Effect of Copolymer Properties on the Phase Behavior of Ibuprofen–PLA/PLGA Mixtures
Prediction of compatibility of the active pharmaceutical ingredient (API) with the polymeric carrier plays an essential role in designing drug delivery systems and estimating their long-term physical stability. A key element in deducing API–polymer compatibility is knowledge of a complete phase diag...
| Main Authors: | , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2023-02-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/15/2/645 |
| _version_ | 1797618695441219584 |
|---|---|
| author | Anton Iemtsev Martin Klajmon Fatima Hassouna Michal Fulem |
| author_facet | Anton Iemtsev Martin Klajmon Fatima Hassouna Michal Fulem |
| author_sort | Anton Iemtsev |
| collection | DOAJ |
| description | Prediction of compatibility of the active pharmaceutical ingredient (API) with the polymeric carrier plays an essential role in designing drug delivery systems and estimating their long-term physical stability. A key element in deducing API–polymer compatibility is knowledge of a complete phase diagram, i.e., the solubility of crystalline API in polymer and mutual miscibility of API and polymer. In this work, the phase behavior of ibuprofen (IBU) with different grades of poly(D,L-lactide-co-glycolide) (PLGA) and polylactide (PLA), varying in composition of PLGA and molecular weight of PLGA and PLA, was investigated experimentally using calorimetry and computationally by the perturbed-chain statistical associating fluid theory (PC-SAFT) equation of state (EOS). The phase diagrams constructed based on a PC-SAFT EOS modeling optimized using the solubility data demonstrated low solubility at typical storage temperature (25 °C) and limited miscibility (i.e., presence of the amorphous–amorphous phase separation region) of IBU with all polymers studied. The ability of PC-SAFT EOS to capture the experimentally observed trends in the phase behavior of IBU–PLA/PLGA systems with respect to copolymer composition and molecular weight was thoroughly investigated and evaluated. |
| first_indexed | 2024-03-11T08:17:08Z |
| format | Article |
| id | doaj.art-9aa3842d772241d2b2b99e703e35ffc7 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T08:17:08Z |
| publishDate | 2023-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-9aa3842d772241d2b2b99e703e35ffc72023-11-16T22:42:43ZengMDPI AGPharmaceutics1999-49232023-02-0115264510.3390/pharmaceutics15020645Effect of Copolymer Properties on the Phase Behavior of Ibuprofen–PLA/PLGA MixturesAnton Iemtsev0Martin Klajmon1Fatima Hassouna2Michal Fulem3Department of Physical Chemistry, University of Chemistry and Technology, Prague, Technická 5, 166 28 Prague, Czech RepublicDepartment of Physical Chemistry, University of Chemistry and Technology, Prague, Technická 5, 166 28 Prague, Czech RepublicFaculty of Chemical Engineering, University of Chemistry and Technology, Prague, Technická 5, 166 28 Prague, Czech RepublicDepartment of Physical Chemistry, University of Chemistry and Technology, Prague, Technická 5, 166 28 Prague, Czech RepublicPrediction of compatibility of the active pharmaceutical ingredient (API) with the polymeric carrier plays an essential role in designing drug delivery systems and estimating their long-term physical stability. A key element in deducing API–polymer compatibility is knowledge of a complete phase diagram, i.e., the solubility of crystalline API in polymer and mutual miscibility of API and polymer. In this work, the phase behavior of ibuprofen (IBU) with different grades of poly(D,L-lactide-co-glycolide) (PLGA) and polylactide (PLA), varying in composition of PLGA and molecular weight of PLGA and PLA, was investigated experimentally using calorimetry and computationally by the perturbed-chain statistical associating fluid theory (PC-SAFT) equation of state (EOS). The phase diagrams constructed based on a PC-SAFT EOS modeling optimized using the solubility data demonstrated low solubility at typical storage temperature (25 °C) and limited miscibility (i.e., presence of the amorphous–amorphous phase separation region) of IBU with all polymers studied. The ability of PC-SAFT EOS to capture the experimentally observed trends in the phase behavior of IBU–PLA/PLGA systems with respect to copolymer composition and molecular weight was thoroughly investigated and evaluated.https://www.mdpi.com/1999-4923/15/2/645biodegradable polymersPLGAPLAamorphous solid dispersionAPI–polymer compatibilityPC-SAFT |
| spellingShingle | Anton Iemtsev Martin Klajmon Fatima Hassouna Michal Fulem Effect of Copolymer Properties on the Phase Behavior of Ibuprofen–PLA/PLGA Mixtures Pharmaceutics biodegradable polymers PLGA PLA amorphous solid dispersion API–polymer compatibility PC-SAFT |
| title | Effect of Copolymer Properties on the Phase Behavior of Ibuprofen–PLA/PLGA Mixtures |
| title_full | Effect of Copolymer Properties on the Phase Behavior of Ibuprofen–PLA/PLGA Mixtures |
| title_fullStr | Effect of Copolymer Properties on the Phase Behavior of Ibuprofen–PLA/PLGA Mixtures |
| title_full_unstemmed | Effect of Copolymer Properties on the Phase Behavior of Ibuprofen–PLA/PLGA Mixtures |
| title_short | Effect of Copolymer Properties on the Phase Behavior of Ibuprofen–PLA/PLGA Mixtures |
| title_sort | effect of copolymer properties on the phase behavior of ibuprofen pla plga mixtures |
| topic | biodegradable polymers PLGA PLA amorphous solid dispersion API–polymer compatibility PC-SAFT |
| url | https://www.mdpi.com/1999-4923/15/2/645 |
| work_keys_str_mv | AT antoniemtsev effectofcopolymerpropertiesonthephasebehaviorofibuprofenplaplgamixtures AT martinklajmon effectofcopolymerpropertiesonthephasebehaviorofibuprofenplaplgamixtures AT fatimahassouna effectofcopolymerpropertiesonthephasebehaviorofibuprofenplaplgamixtures AT michalfulem effectofcopolymerpropertiesonthephasebehaviorofibuprofenplaplgamixtures |