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) Switzerland), 2021-01, Vol.6 (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: Article
Language:English
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
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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.
ISSN:2313-7673
2313-7673
DOI:10.3390/biomimetics6010010