone MT, et al. Drying-induced variations in physico-chemical properties of amorphous pharmaceuticals and their impact on stability (I): stability of a monoclonal antibody. J Pharm Sci. 2006;96(8):1983-2008.
5. Chang L, Shepherd D, Sun J, Ouellette D, Grant KL, Tang X, et al. Mechanism of protein stabilization by sugars during freeze-drying and storage: native structure preservation, specific interaction, and/or immobilization in a glassy matrix? J Pharm Sci. 2005;94(7):1427-44.
6. Chang L, Shepherd D, Sun J, Tang X, Pikal MJ. Effect of sorbitol and residual moisture on the stability of lyophilized antibodies: Implications for the mechanism of protein stabilization in the solid state. J Pharm Sci. 2005;94(7):1445-55.
7. Li Y, Williams TD, Topp E. Effects of excipients on protein conformation in lyophilized solids by hydrogen/deuterium exchange mass spectrometry. Pharm Res. 2008;2:259-67.
8. Chang L, Pikal M. Mechanisms of protein stabilization in the solid state. J Pharm Sci. 2009;98(9):2886-908.
9. Allison SD, Manning MC, Randolph TW, Middleton K, Davis A, Carpenter JF. Optimization of storage stability of lyophilized actin using combinations of disaccharides and dextran. J Pharm Sci. 2000;89:199-214.
10. g-relaxation in pharmaceutical powders and dried proteins by thermally stimulated current. J Pharm Sci. 2009;98:81-93.
11. Pikal MJ, Chang LL, Tang XC. Evaluation of glassy-state dynamics from the width of the glass transition: results from theoretical simulation of differential scanning calorimetry and comparisons with experiment. J Pharm Sci. 2004;93(4):981-94.
12. Duddu SP, Zhang G, Dal Monte PR. The relationship between protein aggregation and molecular mobility below the glass transition temperature of lyophilized formulations containing a monoclonal antibody. Pharm Res. 1997;14(5):596-600.
13. 1H NMR and relation to aggregation-susceptibility. Pharm Res. 1996;13(6):926-30.
14. Yoshioka S, Miyazaki T, Aso Y. β-relaxation of insulin molecule in lyophilized formulations containing trehalose or dextran as a determinant of chemical reactivity. Pharm Res. 2006;23(5):961-6.
15. Yoshioka S, Aso Y. Kojima S Temperature- and glass transition temperature-dependence of bimolecular reaction rates in lyophilized formulations described by the Adam-Gibbs-Vogel equation. J Pharm Sci. 2004;93(4):1062-9.
16. Yoshioka S, Aso Y. Correlation between molecular mobility and chemical stability during storage of amorphous pharmaceuticals. J Pharm Sci. 2006;96(5):960-81.
17. Cicerone MT, Soles CL. Fast dynamics and stabilization of proteins: binary glasses of trehalose and glycerol. Biophys J. 2004;86(6):3836-45.
18. Luthra S, Hodge I, Utz M, Pikal M. Correlation of annealing with chemical stability in lyophilized pharmaceutical glasses. J Pharm Sci. 2008;94(12):5240-51.
19. Bhattacharya S, Suryanarayanan R. Local mobility in amorphous pharmaceuticals-characerization and implications on stability. J Pharm Sci. 2009;98(9):2935-53.
20. Separovic F, Lam YH, Ke X, Chan HK. A solid-state NMR study of protein hydraion and stability. Pharm Res. 1998;15(12):1816-21.
21. Tehei M, Madern D, Pfister C, Zaccai G. Fast dynamics of halophilic malate dehydrogenase and BSA measured by neutron scattering under various solvent conditions influencing protein stability. PNAS. 2001;98(25):14356-61.
22. Yu NT. Comparison of protein structure in crystals, in lyophilized state and in solution by laser Raman scattering III. a-lactalbumin. J Am Chem Soc. 1974;96:4664.
23. Sane SU, Wong R, Hsu CC. Raman spectroscopic characterization of drying-induced structural changes in a therapeutic antibody: correlating structural changes with long-term stability. J Pharm Sci. 2004;93:1005-18.
24. Prestrelski SJ, Tedeschi N, Arakawa T, Carpenter JF. Dehydration-induced conformational transitions in proteins and their inhibition by stabilizers. Biophys J. 1993;65:661-71.
