Abstract
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.
Original language | English |
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Pages (from-to) | 15-28 |
Number of pages | 14 |
Journal | Journal of Microencapsulation |
Volume | 40 |
Issue number | 1 |
DOIs | |
Publication status | Published - 2023 |
Externally published | Yes |
Keywords
- Alzheimer’s disease
- cinnamic acid
- memantine
- polyamidoamine
- polymer-drug conjugate
- tacrine
ASJC Scopus subject areas
- Bioengineering
- Pharmaceutical Science
- Physical and Theoretical Chemistry
- Organic Chemistry
- Colloid and Surface Chemistry