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Deriye İlaç Uygulanması için Transetozomların Formülasyonu ve İn vitro Karakterizasyonu

Year 2019, Volume: 2 Issue: 2, 51 - 59, 06.09.2019
https://doi.org/10.26650/JARHS2019-616323

Abstract

Deriye ilaç taşınmasını modifiye eden topikal taşıyıcılara olan ilgi son dönemlerde oldukça artmıştır. Etken maddelerin penetrasyonunda, derinin en dış tabakası olan stratum corneum önemli bir bariyer oluşturmaktadır. Bu bariyeri aşmaya yönelik birçok formülasyon yaklaşımı denenmiştir. Bu yaklaşımlar arasında veziküler taşıyıcılar olan lipozom, etozom, transferzom ve son dönemlerde transetozomların kullanılması ile özellikle lipofilik etken maddelerin derideki lokalizasyonunun iyileştirilmesi hedeflenmektedir. Fosfolipit, yüzey etken madde ve yüksek oranda etanol içeren transetozomlar, transferzom ve etozomların avantajlarını kombine eden sistemlerdir. Bu çalışmada, model lipofilik etken madde olarak fluvastatin ile yüklenmiş transetozomlar geliştirilmiş ve karakterize edilmiştir. Fluvastatinin domuz derisine in vitro penetrasyonu oklüzif olan ve oklüzif olmayan koşullar altında çalışılarak bantla soyma yöntemi ile kantitatif tayin gerçekleştirilmiştir. Transetozomların deri ile etkileşimi ATR-FTIR spektroskopisi kullanılarak araştırılmıştır. Sonuç olarak, oklüzif olmayan koşullarda uygulandığında derideki etken madde lokalizasyonunu iyileştiren bir transetozom formülasyonu hazırlanmıştır. 

