Controlled penetration of ceramides into and across the stratum corneum using various types of microemulsions and formulation associated toxicity studies |
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| Affiliation: | 1. Department of Pharmaceutical Technology and Biopharmaceutics, Institute of Pharmacy, Martin Luther University Halle-Wittenberg, Halle (Saale), Germany;2. Department of Dermatology and Venereology, Medical Faculty, Martin Luther University Halle-Wittenberg, Halle (Saale), Germany;3. Department of Pharmaceutics and Social Pharmacy, School of Pharmacy, College of Health Sciences, Addis Ababa University, Addis Ababa, Ethiopia;1. Núcleo de Desenvolvimento Farmacêutico e Cosmético, Departamento de Ciências Farmacêuticas, UFPE, Recife, Pernambuco 50739-520, Brazil;2. Departamento de Farmácia, UEPB, Campina Grande, Paraíba 58100-001, Brazil;3. Departamento de Farmácia, UFS, São Cristóvão, Sergipe 49100-000, Brazil;4. Laboratório de Morfologia e Biologia Estrutural, Instituto de Tecnologia e Pesquisa, UNIT, Aracaju, Sergipe 49032-490, Brazil;5. Departamento de Química, UFS, Campus Alberto Carvalho, Itabaiana, Sergipe 49500-000, Brazil;1. Department of Applied Chemistry, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Gyeonggi-do 426-791, Republic of Korea;2. Damy Chemical Co., Material Science Research Institute, 481-10, Gasan-dong, Geumcheon-gu, Seoul 153-803, Republic of Korea;3. Amore-Pacific Co. R&D Center, 314-1, Bora-dong, Giheung-gu, Yongin, Gyeonggi-do 446-729, Republic of Korea;1. Center of Experimental and Applied Cutaneous Physiology, Department of Dermatology and Allergy, Charité – Universitätsmedizin Berlin, Germany;2. Institute of Food Chemistry, Hamburg School of Food Science, University of Hamburg, Germany;3. Klosterfrau Berlin GmbH, Berlin, Germany;4. Laser- und Medizin-Technologie GmbH, Berlin, Germany;1. Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia;2. Institute of Biology, Medicinal Chemistry & Biotechnology, National Hellenic Research Foundation, Athens, Greece;3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia;4. Faculty of Technology, University of Niš, Leskovac, Serbia;5. DCP Hemigal, Leskovac, Serbia;1. Department of Experimental Psychology, Helmholtz Institute, Utrecht University, The Netherlands;2. Department of Neurology, Rudolf Magnus Institute of Neuroscience, University Medical Center Utrecht, The Netherlands;3. Department of Rehabilitation Medicine, Rudolf Magnus Institute of Neuroscience, University Medical Center Utrecht, The Netherlands;4. Cognitive Psychology Laboratory, Vrije Universiteit Amsterdam, The Netherlands |
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| Abstract: | Several skin diseases such as psoriasis and atopic dermatitis are associated with the depletion or disturbance of stratum corneum (SC) lipids such as ceramides (CERs), free fatty acids and cholesterol. Studies suggested that replenishment of these lipids might help to treat diseased, affected or aged skin. With this premises in mind, there are some formulations in the market that contain SC lipids and currently, to facilitate permeation of the lipids deep into the SC, various CERs, and other SC lipid microemulsions (MEs) were developed and characterised using lecithin or TEGO® CARE PL 4 (TCPL4) as base surfactants. However, to date, there are no reports that involve the permeability of SC lipids into and across the SC, and therefore, the penetration of CER [NP] as a model ceramide from various formulations was investigated ex vivo using Franz diffusion cell. Besides, the toxicity of the MEs was assessed using hen’s egg test chorioallantoic membrane (HET-CAM). The results of the study showed that CER [NP] could not permeate into deeper layers of the SC from a conventional hydrophilic cream. Unlike the cream, CER [NP] permeated into the deeper layers of the SC from both type of MEs, where permeation of the CER was more and into deeper layers from droplet type and lecithin-based MEs than bicontinuous (BC) type and TCPL4 based MEs, respectively. The CER also permeated into deeper layers from ME gels which was, however, shallow and to a lesser extent when compared with the MEs. The results of HET-CAM showed that both MEs are safe to be used topically, with lecithin-based MEs exhibiting better safety profiles than TCPL4 based MEs. Concluding, the study showed that the MEs are safe to be used on the skin for the controlled penetration of CER [NP] deep into the SC. |
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| Keywords: | Ceramide HET-CAM Microemulsion Permeation Stratum corneum Toxicity |
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