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Development, Characterization and In-vitro Evaluation of Solid Self-Emulsifying Drug Delivery Systems (S-SEDDS) Containing Valsartan

Yıl 2023, Cilt: 16 Sayı: 3, 672 - 686, 31.12.2023
https://doi.org/10.18185/erzifbed.1332052

Öz

Hipertansiyon, kardiyovasküler hastalık için ana risk faktörüdür. Valsartan, anjiyotensin II'nin anjiyotensin Tip 1 reseptörü üzerindeki etkisini spesifik olarak bloke ederek yaygın olarak kullanılan, etkili ve iyi tolere edilen antihipertansif ajandır. Ancak gastrointestinal sistemin üst kısmından emilir ve buranın asidik ortamı nedeniyle bu bölgede az çözünür ve oral biyoyararlanımı sadece %25'tir. Bu çalışmanın amacı, Valsartan'ın (VST) ticari formülasyonuna alternatif olarak yeni bir dozaj formu geliştirmektir. Bu amaçla, VST’ın çözünürlüğünü artırmak ve pH'tan bağımsız bir çözünürlüğe sahip olan katı kendiliğinden emülsifiye olabilen ilaç taşıyıcı sistem (S-SEDDS) formülasyonu geliştirmek hedeflenmiştir. VST'ın en yüksek çözünürlük gösterdiği SEDDS bileşenlerini belirlemek için çözünürlük çalışmaları yapılmıştır. Çözünürlük çalışmalarına göre; yağ fazı olarak izopropil miristat (3.5 mg/mL), yüzey etkin maddeler olarak Capyrol 90 (19.8 mg/mL) ve Tween 20 (32.5 mg/mL), yardımcı yüzey etkin madde olarak ise Transcutol HP (168.9 mg/mL) kullanılmıştır. Çözünürlük çalışmaları ile belirlenen yardımcı maddeler ile üçgen faz diyagramları çizilmiştir. VST içeren SEDDS formülasyonları Avicel pH101 ve Hidroksipropil metil selüloz’a (HPMC) ayrı ayrı yaş granülasyon tekniği ile adsorbe edilmiş ve karakterizasyon çalışmaları yapılmıştır. Geliştirilen VST-SEDDS, VST-SEDDS-Avicel ve VST-SEDDS-HPMC formülasyonları pH 1.2 ortamında ticari ürüne göre VST salınımı arttırmıştır. Ayrıca VST-SEDDS-Avicel formülasyonunun açlık, tokluk durumlarından ve pH değişiminden etkilenmediği gözlenmiştir. Bu nedenle VST-SEDDS-Avicel formülasyonunun, pH'tan bağımsız çözünürlüğü arttırdığı ve antihipertansif tedavi için potansiyel bir formülasyon adayı olabileceği söylenebilmektedir.

