Physicochemical considerations in the iontophoretic delivery of a small peptide: in vitro studies using arginine vasopressin as a model peptide.

Abstract:

:Transdermal iontophoresis (TI) is a physical enhancement technique to facilitate the delivery of primarily charged molecules across the skin. TI of peptides is influenced by a complex interplay of several factors and one of the main issues in optimizing iontophoretic delivery of peptides is to improve the transport efficiency. From this perspective, this study investigates the effect of the physicochemical parameters on the TI of a peptide arginine vasopressin (AVP). The permeation of AVP showed a linear dependence on the concentration of drug in the donor medium. The iontophoretic flux of AVP was strongly influenced by the pH of the donor solution. Increasing the pH from 5.16 to 7.4 resulted in a decrease in the enhancement ratio by 4.5 times. When the ionic strength was increased by varying the amount of NaCl from 0.05 to 0.25 M the flux was found to decrease by 3.2 times. Replacing normal saline in the receptor compartment by HEPES buffer showed a resultant four times increase in drug permeation. The physiochemical parameters of the donor medium play a significant role in the efficiency of drug delivery by iontophoresis for a small peptide like AVP. Though electrorepulsion would be expected to be the main mechanism involved in the movement of charged molecules across the skin by iontophoresis, for peptides in the molecular weight range of AVP, other associated secondary effects like osmosis, electroosmosis and counter ion flow may also play a significant role in transport across the skin.

journal_name

Pharmacol Res

journal_title

Pharmacological research

authors

Nair V,Panchagnula R

doi

10.1016/s1043-6618(03)00080-x

keywords:

subject

Has Abstract

pub_date

2003-08-01 00:00:00

pages

175-82

issue

2

eissn

1043-6618

issn

1096-1186

pii

S104366180300080X

journal_volume

48

pub_type

杂志文章
  • Curcumin and allopurinol ameliorate fructose-induced hepatic inflammation in rats via miR-200a-mediated TXNIP/NLRP3 inflammasome inhibition.

    abstract::Excess fructose consumption causes high prevalence of metabolic syndrome and inflammatory liver diseases. The aim of the current study was to investigate the therapeutic effects and underlying molecular mechanisms of curcumin and allopurinol in high fructose-induced hepatic inflammation. Male Sprague-Dawley rats were ...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2018.09.021

    authors: Ding XQ,Wu WY,Jiao RQ,Gu TT,Xu Q,Pan Y,Kong LD

    更新日期:2018-11-01 00:00:00

  • Muscarinic M(2) receptors are not primarily involved in the contraction of guinea-pig gallbladder smooth muscle.

    abstract::The presence of M(1)-M(4) receptors in guinea-pig gallbladder smooth muscle cells has been reported recently. The majority of these receptors are said to be of M(2) subtype. However, there are controversial reports about the functional muscarinic receptors that mediate contraction in this tissue. Similar to gallbladde...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1006/phrs.1999.0536

    authors: Akici A,Karaalp A,Skender E,El-Fakahany EE,Oktay S

    更新日期:1999-11-01 00:00:00

  • Postmenopausal exogenous hormone therapy and Melanoma risk in women: A systematic review and time-response meta-analysis.

    abstract::A favourable option to management symptoms during menopausal transition is menopausal hormone therapy (MHT) but relation among MHT and risk of melanoma is controversial. This study aims to identify, analyse and present the evidence surrounding post-menopausal exogenous hormone therapy and the risk for melanoma in wome...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审

    doi:10.1016/j.phrs.2020.105182

    authors: Tang X,Zhang H,Cui Y,Wang L,Wang Z,Zhang Y,Huo J,Cai J,Rinaldi G,Bhagavathula AS,Xiaopeng Y

    更新日期:2020-10-01 00:00:00

  • Physiological and pathological roles of branched-chain amino acids in the regulation of protein and energy metabolism and neurological functions.

