How does the addition of Kollidon®VA64 inhibit the recrystallization and improve ezetimibe dissolution from amorphous solid dispersions?
Authors:
- Joanna Szafraniec-Szczęsny,
- Agata Antosik-Rogóż,
- Mateusz Kurek,
- Karolina Gawlak,
- Anna Górska,
- Sebastian Peralta,
- Justyna Knapik-Kowalczuk,
- Daniel Konrad Kramarczyk,
- Marian Paluch,
- Renata Jachowicz
Abstract
Amorphization serves as a strategy for the improvement of poor dissolution characteristics of many drug compounds. However, in many formulations the content of polymeric stabilizer is high, which is undesirable from the perspective of future applications. Thus, studying the composition-dependent stability of amorphous solid dispersions seems to be demanded. In this paper, we describe the amorphization of ezetimibe, a lipid-lowering drug, in the spray drying process and investigate the effect of polyvinylpyrrolidone-co-poly(vinyl acetate) (PVP/VA) content on the physical stability and dissolution characteristics of the drug. Fully amorphous systems were obtained when the concentration of the polymer in solid dispersion was as low as 20%. The amorphization led to the dissolution enhancement by even 70%, with a noticeable sudden increase at around 40% of PVP/VA content and very small variations for systems having 66–90% PVP/VA. It was also correlated to wettability characteristics of solid dispersions, which may suggest that in the vicinity of 40% of the polymer content, the behavior of the system becomes independent of the PVP/VA content.
- Record ID
- USL71de200d63964b8a84217363b74ce9f4
- Author
- Journal series
- Pharmaceutics, ISSN 1999-4923
- Issue year
- 2021
- Vol
- 13
- No
- 2
- Pages
- 1-15
- Publication size in sheets
- 0.70
- Article number
- 147
- Keywords in English
- ezetimibe; solid dispersion; amorphization; dissolution; contact angle
- ASJC Classification
- DOI
- DOI:10.3390/pharmaceutics13020147 Opening in a new tab
- Handle.net URL
- hdl.handle.net/20.500.12128/18590 Opening in a new tab
- URL
- https://www.mdpi.com/1999-4923/13/2/147 Opening in a new tab
- Language
- eng (en) English
- License
- File
-
- File: 1
- How does the addition of Kollidon®VA64 inhibit the recrystallization and improve ezetimibe dissolution from amorphous solid dispersions?, File Kramarczyk_Paluch_how_does_the_addition.pdf / 2 MB
- Kramarczyk_Paluch_how_does_the_addition.pdf
- publication date: 20-10-2023
- How does the addition of Kollidon®VA64 inhibit the recrystallization and improve ezetimibe dissolution from amorphous solid dispersions?, File Kramarczyk_Paluch_how_does_the_addition.pdf / 2 MB
-
- Score (nominal)
- 100
- Score source
- journalList
- Score
- = 100.0, 20-10-2023, ArticleFromJournal
- Publication indicators
- Citation count
- 13
- PubMed ID
- 33498609 Opening in a new tab
- Uniform Resource Identifier
- https://opus.us.edu.pl/info/article/USL71de200d63964b8a84217363b74ce9f4/
- URN
urn:uni-kat-prod:USL71de200d63964b8a84217363b74ce9f4
* presented citation count is obtained through Internet information analysis, and it is close to the number calculated by the Publish or PerishOpening in a new tab system.