Effect of skin surface lipid on the skin permeation of lidocaine from pressure sensitive adhesives.

Abstract:

:Pressure sensitive adhesives (PSA) tapes containing different concentrations of lidocaine were prepared by a general casting method using styrene-isoprene-styrene block copolymer, and the in vitro skin permeation of lidocaine from each tape was evaluated using diffusion cell and excised hairless rat skin. The skin permeation was proportionally increased by up to 40% lidocaine in the PSA tape and did not change after this concentration. Although the bending point of the steady-state flux via skin concentration curve was found at 40%, saturated concentration or solubility of lidocaine in the tape was estimated to be about 20% by differential scanning calorimetry (DSC) measurement. In addition, the steady-state flux of lidocaine through skin from water or silicone fluid suspension (92 or 120 micrograms/cm2.h, respectively) was very similar to those of 40, 50 and 60% tapes (105, 101 and 112 micrograms/cm2.h, respectively). Decrease in the concentration in tapes during the permeation experiment explained only part of these phenomena. To analyze them further, the drug free PSA tape with or without (control) skin surface lipid was affixed to 50% lidocaine PSA tape for 48 h, and the amount of lidocaine crystal in the layered tapes was measured by DSC. The amount was found to be lower in the lipid-containing tape than in the lipid-free tape, suggesting that skin surface lipid can dissolve lidocaine crystal or solid in PSA tape to decrease its thermodynamic activity. Thus it is important to follow the concentration and thermodynamic activity of lidocaine in PSA tape, skin and the interface between the two layers to exactly assess its skin permeation flux.

journal_name

Biol Pharm Bull

authors

Cheng YH,Hosoya O,Sugibayashi K,Morimoto Y

doi

10.1248/bpb.17.1640

subject

Has Abstract

pub_date

1994-12-01 00:00:00

pages

1640-4

issue

12

eissn

0918-6158

issn

1347-5215

journal_volume

17

pub_type

杂志文章
  • Neuroprotective effect of kaempferol against a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced mouse model of Parkinson's disease.

    abstract::In the present study, we investigated the neuroprotective effects of kaempferol in the mouse model of Parkinson's disease, which was induced by neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). We confirmed that MPTP led to behavioral deficits, depletion of dopamine and its metabolites, reduction in supe...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.34.1291

    authors: Li S,Pu XP

    更新日期:2011-01-01 00:00:00

  • Auxins affected ginsenoside production and growth of hairy roots in Panax hybrid.

    abstract::Hairy roots of interspecific hybrid ginseng (Panax ginseng x P. quinquefolium), induced by Agrobacterium rhizogenes ATCC 15834, grew well in B5 liquid media supplemented with 2.5 microM auxins (3-indole butyric acid (IBA), 1-naphtaleneacetic acid (NAA) and 3-indoleacetic acid (IAA)). The hairy roots cultured in B5 liq...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.27.657

    authors: Washida D,Shimomura K,Takido M,Kitanaka S

    更新日期:2004-05-01 00:00:00

  • Mechanisms Underlying Enhanced Noradrenaline-Induced Femoral Arterial Contractions of Spontaneously Hypertensive Rats: Involvement of Endothelium-Derived Factors and Cyclooxygenase-Derived Prostanoids.

    abstract::We investigated the relationship between noradrenaline (NAd)-induced contractions, endothelial function, and hypertension in femoral arteries isolated from spontaneously hypertensive rats (SHR). In the femoral arteries of SHR, vs. age-matched control Wistar Kyoto (WKY) rats, contractions induced by NAd were increased....