References

  • 1. Albash R., Abdelbary A.A., Refai H., E-Nabarawi M.A. 2019. “Use of transethosomes for enhancing the transdermal delivey of olmesartan medoxomil: in vitro, ex vivo, and in vivo ealuation”, International Journal of Nanomedicine, 14, 1953-1968.
  • 2. Alberti I., Kalia Y.N., Naik A., Bonny J., Guy R.H. 2001. “Effect of  ethanol  and isopropyl myristate on the availability of topical terbinafine in human stratum corneum, in vivo”. International Journal of Pharmaceutics, 21, 11-19.
  • 3. Cal K. Skin disposition of menthol after its application in the presence of drug substances. Biopharm Drug Dispos 2008; 29: 449-454.
  • 4. Celia C., Cilurzo F., Trapasso E., Cosco D., Fresta M., Paolino D. 2012. “Ethosomes and transfersomes containing linoleic acid: physicochemical and technological features of topical drug delivery carriers for the potential treatment of melasma disorders”, Biomed Microdevices, 14, 119-130.
  • 5. Cevc G., Blume G. 2001. “New, highly efficient formulation of diclofenac for the topical, transdermal administration in ultradeformable drug carriers, Transfersomes”, Biochimica et Biophysica Acta, 1514, 191-205.
  • 6. Chessa M., Caddeo C., Valenti D., Manconi M., Sinico C., Fadda A.M. 2011. “Effect of Penetration Enhancer Containing Vesicles on the Percutaneous Delivery of Quercetin through New Born Pig Skin”, Pharmaceutics, 3, 497-509
  • 7. Choi M.J., Maibach H.I. 2005. “Liposomes and niosomes as topical drug delivery systems”, Skin Pharmacology and Physiology, 18, 209-219.
  • 8. Dubey V., Mishra D., Jain N.K. 2007. “Melatonin loaded ethanolic liposomes: physicochemical characterization and enhanced transdermal delivery”, European Journal of Pharmaceutics and Biopharmaceutics, 67, 398-405.
  • 9. El Maghraby G.M.M., Williams A.C., Barry B.W. 2001. “Skin delivery of 5-fluorouracil from ultradeformable and standard liposomes in vitro”, Journal of Pharmacy and Pharmacology, 53, 1069-1077.
  • 10. El Zaafarany G.M., Awad G.A.S., Holayel S.M., Mortada N.M. 2010. “Role of edge activators and surface charge in developing ultradeformable vesciles with enhanced skin delivery”. International Journal of Pharmaceutics, 397, 164-17.
  • 11. Erdal M.S., Peköz A.Y., Aksu B., Araman A. 2014. “Impacts of chemical enhancers on skin permeation and deposition of terbinafine”, Pharmaceutical Development and Technology, 19, 565-570.
  • 12. Funke A.P., Schiller R., Motzkus H.W., Gunther C., Muller R.H., Lipp R. 2002. “Transdermal delivery of highly lipophilic drugs: in vitro fluxes of antioestrogens, permeation enhancers, and solvents from liquid formulations”, Pharmaceutical Research, 19, 661-668.
  • 13. Gangwar M., Singh R., Goel R.K., Nath G. 2012. “Recent advances in various emerging vesicular systems: an overview”, Asian Pacific Journal of Tropical Biomedicine, 1176-1188.
  • 14. Güngör S., Erdal M.S., Özdin D. 2011. “Derinin Yapısının Aydınlatılması ve Geçirgenliğinin Değerlendirilmesinde Kullanılan Biyofiziksel Yöntemler”, Türkiye Klinikleri Dermatoloji Dergisi, 21, 25-39.
  • 15. Güngör S., Erdal M.S., Aksu B. 2013. “New formulation strategies in topical antifungal therapy”, Journal of Cosmetics, Dermatological Sciences and Applications, 3, 56-65.
  • 16. Kim T.G., Byamba D., Wu W.H., Lee M.G. 2011. “Statins inhibit chemotactic interaction between CCL20 and CCR6 in vitro: possible relevance to psoriasis treatment”. Experimental Dermatology, 20, 855-857.
  • 17. Klang V, Schwarz JC, Haberfeld S, Xiao P, Wirth M, Valenta C. 2012. “Skin integrity testing and monitoring of in vitro tape stripping by capacitance-based sensor imaging”, Skin Research and Technology, 1, 1-14.
  • 18. Kumar L., Verma S., Bhardwaj A., Vaidya S., Vaidya B. 2013. “Eradication of superficial fungal infections by conventional and novel approaches: a comprehensive review”, Artificial Cells, Nanomedicine, and Biotechnology, 1-15.
  • 19. Koushlesh Kumar Mishra, Chanchal Deep Kaur, Shekhar Verma, Anil Kumar Sahu, Deepak Kumar Dash, Pankaj Kashyap and Saraswati Prasad Mishra. (2019). Transethosomes and Nanoethosomes: Recent Approach on Transdermal Drug Delivery System, Nanomedicines, Muhammad Akhyar Farrukh, IntechOpen, DOI: 10.5772/intechopen.81152.
  • 20. Pawar A.Y., Khanderao R. J., Laxmikant H. C. 2016. “Transfersome: A novel technique which improves transdermal permeability”, Asian Journal of Pharmaceutics, 10, 425-436.
  • 21. Salem H.F., Kharshoum R.M., Abou-Taleb H.A., AbouTaleb H.A., AbouElhassan K.M. 2018. “Progesterone-loaded nanosized transethosomes for vaginal permeation enhancement: formulation, statistical optimization, and clinical evaluation in anovulatory polycystic ovary syndrome”, Journal of Liposome Research, 13, 1-12.
  • 22. Song C.K., Balakrishnan P., Shim C.K., Chung S.J., Chong S., Kim D.D. 2012. “A novel vesicular carrier, transethosome, for enhanced skin delivery of voriconazole: characterization and in vitro/in vivo evaluation”, Colloids and Surfaces B: Biointerfaces, 92, 299-304.
  • 23. Touitou E., Dayan N., Bergelson L., Godin B., Eliaz M. 2000. “Ethosomes-novel vesicular carriers for enhanced delivery: characterization and skin penetration properties”, Journal of Controlled Release, 65, 403-418.
  • 24. Verma P., Pathak K. 2012. “Nanosized ethanolic vesicles loaded with econazole nitrate for the treatment of deep fungal infections through topical gel formulation”, Nanomedicine, 8, 489-496.

Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery

Year 2019, Volume: 2 Issue: 2, 51 - 59, 06.09.2019
https://doi.org/10.26650/JARHS2019-616323

Abstract

There has been increased interest during recent years in the use of topical vehicles that may modify drug penetration into the skin. However, the complex structure of the skin and especially its uppermost layer, the stratum corneum, function as a rate limiting barrier for topical drug delivery. Various strategies have been employed to achieve the delivery of drugs into the skin. Among these strategies, vesicular carriers such as liposomes, ethosomes, transfersomes, and, more recently, transethosomes have been suggested to serve as efficient promoters of drug localization within the skin. Transethosomes contain phospholipids, surfactants, and a high percentage of ethanol. They have shown to enhance the skin penetration of lipophilic drugs. In this study, transethosomes have been developed, characterized, and loaded with a model lipophilic drug, fluvastatine. The in vitro pig skin penetration of fluvastatine from transethosome dispersion under occlusive and non-occlusive conditions have been determined quantitatively by using the tape stripping method. An ATR-FTIR spectroscopy has been used to study the interaction of transethosomes with the skin lipids. As a result, a topical transethosomal carrier which optimizes drug localization within the skin when applied under non-occlusive conditions has been developed. 

References

  • 1. Albash R., Abdelbary A.A., Refai H., E-Nabarawi M.A. 2019. “Use of transethosomes for enhancing the transdermal delivey of olmesartan medoxomil: in vitro, ex vivo, and in vivo ealuation”, International Journal of Nanomedicine, 14, 1953-1968.
  • 2. Alberti I., Kalia Y.N., Naik A., Bonny J., Guy R.H. 2001. “Effect of  ethanol  and isopropyl myristate on the availability of topical terbinafine in human stratum corneum, in vivo”. International Journal of Pharmaceutics, 21, 11-19.
  • 3. Cal K. Skin disposition of menthol after its application in the presence of drug substances. Biopharm Drug Dispos 2008; 29: 449-454.
  • 4. Celia C., Cilurzo F., Trapasso E., Cosco D., Fresta M., Paolino D. 2012. “Ethosomes and transfersomes containing linoleic acid: physicochemical and technological features of topical drug delivery carriers for the potential treatment of melasma disorders”, Biomed Microdevices, 14, 119-130.
  • 5. Cevc G., Blume G. 2001. “New, highly efficient formulation of diclofenac for the topical, transdermal administration in ultradeformable drug carriers, Transfersomes”, Biochimica et Biophysica Acta, 1514, 191-205.
  • 6. Chessa M., Caddeo C., Valenti D., Manconi M., Sinico C., Fadda A.M. 2011. “Effect of Penetration Enhancer Containing Vesicles on the Percutaneous Delivery of Quercetin through New Born Pig Skin”, Pharmaceutics, 3, 497-509
  • 7. Choi M.J., Maibach H.I. 2005. “Liposomes and niosomes as topical drug delivery systems”, Skin Pharmacology and Physiology, 18, 209-219.
  • 8. Dubey V., Mishra D., Jain N.K. 2007. “Melatonin loaded ethanolic liposomes: physicochemical characterization and enhanced transdermal delivery”, European Journal of Pharmaceutics and Biopharmaceutics, 67, 398-405.
  • 9. El Maghraby G.M.M., Williams A.C., Barry B.W. 2001. “Skin delivery of 5-fluorouracil from ultradeformable and standard liposomes in vitro”, Journal of Pharmacy and Pharmacology, 53, 1069-1077.
  • 10. El Zaafarany G.M., Awad G.A.S., Holayel S.M., Mortada N.M. 2010. “Role of edge activators and surface charge in developing ultradeformable vesciles with enhanced skin delivery”. International Journal of Pharmaceutics, 397, 164-17.
