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Hatanaka, Tomomi; Manabe, Eiichiro; Sugibayashi, Kenji; Morimoto, Yasunori

doi:10.1023/a:1018911926190

Cited by 27 publications

(3 citation statements)

References 12 publications

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“…11,16,21,24,25 It should be kept in mind that there are obvious limitations in applying any manageable model to describe transport through a complex, heterogeneous membrane such as HEM. 11,16,21,24,25 It should be kept in mind that there are obvious limitations in applying any manageable model to describe transport through a complex, heterogeneous membrane such as HEM.…”

Section: Resultsmentioning

confidence: 99%

Quantitative Description of the Effect of Molecular Size upon Electroosmotic Flux Enhancement during Iontophoresis for a Synthetic Membrane and Human Epidermal Membrane

Peck

Srinivasan

et al. 1996

Journal of Pharmaceutical Sciences

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This study focused upon quantitatively determining the influence of permeant molecular size upon flux enhancement which results from electroosmosis. The first phase of the study involved validation of a fundamental model describing the molecular size dependence of flux enhancement which results from convective solvent flow. This was accomplished using a model synthetic membrane (stack of 50 Nuclepore membranes) and four model permeants with a molecular weight range of 60-504 (urea, mannitol, sucrose, and raffinose). The steady-state flux of each permeant was determined under passive conditions and applied voltages of 125, 250, 500, and 1000 mV using side-by-side diffusion cells and a four-electrode potentiostat system. On the basis of the permeability enhancement for each permeant at each applied voltage (relative to the passive permeability) it was possible to calculate the effective solvent flow velocity from each permeant at each field strength. An important finding was that the flux enhancement due to electroosmosis was strongly molecular weight dependent (i.e., the flux enhancement ratio was around 4 times greater for raffinose than for urea, with mannitol and sucrose yielding intermediate values), while the calculated effective flow velocity at each voltage was independent of the molecular weight of the permeant. This coupled with a linear correlation between flow velocity and applied voltage served to establish the validity of the method and model. The second phase of the study was an extension of the model to human epidermal membrane (HEM). These experiments involved simultaneously measuring the fluxes of [14C]urea and [3H]sucrose across HEM samples under passive, 250 mV, and 500 mV conditions. Similar to the Nuclepore system, the observed flux enhancement ratios with HEM were approximately 3 times greater for sucrose than for urea. A detailed analysis of the HEM data showed semiquantitative agreement between predictions of the model and experimental results.

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Section: Resultsmentioning

confidence: 99%

Quantitative Description of the Effect of Molecular Size upon Electroosmotic Flux Enhancement during Iontophoresis for a Synthetic Membrane and Human Epidermal Membrane

Peck

Srinivasan

et al. 1996

Journal of Pharmaceutical Sciences

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“…( n =3–4 independent samples). The osmotic concentration differential was adjusted to 3.08, 0, –3.08 mol/L by adding NaCl to donor or receiver compartments 15 .…”

Section: Methodsmentioning

confidence: 99%

Enhanced delivery of hydrophilic peptides in vitro by transdermal microneedle pretreatment

Zhang

Qiu

Gao

2014

Acta Pharmaceutica Sinica B

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The aims of this study were to investigate the utility of solid microneedle arrays (150 µm in length) in enhancing transdermal delivery of peptides and to examine the relationship between peptide permeation rates and D2O flux. Four model peptides were used (Gly–Gln–Pro–Arg [tetrapeptide-3, 456.6 Da], Val–Gly–Val–Ala–Pro–Gly [hexapeptide, 498.6 Da], AC–Glu–Glu–Met–Gln–Arg–Arg–NH2 [acetyl hexapeptide-3, 889 Da] and Cys–Tyr–Ile–Gln–Asn–Cys–Pro–Leu–Gly–NH2 [oxytocin, 1007.2 Da]). The influence of microneedle pretreatment on skin permeation was evaluated using porcine ear skin with Franze diffusion cell. Peptide permeation across the skin was significantly enhanced by microneedle pretreatment, and permeation rates were dependent on peptide molecular weights. A positive correlation between D2O flux and acetyl hexapeptide-3 clearances suggests that convective solvent flow contributes to the enhanced transdermal peptide delivery. It is concluded that solid microneedle arrays are effective devices to enhance skin delivery of peptides.

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“…It also showed that the enhancement of the skin permeability of a drug by EtOH at a low concentration was due to the action on skin lipids (34,35) and solvent drag effect (36)(37)(38). The former could be characterized as a rather "static effect" mainly governed by the integral amount of EtOH acting on the skin lipids.…”

Section: Resultsmentioning

confidence: 99%

The Enhancing Effect of Ion-pairing on the Skin Permeation of Glipizide

Tan

Zhang

et al. 2009

AAPS PharmSciTech

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The purpose of the present study was to investigate the permeation of glipizide (GP) and observe the effect of an interaction with amines as counter ions, including diethylamine, triethylamine, ethanolamine, diethanolamine, triethanolamine, N-(2-hydroxylethyl) piperidine. Permeation experiments were performed in vitro, using rat abdominal skin as a barrier. The lipophilic donor system consisting of isopropyl myristate (IPM) and ethanol (EtOH; EI system, 8:2) produced a marked enhancement of GP flux through rat skin. All the amines investigated in this study had performed an enhancing effect on GP flux, and triethylamine had the most potent enhancing effect on GP in the vehicle IPM:EtOH = 8:2(w/w). In the presence of counter ions, the solubility of GP in the donor solution (IPM:EtOH = 8:2) was increased and the log K (o/w) of GP was decreased, which may due to higher solubility of the GP in the IPM:EtOH = 8:2(w/w). (13)C NMR spectroscopy was used to identify the ion-pairing formation between GP and the respective counter ion. It was surprising that all the four enhancers examined, such as isopropyl myristate, propylene glycol, N-methyl-2-pyrrolidone, azone, and oleic acid, had no enhancing effect on the percutaneous permeation of GP. This study showed that the formation of ion-pairs between GP and counter ions is a useful method to promote the skin permeation of GP.

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Cited by 27 publications

References 12 publications

Quantitative Description of the Effect of Molecular Size upon Electroosmotic Flux Enhancement during Iontophoresis for a Synthetic Membrane and Human Epidermal Membrane

Quantitative Description of the Effect of Molecular Size upon Electroosmotic Flux Enhancement during Iontophoresis for a Synthetic Membrane and Human Epidermal Membrane

Enhanced delivery of hydrophilic peptides in vitro by transdermal microneedle pretreatment

The Enhancing Effect of Ion-pairing on the Skin Permeation of Glipizide

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