Abstract

In the present study we developed folate conjugated-PEGylated PLGA nanoparticles as an alternate carrier for Docetaxel (DTX) (antineoplastic agent). In order to investigate a more efficient delivery mode, the folate moiety was conjugated to PEGylated PLGA in two ways; firstly it was conjugated to PLGA-PEG diblock copolymer during the synthesis as PLGA-PEG-folate copolymer and secondly it was covalently attached to the surface of PLGA-PEG nanoparticles as surface modified nanoparticles. PLGA-PEG and PLGA-PEG-folate copolymers were synthesized and characterized by 1H NMR, FT-IR and Gel Permeation Chromatography (GPC). DTX loaded nanoparticles (NPs) were prepared by emulsion solvent evaporation technique using sodium cholate as a surfactant and characterized for size, surface charge, and surface density of PEG chains. Influence of folate moieties on drug entrapment, surface properties and in vitro drug release were evaluated. The effects of folate content on the NPs surface and its cytotoxicity were evaluated by MTT assay using KB cell line. The results suggest that the diblock copolymer conjugated folate NPs formulation greatly affected its formulation characteristics and release rate of DTX. From the formulation characteristics and the cytotoxicity results, we conclude that the surface modified NPs formulation could be a promising carrier for DTX.

Keywords: PLGA-PEG, diblock, folate, nanoparticles, docetaxel, cytotoxicity