PREPARATION AND CHARACTERIZATION OF PACLITAXEL-FOLIC ACID CONJUGATES TO TARGET CANCER CELLS

Abstract

The targeted drug delivery system improves the delivery of drugs right to the specific site, without affecting any healthy tissues and organs. It enhances the efficacy of drug at desired site by modifying the carrier to the target site and also improves patient compliance due to decreased dosing frequency. In this study, we developed a new multi-small molecule conjugated Paclitaxel (PTX) delivery system for targeted tumor therapy. Water-soluble small molecules, amino acids (Glu), FA, and fluorescent dye were successfully conjugated to PTX. Conjugation of paclitaxel to the small-molecules was further confirmed by UV, IR, NMR spectroscopic analysis and XRD analysis. In the present investigation, an attempt was made to develop, and characterize paclitaxel-Folic acid conjugates to target cancer cells through the drug-ligand for achieving controlled release. The linkage can be designed to improve water solubility, to enhance presentation of the folate to its receptor, or to release the attached drug in unmodified form only after uptake into the target cell. It also enhances the solubility of synthesized FA-Glu(OtBu)-PTX conjugate. Results of the study therefore concluded that FAGlu( OtBu)-PTX conjugate has been effectively synthesized which could be used for formulation development like transferosomes and might be useful for targeted delivery system in cancer treatment.