Early stage phase separation in pharmaceutical solid dispersion thin films under high humidity: Improved spatial understanding using probe-based thermal and spectroscopic nanocharacterization methods

Molecular Pharmaceutics

Volumn 10, Issue 3, 2013, Pages 918-930

  Qi, Sheng ^a   Moffat, Jonathan G ^a   Yang, Ziyi ^a  

^a UNIVERSITY OF EAST ANGLIA   (United Kingdom)

Author keywords

crystallization; nanocharacterization; phase separation; solid dispersion; thin films

Indexed keywords

FELODIPINE; POLYMER;

ARTICLE; ATOMIC FORCE MICROSCOPY; CRYSTALLIZATION; DISPERSION; FILM; HUMIDITY; INFRARED SPECTROSCOPY; MOLECULAR PROBE; NANOTHERMAL ANALYSIS; PHASE SEPARATION; PHOTOTHERMAL INFRARED MICROSPECTROSCOPY; PRIORITY JOURNAL; SOLID DISPERSION; THERMAL ANALYSIS;

EID: 84874599515     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp300557q     Document Type: Article

References (44)

1. Chiou, W. L.; Riegelman, S. Pharmaceutical applications of solid dispersion systems J. Pharm. Sci. 1971, 60, 1281-1302
2. Ford, J. L. The current status of solid dispersions Pharm. Acta Helv. 1986, 61, 69-88
3. Serajuddin, A. T. Solid dispersion of poorly water-soluble drugs: Early promises, subsequent problems, and recent breakthroughs J. Pharm. Sci. 1999, 88 (10) 1058-66
4. Rumondor, A. C. F.; Stanford, L. A.; Taylor, L. S. Effect of Polymer Type and Storage Relative Humidity on the Kinetics of Felodipine Crystallization from Amorphous Solid Dispersions Pharm. Res. 2009, 26 (12) 2599-2606
5. Rumondor, A. C. F.; Taylor, L. S. Effect of Polymer Hygroscopicity on the Phase Behavior of Amorphous Solid Dispersions in the Presence of Moisture Mol. Pharmaceutics 2010, 7 (2) 477-490
6. Weuts, I.; Van Dycke, F.; Voorspoels, J.; De Cort, S.; Stokbroekx, S.; Leemans, R.; Brewster, M. E.; Xu, D.; Segmuller, B.; Turner, Y. Z. A.; Roberts, C. J.; Davies, M. C.; Qi, S.; Craig, D. Q. M.; Reading, M. Physicochemical properties of the amorphous drug, cast films, and spray dried powders to predict formulation probability of success for solid dispersions: etravirine J. Pharm. Sci. 2011, 100 (1) 260-274
7. Janssens, S.; De Zeure, A.; Paudel, A.; Van Humbeeck, J.; Rombaut, P.; Van den Mooter, G. Influence of preparation methods on solid state supersaturation of amorphous solid dispersions: A case study with itraconazole and Eudragit E100 Pharm. Res. 2010, 27 (5) 775-785
8. Caron, V.; Tajber, L.; Corrigan, O. I.; Healy, A. M. A comparison of spray drying and milling in the production of amorphous dispersions of sulfathiazole/polyvinylpyrrolidone and sulfadimidine/polyvinylpyrrolidone Mol. Pharm. 2011, 8 (2) 532-542
9. Zelikin, A. N. Drug Releasing Polymer Thin Films: New Era of Surface-Mediated Drug Delivery ACS Nano 2010, 4 (5) 2494-2509
10. Bose, A.; Nelson, P. Endovascular thin film devices and methods for treating and preventing stroke. U.S. Patent 6605111, 2003.
11. Ciolino, J. B.; Hoare, T. R.; Iwata, N. G.; Behlau, I.; Dohlman, C. H.; Langer, R.; Kohane, D. S. A Drug-Eluting Contact Lens Invest. Ophthalmol. Vis. Sci. 2009, 50, 3346-3352
