Impact of Molecular Surface Diffusion on the Physical Stability of Co-Amorphous Systems
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Impact of Molecular Surface Diffusion on the Physical Stability of Co-Amorphous Systems. / Liu, Jingwen; Hwu, Ente; Bannow, Jacob; Grohganz, Holger; Rades, Thomas.
In: Molecular Pharmaceutics, Vol. 19, No. 4, 2022, p. 1183-1190.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Impact of Molecular Surface Diffusion on the Physical Stability of Co-Amorphous Systems
AU - Liu, Jingwen
AU - Hwu, Ente
AU - Bannow, Jacob
AU - Grohganz, Holger
AU - Rades, Thomas
N1 - Funding Information: J.L. acknowledges the China Scholarship Council (201806350247) for financial support.
PY - 2022
Y1 - 2022
N2 - In this study, surface diffusion of l-aspartic acid-carvedilol (ASP-CAR) co-amorphous systems at different ASP concentrations is measured and correlated with their physical stability. ASP-CAR films at ASP concentrations of 1-5% (w/w) were prepared by a newly developed method based on a vacuum compression molding process. Surface diffusion measurements were conducted on these systems based on the surface grating decay method using atomic force microscopy (AFM). The results demonstrate that a small amount of ASP (i.e., ≤ 5% w/w) in the co-amorphous systems could significantly slow down the grating decay process compared with that of pure amorphous CAR, indicating a reduced surface diffusion of CAR molecules. The decay time gradually increased in co-amorphous systems with increasing ASP concentration from 1 to 5% (w/w), with the longest observed decay time of around 800 h for the 5%ASP-CAR system, which was more than 200 times longer compared to the decay time of pure amorphous CAR (approximately 3 h). A good correlation between the decay constants of the pure amorphous CAR and co-amorphous films at ASP concentrations of 1-5% (w/w) and the physical stability of corresponding amorphous powder samples was found. Overall, this study provides a new method to prepare co-amorphous films for surface property measurements and reveals the impact of surface diffusion on the physical stability of co-amorphous systems.
AB - In this study, surface diffusion of l-aspartic acid-carvedilol (ASP-CAR) co-amorphous systems at different ASP concentrations is measured and correlated with their physical stability. ASP-CAR films at ASP concentrations of 1-5% (w/w) were prepared by a newly developed method based on a vacuum compression molding process. Surface diffusion measurements were conducted on these systems based on the surface grating decay method using atomic force microscopy (AFM). The results demonstrate that a small amount of ASP (i.e., ≤ 5% w/w) in the co-amorphous systems could significantly slow down the grating decay process compared with that of pure amorphous CAR, indicating a reduced surface diffusion of CAR molecules. The decay time gradually increased in co-amorphous systems with increasing ASP concentration from 1 to 5% (w/w), with the longest observed decay time of around 800 h for the 5%ASP-CAR system, which was more than 200 times longer compared to the decay time of pure amorphous CAR (approximately 3 h). A good correlation between the decay constants of the pure amorphous CAR and co-amorphous films at ASP concentrations of 1-5% (w/w) and the physical stability of corresponding amorphous powder samples was found. Overall, this study provides a new method to prepare co-amorphous films for surface property measurements and reveals the impact of surface diffusion on the physical stability of co-amorphous systems.
KW - atomic force microscopy
KW - co-amorphous
KW - physical stability
KW - surface diffusion
KW - surface mobility
U2 - 10.1021/acs.molpharmaceut.1c00973
DO - 10.1021/acs.molpharmaceut.1c00973
M3 - Journal article
C2 - 35230110
AN - SCOPUS:85126148898
VL - 19
SP - 1183
EP - 1190
JO - Molecular Pharmaceutics
JF - Molecular Pharmaceutics
SN - 1543-8384
IS - 4
ER -
ID: 305394910