Destekleyen Kurum

TUBİTAK

Proje Numarası

117S821

Kaynakça

  • 1. Alǧin, E., Kiliçarslan, M., Karataş, A., Yüksel, N., & Baykara, T. (2004). Effects of polymer type, polymer:direct tabletting agent ratio and tabletting method on verapamil hydrochloride extended release from hydroxypropylmethylcellulose matrix tablets. Ankara Universitesi Eczacilik Fakultesi Dergisi, 33(3), 125–137.
  • 2. Alwadei, M., Kazi, M., & Alanazi, F. K. (2019). Novel oral dosage regimen based on self-nanoemulsifying drug delivery systems for codelivery of phytochemicals – Curcumin and thymoquinone. Saudi Pharmaceutical Journal, 27(6), 866–876. King Saud University. Retrieved from https://doi.org/10.1016/j.jsps.2019.05.008
  • 3. Amrutkar, C., Salunkhe, K., & Chaudhari, S. (2014). Study on self nano emulsifying drug delivery system of poorly water soluble drug rosuvastatin calcium. World Journal of Pharmaceutical Research, 3(4), 2137–1251. Retrieved from www.wjpr.net
  • 4. Aydın, Z., & Öztürk, S. (2014). Hipertansiyon tedavisinde güncel yaklaşımlar. Haseki Tip Bulteni, 52(4), 251–255.
  • 5. Balakumar, K., Vijaya, C., Tamil, N., Hari, R., & Abdu, S. (2013). Colloids and Surfaces B : Biointerfaces Self nanoemulsifying drug delivery system ( SNEDDS ) of Rosuvastatin calcium : Design , formulation , bioavailability and pharmacokinetic evaluation. Colloids and Surfaces B: Biointerfaces, 112(2013), 337–343. Elsevier B.V.
  • 6. Diril, M., Karasulu, Y., Toskas, M., & Nikolakakis, I. (2019). Self-Emulsifying Atorvastatin Calcium Pellets and, (Ldl).
  • 7. Diril, M., Türkyılmaz, G. Y., & Karasulu, H. Y. (2019). Formulation and In Vitro Evaluation of Self Microemulsifying Drug Delivery System Containing Atorvastatin Calcium. Current Drug Delivery, 16(8), 768–779.
  • 8. FDA. (1997). FDA guidance for industry. Dissolution Technologies (Vol. 4).
  • 9. Gülmezoğlu, E., Yıldız Türkyılmaz, G., & Karasulu, H. Y. (2022). Preparation and evaluation of a lipid-based drug delivery system to ımprove valsartan oral bioavailability: pharmacokinetic and pharmacodynamic analysis. Drug Development and Industrial Pharmacy, 48(12), 727–736. Taylor & Francis. Retrieved from https://doi.org/10.1080/03639045.2022.2164588
  • 10. Jianxian, C., Saleem, K., Ijaz, M., & Ur-rehman, M. (2020). Development and in vitro Evaluation of Self-emulsifying Drug Delivery System. International journal of Nanomedicine, 15, 5217–5226.
  • 11. Kalepu, S., Manthina, M., & Padavala, V. (2013). Oral lipid-based drug delivery systems – an overview. Acta Pharmaceutica Sinica B, 3(6), 361–372. Elsevier. Retrieved from http://dx.doi.org/10.1016/j.apsb.2013.10.001
  • 12. Khan, F., Islam, M. S., Roni, M. A., & Jalil, R. U. (2012). Systematic development of self-emulsifying drug delivery systems of atorvastatin with improved bioavailability potential. Scientia Pharmaceutica, 80(4), 1027–1043.
  • 13. Kleberg, K., Jacobsen, J., & Müllertz, A. (2010). Characterising the behaviour of poorly water soluble drugs in the intestine: Application of biorelevant media for solubility, dissolution and transport studies. Journal of Pharmacy and Pharmacology, 62(11), 1656–1668.
  • 14. Klein, S. (2010). The use of biorelevant dissolution media to forecast the in vivo performance of a drug. AAPS Journal, 12(3), 397–406.
  • 15. Mukherjee, S., Ray, S., & Thakur, R. S. (2009). Solid lipid nanoparticles: A modern formulation approach in drug delivery system. Indian Journal of Pharmaceutical Sciences, 71(4), 349–358.
