Research Article


DOI :10.26650/JARHS2019-616323   IUP :10.26650/JARHS2019-616323    Full Text (PDF)

Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery

Aslı GürbüzSevgi GüngörMeryem Sedef Erdal

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. 

DOI :10.26650/JARHS2019-616323   IUP :10.26650/JARHS2019-616323    Full Text (PDF)

Deriye İlaç Uygulanması için Transetozomların Formülasyonu ve İn vitro Karakterizasyonu

Aslı GürbüzSevgi GüngörMeryem Sedef Erdal

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. 


PDF View

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. google scholar
  • 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. google scholar
  • 3. Cal K. Skin disposition of menthol after its application in the presence of drug substances. Biopharm Drug Dispos 2008; 29: 449-454. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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 google scholar
  • 7. Choi M.J., Maibach H.I. 2005. “Liposomes and niosomes as topical drug delivery systems”, Skin Pharmacology and Physiology, 18, 209-219. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar
  • 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. google scholar

Citations

Copy and paste a formatted citation or use one of the options to export in your chosen format


EXPORT



APA

Gürbüz, A., Güngör, S., & Erdal, M.S. (2019). Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery. Journal of Advanced Research in Health Sciences, 2(2), 51-59. https://doi.org/10.26650/JARHS2019-616323


AMA

Gürbüz A, Güngör S, Erdal M S. Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery. Journal of Advanced Research in Health Sciences. 2019;2(2):51-59. https://doi.org/10.26650/JARHS2019-616323


ABNT

Gürbüz, A.; Güngör, S.; Erdal, M.S. Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery. Journal of Advanced Research in Health Sciences, [Publisher Location], v. 2, n. 2, p. 51-59, 2019.


Chicago: Author-Date Style

Gürbüz, Aslı, and Sevgi Güngör and Meryem Sedef Erdal. 2019. “Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery.” Journal of Advanced Research in Health Sciences 2, no. 2: 51-59. https://doi.org/10.26650/JARHS2019-616323


Chicago: Humanities Style

Gürbüz, Aslı, and Sevgi Güngör and Meryem Sedef Erdal. Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery.” Journal of Advanced Research in Health Sciences 2, no. 2 (May. 2024): 51-59. https://doi.org/10.26650/JARHS2019-616323


Harvard: Australian Style

Gürbüz, A & Güngör, S & Erdal, MS 2019, 'Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery', Journal of Advanced Research in Health Sciences, vol. 2, no. 2, pp. 51-59, viewed 18 May. 2024, https://doi.org/10.26650/JARHS2019-616323


Harvard: Author-Date Style

Gürbüz, A. and Güngör, S. and Erdal, M.S. (2019) ‘Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery’, Journal of Advanced Research in Health Sciences, 2(2), pp. 51-59. https://doi.org/10.26650/JARHS2019-616323 (18 May. 2024).


MLA

Gürbüz, Aslı, and Sevgi Güngör and Meryem Sedef Erdal. Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery.” Journal of Advanced Research in Health Sciences, vol. 2, no. 2, 2019, pp. 51-59. [Database Container], https://doi.org/10.26650/JARHS2019-616323


Vancouver

Gürbüz A, Güngör S, Erdal MS. Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery. Journal of Advanced Research in Health Sciences [Internet]. 18 May. 2024 [cited 18 May. 2024];2(2):51-59. Available from: https://doi.org/10.26650/JARHS2019-616323 doi: 10.26650/JARHS2019-616323


ISNAD

Gürbüz, Aslı - Güngör, Sevgi - Erdal, MeryemSedef. Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery”. Journal of Advanced Research in Health Sciences 2/2 (May. 2024): 51-59. https://doi.org/10.26650/JARHS2019-616323



TIMELINE


Submitted08.05.2019
Accepted20.05.2019
Published Online06.09.2019

LICENCE


Attribution-NonCommercial (CC BY-NC)

This license lets others remix, tweak, and build upon your work non-commercially, and although their new works must also acknowledge you and be non-commercial, they don’t have to license their derivative works on the same terms.


SHARE




Istanbul University Press aims to contribute to the dissemination of ever growing scientific knowledge through publication of high quality scientific journals and books in accordance with the international publishing standards and ethics. Istanbul University Press follows an open access, non-commercial, scholarly publishing.