Topical L-Ascorbic Acid: Percutaneous Absorption Studies

Pinnell, Sheldon R.; Yang, Hongqui; Omar, Mostafa M.; Monteiro‐Riviere, Nancy A.; DeBuys, Holly V.; Walker, Linda C.; Wang, Yaohui; Levine, Mark

doi:10.1046/j.1524-4725.2001.00264.x

Cited by 137 publications

(237 citation statements)

References 64 publications

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“…Pinnell et al studied the percutaneous absorption of AA using intact pig skin where AA concentrations in the pig skin were measured. 43) The maximum skin AA concentration was 176.1 ng/mg. In addition, the cumulative permeated amount of AA reached to the steady state at 4 h after the start of the permeation experiment.…”

Section: )mentioning

confidence: 93%

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: )mentioning

confidence: 93%

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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“…However, the required duration of therapy is relatively long (weeks to months) and skin irritation could occur with acidic pH formulations. Therefore, the current formulation is less acidic than those used by Pinnell et al [15]. The pH of our formulation was 3.1.…”

Section: Discussionmentioning

confidence: 82%

“…[19,20]. However, according to Pinnell et al [15], topical application of these Asc derivatives did not increase Asc skin levels. In addition, ascorbyl-6-palmitate is not Asc [21]: Meves et al [22] showed that ascorbyl-6-palmitate contributes to the generation of oxidized lipid metabolites that are toxic to epidermal cells.…”

Section: Discussionmentioning

confidence: 91%

“…For this reason, it is important to develop new stable topical formulations to increase Asc dermis concentrations before ROS cause damage to the skin. Pinnell et al [15] reported the critical importance of formulation pH for percutaneous absorption of Asc. According to these authors, topical application of an acidic pH formulation (less than 3.5) resulted in increasing Asc skin concentrations.…”

Section: Discussionmentioning

confidence: 99%

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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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“…Vitamin C has also been used in different cosmetic and pharmaceutical formulations because of its beneficial effects on the skin (4,5). Vitamin C topical formulations are also applied due to their depigmenting activity (6) and antiwrinkle activity through collagen synthesis promotion (7).…”

Section: Introductionmentioning

confidence: 99%

Modified Cellulose Nanocrystal for Vitamin C Delivery

2014

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Abstract. Cellulose nanocrystal grafted with chitosan oligosaccharide (CNC-CS OS ) was used to encapsulate vitamin C and prepare CNCS/VC complexes using tripolyphosphte via ionic complexation. The stability of vitamin C and the antioxidant activity of the CNCS/VC complexes were elucidated. The formation of the complex was confirmed using DSC and UV-vis spectrophotometry, and TEM was used to study the morphology of the complexes. The encapsulation efficiency of vitamin C at pH 3 and 5 was 71.6%±6.8 and 91.0±1.0, respectively. Strong exothermic peaks observed in isothermal titration calorimetric (ITC) studies at pH 5 could be attributed to additional electrostatic interactions between CNC-CS OS and vitamin C at pH 5. The in vitro release of vitamin C from CNCS/VC complexes showed a sustained release of up to 20 days. The vitamin C released from CNCS/VC complex displayed higher stability compared with the control vitamin C solution, and this was also confirmed from the ITC thermograms. CNC-CS OS possessed a higher scavenging activity and faster antioxidant activity compared with its precursors, i.e., oxidized CNC and CS OS and their physical mixtures. Complexing vitamin C into CNC-CS OS particles yielded a dynamic antioxidant agent, where the vitamin C is released over time and displayed sustained antioxidant properties. Therefore, CNCS/VC can potentially be used in cosmeceutical applications as topical formulations.

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Topical L-Ascorbic Acid: Percutaneous Absorption Studies

Abstract: Delivery of topical L-ascorbic acid into the skin is critically dependent on formulation characteristics.

Cited by 137 publications

References 64 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

Modified Cellulose Nanocrystal for Vitamin C Delivery

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