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.b15-00821

    authors: Matsumoto T,Watanabe S,Iguchi M,Ando M,Oda M,Nagata M,Yamada K,Taguchi K,Kobayashi T

    更新日期:2016-01-01 00:00:00

  • Thyroxine binding properties of glycosylated human serum albumin as measured by fluorescence.

    abstract::Thyroid hormone, thyroxine (T4) binding to glycosylated human serum albumin (G-HSA), and native human serum albumin (HSA) were studied as a function of pH using the fluorescence method. T4 binding affinity for G-HSA was remarkably reduced in an alkaline pH as compared with the native HSA. The thermodynamic parameters ...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.18.154

    authors: Okabe N,Yoshida S

    更新日期:1995-01-01 00:00:00

  • Renin inhibition improves ovariectomy-induced osteoporosis of lumbar vertebra in mice.

    abstract::The skeletal renin–angiotensin system (RAS) is involved in the progression of osteoporosis and the active peptide within the RAS, angiotensin II (ANG II), has deleterious effects on bones. This study was performed to investigate whether suppression of the rate-limiting step of the RAS cascade by the renin inhibitor al...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.b14-00576

    authors: Zhang FY,Yang FJ,Yang JL,Wang L,Zhang Y

    更新日期:2014-01-01 00:00:00

  • Inhibition of itch-scratch response by fruits of Cnidium monnieri in mice.

    abstract::We previously screened the anti-itching activities of 33 herbal medicines in substance P (SP)-induced itching model mice. One of the most potent antipruritogenic extracts, the methanol extract of fruits of Cnidium monnieri (Cnidii Fructus) was studied further. The chloroform-soluble fraction of the methanol extract ma...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.24.1012

    authors: Basnet P,Yasuda I,Kumagai N,Tohda C,Nojima H,Kuraishi Y,Komatsu K

    更新日期:2001-09-01 00:00:00

  • Measurement of sialic acid content is insufficient to assess bioactivity of recombinant human erythropoietin.

    abstract::Assessment of biological potency and its comparison with clinical effects are important in the quality control of therapeutic glycoproteins. Animal models are usually used for evaluating bioactivity of these compounds. However, alternative methods are required to simplify the bioassay and avoid ethical issues associat...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.33.1596

    authors: Yanagihara S,Taniguchi Y,Hosono M,Yoshioka E,Ishikawa R,Shimada Y,Kadoya T,Kutsukake K

    更新日期:2010-01-01 00:00:00

  • FR901724, a novel anti-human immunodeficiency virus (HIV) peptide produced by Streptomyces, shows synergistic antiviral activities with HIV protease inhibitor and 2',3'-dideoxynucleosides.

    abstract::A novel tricyclic 21-amino-acid peptide, FR901724, was isolated from the cultured broth of Streptomyces sp. No. 73264. This peptide appears to possess potent anti-human immunodeficiency virus (HIV) activity in vitro and might represent a lead to a new class of anti-HIV agents; it qualifies as an HIV-cell fusion inhibi...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.19.405

    authors: Nakashima H,Ichiyama K,Inazawa K,Ito M,Hayashi H,Nishihara Y,Tsujii E,Kino T

    更新日期:1996-03-01 00:00:00

  • Induction of CD4+ regulatory T cells by TPA in mice: contra-suppression by CD8+ T cells.

    abstract::Among the eight inbred mouse strains employed in our preceding report, 12-O-tetradecanoylphorbol 13-acetate (TPA) painting alone induced CD4+ regulatory T (Tr) cells in four strains (e.g., C3H/He) at 6-8 weeks of age, but not in the remaining strains (e.g., C57BL/6, BALB/c). In the present study, the effect of growth ...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.25.172

    authors: Negoro T,Satoh K,Iinuma F,Tobe T,Watanabe M

    更新日期:2002-02-01 00:00:00

  • In vivo hair growth-promoting effect of rice bran extract prepared by supercritical carbon dioxide fluid.

    abstract::The potential hair growth-promoting activity of rice bran supercritical CO2 extract (RB-SCE) and major components of RB-SCE, linoleic acid, policosanol, γ-oryzanol, and γ-tocotrienol, were evaluated with the histological morphology and mRNA expression levels of cell growth factors using real-time reverse transcriptase...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.b13-00528

    authors: Choi JS,Jeon MH,Moon WS,Moon JN,Cheon EJ,Kim JW,Jung SK,Ji YH,Son SW,Kim MR

