Enhanced Physical Stability of Amorphous Drug Formulations via Dry Polymer Coating

Capece, Maxx; Davé, Rajesh N.

doi:10.1002/jps.24451

Cited by 17 publications

(18 citation statements)

References 30 publications

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“…The different rates of surface and bulk crystallization can lead to complex crystallization kinetics. 29,40,41 During isothermal storage of amorphous IMC, the degree of crystallinity rises initially and then approximately plateaus below 100 % crystallinity; the plateau is higher if the particle size is smaller. In this two-stage crystallization, the initial rise of crystallinity corresponds to surface crystallization; after the free surface is fully covered, crystallization rate slows because the fast surface process is replaced by the slower bulk process.…”

Section: Surface Mobility and Its Role In The Stability Of Molecmentioning

confidence: 99%

“…Besides IMC, this two-stage crystallization has been reported for amorphous griseofulvin, 31 felodipine, 40 and acetaminophen. 41 Surface Mobility and Fast Bulk Crystallization through Fracture. Small-molecule glasses are brittle and easily fractured.…”

Section: Surface Mobility and Its Role In The Stability Of Molecmentioning

confidence: 99%

“…For systems showing fast surface crystallization, increasing the particle size can slow the rate of overall crystallization (because the surface process affects a smaller fraction of the material). 29,31,40,41 A second way to prevent surface-facilitated transformations is coating the free surface. Under a coating, surface crystal growth on molecular glasses can be inhibited.…”

Section: Surface-enhanced Chemicalmentioning

confidence: 99%

“…Besides solution-applied coatings, dry coatings can be effective for inhibiting surface crystallization. 41,69 Loading amorphous drugs in porous inorganic glasses can improve stability 70 and the effect may involve the reduction of free surfaces and the contact with inert solid surfaces.…”

Section: Surface-enhanced Chemicalmentioning

confidence: 99%

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Surface mobility of molecular glasses and its importance in physical stability

2016

Advanced Drug Delivery Reviews

138

134

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Amorphous molecular materials (molecular glasses) are useful for drug delivery, bio-preservation and organic electronics. A central issue in developing amorphous materials is the stability against crystallization and other transformations that can compromise material performance. We review recent progress in understanding the stability of molecular glasses, particularly the role for surface mobility. Surface diffusion in molecular glasses can be vastly faster than bulk diffusion. This high surface mobility enables fast crystal growth on the free surface. In this process, surface crystals grow upward and laterally, with the lateral growth rate being roughly proportional to surface diffusivity. Surface mobility also influences bulk crystal growth as the process can create fracture and free surfaces. During vapor deposition, surface mobility allows efficient equilibration of newly deposited molecules, producing low-energy, high-density glasses that are equivalent to liquid-cooled glasses aged for thousands of years. Free surfaces can accelerate chemical degradation of proteins. Measures for inhibiting surface-facilitated transformations include minimizing free surfaces, applying surface coatings, and preventing fracture.

show abstract

Section: Surface Mobility and Its Role In The Stability Of Molecmentioning

confidence: 99%

Section: Surface Mobility and Its Role In The Stability Of Molecmentioning

confidence: 99%

Section: Surface-enhanced Chemicalmentioning

confidence: 99%

Section: Surface-enhanced Chemicalmentioning

confidence: 99%

See 2 more Smart Citations

Surface mobility of molecular glasses and its importance in physical stability

2016

Advanced Drug Delivery Reviews

138

134

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“…The temperatures ranged from 2°C to 60°C and the relative humidity varied between 0% and 100%. The duration also varied significantly, with stability studies lasting from 24 h to two years (73,74,81,82,84,86,88,92,93,104,105,109,110,113,115,116,118,120,123,124,126,127,129,130,132,134,135,139,143,146,149,153,158,166,169,172,175,176). While most of the studies did not mention the container used for the physical stability test, a few specified, for example, whether a closed or open container was used (88,92,113,123,132,146).…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago. In this review we try to answer the following questions: What model compounds and excipients have been used in amorphous-based research? How were these two components selected and prepared? What methods have been used to assess the performance of amorphous formulation? What methodology have evolved and/or been standardized since amorphous-based formulation was first introduced and to what extent have we embraced on new methods? Is the extent of research mirrored in the number of marketed amorphous drug products? We have summarized the history and evolution of amorphous formulation and discuss the current status of amorphous formulation-related research practice. We also explore the potential uses of old experimental methods and how they can be used in tandem with computational tools in designing amorphous formulation more efficiently than the traditional trial-and-error approach.

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Amino acids as stabilizers for spray-dried simvastatin powder for inhalation

Rades

Chan

et al. 2019

International Journal of Pharmaceutics

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Enhanced Physical Stability of Amorphous Drug Formulations via Dry Polymer Coating

Cited by 17 publications

References 30 publications

Surface mobility of molecular glasses and its importance in physical stability

Surface mobility of molecular glasses and its importance in physical stability

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

Amino acids as stabilizers for spray-dried simvastatin powder for inhalation

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