    abstract::Branched-chain amino acids (BCAAs: leucine, isoleucine, and valine) are essential amino acids for humans and play an important role as the building blocks of proteins. Recent studies have disclosed that free BCAAs in the tissue amino acid pool function not only as substrates for protein synthesis, but also as regulato...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审

    doi:10.1016/j.phrs.2018.05.014

    authors: Shimomura Y,Kitaura Y

    更新日期:2018-07-01 00:00:00

  • Co-administration of raltegravir reduces daily darunavir exposure in HIV-1 infected patients.

    abstract::The potential drug-to-drug interaction between darunavir and raltegravir in the setting of HIV infection is a highly debated issue still unresolved. In the present study we have evaluated the pharmacokinetics of darunavir and ritonavir in 53 HIV-1 infected patients with or without concomitant raltegravir administratio...

    journal_title:Pharmacological research

    pub_type: 临床试验,杂志文章

    doi:10.1016/j.phrs.2011.09.006

    authors: Cattaneo D,Gervasoni C,Cozzi V,Baldelli S,Fucile S,Meraviglia P,Landonio S,Boreggio G,Rizzardini G,Clementi E

    更新日期:2012-02-01 00:00:00

  • Differential in vivo and in vitro effect of gentamicin on glutamate synthesis and glutamate deamination in rabbit kidney-cortex tubules and mitochondria.

    abstract::The effect of gentamicin on both glutamate synthesis and glutamate deamination was studied in kidney-cortex mitochondria and tubules isolated from both control and gentamicin-treated animals. In kidney-cortex mitochondria which were permeabilized in order to make a free access of substrates and antibiotic to the gluta...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/1043-6618(92)90235-4

    authors: Bryła J,Lietz T,Jarzyna R,Michalik M,Pietkiewicz J

    更新日期:1992-12-01 00:00:00

  • Liu Shen capsule shows antiviral and anti-inflammatory abilities against novel coronavirus SARS-CoV-2 via suppression of NF-κB signaling pathway.

    abstract::Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) has spread worldwide through person-to-person contact, causing a public health emergency of international concern. At present, there is no specific antiviral treatment recommended for SARS-CoV-2 infection. Liu Shen capsule (LS), a traditional Chinese medicin...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2020.104850

    authors: Ma Q,Pan W,Li R,Liu B,Li C,Xie Y,Wang Z,Zhao J,Jiang H,Huang J,Shi Y,Dai J,Zheng K,Li X,Yang Z

    更新日期:2020-08-01 00:00:00

  • The novel anti-inflammatory agent VA694, endowed with both NO-releasing and COX2-selective inhibiting properties, exhibits NO-mediated positive effects on blood pressure, coronary flow and endothelium in an experimental model of hypertension and endotheli

    abstract::Selective cyclooxygenase 2 (COX2) inhibitors (COXIBs) are effective anti-inflammatory and analgesic drugs with improved gastrointestinal (GI) safety compared to nonselective nonsteroidal anti-inflammatory drugs known as traditional (tNSAIDs). However, their use is associated with a cardiovascular (CV) hazard (i.e. inc...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2013.09.008

    authors: Martelli A,Testai L,Anzini M,Cappelli A,Di Capua A,Biava M,Poce G,Consalvi S,Giordani A,Caselli G,Rovati L,Ghelardini C,Patrignani P,Sautebin L,Breschi MC,Calderone V

    更新日期:2013-12-01 00:00:00

  • Pediatric drug development in China: Reforms and challenges.

    abstract::In China, child and adolescent pediatricians often face challenges in treating children with the appropriate medications. Within the last 8 years, the Chinese government has already initiated a series of policies to promote development of age-appropriate medicines for children. In this study,we introduced the current ...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审

    doi:10.1016/j.phrs.2019.104412

    authors: Wu W,Tang Z,Chen J,Gao Y

    更新日期:2019-10-01 00:00:00

  • Loganin possesses neuroprotective properties, restores SMN protein and activates protein synthesis positive regulator Akt/mTOR in experimental models of spinal muscular atrophy.

