The effect of mannitol crystallization in mannitol-sucrose systems on LDH stability during freeze-drying

Journal of Pharmaceutical Sciences

Volumn 101, Issue 7, 2012, Pages 2534-2544

  Al Hussein, Anas ^a   Gieseler, Henning ^a,b  

^a UNIVERSITY OF ERLANGEN NUREMBERG   (Germany)

^b GILYOS GmbH   (Germany)

Author keywords

Crystallization; Excipients; Freeze drying; FTIR; Lyophilization; Protein formulation; Surfactants; Thermal analysis; X ray powder diffraction

Indexed keywords

LACTATE DEHYDROGENASE; MANNITOL; SUCROSE; EXCIPIENT;

ARTICLE; CONTROLLED STUDY; CRYSTALLIZATION; DIFFERENTIAL SCANNING CALORIMETRY; ENZYME ACTIVITY; ENZYME STABILITY; FREEZE DRYING; HYDROGEN BOND; INFRARED SPECTROSCOPY; PROTEIN FUNCTION; PROTEIN STABILITY; PROTEIN STRUCTURE; X RAY POWDER DIFFRACTION; ANIMAL; CHEMISTRY; POWDER DIFFRACTION; RABBIT; X RAY DIFFRACTION;

ANIMALS; CRYSTALLIZATION; ENZYME STABILITY; EXCIPIENTS; FREEZE DRYING; L-LACTATE DEHYDROGENASE; MANNITOL; POWDER DIFFRACTION; RABBITS; SPECTROSCOPY, FOURIER TRANSFORM INFRARED; SUCROSE; X-RAY DIFFRACTION;

EID: 84866281878     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23173     Document Type: Article

References (36)

