Papers - TODO Hiroaki
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Effect of ethanol pretreatment on skin permeation of drugs.
Horita Daisuke, Todo Hiroaki, Sugibayashi Kenji
Biol Pharm Bull 35 ( 8 ) 1343 - 1348 2012
Language：English Publishing type：Research paper (scientific journal)
It has been demonstrated that ethanol (EtOH) can enhance skin permeation of drugs when simultaneously applied with drugs. However, only a few studies have reported on the pretreatment effect of EtOH on skin permeations. In this study, the pretreatment effects of EtOH on skin permeation of drugs were investigated by measuring changes in skin permeation and electrical skin resistance. Permeabilities of deuterium oxide (D2O), isosorbide mononitrate (ISMN), isosorbide dinitrate (ISDN), calcein sodium (CA-Na), and fluorescein isothiocyanate-dextran 4 kDa (FD-4, 3.3-4.4 kDa) were evaluated through Yucatan micropig skin pretreated with different concentrations of EtOH solution. From the results, almost constant skin permeabilities of D2O and ISDN were observed independent of EtOH concentration. Skin permeabilities of ISMN, CA, and FD-4 increased with low concentrations of EtOH, but decreased with high concentrations of EtOH. At 99.5% EtOH pretreatment, skin permeabilities of hydrophilic compounds (ISMN, CA, and FD-4) decreased to non-detectable levels. In addition, low molecular ion transports were almost constant at any EtOH concentration. Since molecular (ion) sizes of ISMN, CA, and FD-4 are larger than Na+, Cl-, and D2O, permeation pathway sizes for hydrophilic compounds in the skin barrier may be remarkably decreased by pretreatment with high concentrations of EtOH. However, the permeability coefficient of ISDN was not influenced by any EtOH concentration, since ISDN is a lipophilic, low-molecular compound that permeated through the lipophilic stratum corneum pathway. The present results show useful information for repeatedly and topically applied formulations containing EtOH, and also contribute to the effective use of alcohol formulations.
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Pretreatment effects of moxibustion on the skin permeation and skin and muscle concentrations of salicylate in rats.
Cao Dianxiu, Tazawa Yuko, Ishii Hiroshi, Todo Hiroaki, Sugibayashi Kenji
Int J Pharm 407 ( 1-2 ) 105 - 110 2011.04
Language：English Publishing type：Research paper (scientific journal)
The effect of moxibustion on the in vitro and in vivo skin permeation of salicylate was evaluated in rats. First, the effect of moxibustion pretreatment on the elimination pharmacokinetics of salicylate after i.v. injection in rats was determined: no clear difference was observed in the plasma profiles of salicylate (SA) with or without moxibustion pretreatment. However, much higher skin and muscle concentrations of salicylate were observed after its i.v. injection. Next, an in vitro skin permeation study of SA was performed after moxibustion pretreatment. Moxibustion pretreatment increased the skin permeation of SA, and the extent of the increase in SA skin permeation was related to the strength of moxibustion ignition. More intense treatments produced higher skin permeation. A similar enhancement effect on the skin permeation of SA was observed in in vivo studies. Interestingly, the skin/plasma and muscle/plasma ratios of SA were markedly increased by moxibustion pretreatment. These results were due to the induction of enhanced skin permeation and lower clearance into the cutaneous vessels by moxibustion ignition. Combination treatment involving moxibustion and the topical application of drugs such as NSAID may be useful for increasing local pharmaceutical effects by enhancing the drug concentration in the skin and muscle underneath the topical application site.
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Iontophoresis-facilitated delivery of prednisolone through throat skin to the trachea after topical application of its succinate salt.
Ishii Hiroshi, Suzuki Tsukasa, Todo Hiroaki, Kamimura Mitsuhiro, Sugibayashi Kenji
Pharm Res 28 ( 4 ) 839 - 847 2011.04
Language：English Publishing type：Research paper (scientific journal)
PURPOSE: The possibility of direct delivery of steroids through the skin to the trachea and the effect of iontophoresis on delivery efficacy were evaluated after the application of an ionic steroidal prodrug, prednisolone sodium succinate (PS-Na), to the throat skin. METHODS: Fluorescein sodium salt (FL-Na) and PS-Na were applied as model compounds at a concentration of 1% in pH 7.4 phosphate-buffered saline to the throat skin of hairless rats, and constant current-cathodal iontophoresis (0.4 mA/cm(2)) was performed for 8 or 10 h. RESULTS: In vitro permeation experiment involving cathodal iontophoresis through excised hairless rat abdominal skin revealed 30- and 10-times higher levels of skin permeation of PS and its active drug, prednisolone (P), than those induced without iontophoresis. In vivo iontophoresis treatment of the rat's throat skin produced 2.6-, 1.6- and 12-times higher FL, PS and P concentrations, respectively, in the trachea than those observed without iontophoresis. CONCLUSION: The present results suggest the usefulness of topical application of the ionic steroidal prodrugs onto throat skin followed by iontophoresis treatment for directly delivering the steroid to the trachea.
