Topical delivery of silymarin constituents via the skin route

Hung, Chi‐Feng; Lin, Yin-Ku; Zhang, Liwen; Chang, Ching-hsien; Fang, Jia‐You

doi:10.1038/aps.2009.186

Cited by 28 publications

(23 citation statements)

References 35 publications

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“…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 side effects [13,14] . Topical delivery via the skin may provide direct selenium targeting to attain sufficient activity for skin prevention/therapy.…”

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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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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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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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“…It is reported that the skin tissue distribution of silibinin is low by oral administration. So its topical delivery via the skin may be capable of reaching enough pharmacological activity (Hung, Lin, Zhang, Chang, & Fang, ).…”

Section: Discussionmentioning

confidence: 99%

Topical silymarin administration for prevention of acute radiodermatitis in breast cancer patients: A randomized, double‐blind, placebo‐controlled clinical trial

Karbasforooshan

Hosseini

Elyasi

et al. 2018

Phytotherapy Research

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Radiation-induced dermatitis is one of the most common side effects of radiotherapy.Silymarin, a flavonoid extracted from the Silybum marianum, exhibits antioxidant and anti-inflammatory activities. The purpose of this study was to investigate the efficacy of silymarin gel in prevention of radiodermatitis in patients with breast cancer. During this randomized, double-blinded, placebo-controlled clinical trial, the preventive effect of silymarin 1% gel was assessed in comparison with placebo, on radiodermatitis occurrence. Forty patients randomly received silymarin gel or placebo formulation on chest wall skin following modified radical mastectomy, once daily starting at the first day of radiotherapy for 5 weeks. Radiodermatitis severity was assessed weekly based on Radiation Therapy Oncology Group (RTOG) and National Cancer Institute Common Terminology for Adverse Events (NCI-CTCAE) criteria radiodermatits grading scale for 5 weeks. The median NCI-CTCAE and RTOG scores were significantly lower in silymarin group at the end of the third to fifth weeks (p value < 0.05). The scores increased significantly in both placebo and silymarin groups during radiotherapy, but there was a delay in radiodermatitis development and progression in silymarin group. Prophylactic administration of silymarin gel could significantly reduce the severity of radiodermatitis and delay its occurrence after 5 weeks of application.

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“…Silybum marianum extract has been used for more than 2000 years to prevent and treat liver disorders (Saller et al , ; Hung et al ). However, to the best of our knowledge, it is the first human study that has evaluated the possible protective effect of silymarin against capecitabine‐induced HFS and clinically proposed the probable useful effects of its topical formulation.…”

Section: Discussionmentioning

confidence: 99%

“…A previous study reported that the skin tissue distribution of silibinin is low by oral administration. So, topical delivery via the skin may be capable of reaching enough pharmacological activity (Hung et al , ). Recent studies showed that silymarin topical formulation could considerably protect against photocarcinogenesis and inhibit UVB and chemical tumor promoter‐induced skin inflammation and edema by exhibiting antioxidant effects.…”

Section: Discussionmentioning

confidence: 99%

Topical Silymarin Administration for Prevention of Capecitabine‐Induced Hand–Foot Syndrome: A Randomized, Double‐Blinded, Placebo‐Controlled Clinical Trial

Elyasi

Rezazadeh-Shojaee

Allahyari

et al. 2017

Phytotherapy Research

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Hand-foot syndrome (HFS) is a frequent dose-limiting adverse reaction of capecitabine in patient with gastrointestinal cancers. Silymarin is a polyphenolic flavonoid extracted from the Silybum marianum that exhibits strong antioxidant and antiinflammatory activities. In this study, we evaluated silymarin efficacy in prevention of capecitabine-induced HFS in patients with gastrointestinal cancers, as the first human study. During this pilot, randomized, double-blinded, placebo-controlled clinical trial, the effect of silymarin gel 1%, which is applied on the palms and soles twice daily starting at the first day of chemotherapy for 9 weeks, on HFS occurrence was assessed. Forty patients fulfilled the inclusion criteria assigned to the silymarin or placebo group. World Health Organization HFS grading scale scores were recorded at baseline and every 3 weeks during these 9 weeks. The median WHO HFS scores were significantly lower in silymarin group at the end of the 9 week (p < 0.05). The scores increased significantly in both placebo and silymarin groups during chemotherapy, but there was a delay for HFS development and progression in silymarin group. Prophylactic administration of silymarin topical formulation could significantly reduce the severity of capecitabine-induced HFS and delays its occurrence in patients with gastrointestinal cancer after 9 weeks of application. Copyright © 2017 John Wiley & Sons, Ltd.

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Topical delivery of silymarin constituents via the skin route

Cited by 28 publications

References 35 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 silymarin administration for prevention of acute radiodermatitis in breast cancer patients: A randomized, double‐blind, placebo‐controlled clinical trial

Topical Silymarin Administration for Prevention of Capecitabine‐Induced Hand–Foot Syndrome: A Randomized, Double‐Blinded, Placebo‐Controlled Clinical Trial

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