Inclusion of an antiplatelet agent inside into β-cyclodextrin for biochemical applications with diverse authentications

Abstract

We aim to develop the complex of ticlopidine hydrochloride (TCP) with β-cyclodextrin (β-CD) and to investigate its antibacterial and cytotoxic activities. The complex was characterized by various physicochemical as well as spectroscopic techniques suggesting the successful inclusion of TCP molecule into the β-CD cavity. TG analysis showed that the thermal stability of TCP was found to improve after complexation. Molecular docking study speculated the most preferred orientation of TCP molecule within the binding pocket of β-CD cavity. In vitro antibacterial activity test demonstrated that the TCP-β-CD complex displayed better activity than pure TCP. TCP-β-CD complex (IC50 = 24 μM) also exhibited significant in vitro cytotoxic activity than pure TCP (IC50 = 44 μM) towards human kidney cancer cell line (ACHN). Furthermore, the complex induces the ROS generation in ACHN cells more pronouncedly than TCP alone, suggesting the increased apoptotic activity of TCP after complexation. These results reveals that inclusion of TCP using β-CD could lead to stabilization of TCP and efficient display of its antibacterial and cytotoxic activities.

Keywords

• Ticlopidine hydrochloride
• β-cyclodextrin
• Thermogravimetric analysis
• Molecular docking
• Antibacterial activity
• Cytotoxicity