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Preparation and evaluation of liquid-crystal formulations with skin-permeation-enhancing abilities for entrapped drugs.
Yamada Keisuke, Yamashita Jun, Todo Hiroaki, Miyamoto Keiko, Hashimoto Satoru, Tokudome Yoshihiro, Hashimoto Fumie, Sugibayashi Kenji
J Oleo Sci 60 ( 1 ) 31 - 40 2011
Language：English Publishing type：Research paper (scientific journal)
The usefulness of liquid crystals (LC) in topical formulations for application to skin was evaluated by measuring the in vitro permeation profile of a model compound, calcein, entrapped in a LC formulation, through excised hairless rat skin and a three-dimensional cultured human-skin model; the viability was determined using the MTT assay. Two physically stable LCs were prepared from a mixture of mono-, di-, and tri-esters 1, and monoesters 2, composed of erythritol and phytanylacetic acid. Cryo-transmission electron microscopy (cryo-TEM), electron diffraction patterns, and small-angle X-ray diffraction (SAXS) observations of the LC nanodispersions showed that the structures of the LCs were reverse hexagonal (LC-A) and cubic (LC-B). The skin-permeation properties of calcein were enhanced by entrapping in the LCs as a result of the increase in calcein partition from the LC dispersion solution into the skin; the properties were analyzed using a skin-permeation-time profile. Drug partitioning could also be modified by the LC structure. No skin damage was caused by the LC formulation in these experiments.The present study suggests that LC dispersions are potential additives in topical drug formulations and cosmetic formulations.
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Increase in ceramide level after application of various sizes of sphingomyelin liposomes to a cultured human skin model.
Tokudome Y, Jinno M, Todo H, Kon T, Sugibayashi K, Hashimoto F
Skin Pharmacol Physiol 24 ( 4 ) 218 - 223 2011
Language：English Publishing type：Research paper (scientific journal)
Sphingomyelin-based liposomes (SPM-L) that were sized (or not) by extrusion through a filter with pores of 100, 200, or 400 nm were applied to a three-dimensional cultured human skin model in order to evaluate which size of SPM-L was most effective at increasing its ceramide level. The diameters of the SPM-L in PBS were 102.7, 181.0, 224.0, and 380.1 nm. The diameters of the liposomes in the culture medium were 117.5, 199.2, 242.1, and 749.8 nm. The diameter of the small liposomes (<200 nm in diameter) did not change much, at least for 7 days. SPM-L in saline or culture medium were applied to the basal layer side or stratum corneum side of the cultured skin model, and ceramide II, III, V, and VI were then extracted from it. The extracted ceramide molecules were separated by HPTLC, and the concentration of each type of ceramide was quantified using a densitometer. When the small SPM-L (110 or 190 nm in diameter) were applied to the basal layer side, the levels of ceramide III and V were increased. When they were applied to the stratum corneum side, the levels of ceramide II, III, V, and VI were significantly increased compared to those of the PBS group, especially after the application of the small SPM-L (110 nm in diameter). Thus, the application of small SPM-L was useful for increasing the ceramide II, III, V, and VI levels of a cultured human skin model.
DOI： 10.1159/000324886
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Preparation and evaluation of liquid-crystal formulations with skin permeation-enhancing abilities for entrapped drug Reviewed
Keisuke Yamada, Jun Yamashita, Keiko Miyamoto, Satoru Hashimoto, Yoshihiro Tokudome, Fumie Hashimoto and Kenji Sugibayashi
Journal of Oleo Science 2010.12
Language：English Publishing type：Research paper (scientific journal)
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Utilization of reconstructed cultured human skin models as an alternative skin for permeation studies of chemical compounds Reviewed
Kano S, Todo H, Sugie K, Fujimoto H, Nakada K, Tokudome Y, Hashimoto F, Sugibayashi K
AATEX 15 ( 2 ) 2010.12
Language：English Publishing type：Research paper (scientific journal)
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Utilization of reconstructed cultured human skin models as an alternative skin for permeation studies of chemical compounds Reviewed
Kano S., Sugie K., Fujimoto H., Nakada K., Tokudome Y., Hashimoto F., Sugibayashi K.
