Characterization of Skin Permeation of Vitamin C: Theoretical Analysis of Penetration Profiles and Differential Scanning Calorimetry Study.

Lee, Ae‐Ri Cho; Tojo, Kakuji

doi:10.1248/cpb.46.174

Cited by 24 publications

(20 citation statements)

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“…34) Teichamann et al 27) showed that the stratum corneum was removed by the 10 times tape stripping operation. Consequently, the permeability of drugs through the skin was enhanced by tape stripping treatment, though the rate of enhancement was dependent on the physicochemical property of drug molecules.…”

Section: Resultsmentioning

confidence: 99%

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

Ito¹,

Maeda²,

Fukushima³

et al. 2010

Chem. Pharm. Bull.

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Ascorbic acid (AA, vitamin C) is a hydrophilic vitamin that cannot be produced endogenously in rats and primates including human and is widely used for the protection of the aging of the skin due to the exposure to the UV light and for the acceleration of the synthesis of collagen in the skin. [1][2][3][4] AA was shown to be absorbed from the gastrointestinal tract by an active transport system, though limited amount of AA was transported by this system. 5) In addition, after AA was absorbed, AA was rapidly eliminated from the body by the oxidative metabolism through both enzymatic and nonenzymatic processes.2) Therefore, even if we intake excess amount of AA, sufficient amount of AA is not absorbed into the systemic circulation and is not delivered to its target tissue, skin.2) To conquer this problem, percutaneous delivery of AA has been challenged. The advantage of percutaneous delivery of AA is (1) to obtain high concentration of AA in the skin and (2) to escape the hepatic first-pass effect before reaching to the systemic circulation. However, when AA is percutaneously administered, the penetration of AA to the dermal tissue is difficult because of the high barrier function of the skin. To increase the permeability of AA, derivatives such asascorbic acid 2-sulfate 8) and disodium isostearyl 2-o-L-ascorbyl phosphate, 9,10) has been developed. Also Gopinath et al. designed ascorbyl palmitate vesicles (Aspasomes) for the transdermal delivery of ascorbic acid.11) Furthermore, recent advances in pharmaceutical technology have promoted the research on the permeability enhancement of AA using physical absorption enhancing method like iontophoresis 12) and microemulsion technologies.11,13) Iontophoresis uses an electric field to drive ionized molecules across the skin by electrophoresis and non-ionized molecules by electro osmosis. 14)Despite concerns about skin irritation, iontophoresis may be useful to deliver some peptides and small proteins.15) On the other hand, microneedles are also one of the physical methods for the percutaneous absorption of drugs. With microneedles, small microconduits are formed on the skin. Recent advance in microfabrication technology has made it possible to prepare microneedles that have a possibility of novel transdermal drug delivery system (TDDS). Since the first publication by Henry et al.,16) microfabrication techniques for the production of silicon, metal, glass and polymer microneedle arrays with micrometer dimensions have been developed. 17-20) The microneedles are either solid or hollow and posses a geometrical shape. Microneedle TDDS is roughly defined by a micron size needle preparation for percutaneous administration. Microneedle TDDSs are classified as follows; (1) extremely small needle through which drug solution can be injected into the skin, (2) metallic and/or silastic microneedles on which surface drug is coated, and (3) metallic and/or silastic microneedles by which microconduits are made on the skin and drug solution is applied after removing the microneedles. H...

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Section: Resultsmentioning

confidence: 99%

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

Ito¹,

Maeda²,

Fukushima³

et al. 2010

Chem. Pharm. Bull.

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“…Lee and Tojo [17] reported the skin permeation rate of unstable compounds such as Asc. In 1998, these authors [18] proved that Asc was found to permeate rapidly through the skin, in spite of its low lipophilicity. The diffusivity determined from the lag time was approximately 1,000 times higher in the stripped skin, compared with whole skin.…”

Section: Discussionmentioning

confidence: 99%

Ex vivo Cutaneous Absorption Assessmentof a Stabilized Ascorbic Acid Formulation Using a Microdialysis System

Lévêque¹,

Muret²,

Makki³

et al. 2004

Skin Pharmacol Physiol

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Background: Reactive oxygen species generated by ultraviolet light result in photocarcinogenic and photoaging changes in the skin. Antioxidants protect the skin from these insults. Objective: The aim of this study was to determine the ex vivo ascorbic acid penetration and its degradation in the skin after its topical application from an 8% new formulation. Method: Ascorbic acid was applied to human skin fragments. Ascorbic acid and its metabolites were collected by microdialysis and assessed by gas chromatography mass spectrometry. Results: After topical application of the new formulation, the ascorbic acid level achieved was 8.5% higher than the normal tissue value. This high ascorbic acid dermal concentration remained constant if a topical application was made every 8 h. No degradation of ascorbic acid was detected. Conclusion: Ascorbic acid penetrates rapidly after its topical application. The persistent reservoir of ascorbic acid provides an important and attractive photoprotection strategy.