  • 16. Nakmode, D., Bhavana, V., Thakor, P., Madan, J., Singh, P. K., Singh, S. B., Rosenholm, J. M., et al. (2022). Fundamental Aspects of Lipid-Based Excipients in Lipid-Based Product Development. Pharmaceutics, 14(4).
  • 17. Panner, S. R., Kulkarni, P. K., & Dixit, M. (2013). Preparation and evaluation of self-nanoemulsifying formulation of efavirenz. Indian Journal of Pharmaceutical Education and Research, 47(1), 47–54.
  • 18. Park, Y. H., & Kim, H. J. (2021). Formulation and stability of horse oil-in-water emulsion by HLB system. Food Science and Biotechnology, 30(7), 931–938. Springer Singapore. Retrieved from https://doi.org/10.1007/s10068-021-00934-8
  • 19. Rehman, F. U., Farid, A., Shah, S. U., Dar, M. J., Rehman, A. U., Ahmed, N., Rashid, S. A., et al. (2022). Self-Emulsifying Drug Delivery Systems (SEDDS): Measuring Energy Dynamics to Determine Thermodynamic and Kinetic Stability. Pharmaceuticals, 15(9).
  • 20. Sarisaltik Yaşin, D., & Teksi̇n, Z. Ş. (2018). Evaluation of biorelevant dissolution media simulating fasted and fed states. Fabad Journal of Pharmaceutical Sciences, 43(3), 217–232.
  • 21. Saydam, M., & Takka, S. (2007). BIOAVAILABILITY FILE: VALSARTAN. FABAD J. Pharm. Sci (Vol. 32, pp. 185–196).
  • 22. Shin, D. J., Chae, B. R., Goo, Y. T., Yoon, H. Y., Kim, C. H., Sohn, S. Il, Oh, D., et al. (2019). Improved dissolution and oral bioavailability of valsartan using a solidified supersaturable self-microemulsifying drug delivery system containing gelucire® 44/14. Pharmaceutics, 11(2).
  • 23. Shirkhedkar, A. A., Chaudhari, S. R., Patil, A. S., & Surana, S. J. (2017). A concise review on analytical profile of valsartan. Eurasian Journal of Analytical Chemistry, 12(4), 337–364.
  • 24. Tadikonda, R. R., & Ade, S. (2020). Preparation and in vitro evaluation of sustained release bilayered matrix tablets of valsartan. World Journal of Pharmacy and Pharmaceutical Sciences, 9(6), 1307–1319.
  • 25. Thakkar, H., Parmar, M., Nangesh, J., & Patel, D. (2011). Formulation and characterization of lipid-based drug delivery system of raloxifene-microemulsion and self-microemulsifying drug delivery system. Journal of Pharmacy and Bioallied Sciences, 3(3), 442. Retrieved from http://www.jpbsonline.org/text.asp?2011/3/3/442/84463
  • 26. Tzeyung, A. S., Md, S., Bhattamisra, S. K., Madheswaran, T., Alhakamy, N. A., Aldawsari, H. M., & Radhakrishnan, A. K. (2019). Fabrication, optimization, and evaluation of rotigotine-loaded chitosan nanoparticles for nose-to-brain delivery. Pharmaceutics, 11(1), 1–17.
  • 27. Varela-Moreira, A., van Leur, H., Krijgsman, D., Ecker, V., Braun, M., Buchner, M., Fens, M. H. A. M., et al. (2022). Utilizing in vitro drug release assays to predict in vivo drug retention in micelles. International Journal of Pharmaceutics, 618(December 2021), 121638. Elsevier B.V. Retrieved from https://doi.org/10.1016/j.ijpharm.2022.121638
  • 28. Zahrychuk, H. Y., Gladkov, E. S., Kyrychenko, A. V., Poliovyi, D. O., Zahrychuk, O. M., Kucher, T. V., & Logoyda, L. S. (2023). Structure-Based Rational Design and Virtual Screening of Valsartan Drug Analogs towards Developing Novel Inhibitors of Angiotensin II Type 1 Receptor. Biointerface Research in Applied Chemistry, 13(5), 1–13.
  • 29. Zarghi, A., Shafaati, A., Foroutan, S. M., & Movahed, H. (2008). Rapid quantification of valsartan in human plasma by liquid chromatography using a monolithic column and a fluorescence detection: Application for pharmacokinetic studies. Scientia Pharmaceutica, 76(3), 439–450.
Yıl 2023, Cilt: 16 Sayı: 3, 672 - 686, 31.12.2023
https://doi.org/10.18185/erzifbed.1332052

