Journal of Bioequivalence & Bioavailability

Solid lipid nanoparticles for the treatment of colorectal cancer

6^th World Congress on Bioavailability & Bioequivalence: BA/BE Studies Summit

August 17-19, 2015 Chicago, USA

Shashank Tummala and M N Satish Kumar

Posters-Accepted Abstracts: J Bioequiv Availab

Abstract:

Site specificity of anti-neoplastics still poses a challenge in the pharmaceutical research. Conventional chemotherapy has limitations
such as site in-specificity, inability of the drug to penetrate inside the tumor, adverse effects there by reducing the clinical
application. So, in this study oxaliplatin solid lipid nanoparticles (OP-SLN) were prepared by micro emulsion method using various
ratios of lipid and then covalently conjugated to TRAIL monoclonal antibody (TR-OP-SLN) for targeting colorectal cancer cells by
receptor mediated internalization of drug. The prepared immuno nanoparticles were characterized for Fourier Transform Infrared
spectroscopy (FT-IR), Differential scanning calorimetry (DSC), X-ray diffraction (XRD), particle size, scanning electron microscopy
(SEM), surface charge, fluorescence intensity and in vitro drug release. These were further characterized for in vitro cytotoxicity
(in HT-29 cells) followed by cellular uptake and internalization by flow cytometry along with protein assay. The optimized OPSLN3
has shown an appreciable particle size (121±1.22 nm), entrapment efficiency (78±0.09%), drug loading (32±1.01%) along
with spherical surface morphology. TR-OP-SLN has shown a drug release of 81±0.01% and 27±0.12% at pH 4.5 and 7.4 respectively
further confirming its ability to release the drug inside the tumor. Fluorescence study confirmed the presence of the antibody on the
surface of the nanoparticles by change in their intensity. A 1.5 fold increase in cytotoxicity of immuno nanoparticles (7.5 ug/ml or
more) was observed. Cellular uptake studies have shown 89% of immuno nanoparticles uptake by the cells and immuno nanoparticle
are majorly internalized in the perinuclear region. In conclusion, we demonstrate a preparation and characterization of oxaliplatin
immuno nanoparticles for receptor mediated targeting of the drug.