  • 11. Erdal M.S., Peköz A.Y., Aksu B., Araman A. 2014. “Impacts of chemical enhancers on skin permeation and deposition of terbinafine”, Pharmaceutical Development and Technology, 19, 565-570.
  • 12. Funke A.P., Schiller R., Motzkus H.W., Gunther C., Muller R.H., Lipp R. 2002. “Transdermal delivery of highly lipophilic drugs: in vitro fluxes of antioestrogens, permeation enhancers, and solvents from liquid formulations”, Pharmaceutical Research, 19, 661-668.
  • 13. Gangwar M., Singh R., Goel R.K., Nath G. 2012. “Recent advances in various emerging vesicular systems: an overview”, Asian Pacific Journal of Tropical Biomedicine, 1176-1188.
  • 14. Güngör S., Erdal M.S., Özdin D. 2011. “Derinin Yapısının Aydınlatılması ve Geçirgenliğinin Değerlendirilmesinde Kullanılan Biyofiziksel Yöntemler”, Türkiye Klinikleri Dermatoloji Dergisi, 21, 25-39.
  • 15. Güngör S., Erdal M.S., Aksu B. 2013. “New formulation strategies in topical antifungal therapy”, Journal of Cosmetics, Dermatological Sciences and Applications, 3, 56-65.
  • 16. Kim T.G., Byamba D., Wu W.H., Lee M.G. 2011. “Statins inhibit chemotactic interaction between CCL20 and CCR6 in vitro: possible relevance to psoriasis treatment”. Experimental Dermatology, 20, 855-857.
  • 17. Klang V, Schwarz JC, Haberfeld S, Xiao P, Wirth M, Valenta C. 2012. “Skin integrity testing and monitoring of in vitro tape stripping by capacitance-based sensor imaging”, Skin Research and Technology, 1, 1-14.
  • 18. Kumar L., Verma S., Bhardwaj A., Vaidya S., Vaidya B. 2013. “Eradication of superficial fungal infections by conventional and novel approaches: a comprehensive review”, Artificial Cells, Nanomedicine, and Biotechnology, 1-15.
  • 19. Koushlesh Kumar Mishra, Chanchal Deep Kaur, Shekhar Verma, Anil Kumar Sahu, Deepak Kumar Dash, Pankaj Kashyap and Saraswati Prasad Mishra. (2019). Transethosomes and Nanoethosomes: Recent Approach on Transdermal Drug Delivery System, Nanomedicines, Muhammad Akhyar Farrukh, IntechOpen, DOI: 10.5772/intechopen.81152.
  • 20. Pawar A.Y., Khanderao R. J., Laxmikant H. C. 2016. “Transfersome: A novel technique which improves transdermal permeability”, Asian Journal of Pharmaceutics, 10, 425-436.
  • 21. Salem H.F., Kharshoum R.M., Abou-Taleb H.A., AbouTaleb H.A., AbouElhassan K.M. 2018. “Progesterone-loaded nanosized transethosomes for vaginal permeation enhancement: formulation, statistical optimization, and clinical evaluation in anovulatory polycystic ovary syndrome”, Journal of Liposome Research, 13, 1-12.
  • 22. Song C.K., Balakrishnan P., Shim C.K., Chung S.J., Chong S., Kim D.D. 2012. “A novel vesicular carrier, transethosome, for enhanced skin delivery of voriconazole: characterization and in vitro/in vivo evaluation”, Colloids and Surfaces B: Biointerfaces, 92, 299-304.
  • 23. Touitou E., Dayan N., Bergelson L., Godin B., Eliaz M. 2000. “Ethosomes-novel vesicular carriers for enhanced delivery: characterization and skin penetration properties”, Journal of Controlled Release, 65, 403-418.
  • 24. Verma P., Pathak K. 2012. “Nanosized ethanolic vesicles loaded with econazole nitrate for the treatment of deep fungal infections through topical gel formulation”, Nanomedicine, 8, 489-496.
There are 24 citations in total.

Details

Primary Language Turkish
Subjects Pharmacology and Pharmaceutical Sciences
Journal Section Research Articles
Authors

Aslı Gürbüz This is me 0000-0002-1389-1581

Sevgi Güngör This is me 0000-0002-8199-3010

Meryem Sedef Erdal This is me 0000-0001-6220-2036

Publication Date September 6, 2019
Submission Date May 8, 2019
Published in Issue Year 2019 Volume: 2 Issue: 2

Cite

MLA Gürbüz, Aslı et al. “Deriye İlaç Uygulanması için Transetozomların Formülasyonu Ve İn Vitro Karakterizasyonu”. Sağlık Bilimlerinde İleri Araştırmalar Dergisi, vol. 2, no. 2, 2019, pp. 51-59, doi:10.26650/JARHS2019-616323.