Influence of monocaprin on the permeability of a diacidic drug BTA-243 across Caco-2 cell monolayers and everted gut sacs.

Abstract:

:This study explores the potential of the monoglyceride monocaprin as an enhancer of the epithelial permeability of the beta(3)-adrenoceptor agonist BTA-243, as an approach to improving the bioavailability of this drug. The permeabilities of BTA-243 and mannitol (paracellular marker) in Caco-2 cell monolayer and everted gut sac models in aqueous buffer (pH 6.8) in the presence of 1.3 and 2.0 mM monocaprin were compared with control (monocaprin-free) solutions over a period of 1 h. The transepithelial electrical resistance (TEER) of the Caco-2 cell monolayers was measured at regular time intervals throughout the experiment and after a recovery period of 30 h. Toxicological damage to the biological models associated with exposure to monocaprin was assessed by scanning electron microscopy and by the measurement of lactate dehydrogenase (LDH) release from everted gut sacs. The permeability of BTA-243 in epithelial monolayers was enhanced in the presence of 1.3 and 2.0 mM monocaprin. Measurements of TEER and mannitol permeability showed partial recovery of barrier properties after a 30 h period following exposure to 1.3 mM monocaprin. No structural damage was evident in these monolayers. Enhancement of Caco-2 permeability to BTA-243 by 2.0 mM monocaprin was significantly greater than by 1.3 mM but was irreversible; monolayers failed to recover their barrier properties after 30 h and changes in their gross morphology were observed. The mucosal to serosal transfer of BTA-243 in everted gut sac was enhanced but to a lesser extent than in the Caco-2 model. LDH release from everted gut sacs exposed to monocaprin was significantly less than that after exposure to Triton X-100, a nonionic surfactant known to cause membrane disruption.

journal_name

Int J Pharm

authors

Brown JR,Collett JH,Attwood D,Ley RW,Sims EE

doi

10.1016/s0378-5173(02)00343-5

keywords:

subject

Has Abstract

pub_date

2002-10-01 00:00:00

pages

133-42

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378517302003435

journal_volume

245

pub_type

杂志文章
  • 3D printed medicines: A new branch of digital healthcare.

    abstract::Three-dimensional printing (3DP) is a highly disruptive technology with the potential to change the way pharmaceuticals are designed, prescribed and produced. Owing to its low cost, diversity, portability and simplicity, fused deposition modeling (FDM) is well suited to a multitude of pharmaceutical applications in di...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2018.07.024

    authors: Awad A,Trenfield SJ,Gaisford S,Basit AW

    更新日期:2018-09-05 00:00:00

  • Impact of blend properties on die filling during tableting.

    abstract::Based on characterization of a wide range of fillers and APIs, thirty divergent blends were composed and subsequently compressed on a rotary tablet press, varying paddle speed and turret speed. The tablet weight variability was determined of 20 grab samples consisting of each 20 tablets. Additionally, the bulk residen...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2018.08.015

    authors: Van Snick B,Grymonpré W,Dhondt J,Pandelaere K,Di Pretoro G,Remon JP,De Beer T,Vervaet C,Vanhoorne V

    更新日期:2018-10-05 00:00:00

  • In vitro and in vivo evaluation of mucoadhesive microspheres consisting of dextran derivatives and cellulose acetate butyrate.

    abstract::The objective of this study was to evaluate mucoadhesive properties and gastrointestinal transit of microspheres made of oppositely charged dextran derivatives and cellulose acetate butyrate (CAB). The microspheres were prepared by emulsion solvent evaporation method. A reference microsphere was made of lactose instea...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(03)00159-5

    authors: Miyazaki Y,Ogihara K,Yakou S,Nagai T,Takayama K

    更新日期:2003-06-04 00:00:00

  • Mucoadhesivity and release properties of quaternary ammonium-chitosan conjugates and their nanoparticulate supramolecular aggregates: an NMR investigation.

    abstract::Selective relaxation rate measurements effectively proved the affinity of dexamethasone 21-phosphate disodium salt for quaternary ammonium-chitosan conjugates, their thiolated derivatives and the corresponding nanostructured aggregates. Affinity was also probed by dynamic dialysis. The release profile of dexamethasone...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.12.018

    authors: Uccello-Barretta G,Balzano F,Aiello F,Senatore A,Fabiano A,Zambito Y

    更新日期:2014-01-30 00:00:00

  • Nanoparticles based on natural, engineered or synthetic proteins and polypeptides for drug delivery applications.

