International Journal of Organic Chemistry, 2019, 9, 47-66 http://www.scirp.org/journal/ijoc ISSN Online: 2161-4695 ISSN Print: 2161-4687 DOI: 10.4236/ijoc.2019.91005 Mar. 15, 2019 47 International Journal of Organic Chemistry Synthesis of Folate-Appended β-Cyclodextrin Using Phenanthroline as Linker for Cancer Targeting Drug Delivery Nadim S. Russel 1 , Punam K. Paul 1 , Mohammad Karim 1* , Byeongwoon Song 2* 1 Department of Chemistry, Tennessee State University, Nashville, USA 2 Department of Microbiology, Immunology, and Physiology, Meharry Medical College, Nashville, USA Abstract Here we have synthesized cancer targeting drug delivery system that contains β-cyclodextrin as a drug carrier and folic acid as a targeting ligand. Folic acid was selected as a cancer targeting ligand because folic acid receptors are highly expressed in a variety of tumor types. β-cyclodextrin and folic acid were connected through a linker [1,10-phenanthroline or 5-(hydroxymethyl) furfural]. β-cyclodextrin and folic acid were attached to the linker by forma- tion of Schiffbase and ester, respectively. Our targeted synthetic products were confirmed by NMR, Mass and IR spectroscopy. We anticipate that our synthetic products can confer cancer cell-specific drug delivery as well as de- sired properties such as nanoparticle formation. Keywords Schiff Base, β-Cyclodextrin, p-Toluenesulfonylchloride, Ethylenediamine, Folic Acid, 2,9-Dimethyl-1,10-Phenanthroline Hemi-Hydrate, 5-(Hydroxymethyl-2-Furaldehyde) 1. Introduction Cyclodextrins (CDs) are cyclic oligosaccharides generated from starch (e.g. corn, potato) and β-cyclodextrin is one type of cyclodextrin that contains 7 glucose units in its structure [1]. The hydrophobic central cavity and the hydrophilic outer surface allow CDs to form water-soluble inclusion complexes with several drug molecules or compounds and help to protect the guest molecules from oxidation and degradation and to increase their solubility and bioavailability. Thus, CDs are frequently used as a drug carrier. Hybrid delivery system for effective transportation of temoporfin was sug- How to cite this paper: Russel, N.S., Paul, P.K., Karim, M. and Song, B. (2019) Syn- thesis of Folate-Appended β-Cyclodextrin Using Phenanthroline as Linker for Cancer Targeting Drug Delivery. International Jour- nal of Organic Chemistry, 9, 47-66. https://doi.org/10.4236/ijoc.2019.91005 Received: January 24, 2019 Accepted: March 12, 2019 Published: March 15, 2019 Copyright © 2019 by author(s) and Scientific Research Publishing Inc. This work is licensed under the Creative Commons Attribution International License (CC BY 4.0). http://creativecommons.org/licenses/by/4.0/ Open Access