Trehalose limits BSA aggregation in spray-dried formulations at high temperatures: Implications in preparing polymer implants for long-term protein delivery

Journal of Pharmaceutical Sciences

Volumn 102, Issue 8, 2013, Pages 2655-2666

  Rajagopal, Karthikan ^a   Wood, Joseph ^a   Tran, Benjamin ^a   Patapoff, Thomas W ^a   Nivaggioli, Thierry ^a  

^a GENENTECH INC   (United States)

Author keywords

Hot melt extrusion; Polymer implants; Protein delivery; Solid state; Spray drying; Stability; Trehalose

Indexed keywords

BOVINE SERUM ALBUMIN; HISTIDINE; PHOSPHATE BUFFERED SALINE; POLYGLACTIN; POLYMER; TREHALOSE;

ARTICLE; DRUG DELIVERY SYSTEM; DRUG STABILITY; HEAT TREATMENT; HIGH TEMPERATURE; IMPLANT; IN VITRO STUDY; LASER DIFFRACTION; PARTICLE SIZE; PH; POLYMER IMPLANT; PROTEIN AGGREGATION; PROTEIN SECONDARY STRUCTURE; PROTEIN STABILITY; PROTEIN UNFOLDING; SPRAY DRYING; SUSTAINED DRUG RELEASE; TEMPERATURE DEPENDENCE; WATER TRANSPORT;

EID: 84880974502     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23634     Document Type: Article

References (37)

1. del Amo EM, Urtti A. 2008. Current and future ophthalmic drug delivery systems. A shift to the posterior segment. Drug Discov Today 13(3-4):135-143.
2. Sinha VR, Trehan A. 2003. Biodegradable microspheres for protein delivery. J Control Release 90(3):261-280.
3. Zhu GZ, Mallery SR, Schwendeman SP. 2000. Stabilization of proteins encapsulated in injectable poly (lactide-co-glycolide). Nat Biotechnol 18(1):52-57.
4. Lee SS, Hughes P, Ross AD, Robinson MR. 2010. Biodegradable implants for sustained drug release in the eye. Pharm Res 27(10):2043-2053.
5. Van Tomme SR, Hennink WE. 2007. Biodegradable dextran hydrogels for protein delivery applications. Expert Rev Med Devices 4(2):147-164.
6. Vintiloiu A, Leroux JC. 2008. Organogels and their use in drug delivery-A review. J Control Release 125(3):179-192.
7. Hatefi A, Amsden B. 2002. Biodegradable injectable in situ forming drug delivery systems. J Control Release 80(1-3):9-28.
8. Krasko MY, Kumar N, Domb AJ. 2006. Protein and peptide release from in situ gelling polymer. Biomacromolecules 7(8):2461-2463.
9. Schoenhammer K, Boisclair J, Schuetz H, Petersen H, Goepferich A. 2010. Biocompatibility of an injectable in situ forming depot for peptide delivery. J Pharm Sci 99(10):4390-4399.
10. Lin C-C, Metters AT. 2006. Hydrogels in controlled release formulations: Network design and mathematical modeling. Adv Drug Deliv Rev 58(12-13):1379-1408.
11. Arifin DY, Lee LY, Wang C-H. 2006. Mathematical modeling and simulation of drug release from microspheres: Implications to drug delivery systems. Adv Drug Deliv Rev 58(12-13):1274-1325.
12. Fredenberg S, Wahlgren M, Reslow M, Axelsson A. 2011. The mechanisms of drug release in poly(lactic-co-glycolic acid)-based drug delivery systems-A review. Int J Pharm 415(1-2):34-52.
13. Rothstein SN, Federspiel WJ, Little SR. 2009. A unified mathematical model for the prediction of controlled release from surface and bulk eroding polymer matrices. Biomaterials 30(8):1657-1664.
14. Sackett CK, Narasimhan B. 2011. Mathematical modeling of polymer erosion: Consequences for drug delivery. Int J Pharm 418(1):104-114.
15. Wolinsky JB, Colson YL, Grinstaff MW. 2012. Local drug delivery strategies for cancer treatment: Gels, nanoparticles, polymeric films, rods, and wafers. J Control Release 159(1):14-26.
16. Repka MA, Shah S, Lu JN, Maddineni S, Morott J, Patwardhan K, Mohammed NN. 2012. Melt extrusion: Process to product. Expert Opin Drug Deliv 9(1):105-125.
17. Qian F, Szymanski A, Gao JM. 2001. Fabrication and characterization of controlled release poly(D, L-lactide-co-glycolide) millirods. J Biomed Mat Res 55(4):512-522.
18. Zhang XC, Wyss UP, Pichora D, Goosen MFA. 1994. A mechanistic study of antibiotic release from biodegradable poly(d, l-lactide) cylinders. J Control Release 31(2):129-144.
19. Haaga JR, Exner AA, Wang YD, Stowe NT, Tarcha PJ. 2006. Combined tumor therapy by using radiofrequency ablation and 5-FU-laden polymer implants: Evaluation in rats and rabbits. Radiology 237(3):911-918.
20. Zhang XC, Wyss UP, Pichora D, Amsden B, Goosen MFA. 1993. Controlled-release of albumin from biodegradable poly(dl-lactide) cylinders. J Control Release 25(1-2):61-69.
21. Jain NK, Roy I. 2009. Effect of trehalose on protein structure. Protein Sci 18(1):24-36.
22. Carpenter JF, Pikal MJ, Chang BS, Randolph TW. 1997. Rational design of stable lyophilized protein formulations: Some practical advice. Pharm Res 14(8):969-975.
23. Ghalanbor Z, Korber M, Bodmeier R. 2009. Improved lysozyme stability and release properties of poly(lactide-co-glycolide) implants prepared by hot-melt extrusion. Pharm Res 27(2):371-379.
24. Jain RA. 2000. The manufacturing techniques of various drug loaded biodegradable poly(lactide-co-glycolide) (PLGA) devices. Biomaterials 21(23):2475-2490.
25. Gill SC, Vonhippel PH. 1989. Calculation of protein extinction coefficients from amino-acid sequence data. Anal Biochem 182(2):319-326.
26. Maa Y-F, Costantino HR, Nguyen P-A, Hsu CC. 1997. The effect of operating and formulation variables on the morphology of spray-dried protein particles. Pharm Dev Technol 2(3):213-223.
27. Costantino HR, Shieh L, Klibanov AM, Langer R. 1997. Heterogeneity of serum albumin samples with respect to solid-state aggregation via thiol-disulfide interchange-Implications for sustained release from polymers. J Control Release 44(2-3):255-261.
28. Vetri V, Librizzi F, Leone M, Militello V. 2007. Thermal aggregation of bovine serum albumin at different pH: Comparison with human serum albumin. Eur Biophys J 36(7):717-725.
29. Bhattacharya M, Jain N, Mukhopadhyay S. 2012. Insights into the mechanism of aggregation and fibril formation from bovine serum albumin. J Phys Chem B 115(14):4195-4205.
30. Pikal MJ, Rigsbee DR, Roy ML. 2007. Solid state chemistry of proteins: I. Glass transition behavior in freeze dried disaccharide formulations of human growth hormone (hGH). J Pharm Sci 96(10):2765-2776.
31. Michnik A. 2003. Thermal stability of bovine serum albumin DSC study. J Therm Anal Calorim 71(2):509-519.
32. Chang LQ, Pikal MJ. 2009. Mechanisms of protein stabilization in the solid state. J Pharm Sci 98(9):2886-2908.
33. Kang JC, Schwendeman SP. 2002. Comparison of the effects of Mg(OH)(2) and sucrose on the stability of bovine serum albumin encapsulated in injectable poly(D, L-lactide-co-glycolide) implants. Biomaterials 23(1):239-245.
34. Shenderova A, Burke TG, Schwendeman SP. 1999. The acidic microclimate in poly(lactide-co-glycolide) microspheres stabilizes camptothecins. Pharm Res 16(2):241-248.
35. Shenderova A, Ding AG, Schwendeman SP. 2004. Potentiometric method for determination of microclimate pH in poly(lactic-co-glycolic acid) films. Macromolecules 37(26):10052-10058.
36. Estey T, Kang J, Schwendeman SP, Carpenter JF. 2006. BSA degradation under acidic conditions: A model for protein instability during release from PLGA delivery systems. J Pharm Sci 95(7):1626-1639.
37. Zhu GZ, Schwendeman SP. 2000. Stabilization of proteins encapsulated in cylindrical poly(lactide-co-glycolide) implants: Mechanism of stabilization by basic additives. Pharm Res 17(3):351-357.