    abstract::Spinal muscular atrophy (SMA) is an autosomal recessive neurodegenerative disease characterized by motor neurons degeneration and muscular atrophy. There is no effective SMA treatment. Loganin is a botanical candidate with anti-inflammatory, anti-oxidant, glucose-lowering and anti-diabetic nephropathy activities. The ...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2016.05.023

    authors: Tseng YT,Chen CS,Jong YJ,Chang FR,Lo YC

    更新日期:2016-09-01 00:00:00

  • Endothelin-1 (ET-1) and vein graft failure and the therapeutic potential of ET-1 receptor antagonists.

    abstract::Despite the exploration of a large number of disparate drugs in animal models and clinical trials, no pharmacological intervention, with the exception of aggressive lipid lowering therapy has reduced late vein graft failure in man. The importance of devising more effective strategies is exemplified by the enormous eco...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审

    doi:10.1016/j.phrs.2010.10.018

    authors: Jeremy JY,Shukla N,Angelini GD,Wan S

    更新日期:2011-06-01 00:00:00

  • CAR-T cells and combination therapies: What's next in the immunotherapy revolution?

    abstract::Cancer immunotherapies are dramatically reshaping the clinical management of oncologic patients. For many of these therapies, the guidelines for administration, monitoring, and management of associated toxicities are still being established. This is especially relevant for adoptively transferred, genetically-modified ...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2017.11.035

    authors: Ramello MC,Haura EB,Abate-Daga D

    更新日期:2018-03-01 00:00:00

  • Targeting SHP2 as a promising strategy for cancer immunotherapy.

    abstract::Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) is a major phosphatase involved in several cellular processes. In recent years, SHP2 has been the focus of significant attention in human diseases, particular in cancer. Several studies have shown that SHP2 plays an important role in regulating immune cel...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审

    doi:10.1016/j.phrs.2019.104595

    authors: Liu Q,Qu J,Zhao M,Xu Q,Sun Y

    更新日期:2020-02-01 00:00:00

  • Allosteric modulation of sigma receptors by BH3 mimetics ABT-737, ABT-263 (Navitoclax) and ABT-199 (Venetoclax).

    abstract::ABT-737, ABT-263 (Navitoclax) and ABT-199 (Venetoclax) are under intensive preclinical and clinical investigation as treatments for hematologic and other malignancies. These small molecules mimic pro-death B-cell lymphoma-2 (Bcl-2) Homology 3 (BH3) domain-only proteins. They also bear a structural resemblance to certa...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2019.01.040

    authors: Lever JR,Fergason-Cantrell EA

    更新日期:2019-04-01 00:00:00

  • Influence of profound hypothermia on the blood-brain barrier permeability during acute arterial hypertension.

    abstract::In hypothermic rats with acute hypertension induced by intravenous injection of adrenalin, regional changes in blood-brain barrier permeability to macromolecules were investigated using Evans blue as indication. Evans blue albumin extravasation was determined as a macroscopic finding and a quantitative estimation with...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:

    authors: Oztaş B,Kaya M,Camurcu S

    更新日期:1992-07-01 00:00:00

  • Antiplatelet and antithrombotic activities of essential oil from wild Ocotea quixos (Lam.) Kosterm. (Lauraceae) calices from Amazonian Ecuador.

    abstract::Ocotea quixos essential oil was shown to possess significant inhibitory activity of platelet aggregation and clot retraction in rodent plasma. This study is aimed at fully characterizing the antiplatelet activity of the whole essential oil and its main components trans-cinnamaldehyde and methyl cinnamate also in human...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2006.09.009

    authors: Ballabeni V,Tognolini M,Bertoni S,Bruni R,Guerrini A,Rueda GM,Barocelli E

    更新日期:2007-01-01 00:00:00

  • Stereoselective biotransformation of cicletanine in cultured rat and human hepatocytes.

    abstract::Cicletanine [(+/-)-C] is a racemic furopyridine derivative used as an antihypertensive agent. Pharmacokinetic and metabolic studies have shown that cicletanine is rapidly and almost fully metabolized into sulfo- and glucuro-conjugated metabolites. However, the stereoselective metabolism of cicletanine is not well-know...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1006/phrs.2000.0660

    authors: Menard C,Lamiable D,Vistelle R,Morin E,Ratanasavanh D

    更新日期:2000-07-01 00:00:00

  • Prescribing habits of general practitioners in choosing an empirical antibiotic regimen for lower respiratory tract infections in adults in Sicily.

