Meryem Sedef ERDAL
(İstanbul Üniversitesi, Eczacılık Fakültesi, Farmasötik Teknoloji Anabilim Dalı, İstanbul, Türkiye)
(İstanbul Üniversitesi, Eczacılık Fakültesi, Farmasötik Teknoloji Anabilim Dalı, İstanbul, Türkiye)
(İstanbul Üniversitesi, Eczacılık Fakültesi, Farmasötik Mikrobiyoloji Anabilim Dalı, İstanbul, Türkiye)
(İstanbul Üniversitesi, Eczacılık Fakültesi, Farmasötik Teknoloji Anabilim Dalı, İstanbul, Türkiye)
Yıldız ÖZSOY
(İstanbul Üniversitesi, Eczacılık Fakültesi, Farmasötik Teknoloji Anabilim Dalı, İstanbul, Türkiye)
Yıl: 2020Cilt: 17Sayı: 1ISSN: 1304-530X / 2148-6247Sayfa Aralığı: 43 - 48İngilizce

59 0
In Vitro Skin Permeation and Antifungal Activity of Naftifine Microemulsions
Objectives: Microemulsions are fluid, isotropic, colloidal systems that have been widely studied as drug delivery systems. The percutaneous transport of active agents can be enhanced by their microemulsion formulation when compared to conventional formulations. The purpose of this study was to evaluate naftifine-loaded microemulsions with the objective of improving the skin permeation of the drug. Materials and Methods: Microemulsions comprising oleic acid (oil phase), Kolliphor EL or Kolliphor RH40 (surfactant), Transcutol (co-surfactant), and water were prepared and physicochemical characterization was performed. In vitro skin permeation of naftifine from microemulsions was investigated and compared with that of its conventional commercial formulation. Attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy was used to evaluate the interaction between the microemulsions and the stratum corneum lipids. Candida albicans American Type Culture Collection (ATCC) 10231 and Candida parapsilosis were used to evaluate the antifungal susceptibility of the naftifine-loaded microemulsions. Results: The microemulsion formulation containing Kolliphor RH40 as co-surfactant increased naftifine permeation through pig skin significantly when compared with the commercial topical formulation (p<0.05). ATR-FTIR spectroscopy showed that microemulsions increased the fluidity of the stratum corneum lipid bilayers. Drug-loaded microemulsions possessed superior antifungal activity against Candida albicans ATCC 10231 and Candida parapsilosis. Conclusion: This study demonstrated that microemulsions could be suggested as an alternative topical carrier with potential for enhanced skin delivery of naftifine.
DergiAraştırma MakalesiErişime Açık
  • 1. Gupta AK, Ryder JE, Cooper EA. Naftifine: A Review. J Cutan Med Surg. 2008;12:51-58.
  • 2. Bondaryk M, Kurzątkowski W, Staniszewska M. Antifungal agents commonly used in the superficial and mucosal candidiasis treatment: mode of action and resistance development. Postep Derm Alergol. 2013;30:293-301.
  • 3. Güngör S, Erdal MS, Aksu B. New Formulation Strategies in Topical Antifungal Therapy. Journal of Cosmetics Dermatological Sciences and Applications. 2013;3:56-65.
  • 4. Sintov AC, Shapiro l. New microemulsion vehicle facilitates percutaneous penetration in vitro and cutaneous drug bioavailability in vivo. J Control Release. 2004;95:173-183.
  • 5. Teichmann A, Heuschkel S, Jacobi U, Presse G, Neubert RH, Sterry W, Ladermann J. Comparison of stratum corneum penetration and localization of a lipophilic model drug applied in an o/w microemulsion and an amphiphilic cream. Eur J Pharm Biopharm. 2007;67:699-706.
  • 6. Baroli B, López-Quintela MA, Delgado-Charro MB, Fadda AM, BlancoMéndez J. Microemulsions for topical delivery of 8-methoxsalen. J Control Release. 2000;69:209-218.
  • 7. Zhao JH, Ji L, Wang H, Chen ZQ, Zhang YT, Liu Y, Feng NP. Microemulsion-based novel transdermal delivery system of tetramethylpyrazine: preparation and evaluation in vitro and in vivo. Int J Nanomedicine. 2011;6:1611-1619.
  • 8. Coneac G, Vlaia V,Olariu I, Muţ AM, Anghel DF, Ilie C, Popoiu C, Lupuleasa D, Vlaia L. Development and evaluation of new microemulsion-based hydrogel formulations for topical delivery of fluconazole. AAPS PharmSciTech. 2015;16:889-904.
  • 9. Sintov AC. Transdermal delivery of curcumin via microemulsion. Int J Pharm. 2015;481:97-103.
  • 10. Lopes LB. Overcoming the cutaneous barrier with microemulsions. Pharmaceutics. 2014;6:52-77.