Öz

Proje Numarası

117S821

Kaynakça

  • 1. Alǧin, E., Kiliçarslan, M., Karataş, A., Yüksel, N., & Baykara, T. (2004). Effects of polymer type, polymer:direct tabletting agent ratio and tabletting method on verapamil hydrochloride extended release from hydroxypropylmethylcellulose matrix tablets. Ankara Universitesi Eczacilik Fakultesi Dergisi, 33(3), 125–137.
  • 2. Alwadei, M., Kazi, M., & Alanazi, F. K. (2019). Novel oral dosage regimen based on self-nanoemulsifying drug delivery systems for codelivery of phytochemicals – Curcumin and thymoquinone. Saudi Pharmaceutical Journal, 27(6), 866–876. King Saud University. Retrieved from https://doi.org/10.1016/j.jsps.2019.05.008
  • 3. Amrutkar, C., Salunkhe, K., & Chaudhari, S. (2014). Study on self nano emulsifying drug delivery system of poorly water soluble drug rosuvastatin calcium. World Journal of Pharmaceutical Research, 3(4), 2137–1251. Retrieved from www.wjpr.net
  • 4. Aydın, Z., & Öztürk, S. (2014). Hipertansiyon tedavisinde güncel yaklaşımlar. Haseki Tip Bulteni, 52(4), 251–255.
  • 5. Balakumar, K., Vijaya, C., Tamil, N., Hari, R., & Abdu, S. (2013). Colloids and Surfaces B : Biointerfaces Self nanoemulsifying drug delivery system ( SNEDDS ) of Rosuvastatin calcium : Design , formulation , bioavailability and pharmacokinetic evaluation. Colloids and Surfaces B: Biointerfaces, 112(2013), 337–343. Elsevier B.V.
  • 6. Diril, M., Karasulu, Y., Toskas, M., & Nikolakakis, I. (2019). Self-Emulsifying Atorvastatin Calcium Pellets and, (Ldl).
  • 7. Diril, M., Türkyılmaz, G. Y., & Karasulu, H. Y. (2019). Formulation and In Vitro Evaluation of Self Microemulsifying Drug Delivery System Containing Atorvastatin Calcium. Current Drug Delivery, 16(8), 768–779.
  • 8. FDA. (1997). FDA guidance for industry. Dissolution Technologies (Vol. 4).
  • 9. Gülmezoğlu, E., Yıldız Türkyılmaz, G., & Karasulu, H. Y. (2022). Preparation and evaluation of a lipid-based drug delivery system to ımprove valsartan oral bioavailability: pharmacokinetic and pharmacodynamic analysis. Drug Development and Industrial Pharmacy, 48(12), 727–736. Taylor & Francis. Retrieved from https://doi.org/10.1080/03639045.2022.2164588
  • 10. Jianxian, C., Saleem, K., Ijaz, M., & Ur-rehman, M. (2020). Development and in vitro Evaluation of Self-emulsifying Drug Delivery System. International journal of Nanomedicine, 15, 5217–5226.
  • 11. Kalepu, S., Manthina, M., & Padavala, V. (2013). Oral lipid-based drug delivery systems – an overview. Acta Pharmaceutica Sinica B, 3(6), 361–372. Elsevier. Retrieved from http://dx.doi.org/10.1016/j.apsb.2013.10.001
  • 12. Khan, F., Islam, M. S., Roni, M. A., & Jalil, R. U. (2012). Systematic development of self-emulsifying drug delivery systems of atorvastatin with improved bioavailability potential. Scientia Pharmaceutica, 80(4), 1027–1043.
  • 13. Kleberg, K., Jacobsen, J., & Müllertz, A. (2010). Characterising the behaviour of poorly water soluble drugs in the intestine: Application of biorelevant media for solubility, dissolution and transport studies. Journal of Pharmacy and Pharmacology, 62(11), 1656–1668.
  • 14. Klein, S. (2010). The use of biorelevant dissolution media to forecast the in vivo performance of a drug. AAPS Journal, 12(3), 397–406.
  • 15. Mukherjee, S., Ray, S., & Thakur, R. S. (2009). Solid lipid nanoparticles: A modern formulation approach in drug delivery system. Indian Journal of Pharmaceutical Sciences, 71(4), 349–358.
  • 16. Nakmode, D., Bhavana, V., Thakor, P., Madan, J., Singh, P. K., Singh, S. B., Rosenholm, J. M., et al. (2022). Fundamental Aspects of Lipid-Based Excipients in Lipid-Based Product Development. Pharmaceutics, 14(4).
  • 17. Panner, S. R., Kulkarni, P. K., & Dixit, M. (2013). Preparation and evaluation of self-nanoemulsifying formulation of efavirenz. Indian Journal of Pharmaceutical Education and Research, 47(1), 47–54.