25. Schersch K, Betz O, Garidel P, Muehlau S, Bassarab S, Winter G. Systematic investigation of the effect of lyophilizate collapse on pharmaceutically relevant proteins I: stability after freeze-drying. J Pharm Sci. 2010;99(5):2256-78.
26. Schersch K, Betz O, Garidel P, Muehlau S, Bassarab S, Winter G. Systematic investigation of the effect of lyophilizate collapse on pharmaceutically relevant proteins, part 2: stability during storage at elevated temperatures. J Pharm Sci. 2012;101(7):2288-306.
27. Ramachander R, Jiang Y, Li C, Eris T, Young M, Dimitrova M, et al. Solid state fluorescence of lyophilized proteins. Anal Biochem. 2008;376(2):173-82.
28. Sharma VK, Kalonia DS. Steady-state tryptophan fluorescence spectroscopy study to probe tertiary structure of proteins in solid powders. J Pharm Sci. 2003;92(4):890-9.
29. Wang W. Lyophylization and development of solid protein pharmaceuticals. Int J Pharm. 2000;203:1-60.
30. Arakawa T, Kita Y, Carpenter J. Protein-solvent interactions in pharmaceutical formulations. Pharm Res. 1991;8(3):285-91.
31. USP General Chapters: <788> Particulate matter in injections. Pharmacopeial Forum. 2009; (28):1930, USP32-NF27.
32. Wang W. Instability, stabilization, and formulation of liquid protein pharmaceuticals. Int J Pharm. 1999;185:129-88.
33. Schule S, Frieb W, Bechtold-Peters K, Garidel P. Conformational analysis of protein secondary structure during spray-drying of antibody/mannitol formulations. Eur J Pharm Biopharm. 2007;65:1-9.
34. Allison SD, Dong A, Carpenter JF. Counteracting effects of thiocyanate and sucrose on chymotrypsinogen secondary structure and aggregation during freezing, drying, and rehydration. Biophys J. 1996;71:2022-32.
35. Tang XC, Pikal MJ. The effect of stabilizers and denaturants on the cold denaturation temperatures of proteins and implications for freeze-drying. Pharm Res. 2005;22(7):1167-75.
36. Lord RC, Yu NT. Laser excited Raman spectroscopy of biomolecules. I. Native lysozyme and its constituent amino acids. J Mol Biol. 1970;50:509-24.
37. Lord RC, Yu NT. Laser-excited Raman spectroscopy of biomolecules. II. Native ribonuclease and α-chymotrypsin. J Mol Biol. 1970;51:203-13.
38. Koenig JL. Raman spectroscopy of biological molecules: a review. J Polymer Sci. 1972;6(1):59-177.
39. Gallivan J, Dougherty D. Cation-π interactions in structural biology. Proc Natl Acad Sci USA. 1999;96(17):9459-64.
40. Wang B, Tchessalov S, Warne N, Pikal MJ. Impact of sucrose level on storage stability of proteins freeze-dried solids: I. Correlation of protein-sugar interaction with native structure preservation. J Pharm Sci. 2009;98(9):3131-44.
41. Chi EY, Krishnan S, Kendrick BS, Chang BS, Carpenter JF, Randolph TW. Roles of conformational stability and colloidal stability in the aggregation of recombinant human GCSF. Protein Sci. 2003;12(5):903-13.
42. Izutsu K, Yoshioka S, Terao T. Decreased protein-stabilizing effects of cryoprotectants due to crystallization. Pharm Res. 1993;8:1232-7.
43. Meyer J, Nayar R, Manning M. Impact of bulking agents on the stability of a lyophilized monoclonal antibody. Eur J Pharm Sci. 2009;38:29-38.
44. Prestrelski SJ, Pikal KA, Arakawa T. Optimization of lyophilization conditions for recombinant human interleukin-1 by dried state conformational analysis using Frourier-transform infrared spectroscopy. Pharm Res. 1995;12(9):1250-9.
45. Brunner H, Holz M. Raman studies of the conformation of the basic pancreatic trypsin inhibitor. Biochimica et Biophysica Acta (BBA)-Protein. Structure. 1975;379(2):408-17.
46. Sharma VK, Kalonia DS. Effect of vacuum drying on protein-mannitol interactions: the physical state of mannitol and protein structure in the dried state. AAPS PharmSciTech. 2004;5(1):1-12. article 10.
47. Kim AI, Akers MJ, Nail SL. The physical state of mannitol after freeze-drying: effect of mannitol concentration, freezing rate, and a noncrystallizing cosolute. J Pharm Sci. 1998;87:931-5.