Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations

M Sedef Erdal,1 Gül Özhan,2 M Cem Mat,3 Yıldız Özsoy,1 Sevgi Güngör1 1Department of Pharmaceutical Technology, 2Department of Pharmaceutical Toxicology, Faculty of Pharmacy, 3Department of Dermatology, Cerrahpasa Medical Faculty, Istanbul University, Ist...

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Autores principales:	Erdal MS, Özhan G, Mat MC, Özsoy Y, Güngör S
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	Naftifine tape stripping in vivo skin penetration microemulsion colloidal carriers Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/ae2db39622bf44b4b8dfbd4c77ce0d83
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spelling	oai:doaj.org-article:ae2db39622bf44b4b8dfbd4c77ce0d832021-12-02T04:58:02ZColloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations1178-2013https://doaj.org/article/ae2db39622bf44b4b8dfbd4c77ce0d832016-03-01T00:00:00Zhttps://www.dovepress.com/colloidal-nanocarriers-for-the-enhanced-cutaneous-delivery-of-naftifin-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013M Sedef Erdal,1 Gül Özhan,2 M Cem Mat,3 Yıldız Özsoy,1 Sevgi Güngör1 1Department of Pharmaceutical Technology, 2Department of Pharmaceutical Toxicology, Faculty of Pharmacy, 3Department of Dermatology, Cerrahpasa Medical Faculty, Istanbul University, Istanbul, Turkey Abstract: In topical administration of antifungals, the drugs should pass the stratum corneum to reach lower layers of the skin in effective concentrations. Thus, the formulation of antifungal agents into a suitable delivery system is important for the topical treatment of fungal infections. Nanosized colloidal carriers have gained great interest during the recent years to serve as efficient promoters of drug penetration into the skin. Microemulsions are soft colloidal nanosized drug carriers, which are thermodynamically stable and isotropic systems. They have been extensively explored for the enhancement of skin delivery of drugs. This study was carried out to exploit the feasibility of colloidal carriers as to improve skin transport of naftifine, which is an allylamine antifungal drug. The microemulsions were formulated by construction of pseudoternary phase diagrams and composed of oleic acid (oil phase), Kolliphor® EL or Kolliphor® RH40 (surfactant), Transcutol® (cosurfactant), and water (aqueous phase). The plain and drug-loaded microemulsions were characterized in terms of isotropy, particle size and size distribution, pH value, refractive index, viscosity, and conductivity. The in vitro skin uptake of naftifine from microemulsions was studied using tape stripping technique in pig skin. The drug penetrated significantly into stratum corneum from microemulsions compared to its marketed cream (P<0.05). Moreover, the microemulsion formulations led to highly significant amount of naftifine deposition in deeper layers of skin than that of commercial formulation (P<0.001). Microemulsion–skin interaction was confirmed by attenuated total reflectance – Fourier transformed infrared spectroscopy data, in vitro. The results of the in vivo tape stripping experiment showed similar trends as the in vitro skin penetration study. Topical application of the microemulsion on human forearms in vivo enhanced significantly the distribution and the amount of naftifine penetrated into the stratum corneum as compared to the marketed formulation (P<0.05). The relative safety of the microemulsion formulations was demonstrated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide viability test. This study indicated that the nanosized colloidal carriers developed could be considered as an effective and safe topical delivery system for naftifine. Keywords: antifungal drug, tape stripping, in vivo skin penetration, microemulsion, colloidal carriersErdal MSÖzhan GMat MCÖzsoy YGüngör SDove Medical PressarticleNaftifinetape strippingin vivo skin penetrationmicroemulsioncolloidal carriersMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 1027-1037 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Naftifine tape stripping in vivo skin penetration microemulsion colloidal carriers Medicine (General) R5-920
spellingShingle	Naftifine tape stripping in vivo skin penetration microemulsion colloidal carriers Medicine (General) R5-920 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
description	M Sedef Erdal,1 Gül Özhan,2 M Cem Mat,3 Yıldız Özsoy,1 Sevgi Güngör1 1Department of Pharmaceutical Technology, 2Department of Pharmaceutical Toxicology, Faculty of Pharmacy, 3Department of Dermatology, Cerrahpasa Medical Faculty, Istanbul University, Istanbul, Turkey Abstract: In topical administration of antifungals, the drugs should pass the stratum corneum to reach lower layers of the skin in effective concentrations. Thus, the formulation of antifungal agents into a suitable delivery system is important for the topical treatment of fungal infections. Nanosized colloidal carriers have gained great interest during the recent years to serve as efficient promoters of drug penetration into the skin. Microemulsions are soft colloidal nanosized drug carriers, which are thermodynamically stable and isotropic systems. They have been extensively explored for the enhancement of skin delivery of drugs. This study was carried out to exploit the feasibility of colloidal carriers as to improve skin transport of naftifine, which is an allylamine antifungal drug. The microemulsions were formulated by construction of pseudoternary phase diagrams and composed of oleic acid (oil phase), Kolliphor® EL or Kolliphor® RH40 (surfactant), Transcutol® (cosurfactant), and water (aqueous phase). The plain and drug-loaded microemulsions were characterized in terms of isotropy, particle size and size distribution, pH value, refractive index, viscosity, and conductivity. The in vitro skin uptake of naftifine from microemulsions was studied using tape stripping technique in pig skin. The drug penetrated significantly into stratum corneum from microemulsions compared to its marketed cream (P<0.05). Moreover, the microemulsion formulations led to highly significant amount of naftifine deposition in deeper layers of skin than that of commercial formulation (P<0.001). Microemulsion–skin interaction was confirmed by attenuated total reflectance – Fourier transformed infrared spectroscopy data, in vitro. The results of the in vivo tape stripping experiment showed similar trends as the in vitro skin penetration study. Topical application of the microemulsion on human forearms in vivo enhanced significantly the distribution and the amount of naftifine penetrated into the stratum corneum as compared to the marketed formulation (P<0.05). The relative safety of the microemulsion formulations was demonstrated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide viability test. This study indicated that the nanosized colloidal carriers developed could be considered as an effective and safe topical delivery system for naftifine. Keywords: antifungal drug, tape stripping, in vivo skin penetration, microemulsion, colloidal carriers
format	article
author	Erdal MS Özhan G Mat MC Özsoy Y Güngör S
author_facet	Erdal MS Özhan G Mat MC Özsoy Y Güngör S
author_sort	Erdal MS
title	Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations
title_short	Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations
title_full	Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations
title_fullStr	Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations
title_full_unstemmed	Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations
title_sort	colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/ae2db39622bf44b4b8dfbd4c77ce0d83
work_keys_str_mv	AT erdalms colloidalnanocarriersfortheenhancedcutaneousdeliveryofnaftifinecharacterizationstudiesandinvitroandinvivoevaluations AT ozhang colloidalnanocarriersfortheenhancedcutaneousdeliveryofnaftifinecharacterizationstudiesandinvitroandinvivoevaluations AT matmc colloidalnanocarriersfortheenhancedcutaneousdeliveryofnaftifinecharacterizationstudiesandinvitroandinvivoevaluations AT ozsoyy colloidalnanocarriersfortheenhancedcutaneousdeliveryofnaftifinecharacterizationstudiesandinvitroandinvivoevaluations AT gungors colloidalnanocarriersfortheenhancedcutaneousdeliveryofnaftifinecharacterizationstudiesandinvitroandinvivoevaluations
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Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations

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