  • 18. Park, Y. H., & Kim, H. J. (2021). Formulation and stability of horse oil-in-water emulsion by HLB system. Food Science and Biotechnology, 30(7), 931–938. Springer Singapore. Retrieved from https://doi.org/10.1007/s10068-021-00934-8
  • 19. Rehman, F. U., Farid, A., Shah, S. U., Dar, M. J., Rehman, A. U., Ahmed, N., Rashid, S. A., et al. (2022). Self-Emulsifying Drug Delivery Systems (SEDDS): Measuring Energy Dynamics to Determine Thermodynamic and Kinetic Stability. Pharmaceuticals, 15(9).
  • 20. Sarisaltik Yaşin, D., & Teksi̇n, Z. Ş. (2018). Evaluation of biorelevant dissolution media simulating fasted and fed states. Fabad Journal of Pharmaceutical Sciences, 43(3), 217–232.
  • 21. Saydam, M., & Takka, S. (2007). BIOAVAILABILITY FILE: VALSARTAN. FABAD J. Pharm. Sci (Vol. 32, pp. 185–196).
  • 22. Shin, D. J., Chae, B. R., Goo, Y. T., Yoon, H. Y., Kim, C. H., Sohn, S. Il, Oh, D., et al. (2019). Improved dissolution and oral bioavailability of valsartan using a solidified supersaturable self-microemulsifying drug delivery system containing gelucire® 44/14. Pharmaceutics, 11(2).
  • 23. Shirkhedkar, A. A., Chaudhari, S. R., Patil, A. S., & Surana, S. J. (2017). A concise review on analytical profile of valsartan. Eurasian Journal of Analytical Chemistry, 12(4), 337–364.
  • 24. Tadikonda, R. R., & Ade, S. (2020). Preparation and in vitro evaluation of sustained release bilayered matrix tablets of valsartan. World Journal of Pharmacy and Pharmaceutical Sciences, 9(6), 1307–1319.
  • 25. Thakkar, H., Parmar, M., Nangesh, J., & Patel, D. (2011). Formulation and characterization of lipid-based drug delivery system of raloxifene-microemulsion and self-microemulsifying drug delivery system. Journal of Pharmacy and Bioallied Sciences, 3(3), 442. Retrieved from http://www.jpbsonline.org/text.asp?2011/3/3/442/84463
  • 26. Tzeyung, A. S., Md, S., Bhattamisra, S. K., Madheswaran, T., Alhakamy, N. A., Aldawsari, H. M., & Radhakrishnan, A. K. (2019). Fabrication, optimization, and evaluation of rotigotine-loaded chitosan nanoparticles for nose-to-brain delivery. Pharmaceutics, 11(1), 1–17.
  • 27. Varela-Moreira, A., van Leur, H., Krijgsman, D., Ecker, V., Braun, M., Buchner, M., Fens, M. H. A. M., et al. (2022). Utilizing in vitro drug release assays to predict in vivo drug retention in micelles. International Journal of Pharmaceutics, 618(December 2021), 121638. Elsevier B.V. Retrieved from https://doi.org/10.1016/j.ijpharm.2022.121638
  • 28. Zahrychuk, H. Y., Gladkov, E. S., Kyrychenko, A. V., Poliovyi, D. O., Zahrychuk, O. M., Kucher, T. V., & Logoyda, L. S. (2023). Structure-Based Rational Design and Virtual Screening of Valsartan Drug Analogs towards Developing Novel Inhibitors of Angiotensin II Type 1 Receptor. Biointerface Research in Applied Chemistry, 13(5), 1–13.
  • 29. Zarghi, A., Shafaati, A., Foroutan, S. M., & Movahed, H. (2008). Rapid quantification of valsartan in human plasma by liquid chromatography using a monolithic column and a fluorescence detection: Application for pharmacokinetic studies. Scientia Pharmaceutica, 76(3), 439–450.
Toplam 29 adet kaynakça vardır.

Ayrıntılar

Birincil Dil İngilizce
Konular Eczacılık Bilimleri, İlaç Dağıtım Teknolojileri
Bölüm Makaleler
Yazarlar

Mine Diril 0000-0002-7154-8511

Gülbeyaz Yıldız Türkyılmaz 0000-0002-8601-0263

Eda Gülmezoğlu 0000-0002-1570-6140

Yesim Karasulu 0000-0002-1860-8255

Proje Numarası 117S821
Erken Görünüm Tarihi 25 Aralık 2023
Yayımlanma Tarihi 31 Aralık 2023
Yayımlandığı Sayı Yıl 2023 Cilt: 16 Sayı: 3

Kaynak Göster

APA Diril, M., Yıldız Türkyılmaz, G., Gülmezoğlu, E., Karasulu, Y. (2023). Development, Characterization and In-vitro Evaluation of Solid Self-Emulsifying Drug Delivery Systems (S-SEDDS) Containing Valsartan. Erzincan University Journal of Science and Technology, 16(3), 672-686. https://doi.org/10.18185/erzifbed.1332052