Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays
A miniaturized assay was optimized to evaluate the enhanced apparent water solubility of pyrazolo[3,4-d]pyrimidine derivatives used extensively as anticancer drug scaffolds. The applied amount of drugs used in the reported strategy ranged from 5-10 μg per formulation which were dispensed by an inkje...
| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
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American Chemical Society
2018
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| Online Access: | https://eprints.nottingham.ac.uk/49478/ |
| _version_ | 1848798006359359488 |
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| author | Sanna, Monica Sicilia, Giovanna Alazzo, Ali Singh, Nishant Musumeci, Francesca Schenone, Silvia Spriggs, Keith Burley, Jonathan C. Garnett, Martin Taresco, Vincenzo Alexander, Cameron |
| author_facet | Sanna, Monica Sicilia, Giovanna Alazzo, Ali Singh, Nishant Musumeci, Francesca Schenone, Silvia Spriggs, Keith Burley, Jonathan C. Garnett, Martin Taresco, Vincenzo Alexander, Cameron |
| author_sort | Sanna, Monica |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | A miniaturized assay was optimized to evaluate the enhanced apparent water solubility of pyrazolo[3,4-d]pyrimidine derivatives used extensively as anticancer drug scaffolds. The applied amount of drugs used in the reported strategy ranged from 5-10 μg per formulation which were dispensed by an inkjet 2D printer directly into a 96-well plate. The selected polymer/drug formulations with high water solubility demonstrated improved cytotoxicity against a human lung adenocarcinoma cancer cell line (A549) compared to the free drugs. We attribute the enhanced efficacy to the improved apparent-solubility of the drug molecules achieved via this methodology. This novel miniaturized method showed promising results in terms of water solubility improvement of the highly hydrophobic pyrazolo[3,4-d]pyrimidine derivatives, requiring only a few μg of each drug per tested polymeric formulation. In addition, the reported experimental evidence may facilitate identification of suitable polymers for combination with drug leading to investigations on biological properties or mechanisms of action in a single formulation. |
| first_indexed | 2025-11-14T20:12:54Z |
| format | Article |
| id | nottingham-49478 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T20:12:54Z |
| publishDate | 2018 |
| publisher | American Chemical Society |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-494782020-05-04T19:28:36Z https://eprints.nottingham.ac.uk/49478/ Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays Sanna, Monica Sicilia, Giovanna Alazzo, Ali Singh, Nishant Musumeci, Francesca Schenone, Silvia Spriggs, Keith Burley, Jonathan C. Garnett, Martin Taresco, Vincenzo Alexander, Cameron A miniaturized assay was optimized to evaluate the enhanced apparent water solubility of pyrazolo[3,4-d]pyrimidine derivatives used extensively as anticancer drug scaffolds. The applied amount of drugs used in the reported strategy ranged from 5-10 μg per formulation which were dispensed by an inkjet 2D printer directly into a 96-well plate. The selected polymer/drug formulations with high water solubility demonstrated improved cytotoxicity against a human lung adenocarcinoma cancer cell line (A549) compared to the free drugs. We attribute the enhanced efficacy to the improved apparent-solubility of the drug molecules achieved via this methodology. This novel miniaturized method showed promising results in terms of water solubility improvement of the highly hydrophobic pyrazolo[3,4-d]pyrimidine derivatives, requiring only a few μg of each drug per tested polymeric formulation. In addition, the reported experimental evidence may facilitate identification of suitable polymers for combination with drug leading to investigations on biological properties or mechanisms of action in a single formulation. American Chemical Society 2018-01-29 Article PeerReviewed Sanna, Monica, Sicilia, Giovanna, Alazzo, Ali, Singh, Nishant, Musumeci, Francesca, Schenone, Silvia, Spriggs, Keith, Burley, Jonathan C., Garnett, Martin, Taresco, Vincenzo and Alexander, Cameron (2018) Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays. ACS Medicinal Chemistry Letters, 9 (3). pp. 193-197. ISSN 1948-5875 Miniaturized assay; inkjet 2D printing; amorphous solid dispersion; water solubility enhancement and pyrazolo[ 3 4-d]pyrimidines http://pubs.acs.org/doi/10.1021/acsmedchemlett.7b00456 doi:10.1021/acsmedchemlett.7b00456 doi:10.1021/acsmedchemlett.7b00456 |
| spellingShingle | Miniaturized assay; inkjet 2D printing; amorphous solid dispersion; water solubility enhancement and pyrazolo[ 3 4-d]pyrimidines Sanna, Monica Sicilia, Giovanna Alazzo, Ali Singh, Nishant Musumeci, Francesca Schenone, Silvia Spriggs, Keith Burley, Jonathan C. Garnett, Martin Taresco, Vincenzo Alexander, Cameron Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays |
| title | Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays |
| title_full | Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays |
| title_fullStr | Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays |
| title_full_unstemmed | Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays |
| title_short | Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays |
| title_sort | water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays |
| topic | Miniaturized assay; inkjet 2D printing; amorphous solid dispersion; water solubility enhancement and pyrazolo[ 3 4-d]pyrimidines |
| url | https://eprints.nottingham.ac.uk/49478/ https://eprints.nottingham.ac.uk/49478/ https://eprints.nottingham.ac.uk/49478/ |