Abstract

LIGAND CONJUGATED NANOPARTICLES OF LYCOPENE FOR TARGETING BREAST CANCER CELLS

Tumpa Kumari and Dinesh Kaushik*

ABSTRACT

Nanotechnology is a modern field of science which plays a dominant role in day to day life aspects. There are different ideal methods for nanoparticles to get synthesized. Site-specific targeting can be achieved by attaching targeting ligands to surface of particles or use of magnetic guidance. Materials: Lycopene (Loba chemie), Gelatin (Fisher Scientific), Dimethyl Sulfoxide (Rankem), 3-(4, 5di-methylthiazol-2yl)-2 (Rankem), 5-diphenyltetrazolium bromide (MTT) (Rankem), Gultaraldehyde (Loba chemie). Result and Discussion: The main aim of the present research work was to develop a ligand conjugated nanoparticles of lycopene for targeting breast cancer cells. On characterization spherical nanoparticles with smooth surface and spherical were observed under transmission electron microscopy (TEM). The PXRD pattern of lycopene showed peaks that were intense and sharp indicating its crystalline structure. The physical mixture of LYC, PLGA and sailic acid showed sharp peaks with maximum intensities. Though this signifies crystalline structure of all mixtures. DSC curve of Lycopene showed a sharp endothermic peak near 177ºC that is indicative of its melting temperature. DSC curve of sailic acid also endothermic peak at 186ºC. Percentage efficiency of lycopene loaded nanoparticles was found to be satisfactory and percentage efficiency of sailic acid conjugated lycopene loaded PLGA nanoparticles was found to be satisfactory. Drug release was found to follow a first-order release kinetic at both, pH~5.8 and pH ~7.4 with characteristics of biphasic release. Release rate constants for two phases were given by the slopes. The absorbance was read at 471 nm using UV-VIS spectrophotometer. DSC curve of Lycopene showed a sharp endothermic peak near 177ºC that is indicative of its melting temperature. Percentage efficiency of lycopene loaded nanoparticles was found to be 91.3±2.9%. In vitro release of lycopene from nanoparticles was analyzed by dynamic dialysis method in PBS of pH ~5.6 and 7.4 to simulate the cancer cell compartment and normal body physiology milieu. Lycopene (LYC), an anticancer agent acts by de-stabilizing the cancer cells. However, its pharmacokinetics and pharmacodynamic properties are affected by low aqueous solubility and oral bioavailability. We have synthesized ligand decorated nanoparticles using gelatin for targeting breast cancer cells. Conclusion: In vitro cytotoxicity and cellular uptake study confirmed that LYC-ES-GNs with greater efficacy compared with LYC alone and LYC-GNs may potentially be used for targeting breast cancer cells.

Keywords: Lycopene nanoparticles, Cancer, Nanotechnology.