API solubility in semi-crystalline polymer: Kinetic and thermodynamic phase behavior of PVA-based solid dispersions
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F22%3A43924992" target="_blank" >RIV/60461373:22340/22:43924992 - isvavai.cz</a>
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S0378517322004100" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0378517322004100</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ijpharm.2022.121855" target="_blank" >10.1016/j.ijpharm.2022.121855</a>
Alternative languages
Result language
angličtina
Original language name
API solubility in semi-crystalline polymer: Kinetic and thermodynamic phase behavior of PVA-based solid dispersions
Original language description
The formulation of amorphous solid dispersions (ASDs) represents a promising strategy for improving the poor bioavailability of many active pharmaceutical ingredients (APIs). The objective of this study was to investigate and compare the long-term physical stability (LTPS) of polyvinyl alcohol (PVA)-based solid dispersions formulated via hot-melt extrusion (HME) with their respective API–PVA temperature–composition (T–C) phase diagram. Furthermore, the impact of API glass-forming ability (GFA) on the LTPS was evaluated through the selection of two APIs with contrasting GFA (i.e., indomethacin (IND; good GFA) and naproxen (NAP; poor GFA)). Even though the predicted solubility of both APIs in PVA was less than 1 wt% at T = 25 °C, IND remained fully amorphous in HME-formulated IND–PVA extrudates with initial API loadings of 50, 40, and 30 wt% after a 24-month storage period. Meanwhile, NAP recrystallized to a considerable degree in each analogous sample with an amorphous NAP content of 22.5–23.5 wt% remaining after a 12-month storage period. While the constructed T–C phase diagrams were still in agreement with their respective LTPS study, they did not account for the impact of water uptake as well as potential HME-induced effects on the extrudate glass-transition temperature. This work may serve as a useful reference point for researchers who are interested in determining the solubility of an API in a semi-crystalline polymer and the challenges therein. © 2022 Elsevier B.V.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10404 - Polymer science
Result continuities
Project
<a href="/en/project/GA22-07164S" target="_blank" >GA22-07164S: Rational design of drug delivery systems based on tailored biodegradable polymers using an iterative in silico and experimental approach</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2022
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
International Journal of Pharmaceutics
ISSN
0378-5173
e-ISSN
1873-3476
Volume of the periodical
623
Issue of the periodical within the volume
červenec 2022
Country of publishing house
US - UNITED STATES
Number of pages
12
Pages from-to
121855
UT code for WoS article
000830017200004
EID of the result in the Scopus database
2-s2.0-85132941348