Telmisartan loaded Solid Lipid Nanoparticles augmented cytotxicity in cervical cancer cells: Optimization and in vitro characterization

Abstract

Cervical cancer, a malignant cancer is leading second most cancer found in women. Telmisartan has 3000 times more affinity toward angiotensin II receptor type 1 (AT1) receptor than AT2 and inhibited neovascularization by down-regulating VEGF acting on endothelial cells with antagonized activity of Angiotensin II. Despite well-known therapeutic potential of telmisartan in malignant cancer, poor physicochemical properties and pharmacokinetic properties including meageraqueous solubility (0.078 mg/mL), low oral bioavailability (45-58%), and erratic biodistribution not only limit the therapeutic potential of telmisartan in treatment of malignant cancer but also appeal for development of dosage form with enhanced oral bioavailability. Telmisartan encapsulated stearic acid nanostructured solid lipid particles were developed by solvent diffusion method. On applying of box behnken design with three factors and three levels, 17 different formulations were yielded and prepared with Response of particle size (Y1) and percentage drug entrapment (Y2) for 17 formulations were evaluated. The IC50 value of optimized telmisartan loaded lipid nanoparticle and market preparation, indicated telmisartan loaded solid lipid nanoparticle expressed lower IC50 value of 30.28 μM with significant anticancer activity against HeLa cancer cell line in comparison to higher IC50 value 58.69 μM of market preparation. In conclusion, telmisartan loaded solid lipid nanoparticles may be a promising drug delivery systems for cervical cancer. Keywords: Telmisarn, cervical cancer; solid lipid nanoparticles; cytotxicity