    更新日期:2014-01-01 00:00:00

  • Relaxin Ameliorates Renal Fibrosis and Expression of Endothelial Cell Transition Markers in Rats of Isoproterenol-Induced Heart Failure.

    abstract::There may be cardio-renal interactions in rats of isoproterenol-induced heart failure, which may be associated with renal fibrosis and endothelial-to-mesenchymal transition (EndMT). Since its discovery, relaxin (RLX) which was regarded as a reproductive hormone for a long time, is recently considered an effective anti...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.b16-00882

    authors: Zheng G,Cai J,Chen X,Chen L,Ge W,Zhou X,Zhou H

    更新日期:2017-01-01 00:00:00

  • Proportionality of protease activities in malignant cells to their metastatic potentials.

    abstract::It has been suggested that the activities of type IV collagenase and/or ectopeptidases possessed by malignant cells are related to their metastatic potentials. In the present study, we examined the activities of three aminopeptidases, two serine proteases, as well as type IV collagenase, in three kinds of cell lines o...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.17.1118

    authors: Funahashi T,Shimamura M,Kocha T,Fukuda T,Aoyagi T

    更新日期:1994-08-01 00:00:00

  • Essential and Non-essential Elements in Scalp Hair of Diabetics: Correlations with Glycated Hemoglobin (HbA1c).

    abstract::Essential elements (Ca, Mg, Zn, Cu, Fe, Cr, Mn and V) and non-essential elements (As, Cd, Hg and Pb) were measured in scalp hair samples of 45 diabetic subjects and 59 control subjects in Japan using inductively coupled plasma mass spectrometry. All diabetic subjects took insulin and/or antidiabetic agents, with glyca...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.b18-00029

    authors: Hotta Y,Fujino R,Kimura O,Endo T

    更新日期:2018-01-01 00:00:00

  • Inhibition of cyclooxygenase-2 expression by diarylheptanoids from the bark of Alnus hirsuta var. sibirica.

    abstract::Two known diarylheptanoids, oregonin (1), (5S)-1,7-bis-(3,4-dihydroxyphenyl)-heptane-3-one-5-O-beta-D-xylopyranosi de and hirsutanonol (2), (5S)-1,7-bis-(3,4-dihydroxyphenyl)-5-hydroxyheptane-3-one isolated from the bark of Alnus hirsuta var. sibirica, showed significant inhibitory effects on 12-O-tetradecanoylphorbol...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.23.517

    authors: Lee MW,Kim JH,Jeong DW,Ahn KH,Toh SH,Surh YJ

    更新日期:2000-04-01 00:00:00

  • Gene expression of CCAAT/enhancer-binding protein delta mediated by autoregulation is repressed by related gene family proteins.

    abstract::CCAAT/enhancer-binding protein delta (C/EBPdelta) transcription factor is rapidly induced at an early stage of acute phase response. We previously reported that this induction was mainly mediated by acute phase response factor/signal transducers and activators of transcription 3 (APRF/STAT3). Furthermore, the high exp...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.23.1424

    authors: Tanabe A,Kumahara C,Osada S,Nishihara T,Imagawa M

    更新日期:2000-12-01 00:00:00

  • Intracellular lectins involved in folding and transport in the endoplasmic reticulum.

    abstract::Glycosylation is a highly sophisticated post-translational modification of proteins that occurs in the endoplasmic reticulum (ER) and the Golgi apparatus. The vital biological functions served by protein glycosylation can be separated into two types. The first is the role of glycosylation in the extracellular environm...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.32.767

    authors: Yamamoto K

    更新日期:2009-05-01 00:00:00

  • In Vitro Inhibitory Effects of Sesamin on CYP4F2 Activity.

