In vitro assessment of skin permeation properties of enzymatically derived oil-based fatty acid esters of vitamin C
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2024
Authors
Ćorović, MarijaVeljković, Milica
Milivojević, Ana
Ivanković, Anja P.
Blagojević, Stevan
Pjanović, Rada
Bezbradica, Dejan
Article (Published version)
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Current topical formulations containing vitamin C face limitations in therapeutic effectiveness due to the skin's selective properties that impede drug deposition. Consequently, the widespread use of toxic and irritating chemical permeation enhancers is common. Hereby, we investigated enzymatically derived fatty acid ascorbyl esters (FAAEs) obtained using natural oils for their skin permeation properties using the Strat-M® skin model in a Franz cell diffusion study. By evaluating various cosmetic formulations without added enhancers, we found that emulgel is most suitable for enhancing the cutaneous and transdermal delivery of FAAEs. Furthermore, medium-chain coconut oil-derived FAAEs exhibited faster diffusion rates compared to sunflower oil-based FAAEs with long-side acyl residues, including the commonly applied ascorbyl palmitate. Experimental data were successfully fitted using the Peppas and Sahlin model, which accounted for a lag phase and the combined effect of Fickian diffusion... and polymer relaxation. In the case of long-chain esters, the lag phase was prolonged, and the calculated effective diffusion coefficients (Deff) were lower compared to medium-chain FAAEs. Accordingly, the highest Deff value was observed for ascorbyl caprylate, being even 60 times higher than for ascorbyl palmitate. These results suggest the emerging potential of emulgel with incorporated coconut oil-derived FAAEs for efficiently delivering vitamin C into the skin.
Keywords:
ascorbyl ester / coconut oil / diffusion / sunflower oil / transdermal deliverySource:
Archiv der Pharmazie, 2024Publisher:
- John Wiley and Sons Inc.
Funding / projects:
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200135 (University of Belgrade, Faculty of Technology and Metallurgy) (RS-MESTD-inst-2020-200135)
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200287 (Innovation Center of the Faculty of Technology and Metallurgy) (RS-MESTD-inst-2020-200287)
- PrIntPrEnzy - Prebiotics for functional food and bioactive cosmetics produced in intensified enzymatic processes (RS-ScienceFundRS-Ideje-7750109)
- TwinPrebioEnz - Twinning for intensified enzymatic processes for production of prebiotic-containing functional food and bioactive cosmetics (EU-HE-CSA-101060130)
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Tehnološko-metalurški fakultetTY - JOUR AU - Ćorović, Marija AU - Veljković, Milica AU - Milivojević, Ana AU - Ivanković, Anja P. AU - Blagojević, Stevan AU - Pjanović, Rada AU - Bezbradica, Dejan PY - 2024 UR - http://TechnoRep.tmf.bg.ac.rs/handle/123456789/7641 AB - Current topical formulations containing vitamin C face limitations in therapeutic effectiveness due to the skin's selective properties that impede drug deposition. Consequently, the widespread use of toxic and irritating chemical permeation enhancers is common. Hereby, we investigated enzymatically derived fatty acid ascorbyl esters (FAAEs) obtained using natural oils for their skin permeation properties using the Strat-M® skin model in a Franz cell diffusion study. By evaluating various cosmetic formulations without added enhancers, we found that emulgel is most suitable for enhancing the cutaneous and transdermal delivery of FAAEs. Furthermore, medium-chain coconut oil-derived FAAEs exhibited faster diffusion rates compared to sunflower oil-based FAAEs with long-side acyl residues, including the commonly applied ascorbyl palmitate. Experimental data were successfully fitted using the Peppas and Sahlin model, which accounted for a lag phase and the combined effect of Fickian diffusion and polymer relaxation. In the case of long-chain esters, the lag phase was prolonged, and the calculated effective diffusion coefficients (Deff) were lower compared to medium-chain FAAEs. Accordingly, the highest Deff value was observed for ascorbyl caprylate, being even 60 times higher than for ascorbyl palmitate. These results suggest the emerging potential of emulgel with incorporated coconut oil-derived FAAEs for efficiently delivering vitamin C into the skin. PB - John Wiley and Sons Inc. T2 - Archiv der Pharmazie T1 - In vitro assessment of skin permeation properties of enzymatically derived oil-based fatty acid esters of vitamin C DO - 10.1002/ardp.202400538 ER -
@article{ author = "Ćorović, Marija and Veljković, Milica and Milivojević, Ana and Ivanković, Anja P. and Blagojević, Stevan and Pjanović, Rada and Bezbradica, Dejan", year = "2024", abstract = "Current topical formulations containing vitamin C face limitations in therapeutic effectiveness due to the skin's selective properties that impede drug deposition. Consequently, the widespread use of toxic and irritating chemical permeation enhancers is common. Hereby, we investigated enzymatically derived fatty acid ascorbyl esters (FAAEs) obtained using natural oils for their skin permeation properties using the Strat-M® skin model in a Franz cell diffusion study. By evaluating various cosmetic formulations without added enhancers, we found that emulgel is most suitable for enhancing the cutaneous and transdermal delivery of FAAEs. Furthermore, medium-chain coconut oil-derived FAAEs exhibited faster diffusion rates compared to sunflower oil-based FAAEs with long-side acyl residues, including the commonly applied ascorbyl palmitate. Experimental data were successfully fitted using the Peppas and Sahlin model, which accounted for a lag phase and the combined effect of Fickian diffusion and polymer relaxation. In the case of long-chain esters, the lag phase was prolonged, and the calculated effective diffusion coefficients (Deff) were lower compared to medium-chain FAAEs. Accordingly, the highest Deff value was observed for ascorbyl caprylate, being even 60 times higher than for ascorbyl palmitate. These results suggest the emerging potential of emulgel with incorporated coconut oil-derived FAAEs for efficiently delivering vitamin C into the skin.", publisher = "John Wiley and Sons Inc.", journal = "Archiv der Pharmazie", title = "In vitro assessment of skin permeation properties of enzymatically derived oil-based fatty acid esters of vitamin C", doi = "10.1002/ardp.202400538" }
Ćorović, M., Veljković, M., Milivojević, A., Ivanković, A. P., Blagojević, S., Pjanović, R.,& Bezbradica, D.. (2024). In vitro assessment of skin permeation properties of enzymatically derived oil-based fatty acid esters of vitamin C. in Archiv der Pharmazie John Wiley and Sons Inc... https://doi.org/10.1002/ardp.202400538
Ćorović M, Veljković M, Milivojević A, Ivanković AP, Blagojević S, Pjanović R, Bezbradica D. In vitro assessment of skin permeation properties of enzymatically derived oil-based fatty acid esters of vitamin C. in Archiv der Pharmazie. 2024;. doi:10.1002/ardp.202400538 .
Ćorović, Marija, Veljković, Milica, Milivojević, Ana, Ivanković, Anja P., Blagojević, Stevan, Pjanović, Rada, Bezbradica, Dejan, "In vitro assessment of skin permeation properties of enzymatically derived oil-based fatty acid esters of vitamin C" in Archiv der Pharmazie (2024), https://doi.org/10.1002/ardp.202400538 . .