Abstract

DESIGN AND DEVELOPMENT OF SOLID LIPID NANOPARTICLES OF TELMISARTAN FOR TARGETING PROSTATE CANCER

Pooja* and Rahul Sharma

ABSTRACT

Recently, the anticancer action of telmisartan (TEL) has been discovered against prostate cancer. However, although good therapeutic profile, poor aqueous solubility and suboptimal oral bioavailability slow down the anticancer efficiency of Telmisartan. Consequently, in present research, Solid lipid nanoparticles of Telmisartan were prepared for targeting prostate cancer, PC-3 cells. The mean particle size of TEL-SLNs was measured to be 95.3 ± 3.4nm, Correspondingly, zeta-potential of SLNs was measured to be -23.6 ± 2.9 mV significantly lower than -38.6 ± 6.3mV of TEL loaded SLNs. The encapsulation efficiency of Telmisartan loaded solid lipid nanoparticles was estimated to be 89.6±6.5%. FT-IR and PXRD recognized the molecular encapsulation of the drug in amorphous state. In vitro drug release study was conducted to conclude the drug delivery potential of lipid nanoparticles. These data indicate that only 35% of TEL is released in 8 hours compared to the TEL loaded SLNs which releases significantly higher amount 80% of drug in the same time interval. The IC50 of Telmisartan was measured to be 15.9μM significantly higher than 7.5μM presented by TEL-SLNs in PC-3 cells. We elucidated that TEL- SLNs entered the PC-3 cells through receptor mediated endocytosis pathway and therefore exhibited greater cytotoxicity and greater extent of cellular uptake in PC-3 cells.

Keywords: Telmisartan, prostate cancer, solid lipid nanoparticles, cytotoxicity, cellular uptake.