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.
Disclosure statement
No potential conflict of interest was reported by the author(s).