Abstract
Incorporation of antioxidants into sunscreens is a logical approach, yet co-delivery of them with UV filters is a challenge. Here, we purposed a combination therapy, in which the chemical UV filter, octyl methoxycinnamate, was accumulated on upper skin while the antioxidant, melatonin, can penetrate deeper layers to show its effects. Melatonin-loaded elastic niosomes and octyl methoxycinnamate Pickering emulsion were prepared separately. Lyophilized elastic niosomes were dispersed into the Pickering emulsion to prepare the proposed combination formulation. The characterization studies of the formulations revealed that elastic niosomes can be prepared with tunable nanometer sizes, whereas Pickering emulsions can encapsulate the UV filter in micrometer-sized droplets. Melatonin-loaded elastic niosomes prepared with Tween80/Span80 mixture were 146 nm with a PI of 0.438, and 58.42% entrapment efficiency was achieved. The mean diameter size of the combination formulation was 27.8 μm. Ex vivo permeation studies revealed that 7.40% of octyl methoxycinnamate and 58% of melatonin were permeated through the rat skin while 27.6% octyl methoxycinnamate and 37% of melatonin accumulated in the skin after 24 h. Cell culture studies with real-time cell analyzer showed that the proposed formulation consist of melatonin-loaded elastic niosomes and octyl methoxycinnamate Pickering emulsion had no negative effect on the cell proliferation and viability. According to α,α-diphenyl-β-picrylhydrazyl free radical scavenging method, the proposed formulation showed as high antioxidant activity as melatonin itself. It is concluded that the proposed formulation would be a promising dual therapy for UV-induced skin damage with co-delivery strategy.
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Acknowledgements
This study was supported by the Ege University, Scientific Research Projects No. 13-ECZ-003. The authors would like to thank the Ege University, Faculty of Pharmacy, Pharmaceutical Sciences Research Center (FABAL), for the provided instrumentation. Authors are pursuing a patent from Turkish Patent Institute for this work. Patent application and research was conducted by the Ege University Technology Transfer Office, EBILTEM. Authors would like to thank Izmir Institute of Technology Center for Materials Research and Zehra Sinem YILMAZ for their help with the SEM studies and Yalçın Erzurumlu for his help with cell culture studies.
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Arslan Azizoglu, G., Tuncay Tanriverdi, S., Aydin Kose, F. et al. Dual-Prevention for UV-Induced Skin Damage: Incorporation of Melatonin-Loaded Elastic Niosomes into Octyl Methoxycinnamate Pickering Emulsions. AAPS PharmSciTech 18, 2987–2998 (2017). https://doi.org/10.1208/s12249-017-0786-1
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DOI: https://doi.org/10.1208/s12249-017-0786-1