Biological Evaluation of Oil-in-Water Microemulsions as Carriers of Benzothiophene Analogues for Dermal Applications

During the last decade, many studies have been reported on the design and formulation of novel drug delivery systems proposed for dermal or transdermal administration. The efforts focus on the development of biocompatible nanodispersions that can be delivered to the skin and treat severe skin disord...

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Bibliographic Details
Published in:	Biomimetics (Basel, Switzerland) Vol. 6; no. 1; p. 10
Main Authors:	Theochari, Ioanna, Ilic, Tanja, Nicolic, Ines, Dobricic, Vladimir, Tenchiou, Alia, Papahatjis, Demetris, Savic, Snezana, Xenakis, Aristotelis, Papadimitriou, Vassiliki, Pletsa, Vasiliki
Format:	Journal Article
Language:	English
Published:	Switzerland MDPI AG 27-01-2021 MDPI
Subjects:	Amino acids Bioavailability Cancer therapies Cell growth Cell proliferation cell viability Chemotherapy Colorectal cancer Cytotoxicity differential tape stripping Drug delivery Drug delivery systems Drug development Drug dosages Follicles Franz diffusion cell Kinases Lipophilic Medical research Melanoma Microemulsions Pharmaceuticals Skin cancer Skin diseases skin permeation Stratum corneum Western blotting Serbia United States > US Germany skin permeation differential tape stripping cell viability drug delivery Franz diffusion cell chemotherapy
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Summary:	During the last decade, many studies have been reported on the design and formulation of novel drug delivery systems proposed for dermal or transdermal administration. The efforts focus on the development of biocompatible nanodispersions that can be delivered to the skin and treat severe skin disorders, including cancer. In this context, oil-in-water (O/W) microemulsions have been developed to encapsulate and deliver lipophilic bioactive molecules for dermal application. An O/W biocompatible microemulsion composed of PBS buffer, Tween 80, and triacetin was assessed for its efficacy as a drug carrier of DPS-2, a lead compound, initially designed in-house to inhibit BRAF oncogenic kinase. The system was evaluated through both in vitro and ex vivo approaches. The cytotoxic effect, in the presence and absence of DPS-2, was examined through the thiazolyl blue tetrazolium bromide (MTT) cell proliferation assay using various cell lines. Further investigation through Western blotting revealed that cells died of necrosis. Porcine ear skin was used as a skin model to evaluate the degree of permeation of DPS-2 through skin and assess its retention. Through the ex vivo experiments, it was clarified that encapsulated DPS-2 was distributed within the full thickness of the stratum corneum (SC) and had a high affinity to hair follicles.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	2313-7673 2313-7673
DOI:	10.3390/biomimetics6010010