Iontophoresis promotes percutaneous absorption of l-ascorbic acid in rat skin

Ebihara, Mutsuhito; Akiyama, Minoru; Ohnishi, Yoshihiro; Tajima, S.; Komata, Ki-ichi; Mitsui, Yukio

doi:10.1016/s0923-1811(03)00105-1

Cited by 32 publications

(26 citation statements)

References 15 publications

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“…On the other hand, to increase the percutaneous absorption of AA, physical methods like iontophoresis have been challenged. 12) In addition, many AA derivatives have been synthesized. [6][7][8][9][10]50) However, no percutaneous AA preparation has been clinically available up to now.…”

Section: )mentioning

confidence: 99%

“…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.…”

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confidence: 99%

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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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confidence: 99%

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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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“…Iontophoresis has been investigated as a way to enhance skin penetration since an AP salt molecule includes 2 -3 anions [6,8]. Iontophoresis is an effective and non-invasive method which uses mild electric currents that do not damage the skin barrier.…”

Section: Introductionmentioning

confidence: 99%

Enhanced Iontophoretic Delivery of Magnesium Ascorbyl 2-Phosphate and Sodium Fluorescein to Hairless and Hairy Mouse Skin

Kang¹,

Kim²,

Sung³

et al. 2012

JCDSA

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We recently reported that L-ascorbic acid 2-phosphate (AP) stimulates the growth of human dermal papilla (DP) cells, induces secretion of IGF-1 from the DP cells to promote hair shafts elongation in cultured human hair follicles, and triggers early progression from the telogen to anagen phase in mice. Since the magnesium salt of AP (APMg) is a highly hydrophilic ionic molecule, it is not easy to deliver this reagent to the skin or hair follicles by topical application alone. In order to enhance skin penetration of APMg without changing any molecular properties, a non-invasive iontophoretic delivery method was introduced. Iontophoresis of the negatively charged APMg under the electrode bearing same charge (cathode) significantly enhanced the in vitro penetration of APMg into a Franz cell equipped with mouse dorsal skin. In contrast, iontophoretic movement with the anode inhibited APMg penetration achieved with passive diffusion alone. The effect of iontophoresis on enhancing the penetration of APMg was also found to be much higher in the skin of hairy mice (3 -8 times) compared to hairless mice (1.5 -2.5 times). These findings indicated that iontophoretic movement induced the transfollicular pathway more strongly and effectively than the transdermal pathway. This phenomena was also demonstrated by the in vivo iontophoretic delivery of sodium fluorescein using hairy and hairless mice. The degree of iontophoretic enhancement during APMg penetration was also dependent on various conditions such as current density and application duration.

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“…1) is the most active water soluble antioxidant in many biological systems [11]. It exerts its properties by neutralizing toxic peroxides and by stabilizing free radicals, thus protecting lipids, proteins, and other bio-components from oxidative damage [12].…”

Section: Introductionmentioning

confidence: 99%

Selective determination of catechin, epicatechin and ascorbic acid in human urine using chiral capillary electrophoresis

El‐Hady¹,

Gotti

El‐Maali

2008

J of Separation Science

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Chiral CE was successfully applied to the separation and quantification of catechin, epicatechin and ascorbic acid in some commercial drinks and human urine. Analysis involved the separation of analytes in less than 5.0 min at 240 nm with an untreated fused-silica capillary under hydrodynamic injection mode. The running buffer consisted of 50 mM borate buffer with 3 mM beta-CD at pH 8.35. Detection limits for catechin, epicatechin and ascorbic acid were 0.028, 0.011 and 0.004 microg/mL, respectively. Linearity was investigated by selecting the ranges of calibration according to the amount of analytes in urine giving correlation coefficient percent (% r(2)) ranging between 99.4 and 99.6 at 99% confidence level. The maximum urinary excretion of catechin and epicatechin were noted at 2.0 and 4.0 h of the administrated dose. Unchanged catechin, epicatechin and ascorbic acid amounted to about 1.500, 8.696 and 0.003% of the administered dose in the 48.0 h urine collection. The proposed method achieved 99.2% completeness (n = 20) in urine media.

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Iontophoresis promotes percutaneous absorption of l-ascorbic acid in rat skin

Cited by 32 publications

References 15 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

Enhanced Iontophoretic Delivery of Magnesium Ascorbyl 2-Phosphate and Sodium Fluorescein to Hairless and Hairy Mouse Skin

Selective determination of catechin, epicatechin and ascorbic acid in human urine using chiral capillary electrophoresis

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