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Biological evaluation of oil-in-water microemulsions as carriers of benzothiophene analogues for dermal applications

Theochari, Ioanna; Ilić, Tanja; Nikolić, Ines; Dobričić, Vladimir; Tenchiou, Alia; Papahatjis, Demetris; Savić, Snežana; Xenakis, Aristotelis; Papadimitriou, Vassiliki; Pletsa, Vasiliki

(MDPI AG, 2021)

TY  - JOUR
AU  - Theochari, Ioanna
AU  - Ilić, Tanja
AU  - Nikolić, Ines
AU  - Dobričić, Vladimir
AU  - Tenchiou, Alia
AU  - Papahatjis, Demetris
AU  - Savić, Snežana
AU  - Xenakis, Aristotelis
AU  - Papadimitriou, Vassiliki
AU  - Pletsa, Vasiliki
PY  - 2021
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3801
AB  - 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 BRAFV600E 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.
PB  - MDPI AG
T2  - Biomimetics
T1  - Biological evaluation of oil-in-water microemulsions as carriers of benzothiophene analogues for dermal applications
VL  - 6
IS  - 1
SP  - 1
EP  - 15
DO  - 10.3390/biomimetics6010010
ER  - 
@article{
author = "Theochari, Ioanna and Ilić, Tanja and Nikolić, Ines and Dobričić, Vladimir and Tenchiou, Alia and Papahatjis, Demetris and Savić, Snežana and Xenakis, Aristotelis and Papadimitriou, Vassiliki and Pletsa, Vasiliki",
year = "2021",
abstract = "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 BRAFV600E 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.",
publisher = "MDPI AG",
journal = "Biomimetics",
title = "Biological evaluation of oil-in-water microemulsions as carriers of benzothiophene analogues for dermal applications",
volume = "6",
number = "1",
pages = "1-15",
doi = "10.3390/biomimetics6010010"
}
Theochari, I., Ilić, T., Nikolić, I., Dobričić, V., Tenchiou, A., Papahatjis, D., Savić, S., Xenakis, A., Papadimitriou, V.,& Pletsa, V.. (2021). Biological evaluation of oil-in-water microemulsions as carriers of benzothiophene analogues for dermal applications. in Biomimetics
MDPI AG., 6(1), 1-15.
https://doi.org/10.3390/biomimetics6010010
Theochari I, Ilić T, Nikolić I, Dobričić V, Tenchiou A, Papahatjis D, Savić S, Xenakis A, Papadimitriou V, Pletsa V. Biological evaluation of oil-in-water microemulsions as carriers of benzothiophene analogues for dermal applications. in Biomimetics. 2021;6(1):1-15.
doi:10.3390/biomimetics6010010 .
Theochari, Ioanna, Ilić, Tanja, Nikolić, Ines, Dobričić, Vladimir, Tenchiou, Alia, Papahatjis, Demetris, Savić, Snežana, Xenakis, Aristotelis, Papadimitriou, Vassiliki, Pletsa, Vasiliki, "Biological evaluation of oil-in-water microemulsions as carriers of benzothiophene analogues for dermal applications" in Biomimetics, 6, no. 1 (2021):1-15,
https://doi.org/10.3390/biomimetics6010010 . .
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