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

Loading next page...
 
/lp/elsevier/comparative-studies-on-physicochemical-stability-of-cyclosporine-a-T4HIKhp51g
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

You’re reading a free preview. Subscribe to read the entire article.


DeepDyve is your
personal research library

It’s your single place to instantly
discover and read the research
that matters to you.

Enjoy affordable access to
over 12 million articles from more than
10,000 peer-reviewed journals.

All for just $49/month

Explore the DeepDyve Library

Unlimited reading

Read as many articles as you need. Full articles with original layout, charts and figures. Read online, from anywhere.

Stay up to date

Keep up with your field with Personalized Recommendations and Follow Journals to get automatic updates.

Organize your research

It’s easy to organize your research with our built-in tools.

Your journals are on DeepDyve

Read from thousands of the leading scholarly journals from SpringerNature, Elsevier, Wiley-Blackwell, Oxford University Press and more.

All the latest content is available, no embargo periods.

See the journals in your area

Monthly Plan

  • Read unlimited articles
  • Personalized recommendations
  • No expiration
  • Print 20 pages per month
  • 20% off on PDF purchases
  • Organize your research
  • Get updates on your journals and topic searches

$49/month

Start Free Trial

14-day Free Trial

Best Deal — 39% off

Annual Plan

  • All the features of the Professional Plan, but for 39% off!
  • Billed annually
  • No expiration
  • For the normal price of 10 articles elsewhere, you get one full year of unlimited access to articles.

$588

$360/year

billed annually
Start Free Trial

14-day Free Trial