In Vitro Skin Permeation and Antifungal Activity of Naftifine Microemulsions/Naftifin Mikroemulsiyonlarinin In Vitro Deriden Permeasyonu ve Antifungal Aktivitesi

• Published in: Turkish Journal of Pharmaceutical Sciences Vol. 17; no. 1; p. 43
• Main Authors: Erdal, Meryem Sedef, Gurbuz, Asli, Birteksoz Tan, Seher, Gungor, Sevgi, Ozsoy, Yildiz
• Format: Journal Article
• Language: English
• Published: Galenos Yayinevi Tic. Ltd 01.02.2020
• Subjects: Antifungal agents; Characterization; Comparative analysis; Dermatologic agents; Drug delivery systems; Fatty acids; Lipids; Monounsaturated fatty acids; Naftifine; Skin; Spectroscopy; Surface active agents; Swine; Transdermal drug delivery systems; Unsaturated fatty acids; Germany
• ISSN: 1304-530X
• DOI: 10.4274/tjps.galenos.2018.87699

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. Key words: Naftifine, microemulsion, colloidal drug carrier system, topical antifungal Amac: Mikroemulsiyonlar, ilac tasiyici sistemler olarak cok calisilan; sivi, izotropik, kolloidal sistemlerdir. Aktif maddelerin mikroemulsiyonlardan perkutan absorpsiyonu konvansiyonel formulasyona gore iyilesebilmektedir. Bu calismanin amaci, naftifin yuklu mikroemulsiyonlarin, ilacin deriden permeasyonunun iyilestirilmesine yonelik olarak degerlendirilmesidir. Gerec ve Yontemler: Oleik asit (yag fazi), Kolliphor EL veya Kolliphor RH40 (surfaktan), Transcutol (ko-surfaktan) ve sudan olusan mikroemulsiyonlar hazirlanarak fizikokimyasal karakterizasyonlari gerceklestirilmistir. Naftifinin in vitro deriden permeasyonu calisilmis ve konvansiyonel ticari preparati ile karsilastirilmistir. Zayiflatilmis toplam yansima-Fourier donusumu (ATR-FTIR) spektroskopisi, mikroemulsiyonlar ile stratum corneum lipitleri arasindaki etkilesimin arastirilmasi icin kullanilmistir. Naftifin yuklu mikroemulsiyonlarin antifungal aktiviteleri Candida albicans Amerikan Tip Kultur Koleksiyonu (ATCC) 10231 ve Candida parapsilosis kullanilarak degerlendirilmistir. Bulgular: Ko-surfaktan olarak Kolliphor RH40 iceren mikroemulsiyon formulasyonu, naftifinin topikal ticari formulasyonu ile karsilastirildiginda, domuz derisinden naftifin permeasyonunu istatistiksel olarak anlamli derecede arttirmistir (p<0,05). ATR-FTIR spektroskopisi, mikroemulsiyonlarin stratum corneum lipit cifte tabakalarinin akiskanligini arttirdigini gostermistir. Ilac yuklu mikromulsiyonlar, Candida albicans ATCC 10231 ve Candida parapsilosis turlerine karsi yuksek antifungal aktivite gostermislerdir. Sonuc: Sonuc olarak, bu calismada mikroemulsiyonlarin, naftifinin deriden permeasyonunun iyilestirilmesinde alternatif topikal tasiyicilar olarak kabul edilebilecekleri gosterilmistir. Anahtar kelimeler: Naftifin, mikroemulsiyon, kolloidal ilac tasiyici sistem, topikal antifungal