Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique
Yıl: 2020 Cilt: 17 Sayı: 5 Sayfa Aralığı: 492 - 499 Metin Dili: İngilizce DOI: 10.4274/tjps.galenos.2019.76402 İndeks Tarihi: 10-05-2021
Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique
Öz: bjectives: Telmisartan (TLM) is an antihypertensive drug that has been shown to have antiproliferative effects on cancer cells. It has low solubility and suboptimal oral bioavailability. To investigate the potential anticancer effect of TLM on breast cancer cells, poly (D, L-lactide) (PLA) nanoparticles were formulated with the benefit of improving its solubility.Materials and Methods: TLM-loaded PLA nanoparticles were prepared by emulsion solvent evaporation. The effects of sonication time and polymer:drug ratio on nanoparticle size and drug encapsulation were investigated. TLM-loaded nanoparticles were tested against MCF-7 and MDA-MB-231 breast cancer cell lines for antiproliferative effects.Results: Nanoparticles with mean particle size 272 nm and 79% encapsulation efficiency were obtained. Sustained release TLM nanoparticles (40% in 24 h) decreased cell viability to 45% for MCF-7 cells at 72 h, even at the lowest TLM concentration, indicating better anticancer efficiency than TLM solution.Conclusion: TLM nanoparticles could be potential anticancer agents for breast cancer and deserve further studies.
Anahtar Kelime: Emülsiyon-Çözücü Buharlaştırma Tekniği ile Hazırlanan Telmisartan Nanopartiküllerinin Formülasyonu ve İn Vitro Değerlendirilmesi
Öz: Amaç: Telmisartan (TLM), kanser hücreleri üzerinde antiproliferatif etkisi olduğu gösterilmiş antihipertansif bir ilaçtır. Düşük çözünürlüğe, suboptimal oral biyoyararlanıma sahiptir. TLM’nin meme kanseri hücreleri üzerindeki potansiyel antikanser etkisini araştırmak için, TLM’nin çözünürlüğünü iyileştiren poli (D, L-laktid) PLA nanopartikülleri formüle edilmiştir.Gereç ve Yöntemler: TLM yüklü PLA nanopartikülleri emülsiyon hazırlama-çözücü buharlaştırma yöntemiyle hazırlanmıştır. Sonikasyon süresi ve polimer: ilaç oranının nanopartikül büyüklüğü ve ilaç enkapsülasyonu üzerindeki etkisi araştırılmıştır. TLM yüklü nanopartiküllerin, antiproliferatif etkileri MCF-7 ve MDA-MB-231 meme kanseri hücre hatları kullanılarak test edilmiştir.Bulgular: Ortalama partikül büyüklüğü 272 nm ve %79 enkapsülasyon etkinliğine sahip nanopartiküller elde edilmiştir. Sürekli salım gösteren TLM nanopartikülleri (24 saatte %40) MCF-7 hücrelerinde, TLM çözeltisinden daha iyi antikanser aktivite göstererek, en düşük TLM konsantrasyonunda bile hücre canlılığını 72 saatte %45’e düşürmüştür.Sonuç: TLM nanopartiküllerinin, meme kanseri için potansiyel antikanser ajanlar olabileceği ve daha ileri çalışmalarda araştırılmaya değer olduğu sonucuna varılmıştır.
Anahtar Kelime: Belge Türü: Makale Makale Türü: Araştırma Makalesi Erişim Türü: Erişime Açık
- Li J, Chen L, Yu P, Liu B, Zhu J, Yang Y. Telmisartan exerts anti-tumor effects by activating peroxisome proliferator-activated receptor-gamma in human lung adenocarcinoma A549 cells. Molecules. 2014;19:2862-2876.
- Koyama N, Nishida Y, Ishii T, Yoshida T, Furukawa Y, Narahara H. Telmisartan induces growth inhibition, DNA double-strand breaks and apoptosis in human endometrial cancer cells. PLoS One. 2014;9:e93050.
- Matsuyama M, Funao K, Kuratsukuri K, Tanaka T, Kawahito Y, Sano H, Chargui J, Touraine JL, Yoshimura N, Yoshimura R. Telmisartan inhibits human urological cancer cell growth through early apoptosis. Exp Ther Med. 2010;1:301-306.
- Kozako T, Soeda S, Yoshimitsu M, Arima N, Kuroki A, Hirata S, Tanaka H, Imakyure O, Tone N, Honda S-I, Soeda S. Angiotensin II type 1 receptor blocker telmisartan induces apoptosis and autophagy in adult T-cell leukemia cells. FEBS Open Bio. 2016;6:442-460.
- Takahashi S, Uemura H, Seeni A, Tang M, Komiya M, Long N, Ishiguro H, Kubota Y, Shirai T. Therapeutic targeting of angiotensin II receptor type 1 to regulate androgen receptor in prostate cancer. Prostate. 2012;72:1559-1572.