12. Wendlandt, M.; Kerle, T.; Heuberger, M.; Klein, J. Phase Separation in Thin Films of Polymer Blends: The Influence of Symmetric Boundary Conditions J. Polym. Sci., Polym. Phys. 2000, 38, 831-837
13. Wang, H.; Composto, R. J. Wetting and Phase Separation in Polymer Blend Films: Identification of Four Thickness Regimes with Distinct Morphological Pathways Interface Sci. 2003, 11, 237-248
14. Karim, A.; Slawecki, T. M.; Kumar, S. K.; Douglas, J. F.; Satija, S. K.; Han, C. C.; Russell, T. P.; Liu, Y.; Overney, R.; Sokolov, J.; Rafailovich, M. H. Phase-Separation-Induced Surface Patterns in Thin Polymer Blend Films Macromolecules 1998, 31, 857-862
15. Vogt, B. D.; Soles, C. L.; Lee, H. J.; Lin, E. K.; Wu, W. L. Moisture absorption into ultrathin hydrophilic polymerfilms on different substrate surfaces Polymer 2005, 46 (5) 1635-1642
16. Lee, S. S.; Muralidharan, S.; Woll, A.; Loth, M. A.; Li, Z.; Anthony, J. E.; Haataja, M.; Loo, Y.-L. Understanding heterogeneous nucleation in binary, solution-processed, organic semiconductor thin films Chem. Mater. 2012, 24, 2920-2928
17. Huang, I.-H.; Chang, L.; Woo, E. M. Tannin induced single crystalline morphology in poly(ethylene succinate) Macromol. Chem. Phys. 2011, 212, 1155-1164
18. Qi, S.; Marchaud, D.; Craig, D. Q. M. An Investigation into the Mechanism of Dissolution Rate Enhancement of Poorly Water-Soluble Drugs from Spray Chilled Gelucire 50/13 Microspheres J. Pharm. Sci. 2010, 99 (1) 262-274
19. Konno, H.; Taylor, L. S. Ability of Different Polymers to Inhibit the Crystallization of Amorphous Felodipine in the Presence of Moisture Pharm. Res. 2008, 25 (4) 969-978
20. Marsac, P. J.; Rumondor, A. C. F.; Nivens, D. E.; Kestur, U. S.; Stanciu, L.; Taylor, L. S. Effect of Temperature and Moisture on the Miscibility of Amorphous Dispersions of Felodipine and Poly(vinyl pyrrolidone) J. Pharm. Sci. 2010, 99 (1) 169-185
21. Rumondor, A. C. F.; Jackson, M. J.; Taylor, L. S. Effects of Moisture on the Growth Rate of Felodipine Crystals in the Presence and Absence of Polymers Cryst. Growth Des. 2010, 10 (2) 747-753
22. Trasi, N. S.; Taylor, L. S. Effect of polymers on nucleation and crystal growth of amorphous acetaminophen CrystEngComm 2012, 14, 5188-5197
23. ® E prepared by hot-melt extrusion using thermal, microthermal and spectroscopic analysis Int. J. Pharm. 2008, 354 (1-2) 158-167
24. Harding, L.; Qi, S.; Hill, G.; Reading, M.; Craig, D. Q. M. The development of microthermal analysis and photothermal microspectroscopy as novel approaches to drug-excipient compatibility studies Int. J. Pharm. 2008, 354 (1-2) 149-157
25. Qi, S.; Belton, P.; Nollenberger, K.; Gryczke, A.; Craig, D. Q. M. Compositional analysis of low quantities of phase separation in hot melt extruded solid dispersions: a combined atomic force microscopy, photothermal Fourier-transform infrared microspectroscopy and localised thermal analysis approach Pharm. Res. 2011, 28 (9) 2311-2326