    abstract::Medicine formulations at the nanoscale, referred to as nanomedicines, have managed to overcome key challenges encountered during the development of new medical treatments and entered clinical practice, but considerable improvement in terms of local efficacy and reduced toxicity still need to be achieved. Currently, th...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119537

    authors: Georgilis E,Abdelghani M,Pille J,Aydinlioglu E,van Hest JCM,Lecommandoux S,Garanger E

    更新日期:2020-08-30 00:00:00

  • Determination of ornidazole in pharmaceutical dosage forms based on reduction at an activated glassy carbon electrode.

    abstract::The electrochemical reduction of ornidazole was studied at a glassy carbon electrode activated by applying a new pretreatment. The dependence of intensities of currents and potentials on pH, concentration, scan rate, nature of the solvent (aqueous media, mixed aqueous-organic systems) and surfactant was investigated. ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(97)00208-1

    authors: Özkan SA,Senturk Z,Biryol I I

    更新日期:1997-11-28 00:00:00

  • Evaluation of toxicity of glycerol monooleate nanoparticles on PC12 cell line.

    abstract::An innovative approach to improve drug delivery is the use of glycerol monooleate nanoparticles. Numerous studies describe their high versatility, low toxicity and ability to carry relatively high loads of conjugated compounds including scarcely soluble ones, providing sustained drug release and increasing drug diffus...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2018.01.035

    authors: Valente F,Bysell H,Simoni E,Boge L,Eriksson M,Martini A,Astolfi L

    更新日期:2018-03-25 00:00:00

  • Mathematical modeling of the fluid dynamics in the flow-through cell.

    abstract::The fluid dynamics in the flow-through cell (USP apparatus 4) has been predicted using the mathematical modeling approach of computational fluid dynamics (CFD). The degree to which flow structures in this apparatus can be qualified as 'ideal' both spatially and temporally has been assessed. The simulations predict the...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.04.012

    authors: Kakhi M

    更新日期:2009-07-06 00:00:00

  • Anti-tumor effect via passive anti-angiogenesis of PEGylated liposomes encapsulating doxorubicin in drug resistant tumors.

    abstract::The PEGylated liposomal (PEG-LP) Doxorubicin, PEG-LP (DOX), with a diameter of around 100nm, accumulates in tumors via the enhanced permeability and retention (EPR) effect, and is used clinically for the treatment of several types of cancer. However, there are a number of tumor types that are resistant to DOX. We repo...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.05.047

    authors: Kibria G,Hatakeyama H,Sato Y,Harashima H

    更新日期:2016-07-25 00:00:00

  • Glycerosomes: Investigation of role of 1,2-dimyristoyl-sn-glycero-3-phosphatidycholine (DMPC) on the assembling and skin delivery performances.

    abstract::Glycerosomes were formulated using 1,2-dimyristoyl-sn-glycero-3-phosphatidycholine (DMPC), diclofenac sodium salt and 10, 20 or 30% glycerol in the water phase, while corresponding liposomes were prepared with the same amount of DMPC and diclofenac, without glycerol. The aim of the present work was to evaluate the eff...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.09.026

    authors: Manca ML,Manconi M,Zaru M,Valenti D,Peris JE,Matricardi P,Maccioni AM,Fadda AM

    更新日期:2017-10-30 00:00:00

  • Interactions between a poorly soluble cationic drug and sodium dodecyl sulfate in dissolution medium and their impact on in vitro dissolution behavior.

    abstract::In the pharmaceutical industry, in vitro dissolution testing ofsolid oral dosage forms is a very important tool for drug development and quality control. However, ion-pairing interaction between the ionic drugand surfactants in dissolution medium often occurs, resulting in inconsistent and incomplete drug release. The...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.10.063

    authors: Huang Z,Parikh S,Fish WP

    更新日期:2018-01-15 00:00:00

  • Nanoparticle encapsulation of emulsion droplets.

    abstract::The overall aim of this study is to coat emulsion droplets with nanoparticles using a simple heterocoagulation process in aqueous dispersion and determine: the adsorption behavior and interfacial layer microstructure, droplet physical stability against flocculation and coalescence, and the release profile of a model l...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.06.044

    authors: Prestidge CA,Simovic S

    更新日期:2006-10-31 00:00:00

  • Lectin-coated PLGA microparticles: thermoresponsive release and in vitro evidence for enhanced cell interaction.

