The “in vitro” percutaneous penetration of three antioxidant compounds

Marti‐Mestres, Gilberte; Mestres, J. P.; Brès, J.; Martin, Sabine; Ramos, Jeanne; Vian, Laurence

doi:10.1016/j.ijpharm.2006.09.020

Cited by 51 publications

(34 citation statements)

References 16 publications

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“…Cumulative and prolonged exposure to UVB is now known to induce deleterious reactions in human skin, including cutaneous aging, immunosuppression, photo-carcinogenesis, and various inflammatory skin disorders [17] . Supplying topical exogenous antioxidants to the skin can prevent or minimize UVB-induced damage [18] .…”

Section: Discussionmentioning

confidence: 99%

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In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

Lin

Fang²,

Al‐Suwayeh

et al. 2011

Acta Pharmacol Sin

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Aim: To investigate the in vitro and in vivo percutaneous absorption of seleno-L-methionine (Se-L-M), an ultraviolet (UV)-protecting agent, from aqueous solutions. Methods: Aqueous solutions of Se-L-M were prepared in pH 4, 8, and 10.8 buffers. The pH 8 buffer contained 30% glycerol, propylene glycol (PG) and polyethylene glycol (PEG) 400. The in vitro skin permeation of Se-L-M via porcine skin and nude mouse skin was measured and compared using Franz diffusion cells. The in vivo skin tolerance study was performed, which examined transepidermal water loss (TEWL), skin pH and erythema. Results: In the excised porcine skin, the flux was 0.1, 11.4 and 8.2 μg· cm -2 ·h -1 for the pH 4, 8, and 10.8 buffers, respectively. A linear correlation between the flux and skin deposition was determined. According to permeation across skin with different treatments (stripping, delipidation, and ethanol treatments), it was determined that the intracellular route comprised the predominant pathway for Se-L-M permeation from pH 8 buffer. Aqueous solutions of seleno-DL-methionine (Se-DL-M), selenium sulfide and selenium-containing quantum dot nanoparticles were also used as donor systems. The DL form showed a lower flux (7.0 vs 11.4 μg· cm -2 ·h -1 ) and skin uptake (23.4 vs 47.3 μg/g) as compared to the L form, indicating stereoselective permeation of this compound. There was no or only negligible permeation of selenium sulfide and quantum dots into and across the skin. With in vivo topical application for 4 and 8 h, the skin deposition of Se-L-M was about 7 μg/g, and values were comparable to each other. The topical application of Se-L-M for up to 5 d did not caused apparent skin irritation. However, slight inflammation of the dermis was noted according to the histopathological examination. Conclusion: Se-L-M was readily absorbed by the skin in both the in vitro and in vivo experiments. The established profiles of Se-L-M skin absorption will be helpful in developing topical products of this compound.Keywords: seleno-L-methionine; selenium; percutaneous absorption; topical delivery; skin [5] . In humans, a low selenium status is associated with up to a 4-fold increased risk of developing skin cancer [6] . Topical selenium compounds also increase the minimum dose of UV radiation required to cause skin reddening and protect against skin damage caused by UVB [7,8] . Seleno-L-methionine (Se-L-M), the major component of dietary selenium, represents an organic form of selenium which may provide enhanced protection of the skin [9] . Se-L-M also decreases the oxidative stress of neurodegenerative diseases, rheumatoid arthritis, and HIV/AIDS [10,11] . Most ingested selenium, whether in organic or inorganic form, is converted by liver metabolism [3] . In addition, selenium toxicity can produce gastrointestinal problems [12] . Delivery of pharmacologically active compounds via the skin is an attractive alternative to oral dosing for numerous reasons including stable plasma concentrations, bypass of firstpass effects, and reduction of some si...