    abstract::Sesamin is a major lignan in sesame seeds, and a recent meta-analysis of controlled trials indicated that sesamin intake decreases blood pressure. The antihypertensive effect of sesamin has been suggested to be due to sesamin-mediated suppression of 20-hydroxyeicosatetraenoic acid production catalyzed by CYP4F2. Howev...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.b19-00953

    authors: Watanabe H,Yamaori S,Kamijo S,Aikawa K,Ohmori S

    更新日期:2020-01-01 00:00:00

  • A metabolic phenotyping approach to characterize the effects of cantonese herbal tea on restraint stressed rats.

    abstract::Restraint stressed rats were used as a model of Shanghuo and a global metabolic investigation of the effects of cantonese herbal tea (CHT) on the model rats was then performed by gas chromatography-mass spectrometry (GC/MS) metabonomics in an attempt to characterize the metabolic changes underlying such stress and any...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.b14-00203

    authors: You R,Pang Q,Li L

    更新日期:2014-01-01 00:00:00

  • Long term administration of Hypericum perforatum improves spatial learning and memory in the water maze.

    abstract::The aim of the present study is to investigate the effects of long-term Hypericum perforatum treatment on spatial learning and memory in rats. Hypericum preparation (HP) standardized to 0.3% hypericin content was administered orally for 9 weeks in doses of 4.3 and 13 microg/kg corresponding to therapeutic dosages in h...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.25.1289

    authors: Widy-Tyszkiewicz E,Piechal A,Joniec I,Blecharz-Klin K

    更新日期:2002-10-01 00:00:00

  • Probing AKR1C30 and AKR1C31 with site-directed mutagenesis: identifying the roles of residues 54 and 56 in the binding of substrates and inhibitors.

    abstract::Five rabbit aldo-keto reductases (AKRs) that participate in the reduction of drug ketones and endogenous ketosteroids have recently been cloned and characterized. Among them, AKR1C30 and AKR1C31 show the highest amino acid sequence identity of 91%, but markedly differ in their substrate specificity and inhibitor sensi...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.b14-00555

    authors: Endo S,Arai Y,Matsunaga T,Ikari A,El-Kabbani O,Hara A,Kitade Y

    更新日期:2014-01-01 00:00:00

  • An alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonist and an N-methyl-D-aspartate (NMDA) channel blocker synergistically impair spatial memory in rats.

    abstract::The interaction of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonist YM90K with the competitive N-methyl-D-aspartate (NMDA) antagonist CGS19755 or with the NMDA channel blocker MK801 on the spatial memory of rats was examined by the 4-arm-baited radial maze task. When administered alone, t...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.21.1228

    authors: Li H,Matsumoto K,Watanabe H

    更新日期:1998-11-01 00:00:00

  • Rho kinase inhibition by fasudil has anti-inflammatory effects in hypercholesterolemic rats.

    abstract::Inhibition of Rho kinase (ROCK) ameliorates many cardiovascular dysfunctions. The aim of the current study is to investigate the anti-inflammatory effects of fasudil, a selective ROCK inhibitor, on high cholesterol diet-induced hypercholesterolemic rats and its possible mechanisms. In hypercholesterolemic rats, we fou...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.34.1684

    authors: Ma Z,Zhang J,Du R,Ji E,Chu L

    更新日期:2011-01-01 00:00:00

  • Anthracyclines, small-molecule inhibitors of hypoxia-inducible factor-1 alpha activation.

    abstract::Hypoxia-inducible factor-1 (HIF-1) is a central mediator of cellular responses to low oxygen and has recently become an important therapeutic target for solid tumor therapy. To identify small molecule inhibitors of the HIF-1 transcriptional activation, we have established a high through-put assay system using a stable...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.29.1999

    authors: Yamazaki Y,Hasebe Y,Egawa K,Nose K,Kunimoto S,Ikeda D

    更新日期:2006-10-01 00:00:00

  • Identification of in vitro metabolites of 2,4,6,2',4',6'-hexachlorobiphenyl from phenobarbital-treated dog liver microsomes.

