Molecular encapsulation of lidocaine and procaine into β-cyclodexrin cavity: in vitro cytotoxic evaluation

Abstract

Among the potent anticancer agent, Local Anesthetics (LA) have been found to be efficient against many different types of cancer cell lines. However, the major disadvantage associated with the use of LA its low systemic bio-availability when administered due to its poor aqueous solubility. Our present work concentrates on improving the bio-availability by complexing with β-Cyclodextrin. We synthesized the inclusion complexes of selective LAs by co-precipitation method which is an efficient method among others and characterized the formulation of complex by UV, steady state and time resolved fluorescence studies. The optimization and orientation of the free LA and the complexes have also been studied by molecular docking with the help of Patch-Dock server. An in vitro study of cytotoxicity against breast cancer cell line is performed. Our study shows the formation of the complex with 1:1 ratio and the result showed that the improved CT activity for LDC:β-CD than the free LDC. For PRC and its complex with β-CD has no much activity even after forming a complex.

Keywords:

• Local anesthetics
• cyclodextrin: inclusion complex
• Patch-Dock server
• in vitro cytotoxicity