    abstract::The survey was carried out, between September 1995 and May 1996, in order to describe the prescriptive behaviour among Sicilian general practitioners (GPs) in choosing an empirical antibiotic regimen for LRTIs in adult patients and begin an educational process which involves the same GPs in decisions regarding their p...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1006/phrs.1998.0484

    authors: Mazzaglia G,Arcoraci V,Greco S,Cucinotta G,Cazzola M,Caputi AP

    更新日期:1999-07-01 00:00:00

  • Inhibition of cell proliferation, cytotoxicity and induction of apoptosis of 1,4-bis(1-naphthyl)-2,3-dinitro-1,3-butadiene in gastrointestinal tumour cell lines and preliminary evaluation of its toxicity in vivo.

    abstract::Our preliminary data suggested that 1,4-bis(1-naphthyl)-2,3-dinitro-1,3-butadiene [Viale M, Ottone M, Chiavarina B, Mariggiò MA, Prevosto C, Dell'Erba C, et al. Preliminary evaluation in vitro of the inhibition of cell proliferation, cytotoxicity and induction of apoptosis by 1,4-bis(1-naphthyl)-2,3-dinitro-1,3-butadi...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2005.03.011

    authors: Dell'Erba C,Chiavarina B,Fenoglio C,Petrillo G,Cordazzo C,Boncompagni E,Spinelli D,Ognio E,Aiello C,Mariggiò MA,Viale M

    更新日期:2005-09-01 00:00:00

  • To fingolimod and beyond: The rich pipeline of drug candidates that target S1P signaling.

    abstract::Sphingosine 1-phosphate (S1P) is an extracellular lipid signaling molecule that acts as a selective, high-affinity ligand for a family of five G protein-coupled receptors. This signaling system was first identified twenty years ago, and has since been shown to regulate a diverse range of physiological processes and di...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审

    doi:10.1016/j.phrs.2016.09.025

    authors: Chew WS,Wang W,Herr DR

    更新日期:2016-11-01 00:00:00

  • The importance of regulating the education and training of Traditional Chinese Medicine practitioners and a potential role for ISO/TC 249.

    abstract::As Traditional Chinese Medicine (TCM) transcends its cultural boundaries and becomes widely used in many countries around the world, one of the major risks to the growing use of TCM internationally is the damage caused to its reputation and to community safety when TCM practitioners are not adequately trained. Ensurin...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2020.105217

    authors: Li J,Graham D

    更新日期:2020-11-01 00:00:00

  • Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system.

    abstract::Coronavirus Disease 2019 (COVID-19) caused by the emerging severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is associated with a crude case fatality rate of about 0.5-10 % depending on locality. A few clinically approved drugs, such as remdesivir, chloroquine, hydroxychloroquine, nafamostat, camostat, and ...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2020.104960

    authors: Yuan S,Chan JFW,Chik KKH,Chan CCY,Tsang JOL,Liang R,Cao J,Tang K,Chen LL,Wen K,Cai JP,Ye ZW,Lu G,Chu H,Jin DY,Yuen KY

    更新日期:2020-09-01 00:00:00

  • Role of thioredoxin-1 in ischemic preconditioning, postconditioning and aged ischemic hearts.

    abstract::Thioredoxin is one of the most important cellular antioxidant systems known to date, and is responsible of maintaining the reduced state of the intracellular space. Trx-1 is a small cytosolic protein whose transcription is induced by stress. Therefore it is possible that this antioxidant plays a protective role agains...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审

    doi:10.1016/j.phrs.2016.03.009

    authors: D'Annunzio V,Perez V,Boveris A,Gelpi RJ,Poderoso JJ

    更新日期:2016-07-01 00:00:00

  • Simvastatin improves the attenuated heart rate recovery of type 2 diabetics.