- Marasini N, Tran TH, Poudel BK, Cho HJ, Choi YK, Chi SC, Choi HG, Yong CS, Kim JO. Fabrication and evaluation of pH-modulated solid dispersion for telmisartan by spray-drying technique. Int J Pharm. 2013;441:424-432.
- Zhong L, Zhu X, Luo X, Su W. Dissolution properties and physical characterization of telmisartan-chitosan solid dispersions prepared by mechanochemical activation. AAPS PharmSciTech. 2013;14:541-550.
- Stangier J, Schmid J, Turck D, Switek H, Verhagen A, Peeters PA, van Marle SP, Tamminga WJ, Sollie FA, Jonkman JH. Absorption, metabolism, and excretion of intravenously and orally administered [14C] telmisartan in healthy volunteers. J Clin Pharmacol. 2000;40:1312-1322.
- Patel J, Dhingani A, Garala K, Raval M, Sheth N. Design and development of solid nanoparticulate dosage forms of telmisartan for bioavailability enhancement by integration of experimental design and principal component analysis. Powder Technology. 2014;258:331-343.
- Meredith PA. Optimal dosing characteristics of the angiotensin II receptor antagonist telmisartan. The American Journal of Cardiology. 1999;84:7-12.
- McCall RL, Sirianni RW. PLGA nanoparticles formed by single- or double-emulsion with vitamin E-TPGS. J Vis Exp. 2013:51015.
- Fujimoto Y, Sasaki T, Tsuchida A, Chayama K. Angiotensin II type 1 receptor expression in human pancreatic cancer and growth inhibition by angiotensin II type 1 receptor antagonist. FEBS Letters. 2001;495:197-200.
- Miyajima A, Kosaka T, Asano T, Asano T, Seta K, Kawai T, Hayakawa M. Angiotensin II type I antagonist prevents pulmonary metastasis of murine renal cancer by inhibiting tumor angiogenesis. Cancer Research. 2002;62:4176-4179.
- Inwang ER, Puddefoot JR, Brown CL, Goode AW, Marsigliante S, Ho MM, Payne JG, Vinson GP. Angiotensin II type 1 receptor expression in human breast tissues. Br J Cancer. 1997;75:1279-1283.
- Kosaka T, Miyajima A, Takayama E, Kikuchi E, Nakashima J, Ohigashi T, Asano T, Sakamoto M, Okita H, Murai M, Hayakawa M. Angiotensin II type 1 receptor antagonist as an angiogenic inhibitor in prostate cancer. Prostate. 2007;67:41-49.
- Kosugi M, Miyajima A, Kikuchi E, Horiguchi Y, Murai M. Angiotensin II type 1 receptor antagonist candesartan as an angiogenic inhibitor in a xenograft model of bladder cancer. Clin Cancer Res. 2006;12:2888-2893.
- Huang W, Wu YL, Zhong J, Jiang FX, Tian XL, Yu LF. Angiotensin II type 1 receptor antagonist suppress angiogenesis and growth of gastric cancer xenografts. Dig Dis Sci. 2008;53:1206-1210.
- Asmar R. Telmisartan in High Cardiovascular Risk Patients. European Cardiology Review. 2012;8:10-16.
- Puri R, Kaur Bhatia R, Shankar Pandey R, Kumar Jain U, Katare OP, Madan J. Sigma-2 receptor ligand anchored telmisartan loaded nanostructured lipid particles augmented drug delivery, cytotoxicity, apoptosis and cellular uptake in prostate cancer cells. Drug Dev Ind Pharm. 2016;42:2020-2030.
- Funao K, Matsuyama M, Kawahito Y, Sano H, Chargui J, Touraine JL, Nakatani T, Yoshimura R. Telmisartan as a peroxisome proliferator-activated receptor-gamma ligand is a new target in the treatment of human renal cell carcinoma. Mol Med Rep. 2009;2:193-198.
- Tyagi S, Gupta P, Saini AS, Kaushal C, Sharma S. The peroxisome proliferator-activated receptor: A family of nuclear receptors role in various diseases. J Adv Pharm Technol Res. 2011;2:236-240.
- Isaac J, Ganguly S, Ghosh A. Co-milling of telmisartan with poly(vinyl alcohol)--An alkalinizer free green approach to ensure its bioavailability. Eur J Pharm Biopharm. 2016;101:43-52.
- Mokale V, Naik J, Verma U, Yadava S. Preparation and Characterization of Biodegradable Glimepiride Loaded PLA Nanoparticles by o/w Solvent Evaporation Method Using High Pressure Homogenizer A Factorial Design Approach. SAJ Pharmacy and Pharmacology. 2014;1:1.
