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

  • Rahul Sharma
  • Satish Sardana
  • Jitender Madan


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


Download data is not yet available.


1. Sharma A., Jyoti K., Bansal V., Jain U.K., Bhushanb B., Madan J. Soluble telmisartan bearing poly (ethylene glycol) conjugated chitosan nanoparticles augmented drug delivery, cytotoxicity, apoptosis and cellular uptake in human cervical cancer cells, Materials Science and Engineering C. 2017; 72: 69–76.
2. Wienen W., Entzeroth M., VanMeel J.C.A., Stangier J., Busch U., Ebner T., Schmid J., Lehmann H., Matzek K., Rawson J.K., Gladigau V., Hauel N.H. A review on telmisartan: anovel, long-acting angiotensin II-receptor antagonist. Cardiovascular Drug Reviews. 2000; 18: 127–154
3. Shimizu K., Takashima T., Yamane T., Sasaki M., Kageyama H., Hashizume Y., Maeda K., Sugiyama Y., Watanabe Y., Senda M. Whole-body distribution and radiation dosimetry of [11C] telmisartan as a biomarker for hepatic organic anion transporting polypeptide (OATP) 1B3.Nuclear Medicine and Biology. 2012; 39: 847-853.
4. Park J., Cho W., Cha K.H., Ahn J., Han K., Hwang S.J. Solubilization of the poorly water soluble drug, telmisartan, using supercritical anti-solvent (SAS) process. International Journal of Pharmaceutics. 2013; 441: 50–55.
5. Ratain MJ, Mick R. Principles of pharmacokinetics and pharmacodynamics, in: Schilsky R.L., Milano G.A., Ratain M.J., editors. Principles of Antineoplastic Drug Development and Pharmacology. New York (NY): Marcel Dekker; 1996; p. 123–142.
6. Torchilin VP. Passive and active drug targeting: drug delivery to tumors as an example. Hands Exp Pharmacol. 2010; 197:3-53.
7. Jong D., Borm P.J. Drug delivery and nanoparticles: applications and hazards. Int J Nanomed. 2008; 3: 133.
8. Kreuter J. Peroral administration of nanoparticles. Adv Drug Deliv Rev. 1991; 7: 71-86.
9. Yasir M., Sara U.V.S. Preparation and optimization of haloperidol loaded solid lipid nanoparticles by Box Behnken design. J Pharmacy Res. 2013; 7: 551-558.
10. Baig M.S., Ahad A., Aslam M., Imam S.S., Aqil M., Ali A. Application of Box–Behnken design for preparation of levofloxacin-loaded stearic acid solid lipid nanoparticles for ocular delivery: Optimization, in vitro release, ocular tolerance, and antibacterial activity, Int J Biol Macromol. 2016; 85: 258-70.
104 Views | 61 Downloads
How to Cite
Sharma R, Sardana S, Madan J. Telmisartan loaded Solid Lipid Nanoparticles augmented cytotxicity in cervical cancer cells: Optimization and in vitro characterization. JDDT [Internet]. 19Nov.2019 [cited 16Jan.2021];9(2):612-24. Available from: