Enhancement effect of menthoxypropandiol and menthol on the penetration of indomethacin through Yucatan micropig skin in vitro.

Fujii, Makiko; Yamanouchi, Shizuka; Nagakura, Kazumi; Takeda, Yasuhiro; Maeda, Mitsuo

doi:10.2745/dds.12.127

Cited by 5 publications

(7 citation statements)

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“…MPD has also been used as a skin permeation enhancer for other therapeutic drugs. 119,120 MPD showed activation of the TRPM8 channel in MEK cells at an EC 50 of 6 μM. 97 Takasago also claimed similar cooling compounds, hydroxyethyl-menthyl ether (37, Coolact-5, FEMA 4154), and an analogue of MPD with an additional methyl group in the glycerine part of molecule 38 (FEMA 3849).…”

Section: ■ Menthol Inspired Synthetic Coolantsmentioning

confidence: 92%

“…While the cooling strength of 36 is accepted as being about 20–25% that of menthol, interestingly, in a vaseline ointment, 36 showed a cool feeling 2.0 to 2.5 times stronger than that of menthol. , MPD ( 36 ) is produced from a reaction between glycerine with l -menthol by ether conjugation, − resulting in MPD being more hydrophilic (log P 2.5) than l -menthol (log P 3.2). MPD has also been used as a skin permeation enhancer for other therapeutic drugs. , MPD showed activation of the TRPM8 channel in MEK cells at an EC 50 of 6 μM . Takasago also claimed similar cooling compounds, hydroxyethyl-menthyl ether ( 37 , Coolact-5, FEMA 4154), and an analogue of MPD with an additional methyl group in the glycerine part of molecule 38 (FEMA 3849) .…”

Section: Menthol Inspired Synthetic Coolantsmentioning

confidence: 99%

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Modulation of Thermoreceptor TRPM8 by Cooling Compounds

Bharate

2012

ACS Chem. Neurosci.

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ThermoTRPs, a subset of the Transient Receptor Potential (TRP) family of cation channels, have been implicated in sensing temperature. TRPM8 and TRPA1 are both activated by cooling. TRPM8 is activated by innocuous cooling (<30 °C) and contributes to sensing unpleasant cold stimuli or mediating the effects of cold analgesia and is a receptor for menthol and icilin (mint-derived and synthetic cooling compounds, respectively). TRPA1 (Ankyrin family) is activated by noxious cold (<17 °C), icilin, and a variety of pungent compounds. Extensive amount of medicinal chemistry efforts have been published mainly in the form of patent literature on various classes of cooling compounds by various pharmaceutical companies; however, no prior comprehensive review has been published. When expressed in heterologous expression systems, such as Xenopus oocytes or mammalian cell lines, TRPM8 mediated currents are activated by a number of cooling compounds in addition to menthol and icilin. These include synthetic p-menthane carboxamides along with other class of compounds such as aliphatic/alicyclic alcohols/esters/amides, sulphones/sulphoxides/sulphonamides, heterocyclics, keto-enamines/lactams, and phosphine oxides. In the present review, the medicinal chemistry of various cooling compounds as activators of thermoTRPM8 channel will be discussed according to their chemical classes. The potential of these compounds to emerge as therapeutic agents is also discussed.

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Section: ■ Menthol Inspired Synthetic Coolantsmentioning

confidence: 92%

Section: Menthol Inspired Synthetic Coolantsmentioning

confidence: 99%

Modulation of Thermoreceptor TRPM8 by Cooling Compounds

Bharate

2012

ACS Chem. Neurosci.

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“…2: T lag = L 2 /6D, where C D is the initial concentration of ALA in the donor compartment and L is the diffusion path length, that is, the thickness of YMP skin. According to the previous paper, 0.2 cm to L was assigned in this study [26] .…”

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confidence: 99%

Effect of Ethanol on Iontophoretic Transdermal Delivery of 5-Aminolevulinic Acid through Yucatan Micropig Full-thickness Skin

Asai¹,

Ochiai²,

Kawashima³

et al. 2019

pharmaceutical-sciences

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Asai et al.: Effect of Ethanol on Iontophoresis of ALAThe effect of ethanol was investigated on iontophoretic transdermal delivery of 5-aminolevulinic acid through Yucatan micropig full-thickness skin. When 20 % ethanol was added into an aqueous 5-aminolevulinic acid solution, the iontophoretic permeation of 5-aminolevulinic acid through Yucatan micropig full-thickness skin was enhanced. The addition of ethanol also enlarged the partition of 5-aminolevulinic acid into Yucatan micropig full-thickness skin, which gave rise to enhancement of 5-aminolevulinic acid permeation. This result suggested that the combination system of iontophoretic delivery and 20 % ethanol could be a promising approach for the promotion of 5-aminolevulinic acid skin permeation.

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“…4,5) However, there are fewer reports on the effect of commonly used oily vehicles for the treatment of skin diseases, such as white petrolatum (WP) or liquid paraffin (LP), on skin penetration of drugs.…”

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confidence: 99%

“…8), glycyrrhetinic acid (log P=5. 5), and tocopherol acetate ester (log P=10. 7), are used in clinical treatment of skin diseases.…”

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confidence: 99%

Influence of Characteristics of Oily Vehicle on Skin Penetration of Ufenamate

Iino

Fujii

Fujino

et al. 2017

Biological & Pharmaceutical Bulletin

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Skin penetration amounts of a highly lipophilic drug, ufenamate, prepared in four oily vehicles, including white petrolatum (WP), liquid paraffin (LP), isopropyl myristate (IPM), and isocetyl stearate (ICS), were compared. Ufenamate was mixed in each vehicle at 5% and applied at a rate of 2 mg/cm 2 to intact, stripped, and delipidized Yucatan micropig skin. The amounts of ufenamate and IPM in the stratum corneum (SC), epidermis, and dermis were determined. The skin penetration amounts of ufenamate from liquid oils were significantly higher than those from WP; the amounts of ufenamate were in the order WP

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Enhancement effect of menthoxypropandiol and menthol on the penetration of indomethacin through Yucatan micropig skin in vitro.

Cited by 5 publications

References 0 publications

Modulation of Thermoreceptor TRPM8 by Cooling Compounds

Modulation of Thermoreceptor TRPM8 by Cooling Compounds

Effect of Ethanol on Iontophoretic Transdermal Delivery of 5-Aminolevulinic Acid through Yucatan Micropig Full-thickness Skin

Influence of Characteristics of Oily Vehicle on Skin Penetration of Ufenamate

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