26. Konno, H.; Taylor, L. S. Influence of Different Polymers on the Crystallization Tendency of Molecularly Dispersed Amorphous Felodipine J. Pharm. Sci. 2006, 95 (12) 2692-2705
27. Kestur, U. S.; Ivanisevic, I.; Alonzo, D. E.; Taylor, L. S. Influence of Particle Size on the Crystallization Kinetics of Amorphous Felodipine Powders. Powder Technol. 2012, in press.
28. Marsac, P. J.; Konno, H.; Rumondor, A. C. F.; Taylor, L. S. Recrystallization of Nifedipine and Felodipine from Amorphous Molecular Level Solid Dispersions Containing Poly(vinylpyrrolidone) and Sorbed Water Pharm. Res. 2008, 25 (3) 647-656
29. Hammiche, A.; Pollock, H. M.; Reading, M.; Claybourn, M.; Turner, P. H.; Jewkes, K. Photothermal FT-IR Spectroscopy: A Step Towards FT-IR Microscopy at a Resolution Better Than the Diffraction Limit Appl. Spectrosc. 1999, 53 (7) 810-815
30. Bozec, L.; Hammiche, A.; Pollock, H. M.; Conroy, M.; Chalmers, J. M.; Everall, N. J.; Turin, L. Localized photothermal infrared spectroscopy using a proximal probe J. Appl. Phys. 2001, 90, 5159-5165
31. Jones, B. A.; Torkelson, J. M. Large melting point depression of 2-3-nm length-scale nanocrystals formed by the self-assembly of an associative polymer: Telechelic, pyrene-labeled poly(dimethylsiloxane) Polym. Phys. 2004, 42 (18) 3470-3475
32. Liang, L. H.; Li, J. C.; Jiang, Q. Size-dependent melting depression and lattice contraction of Bi nanocrystals Phys. B 2003, 334 (1-2) 49-53
33. Jiang, Q.; Zhang, Z.; Li, J. C. Melting thermodynamics of nanocrystals embedded in a matrix Acta Mater. 2000, 48, 4791-4795
34. Witten, T. A.; Sander, L. M. Diffusion-limited aggregation, a kinetic critical phenomenon Phys. Rev. Lett. 1981, 47, 1400-1403
35. Fox, T. G. Influence of diluent and of copolymer composition on the glass temperature of a polymer system Bull. Am. Phys. Soc. 1956, 1, 123
36. Van Alsten, J. G.; Lustig, S. R. Polymer mutual diffusion measurements using infrared ATR spectroscopy Macromolecules 1992, 25 (19) 5069-5073
37. g Pharm. Res. 2006, 23 (10) 2350-2355
38. Zhu, L.; Wong, L.; Yu, L. Surface-enhanced crystallization of amorphous nifedipine Mol. Pharmaceutics 2008, 5, 921-926
39. Sun, Y.; Zhu, L.; Kearns, K. L.; Ediger, M. D.; Yu, L. Glass crystallize rapidly at free surfaces by growing crystals upward Proc. Natl. Acad. Sci. U.S.A. 2011, 108 (15) 5990-5995
40. g Pharm. Res. 2010, 27 (8) 1558-1567
41. Ishida, H.; Wu, T.; Yu, L. Sudden Rise of Crystal Growth Rate of Nifedipine near Tg with out and with Polyvinylpyrrolidone J. Pharm. Sci. 2007, 96 (5) 1131-1138
42. Wu, T.; Sun, Y.; Li, N.; de Villiers, M. M.; Yu, L. Inhibiting surface crystallization of amorphous indomethacin by nanocoating Langmuir 2007, 23 (9) 5148-5153
43. Cai, T.; Zhu, L.; Yu, L. Crystallisaiton of Organic Glasses: Effects of Polymer Additives on Bulk and Surface Crystal Growth in Amorphous Nifedipine Pharm. Res. 2011, 28, 2458-2466
44. Wang, M.; Braun, H. G.; Meyer, E. Transition of Crystal Growth as a Result of Changing Polymer States in Ultrathin Poly(ethylene oxide)/Poly(methyl methacrylate) Blend Films with Thickness of <3 nm Macromolecules 2004, 37, 437-445