The aim of this research work was to develop
Bombesin peptide (BBN) conjugated,
docetaxel loaded nanocarrier for the treatment of
breast cancer.
Docetaxel loaded nanoparticles (DNP) were prepared by
solvent evaporation method using
sodium cholate as
surfactant. BBN was conjugated to DNP surface through covalent bonding. Both DNP and BBN conjugated DNP (
BDNP) were characterized by various techniques such as dynamic light scattering, Fourier transform infrared spectroscopy (FTIR), atomic force microscopy (AFM),
powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and thermogravimetric analysis. The particle diameter and zeta potential of
BDNP were 136±3.95 nm and -10.8±2.7 mV, respectively. The change in surface charge and FTIR studies confirmed the formation of
amide linkage between BBN and DNP. AFM analysis showed that nanoparticles were spherical in shapes. In nanoparticles,
docetaxel was present in its amorphous form as confirmed by DSC and PXRD analysis and was stable during the thermal studies. The formulations showed the sustained release of DTX over the period of 120 h. During cellular toxicity assay in
gastrin releasing peptide receptor positive
breast cancer cells (MDA-MB-231),
BDNP were found to be 12 times more toxic than pure DTX and
Taxotere. The IC50 value for DTX,
Taxotere, DNP and
BDNP was >375, >375, 142.23 and 35.53 ng/ml, respectively. The above studies showed that
Bombesin conjugated nanocarrier system could be a promising carrier for active targeting of anticancer drugs in GRP receptor over expressing
cancer cells.