- Feng C, Yuan X, Chu K, Zhang H, Ji W, Rui M. Preparation and optimization of poly (lactic acid) nanoparticles loaded with fisetin to improve anti-cancer therapy. Int J Biol Macromol. 2019;125:700-710.
- Mainardes RM, Evangelista RC. PLGA nanoparticles containing praziquantel: effect of formulation variables on size distribution. Int J Pharm. 2005;290:137-144.
- Bilati U, Allémann E, Doelker E. Sonication parameters for the preparation of biodegradable nanocapsules of controlled size by the double emulsion method. Pharmaceutical development and technology. 2003;8:1-9.
- Cun D, Foged C, Yang M, Frøkjær S, Nielsen HM. Preparation and characterization of poly (DL-lactide-co-glycolide) nanoparticles for siRNA delivery. International journal of pharmaceutics. 2010;390:70-75.
- Fonte P, Soares S, Costa A, Andrade JC, Seabra V, Reis S, Sarmento B. Effect of cryoprotectants on the porosity and stability of insulin-loaded PLGA nanoparticles after freeze-drying. Biomatter. 2012;2:329-339.
- De Chasteigner S, Cavé G, Fessi H, Devissaguet JP, Puisieux F. Freeze-drying of itraconazole-loaded nanosphere suspensions: a feasibility study. Drug Development Research. 1996;38:116-124.
- Panyam J, Williams D, Dash A, Leslie-Pelecky D, Labhasetwar V. Solid-state solubility influences encapsulation and release of hydrophobic drugs from PLGA/PLA nanoparticles. J Pharm Sci. 2004;93:1804-1814.
- Chella N, Narra N, Rama Rao T. Preparation and characterization of liquisolid compacts for improved dissolution of telmisartan. Journal of drug delivery. 2014;2014:692793.
- Kociecka B., Surazynski A., Miltyk W., Palka J. The effect of Telmisartan on collagen biosynthesis depends on the status of estrogen activation in breast cancer cells. Eur J Pharmacol. 2010;628:51-56.
| APA | Ozturk N, KARA A, Vural I (2020). Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique. , 492 - 499. 10.4274/tjps.galenos.2019.76402 |
| Chicago | Ozturk Naile,KARA ASLI,Vural Imran Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique. (2020): 492 - 499. 10.4274/tjps.galenos.2019.76402 |
| MLA | Ozturk Naile,KARA ASLI,Vural Imran Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique. , 2020, ss.492 - 499. 10.4274/tjps.galenos.2019.76402 |
| AMA | Ozturk N,KARA A,Vural I Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique. . 2020; 492 - 499. 10.4274/tjps.galenos.2019.76402 |
| Vancouver | Ozturk N,KARA A,Vural I Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique. . 2020; 492 - 499. 10.4274/tjps.galenos.2019.76402 |
| IEEE | Ozturk N,KARA A,Vural I "Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique." , ss.492 - 499, 2020. 10.4274/tjps.galenos.2019.76402 |
| ISNAD | Ozturk, Naile vd. "Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique". (2020), 492-499. https://doi.org/10.4274/tjps.galenos.2019.76402 |
| APA | Ozturk N, KARA A, Vural I (2020). Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique. Turkish Journal of Pharmaceutical Sciences, 17(5), 492 - 499. 10.4274/tjps.galenos.2019.76402 |
| Chicago | Ozturk Naile,KARA ASLI,Vural Imran Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique. Turkish Journal of Pharmaceutical Sciences 17, no.5 (2020): 492 - 499. 10.4274/tjps.galenos.2019.76402 |
| MLA | Ozturk Naile,KARA ASLI,Vural Imran Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique. Turkish Journal of Pharmaceutical Sciences, vol.17, no.5, 2020, ss.492 - 499. 10.4274/tjps.galenos.2019.76402 |
| AMA | Ozturk N,KARA A,Vural I Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique. Turkish Journal of Pharmaceutical Sciences. 2020; 17(5): 492 - 499. 10.4274/tjps.galenos.2019.76402 |
| Vancouver | Ozturk N,KARA A,Vural I Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique. Turkish Journal of Pharmaceutical Sciences. 2020; 17(5): 492 - 499. 10.4274/tjps.galenos.2019.76402 |
| IEEE | Ozturk N,KARA A,Vural I "Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique." Turkish Journal of Pharmaceutical Sciences, 17, ss.492 - 499, 2020. 10.4274/tjps.galenos.2019.76402 |
| ISNAD | Ozturk, Naile vd. "Formulation and In Vitro Evaluation of Telmisartan Nanoparticles Prepared by Emulsion-Solvent Evaporation Technique". Turkish Journal of Pharmaceutical Sciences 17/5 (2020), 492-499. https://doi.org/10.4274/tjps.galenos.2019.76402 |
