Comparative studies on physicochemical stability of cyclosporine A-loaded amorphous solid dispersions

Comparative studies on physicochemical stability of cyclosporine A-loaded amorphous solid... Article history: The present study aimed to evaluate the physical stability on amorphous solid dispersion (SD) of Received 29 August 2011 cyclosporine A (CsA) employing hydroxypropyl cellulose (HPC). SD formulations (5–30% CsA) of CsA such Received in revised form 8 December 2011 wet-milled SD (WM/SD) and freeze-dried SD (FD/SD) were prepared, and both SD formulations were Accepted 11 January 2012 stored at 40 C/75% relative humidity for 8 weeks. Transitions in morphology, dissolution behavior, crys- Available online 20 January 2012 tallinity and thermal behavior of CsA were evaluated. There was at least 84-fold improvement in initial dissolution rate of SD formulations compared with that of amorphous CsA powder, although their disso- Keywords: lution rate was gradually decreased under accelerated conditions. In particular, aged FD/SD with a drug Cyclosporine A load of 30% exhibited highly limited dissolution as evidenced by 40% reduction of solubility after 8 weeks Amorphous of storage. In contrast, aged WM/SD exhibited less reduction in dissolution rate compared with FD/SD. No Solid dispersion significant changes were seen in crystallinity and thermal behavior after aging of SD formulations for 8 Solid solution Stability weeks; however, electron microscopic observations revealed aggregation of drug molecules/particles in the aged FD/SD, possibly http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png International Journal of Pharmaceutics Elsevier

Comparative studies on physicochemical stability of cyclosporine A-loaded amorphous solid dispersions

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Publisher
Elsevier
Copyright
Copyright © 2012 Elsevier B.V.
ISSN
0378-5173
D.O.I.
10.1016/j.ijpharm.2012.01.022
Publisher site
See Article on Publisher Site

Abstract

Article history: The present study aimed to evaluate the physical stability on amorphous solid dispersion (SD) of Received 29 August 2011 cyclosporine A (CsA) employing hydroxypropyl cellulose (HPC). SD formulations (5–30% CsA) of CsA such Received in revised form 8 December 2011 wet-milled SD (WM/SD) and freeze-dried SD (FD/SD) were prepared, and both SD formulations were Accepted 11 January 2012 stored at 40 C/75% relative humidity for 8 weeks. Transitions in morphology, dissolution behavior, crys- Available online 20 January 2012 tallinity and thermal behavior of CsA were evaluated. There was at least 84-fold improvement in initial dissolution rate of SD formulations compared with that of amorphous CsA powder, although their disso- Keywords: lution rate was gradually decreased under accelerated conditions. In particular, aged FD/SD with a drug Cyclosporine A load of 30% exhibited highly limited dissolution as evidenced by 40% reduction of solubility after 8 weeks Amorphous of storage. In contrast, aged WM/SD exhibited less reduction in dissolution rate compared with FD/SD. No Solid dispersion significant changes were seen in crystallinity and thermal behavior after aging of SD formulations for 8 Solid solution Stability weeks; however, electron microscopic observations revealed aggregation of drug molecules/particles in the aged FD/SD, possibly

Journal

International Journal of PharmaceuticsElsevier

Published: Apr 15, 2012

References

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