1. Goodman M. 2009. Sales of biologics to show robust growth through to 2013. Nat Rev Drug Discov 8:837-838.
2. Wang W. 2000. Lyophilization and development of solid protein pharmaceuticals. Int J Pharm 203:1-60.
3. Pikal MJ. 1990. Freeze-drying of proteins. Part I: Process design. BioPharm 3:18-28.
4. Pikal MJ. 1990. Freeze-drying of proteins. Part II: Formulation selection. BioPharm 3:26-30.
5. Liao X, Krishnamurthy R, Suryanarayanan R. 2005. Influence of the active pharmaceutical ingredient concentration on the physical state of mannitol-Implications in freeze-drying. Pharm Res 22:1978-1985.
6. Timasheff SN. 1993. The control of protein stability and association by weak interactions with water: How do solvents affect these processes? Annu Rev Biophy Biomol Struct 22:67-97.
7. Carpenter JF, Crowe JH, Arakawa T. 1990. Comparison of solute-induced protein stabilization in aqueous solution and in frozen and dried state. J Dairy Sci 73:3627-3636.
8. Tang XC, Pikal MJ. 2004. Design of freeze-drying processes for pharmaceuticals: Practical advice. Pharm Res 21:91-200.
9. Izutsu K, Yoshioka S, Terao T. 1994. The effect of mannitol crystallinity on the stabilization of enzymes during freeze-drying. Chem Pharm Bull 42:5-8.
10. Schneid S, Riegger X, Gieseler H. 2008. Influence of common excipients on the crystalline modification of freeze-dried mannitol. Pharm Technol 3:178-184.
11. Kim AI, Akers MJ, Nail SL. 1998. The physical state of mannitol after freeze-drying: Effects of mannitol concentration, freezing rate, and a noncrystallizing cosolute. J Pharm Sci 87:931-935.
12. Jiang S, Nail SL. 1998. Effect of process conditions on recovery of protein activity after freezing and freeze-drying. Eur J Pharm Biopharm 45:249-257.
13. Schersch K, Betz O, Garidel P, Muehlau S, Bassarab S, Winter G. 2010. Systematic investigation of the effect of lyophilizate collapse on pharmaceutically relevant proteins I: Stability after freeze-drying. J Pharm Sci 99:2256-2278.
14. Pyne A, Chatterjee K, Suryanarayanan R. 2003. Solute crystallization in mannitol-glycine systems-Implications on protein stabilization in freeze-dried formulations. J Pharm Sci 92:2272-2283.
15. Izutsu K, Yoshioka S, Terao T. 1993. Decreased protein stabilizing effects of cryoprotectants due to crystallization. Pharm Res 10:1232-1237.
16. Izutsu K, Kojima S. 2002. Excipient crystallinity and its protein-structure stabilizing effect during freeze-drying. J Pharm Pharmacol 54(8):1033-1039.
17. Carpenter JF, Prestrelski SJ, Arakawa T. 1993. Separation of freezing- and drying-induced denaturation of lyophilized proteins using stress-specific stabilization. I. Enzyme activity and calorimetric studies. Arch Biochem Biophys 303:456-464.
18. Anchordoquy TJ, Carpenter JF. 1996. Polymers protect lactate dehydrogenase during freeze-drying by inhibiting dissociation in the frozen state. Arch Biochem Biophys 332:231-238.
19. Torrado S, Torrado S. 2002. Characterization of physical state of mannitol after freeze-drying: Effect of acetylsalicylic acid as a second crystalline cosolute. Chem Pharm Bull 50(5):567-570.
20. Barth A. 2007. Infrared spectroscopy of proteins. Biochim Biophys Acta 1767:1073-1101.
21. Kong J, Yu S. 2007. Fourier transform infrared spectroscopic analysis of protein secondary structures. Acta Biochim Biophys Sinica 39:549-559.
22. Dong A, Prestrelski SJ, Allison SD, Carpenter JF. 1995. Infrared spectroscopic studies of lyophilization- and temperature-induced protein aggregation. J Pharm Sci 84:415-424.
23. Barth A, Zscherp C. 2002. What vibrations tell us about proteins. Quart Rev Biophys 35:369-430.
24. Vonhoff S, Condliffe J, Schiffter H. 2010. Implementation of an FTIR calibration curve for fast and objective determination of changes in protein secondary structure during formulation development. J Pharm Biomed Anal 51:39-45.
25. Prestrelski SJ, Tedeschi N, Arakawa T, Carpenter JF. 1993. Dehydration-induced conformational transitions in proteins and their inhibition by stabilizers. Biophys J 65:661-671.
26. Carpenter JF, Prestrelski SJ, Dong A. 1998. Application of infrared spectroscopy to development of stable lyophilized protein formulations. Eur J Pharm Biopharm 45:231-238.
27. Tian F, Middaugh CR, Offerdahl T, Munson E, Sane S, Rytting JH. 2007. Spectroscopic evaluation of the stabilization of humanized monoclonal antibodies in amino acid formulations. Int J Pharm 335:20-31.
28. Burger A, Henck JO, Hetz S, Rollinger JM, Weissnicht AA, Stoettner H. 2000. Energy/temperature diagram and compression behavior of the polymorphs of d-mannitol. J Pharm Sci 89:457-468.
29. Cavatur RK, Vemuri N M, Pyne A, Chrzan Z, Velasquez DT, Suryanarayanan R. 2002. Crystallization behavior of mannitol in frozen aqueous solutions. Pharm Res 19:894-900.
30. Crowe JH, Crowe LM, Carpenter JF. 1993. Preserving dry biomaterials: The water replacement hypothesis. BioPharm 6:28-37.
31. Allison SD, Randolph TW, Manning MC, Middleton K, Davis A, Carpenter JF. 1998. Effects of drying methods and additives on structure and function of actin: Mechanisms of dehydration-induced damage and its inhibition. Arch Biochem Biophy 358:171-181.
32. Pikal MJ. 2002. Freeze drying. In Encyclopedia of pharmaceutical technology; Swarbrick J, Ed. Vol. 2. New York: Marcel Dekker Publishing Company, pp 1299-1326.
33. Cleland JL, Lam X, Kendrick B, Yang J, Overcashier D, Brooks D, Hsu C, Carpenter JF. 2001. A specific molar ratio of stabilizer to protein is required for storage stability of a lyophilized monoclonal antibody. J Pharm Sci 90:310-321.
34. Strambini GB, Gabellieri E. 1996. Proteins in frozen solutions evidence of ice-induced partial unfolding. Biophys J 70:971-976.
35. Bam NB, Randolph TW, Cleland JL. 1995. Stability of protein formulations: Investigation of surfactant effects by a novel EPR spectroscopic technique. Pharm Res 12:2-11.
36. Schwegman JJ, Carpenter JF, Nail SL. 2009. Evidence of partial unfolding of proteins at the ice/freeze-concentrate interface by infrared microscopy. J Pharm Sci 98:3239-3246.