    abstract::Heart rate recovery at 1min (HRR1) is a strong predictor of all-cause mortality. The effects of statins on the autonomic nervous system may account for their beneficial effects in survival. Our aim was to determine if statin therapy improves heart rate recovery in hypercholesterolemic patients with type 2 diabetes mel...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2006.09.002

    authors: Tekin G,Tekin A,Canatar T,Sipahi I,Unsal A,Katircibaşi T,Koçum T,Erol T,Yiğit F,Demircan S,Ermiş N,Sezgin AT,Müderrisoğlu H

    更新日期:2006-12-01 00:00:00

  • The multiplicity of spinal AA-5-HT anti-nociceptive action in a rat model of neuropathic pain.

    abstract::There is considerable evidence to support the role of anandamide (AEA), an endogenous ligand of cannabinoid receptors, in neuropathic pain modulation. AEA also produces effects mediated by other biological targets, of which the transient receptor potential vanilloid type 1 (TRPV1) has been the most investigated. Both,...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2016.06.012

    authors: Malek N,Kostrzewa M,Makuch W,Pajak A,Kucharczyk M,Piscitelli F,Przewlocka B,Di Marzo V,Starowicz K

    更新日期:2016-09-01 00:00:00

  • Biochemical and hematological side effects of clofazimine in leprosy patients.

    abstract::Gastrointestinal toxicity and red skin discoloration were the major side effects observed in leprosy patients undergoing long-term treatment with clofazimine (CFZ). Hematological and biochemical alterations have been cited among other side effects; however, their real magnitude and clinical significance at the doses c...

    journal_title:Pharmacological research

    pub_type: 临床试验,杂志文章

    doi:10.1016/s1043-6618(02)00086-5

    authors: Costa Queiroz RH,de Souza AM,Sampaio SV,Melchior E Jr

    更新日期:2002-08-01 00:00:00

  • Mfsd2a-based pharmacological strategies for drug delivery across the blood-brain barrier.

    abstract::The blood-brain barrier (BBB) keeps the central nervous system (CNS) safe from various brain diseases, while the BBB makes it difficult for effective drugs to enter the CNS. Mfsd2a is specifically expressed on the cell membrane of brain-microvascular endothelial cell (BMEC) and is implicated in the delivery of some su...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2015.12.024

    authors: Wang JZ,Xiao N,Zhang YZ,Zhao CX,Guo XH,Lu LM

    更新日期:2016-02-01 00:00:00

  • Allergic contact dermatitis: From pathophysiology to development of new preventive strategies.

    abstract::As the body's first line of defense, the skin is the organ most frequently exposed to chemicals present in personal hygiene products, household products, or materials used in the work environment. In this context, skin disorders account for more than 40 % of all occupational and work-related diseases, constituting a s...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2020.105282

    authors: Brites GS,Ferreira I,Sebastião AI,Silva A,Carrascal M,Neves BM,Cruz MT

    更新日期:2020-12-01 00:00:00

  • Influence of a 3-day regimen of azithromycin on the disposition kinetics of cyclosporine A in stable renal transplant patients.

    abstract::Some macrolide antibiotics have been shown to produce significant drug-drug interactions through the inhibition of cytochrome P450 (CYP) enzymes. In renal transplant patients these interactions pose potentially serious problems for the safe administration of cyclosporine A (CSA), a substrate of CYP3A4. The effects of ...

    journal_title:Pharmacological research

    pub_type: 临床试验,杂志文章

    doi:10.1016/s1043-6618(03)00018-5

    authors: Bachmann K,Jauregui L,Chandra R,Thakker K

    更新日期:2003-06-01 00:00:00

  • Echinomycin and a novel analogue induce apoptosis of HT-29 cells via the activation of MAP kinases pathway.

    abstract::Echinomycin, in typical DNA minor groove binder, had comparable efficacy compared to 5-FU in the phase II trail of colon cancer treatment. To improve echinomycin's drawback (hydrophobicity, toxicity), we synthesized the YK-2000 series (echinomycin analogues). Among these, YK-2000 had the best in vitro cytotoxicity on ...

    journal_title:Pharmacological research

    pub_type: 杂志文章

    doi:10.1016/j.phrs.2004.01.005

    authors: Park JY,Park SJ,Shim KY,Lee KJ,Kim YB,Kim YH,Kim SK

    更新日期:2004-08-01 00:00:00