Polymer drug conjugates containing memantine, tacrine and cinnamic acid : promising nanotherapeutics for the treatment of Alzheimer's disease
AIM: To prepare polymer-drug conjugates containing a combination of memantine, tacrine, and E)-N-(3-aminopropyl)cinnamide, promising therapeutics for the treatment of neurodegenerative disorders.
METHODS: The conjugates were characterised by 1HNMR, particle size analysis, SEM, LC-MS, TEM/EDX, and XRD, followed by in vitro anti-acetylcholinesterase and drug release studies.
RESULTS: 1H NMR analysis revealed successful drug conjugation with drug mass percentages in the range of 1.3-6.0% w/w. The drug release from the conjugates was sustained for 10 h in the range of 20-36%. The conjugates' capability to inhibit acetylcholinesterase (AChE) activity was significant with IC50 values in the range of 13-44.4 µm which was more effective than tacrine (IC50 =1698.8 µm). The docking studies further confirmed that the conjugation of the drugs into the polymer improved their anti-acetylcholinesterase activity.
CONCLUSION: The drug release profile, particle sizes, and in vitro studies revealed that the conjugates are promising therapeutics for treating neurodegenerative disorders.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:40 |
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| Enthalten in: |
Journal of microencapsulation - 40(2023), 1 vom: 09. Jan., Seite 15-28 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Naki, Tobeka [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 28.02.2023 Date Revised 28.02.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1080/02652048.2023.2167011 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM351339523 |
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| 245 | 1 | 0 | |a Polymer drug conjugates containing memantine, tacrine and cinnamic acid |b promising nanotherapeutics for the treatment of Alzheimer's disease |
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| 500 | |a Date Completed 28.02.2023 | ||
| 500 | |a Date Revised 28.02.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a AIM: To prepare polymer-drug conjugates containing a combination of memantine, tacrine, and E)-N-(3-aminopropyl)cinnamide, promising therapeutics for the treatment of neurodegenerative disorders | ||
| 520 | |a METHODS: The conjugates were characterised by 1HNMR, particle size analysis, SEM, LC-MS, TEM/EDX, and XRD, followed by in vitro anti-acetylcholinesterase and drug release studies | ||
| 520 | |a RESULTS: 1H NMR analysis revealed successful drug conjugation with drug mass percentages in the range of 1.3-6.0% w/w. The drug release from the conjugates was sustained for 10 h in the range of 20-36%. The conjugates' capability to inhibit acetylcholinesterase (AChE) activity was significant with IC50 values in the range of 13-44.4 µm which was more effective than tacrine (IC50 =1698.8 µm). The docking studies further confirmed that the conjugation of the drugs into the polymer improved their anti-acetylcholinesterase activity | ||
| 520 | |a CONCLUSION: The drug release profile, particle sizes, and in vitro studies revealed that the conjugates are promising therapeutics for treating neurodegenerative disorders | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Alzheimer’s disease | |
| 650 | 4 | |a cinnamic acid | |
| 650 | 4 | |a memantine | |
| 650 | 4 | |a polyamidoamine | |
| 650 | 4 | |a polymer-drug conjugate | |
| 650 | 4 | |a tacrine | |
| 650 | 7 | |a Cholinesterase Inhibitors |2 NLM | |
| 650 | 7 | |a cinnamic acid |2 NLM | |
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| 650 | 7 | |a Memantine |2 NLM | |
| 650 | 7 | |a W8O17SJF3T |2 NLM | |
| 650 | 7 | |a Tacrine |2 NLM | |
| 650 | 7 | |a 4VX7YNB537 |2 NLM | |
| 650 | 7 | |a Nanoparticle Drug Delivery System |2 NLM | |
| 650 | 7 | |a Polymers |2 NLM | |
| 700 | 1 | |a Matshe, William Morwa Reagile |e verfasserin |4 aut | |
| 700 | 1 | |a Balogun, Mohammed Olusegun |e verfasserin |4 aut | |
| 700 | 1 | |a Sinha Ray, Suprakas |e verfasserin |4 aut | |
| 700 | 1 | |a Egieyeh, Samuel Ayodele |e verfasserin |4 aut | |
| 700 | 1 | |a Aderibigbe, Blessing Atim |e verfasserin |4 aut | |
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