AATEX 15 ( 2 ) 61 - 70 2010.12
Authorship：Second author Language：English Publishing type：Research paper (scientific journal)
Other Link： http://libir.josai.ac.jp/il/meta_pub/G0000284repository_JOS-13440411-15_2
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Macromolecular delivery into skin using hollow microneedles Reviewed
Wonglertnirant N., Opanasopit P., Ngawhirunpat T., Sugibayashi K
Biological & Pharmaceutical Bulletin 2010.12
Authorship：Second author Language：English Publishing type：Research paper (scientific journal)
Other Link： http://libir.josai.ac.jp/il/meta_pub/G0000284repository_JOS-bpb.33.1988
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Moisture enhancement of noisomes entrapped with mineral water in pig ear skin Reviewed
Manosroi A., Witkittilak W., Chutoprapat R., Sugibayashi K., Manosroi W., Manosroi J.
Chiang Mai J. Sci. 2010.10
Language：English Publishing type：Research paper (scientific journal)
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Transdermal drug delivery by in-skin electroporation using a microneedle array Reviewed
Keshu Yan, Hiroaki Todo, Kenji Sugibayashi
International Journal of Pharmaceutics 397 ( 1-2 ) 77 - 83 2010.09
Authorship：Second author Language：English Publishing type：Research paper (scientific journal)
Other Link： http://libir.josai.ac.jp/il/meta_pub/G0000284repository_JOS-j.ijpharm.2010.06.052
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Permeation pathway of macromolecules and nanospheres through skin Reviewed
Kimura E., Yasuno H., Tokudome Y., Hashimoto F., Ikarashi Y., Sugibayashi K.
Biol. Pharm. Bull. 2010.09
Authorship：Lead author Language：English Publishing type：Research paper (scientific journal)
Other Link： http://libir.josai.ac.jp/il/meta_pub/G0000284repository_JOS-bpb.33.1394
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Effect of negative charged particles on the recovery of skin barrier function after EP treatment Reviewed
K. Sugibayashi, H. Todo, K. Yamaguchi
Journal of Drug Delivery Science and Technology 20 ( 6 ) 2010.04
Language：English Publishing type：Research paper (scientific journal)
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Macromolecular delivery into skin using a hollow microneedle Reviewed
Nanthida Wonglertnirant, Hiroaki Todo, Praneet Opanasopit, Tanasait Ngawhirunpat, Kenji Sugibayashi
Biological and Pharmaceutical Bulletin 33 ( 12 ) 2010.04
Language：English Publishing type：Research paper (scientific journal)
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Effect of thermodynamic activity on skin permeation and skin concentration of triamcinolone acetonide Reviewed
Hiroshi Ishii, Hiroaki Todo, Kenji Sugibayashi
Chemical and Pharmaceutical Bulletin 58 ( 4 ) 2010.04
Language：English Publishing type：Research paper (scientific journal)
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Effect of sebum and ointment rubbing on the skin permeation of triamcinolone acetonide from white petrolatum ointment Reviewed
Ishii H., Todo H., Sugibayashi K.
Biol. Pharm. Bull. 2010.04
Language：English Publishing type：Research paper (scientific journal)
Other Link： http://libir.josai.ac.jp/il/meta_pub/G0000284repository_JOS-bpb.33.876
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Mathematical model to predict skin concentration of drugs: Toward utilization of silicone membrane to predict skin concentration of drugs as an animal testing alternative, Reviewed
Sugibayashi K., Todo H., Oshizaka T., Owada Y.
Pharm. Res. 2010.04
Authorship：Second author Language：English Publishing type：Research paper (scientific journal)
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静脈内および経口投与後のディオスゲニンのラットにおける体内動態 Reviewed
大川原正喜、徳留嘉寛、藤堂浩明、杉林堅次、橋本フミ惠
薬剤学 2010.04
Language：Japanese Publishing type：Research paper (scientific journal)
Other Link： http://libir.josai.ac.jp/il/meta_pub/G0000284repository_JOS-03727629-70_82
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Possibility and effectiveness of drug delivery to skin by needle-free injector Reviewed
Inoue N., Iidaka D., Tokudome Y., Hashimoto F., Kishino T., Sugibayashi K.
Int. J. Pharm. 391 2010.03
Authorship：Second author Language：English Publishing type：Research paper (scientific journal)
Other Link： http://libir.josai.ac.jp/il/meta_pub/G0000284repository_JOS-j.ijpharm.2010.02.019
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Effect of topically applied sphingomyelin-based liposomes on the ceramide level in a three dimensional cultured human skin model Reviewed
Tokudome Y, Uchida, Yokote T., Todo H., Hada N., Kon T., Yasuda J., Hayashi H., Hashimoto F., Sugibayashi K.
J. Liposome Res 20 ( 1 ) 49 - 54 2010.03
Language：English Publishing type：Research paper (scientific journal)
Other Link： http://libir.josai.ac.jp/il/meta_pub/G0000284repository_JOS-08982100903062597