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Section: Discussionmentioning

confidence: 99%

“…Se-L-M fits this criterion (Mw 196.1 Da). Poor absorption is more likely when the octanol/water partition coefficient (logP) is >5 or <-1 [17] . Se-L-M showed a logP of -3.01 [22] , which does not fulfill the criterion.…”

Section: Discussionmentioning

confidence: 99%

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

Lin

Fang²,

Al‐Suwayeh

et al. 2011

Acta Pharmacol Sin

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“…Skin absorption of a drug is determined by its physicochemical properties, in particular, the molecular weight and lipophilicity which play major roles in the process [20,28] . SB, SD, and SC possess the same molecular weight of 482.4 Da.…”

Section: Discussionmentioning

confidence: 99%

Topical delivery of silymarin constituents via the skin route

et al. 2009

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Aim: Silibinin (SB), silydianin (SD), and silychristin (SC) are components of silymarin. These compounds can be used to protect the skin from oxidative stress induced by ultraviolet (UV) irradiation and treat it. To this end, the absorption of silymarin constituents via the skin was examined in the present report. Methods: Transport of SB, SD, and SC under the same thermodynamic activity through and into the skin and the effects of pH were studied in vitro using a Franz diffusion assembly. Results: The lipophilicity increased in the order of SC

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“…ochemical properties, in particular the molecular weight and lipophilicity, which play major roles in the process. 19) More-lipophilic components may penetrate the SC more readily. There is also good evidence that the SC is much more permeable to neutral molecules than to ions of weak acids or bases.…”

Section: Discussionmentioning

confidence: 99%

Delivery of Resveratrol, a Red Wine Polyphenol, from Solutions and Hydrogels <i>via</i> the Skin

Hung

Lin

Huang

et al. 2008

Biological & Pharmaceutical Bulletin

104

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Resveratrol is a naturally occurring polyphenolic compound which has received much attention in the prevention of and therapy for cardiovascular diseases and cancers ( Fig. 1).1) Red grapes and wines contain considerable amounts of resveratrol. Resveratrol has many benefits for the skin. Topically applied resveratrol has been shown to possess strong antiproliferative and chemopreventive properties against skin carcinogenesis.2-4) Resveratrol affords substantial protection against skin damage from ultraviolet B (UVB) exposure. 5,6) Resveratrol shows antimicrobial activity against dermatophytes and herpes simplex virus. 7,8) Resveratrol can also be used in the dermocosmetic field because of its role as a phytoestrogen based on its ability to activate estrogen receptors. 9)The oral bioavailability of resveratrol is poor, leading to an irrelevant in vivo effect with oral administration compared to its powerful in vitro efficacy. 10) Resveratrol also has a short initial half-life (8-14 min) and is extensively metabolized in the body.11) Several phase I clinical trials are currently underway for oral resveratrol in humans at doses of as high as 7.5 g per day. This would require 2.7 kg of resveratrol a year at a current cost of ca. US$6800. Therefore it is becoming increasingly important to find ways to improve the bioavailability of and block the metabolism of resveratrol. Delivery of resveratrol via the skin is an attractive alternative to oral dosing for both topical and transdermal applications.No evidence currently exists in the literature to support the notion that a sufficient amount of resveratrol can be delivered to produce therapeutic benefits via a skin route. Designs of optimal formulations for resveratrol permeation via the skin are also lacking. The purposes of this study were to establish basic profiles of resveratrol permeability into and across the skin. The optimal pH and co-solvent of the vehicles for resveratrol were investigated for better permeation. The present study utilized Franz cells to explore the in vitro skin permeation of resveratrol. The drug amount retained within the skin reservoir was determined by in vitro and in vivo methods. Various skin membranes, including nude mouse skin, stratum corneum (SC)-stripped skin, delipidized skin, and cellulose membranes, were used as permeation barriers to elucidate the mechanisms and pathways. One particular problem common to drug delivery systems designed for use on the skin is the poor retention at the site of application. This problem can be resolved by incorporating bioadhesive hydrogels within the system. Hence, the ability of a series of hydrogel formulations to deliver topically applied resveratrol was examined. The permeability of piceatannol (Fig. 1), a resveratrol analogue with considerably higher activity, was also evaluated in this study. Resveratrol, the main active polyphenol in red wine, has been demonstrated to show benefits against skin disorders. The bioavailability of orally administered resveratrol is insufficient to permit high...

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The “in vitro” percutaneous penetration of three antioxidant compounds

Cited by 51 publications

References 16 publications

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

Topical delivery of silymarin constituents via the skin route

Delivery of Resveratrol, a Red Wine Polyphenol, from Solutions and Hydrogels <i>via</i> the Skin

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