  • 11. Talegaonkar S, Azeem A, Ahmad FJ, Khar RK, Pathan SA, Khan ZI. Microemulsions: a novel approach to enhanced drug delivery. Recent Pat Drug Deliv Formul. 2008;2:238-257.
  • 12. Erdal MS, Özhan G, Mat MC, Özsoy Y, Güngör S. Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations. Int J Nanomedicine. 2016;11:1027-1037.
  • 13. Bommannan D, Potts RO, Guy RH. Examination of stratum corneum barrier function in vivo by infrared spectroscopy. J Invest Dermatol. 1990;95:403-408.
  • 14. CLSI. Performance Standards for Antimicrobial Susceptibility Testing. 27th ed. CLSI supplement M100. Wayne, PA: Clinical and Laboratory Standards Institute; 2017.
  • 15. CLSI. Reference Method for Broth Dilution Antifungal Susceptibility Testing of Yeasts 4th ed. CLSI standard M27. Clinical and Laboratory Standards Institute; 2017.
  • 16. Chryssanthou E, Cuenca-Estrella M. Comparison of the Antifungal Susceptibility Testing Subcommittee of the European Committee on Antibiotic Susceptibility Testing proposed standard and the E-test with the NCCLS broth microdilution method for voriconazole and caspofungin susceptibility testing of yeast species. J Clin Microbiol. 2002;40:3841-3844.
  • 17. Ge S, Lin Y, Lu H, Li Q, He J, Chen B, Wu C, Xu Y. Percutaneous delivery of econazole using microemulsion as vehicle: Formulation, evaluation and vesicle-skin interaction. Int J Pharm. 2014;465:120-131.
  • 18. Hosmer J, Reed R, Bentley MV, Nornoo A, Lopes LB. Microemulsions containing medium-chain glycerides as transdermal delivery systems for hydrophilic and hydrophobic drugs. AAPS PharmSciTech. 2009;10:589-596.
  • 19. Rhee YS, Choi JG, Park ES, Chi SC. Transdermal delivery of ketoprofen using microemulsions. Int J Pharm. 2001;228:161-170.
  • 20. Panapisal V, Charoensri S, Tantituvanont A. Formulation of microemulsion systems for dermal delivery of silymarin. AAPS PharmSciTech. 2012;13:389-399.
  • 21. Kajbafvala A, Salabat A, Salimi A. Formulation, characterization, and in vitro/ex vivo evaluation of quercetin-loaded microemulsion for topical application. Pharm Dev Technol. 2018;23:741-750.
  • 22. Butani D, Yewale C, Misra A. Amphotericin B topical microemulsion: formulation, characterization and evaluation. Colloids Surf B Biointerfaces. 2014;116:351-358.
  • 23. Lin YH, Tsai MJ, Fang YP, Fu YS, Hung YB, Wu PC. Microemulsion formulation design and evaluation for hydrophobic compound: Catechin topical application. Colloids Surf B Biointerfaces. 2018;161:121-128.
  • 24. Schwarz JC, Pagitsch E, Valenta C. Comparison of ATR-FTIR spectra of porcine vaginal and buccal mucosa with ear skin and penetration analysis of drug and vehicle components into pig ear. Eur J Pharm Sci. 2013;50:595-600.
  • 25. Uzqueda M, Martín C, Zornoza A, Sánchez M, Martínez-Ohárriz MC, Vélaz I. Characterization of complexes between naftifine and cyclodextrins in solution and in the solid state. Pharm Res. 2006;23:980-988.
  • 26. Raju YP, N H, Chowdary VH, Nair RS, Basha DJ, N T. In vitro assessment of non-irritant microemulsified voriconazole hydrogel system. Artif Cells Nanomed Biotechnol. 2017;45:1539-1547.
  • 27. Jadhav KR, Shetye SL, Kadam VJ. Design and Evaluation of Microemulsion Based Drug Delivery System. Int J Adv Pharm. 2010;1:156-166.
  • 28. El-Hadidy GN, Ibrahim HK, Mohamed MI, El-Milligi MF. Microemulsions as vehicles for topical administration of voriconazole: formulation and in vitro evaluation. Drug Dev Ind Pharm. 2012;38:64-72.
  • 29. Gelderblom H, Verweij J, Nooter K, Sparreboom A. Cremophor EL: the drawbacks and advantages of vehicle selection for drug formulation. Eur J Cancer. 2001;37:1590-1598.
  • 30. Khattab A, Ismail S. Formulation and evaluation of oxiconazole mucoadhesive nanoemulsion based gel for treatment of fungal vaginal infection. Int J Pharmacy and Pharm Sci. 2016;8:33-40.
  • 31. Abd-Elsalam WH, El-Zahaby SA, Al-Mahallawi AM. Formulation and in vivo assessment of terconazole-loaded polymeric mixed micelles enriched with Cremophor EL as dual functioning mediator for augmenting physical stability and skin delivery. Drug Deliv. 2018;25:484-492.

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