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“…These authors extended their work still further (Lee and Tojo 1998) by postulating that the high skin penetration of Ascorbic Acid could be explained by its interaction with proteins in the stratum corneum. They again used freshly excised hairless mouse skin mounted between the half cells of their in vitro skin permeation system.…”

Section: In Vitro Studiesmentioning

confidence: 96%

Final Report of the Safety Assessment of L-Ascorbic Acid, Calcium Ascorbate, Magnesium Ascorbate, Magnesium Ascorbyl Phosphate, Sodium Ascorbate, and Sodium Ascorbyl Phosphate as Used in Cosmetics1

2005

Int J Toxicol

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L-Ascorbic Acid, Calcium Ascorbate, Magnesium Ascorbate, Magnesium Ascorbyl Phosphate, Sodium Ascorbate, and Sodium Ascorbyl Phosphate function in cosmetic formulations primarily as antioxidants. Ascorbic Acid is commonly called Vitamin C. Ascorbic Acid is used as an antioxidant and pH adjuster in a large variety of cosmetic formulations, over 3/4 of which were hair dyes and colors at concentrations between 0.3% and 0.6%. For other uses, the reported concentrations were either very low (<0.01%) or in the 5% to 10% range. Calcium Ascorbate and Magnesium Ascorbate are described as antioxidants and skin conditioning agents--miscellaneous for use in cosmetics, but are not currently used. Sodium Ascorbyl Phosphate functions as an antioxidant in cosmetic products and is used at concentrations ranging from 0.01% to 3%. Magnesium Ascorbyl Phosphate functions as an antioxidant in cosmetics and was reported being used at concentrations from 0.001% to 3%. Sodium Ascorbate also functions as an antioxidant in cosmetics at concentrations from 0.0003% to 0.3%. Related ingredients (Ascorbyl Palmitate, Ascorbyl Dipalmitate, Ascorbyl Stearate, Erythorbic Acid, and Sodium Erythorbate) have been previously reviewed by the Cosmetic Ingredient Review (CIR) Expert Panel and found "to be safe for use as cosmetic ingredients in the present practices of good use." Ascorbic Acid is a generally recognized as safe (GRAS) substance for use as a chemical preservative in foods and as a nutrient and/or dietary supplement. Calcium Ascorbate and Sodium Ascorbate are listed as GRAS substances for use as chemical preservatives. L-Ascorbic Acid is readily and reversibly oxidized to L-dehydroascorbic acid and both forms exist in equilibrium in the body. Permeation rates of Ascorbic Acid through whole and stripped mouse skin were 3.43 +/- 0.74 microg/cm(2)/h and 33.2 +/- 5.2 microg/cm(2)/h. Acute oral and parenteral studies in mice, rats, rabbits, guinea pigs, dogs, and cats demonstrated little toxicity. Ascorbic Acid and Sodium Ascorbate acted as a nitrosation inhibitor in several food and cosmetic product studies. No compound-related clinical signs or gross or microscopic pathological effects were observed in either mice, rats, or guinea pigs in short-term studies. Male guinea pigs fed a control basal diet and given up to 250 mg Ascorbic Acid orally for 20 weeks had similar hemoglobin, blood glucose, serum iron, liver iron, and liver glycogen levels compared to control values. Male and female F344/N rats and B6C3F(1) mice were fed diets containing up to 100,000 ppm Ascorbic Acid for 13 weeks with little toxicity. Chronic Ascorbic Acid feeding studies showed toxic effects at dosages above 25 mg/kg body weight (bw) in rats and guinea pigs. Groups of male and female rats given daily doses up to 2000 mg/kg bw Ascorbic Acid for 2 years had no macro- or microscopically detectable toxic lesions. Mice given Ascorbic Acid subcutaneous and intravenous daily doses (500 to 1000 mg/kg bw) for 7 days had no changes in appetite, weight gain, and general behavior; a...

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Characterization of Skin Permeation of Vitamin C: Theoretical Analysis of Penetration Profiles and Differential Scanning Calorimetry Study.

Cited by 24 publications

References 0 publications

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

Ex vivo Cutaneous Absorption Assessmentof a Stabilized Ascorbic Acid Formulation Using a Microdialysis System

Final Report of the Safety Assessment of L-Ascorbic Acid, Calcium Ascorbate, Magnesium Ascorbate, Magnesium Ascorbyl Phosphate, Sodium Ascorbate, and Sodium Ascorbyl Phosphate as Used in Cosmetics1

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