    abstract::We studied in vitro metabolites of 2,4,6,2',4',6'-hexachlorobiphenyl (HCB, IUPAC PCB No. 155) produced by liver microsomes of a phenobarbital (PB)-treated beagle dog. The major metabolites were 3-hydroxy-2,4,6,2',4',6'-HCB (M-1), 4-hydroxy-2,6,2',4',6'-pentachlorobiphenyl (PenCB, M-2) and 3,4-dihydroxy-2,6,2',4',6'-Pe...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.16.852

    authors: Ariyoshi N,Yoshimura H,Oguri K

    更新日期:1993-09-01 00:00:00

  • Protective effects of berberine on doxorubicin-induced hepatotoxicity in mice.

    abstract::Doxorubicin, a very potent and often used anti-cancer drug, is largely limited due to the dose-related toxic effects. The present study investigated whether berberine, a natural product alkaloid, can reduce the liver injury induced by doxorubicin. Mice of either gender were randomly divided into four groups: the contr...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.35.796

    authors: Zhao X,Zhang J,Tong N,Chen Y,Luo Y

    更新日期:2012-01-01 00:00:00

  • Enhanced expression of membrane-associated sialidase Neu3 decreases GD3 and increases GM3 on the surface of Jurkat cells during etoposide-induced apoptosis.

    abstract::We previously reported that, in Jurkat human T cells, the topoisomerase II inhibitor etoposide enhances sialidase activity and reduces cell surface sialic acid levels at an early stage of apoptosis and that the decreases in sialic acid are suppressed by the sialidase inhibitor 2,3-dehydro-2-deoxy-N-acetylneuraminic ac...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.30.1680

    authors: Azuma Y,Sato H,Higai K,Matsumoto K

    更新日期:2007-09-01 00:00:00

  • Targeting the extracellular signal-regulated kinase pathway in cancer therapy.

    abstract::The extracellular signal-regulated kinase (ERK) pathway is a major determinant in the control of diverse cellular processes such as proliferation, survival, and motility. This pathway is often upregulated in human cancers and as such represents an attractive target for mechanism-based approaches to cancer treatment. H...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章,评审

    doi:10.1248/bpb.34.1781

    authors: Kohno M,Tanimura S,Ozaki K

    更新日期:2011-01-01 00:00:00

  • Reaction of malondialdehyde (MDA) with alpha-N-acetylhistidine in the presence of alkanal.

    abstract::The reaction of malondialdehyde (MDA) with alpha-N-acetyl-histidine (Ac-His) in the presence of alkanal was investigated. MDA alone did not react with Ac-His but when alkanal was present, a reaction took place. A similar result was obtained for the reaction of MDA with imidazole in the presence of alkanal. In addition...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.17.554

    authors: Ohya T

    更新日期:1994-04-01 00:00:00

  • Characterization of an apoptosis-inducing factor in Habu snake venom as a glycyrrhizin (GL)-binding protein potently inhibited by GL in vitro.

    abstract::By means of successive heparin-affinity and glycyrrhizin (GL)-affinity column chromatographies (HPLC), a 55 kDa GL-binding protein (gp55) was purified to apparent homogeneity from the Superdex P-I fraction of Habu snake venom. This gp55 was identified as an apoxin I-like protein, because (i) its 20 N-terminal amino ac...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.21.924

    authors: Abe Y,Shimoyama Y,Munakata H,Ito J,Nagata N,Ohtsuki K

    更新日期:1998-09-01 00:00:00

  • Screening of antibiotics that interact with organic anion-transporting polypeptides 1B1 and 1B3 using fluorescent probes.

    abstract::Hepatic organic anion transporters OATP1B1 and OATP1B3 are expressed at the sinusoidal membrane of hepatocytes and contribute to the hepatic uptake of a wide variety of clinically used drugs. To identify the antibiotics that interact with the human organic anion transporters OATP1B1 and OATP1B3, we applied a screening...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/bpb.34.389

    authors: Yamaguchi H,Takeuchi T,Okada M,Kobayashi M,Unno M,Abe T,Goto J,Hishinuma T,Shimada M,Mano N

    更新日期:2011-01-01 00:00:00