    abstract::PLGA-microparticles with 4.7 μm in diameter were prepared by the double emulsion technique and loaded with 1.7 μg fluorescein/mg PLGA mimicking a hydrophilic API. In an effort to further elucidate the release and bioadhesive characteristics of lectin-grafted formulations in vitro, the particles were coated with wheat ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.07.025

    authors: Wang XY,Koller R,Wirth M,Gabor F

    更新日期:2012-10-15 00:00:00

  • In vivo antiviral activity of ribavirin/alpha-cyclodextrin complex: evaluation on experimental measles virus encephalitis in mice.

    abstract::Intracranial injection of the rodent adapted CAM/RB strain of measles virus (MV) induces encephalitis in CBA/ca mice. It has already been shown that cyclodextrins can be used as carriers to increase the antiviral activity of ribavirin (RBV) against MV in cellular model. In this study, the antiviral activity of a RBV/a...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.01.043

    authors: Jeulin H,Grancher N,Kedzierewicz F,Finance C,Le Faou AE,Venard V

    更新日期:2008-06-05 00:00:00

  • Lysozyme-loaded, electrospun chitosan-based nanofiber mats for wound healing.

    abstract::In this study, a blend mixture of chitosan-ethylenediaminetetraacetic acid (CS 2 wt%-EDTA) at a weight ratio of 30/70 and polyvinyl alcohol (PVA) solution (10 wt%) was electrospun to produce fibrous mats with lysozyme (10, 20 and 30 wt%) used for wound healing. The morphology and diameter of the electrospun fiber mats...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.02.010

    authors: Charernsriwilaiwat N,Opanasopit P,Rojanarata T,Ngawhirunpat T

    更新日期:2012-05-10 00:00:00

  • Targeting energy metabolism of cancer cells: Combined administration of NCL-240 and 2-DG.

    abstract::Cancer cells increase their metabolism to produce the energy and biomolecules necessary for growth and proliferation. Thus, energy metabolism pathways may serve as targets for anti-cancer therapy. NCL-240 is a second generation anti-cancer drug belonging to the PITenins class of PI3K-Akt inhibitors. Our analysis sugge...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.08.095

    authors: Pattni BS,Jhaveri A,Dutta I,Baleja JD,Degterev A,Torchilin V

    更新日期:2017-10-30 00:00:00

  • On the selection of an opioid for local skin analgesia: Structure-skin permeability relationships.

    abstract::Recent studies demonstrated that post-herpetical and inflammatory pain can be locally managed by morphine gels, empirically chosen. Aiming to rationalize the selection of the most suitable opioid for the cutaneous delivery, we studied the in vitro penetration through human epidermis of eight opioids, evidencing the cr...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.04.071

    authors: Musazzi UM,Matera C,Dallanoce C,Vacondio F,De Amici M,Vistoli G,Cilurzo F,Minghetti P

    更新日期:2015-07-15 00:00:00

  • Preliminary evaluation of a novel oral delivery system for rhPTH1-34: in vitro and in vivo.

    abstract::rhPTH1-34 is clinically used for osteoporosis treatment. However, this peptide drug has no oral bioavailability because of proteolysis and low membrane permeability in gastrointestinal gut. This study explored the possibility of absorption enhancement for rhPTH1-34 through the oral delivery of the microemulsion. The m...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.08.029

    authors: Guo L,Ma E,Zhao H,Long Y,Zheng C,Duan M

    更新日期:2011-11-25 00:00:00

  • Taste sensing systems (electronic tongues) for pharmaceutical applications.

    abstract::Electronic tongues are sensor array systems able to detect single substances as well as complex mixtures by means of particular sensor membranes and electrochemical techniques. Two systems are already commercially available, the Insent taste sensing system and the αAstree electronic tongue. In addition, various labora...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2010.11.028

    authors: Woertz K,Tissen C,Kleinebudde P,Breitkreutz J

    更新日期:2011-09-30 00:00:00

  • 3D printing in pharmaceutics: A new tool for designing customized drug delivery systems.

    abstract::Three-dimensional printing includes a wide variety of manufacturing techniques, which are all based on digitally-controlled depositing of materials (layer-by-layer) to create freeform geometries. Therefore, three-dimensional printing processes are commonly associated with freeform fabrication techniques. For years, th...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2015.12.071

    authors: Goole J,Amighi K

    更新日期:2016-02-29 00:00:00

  • Characterization and antimicrobial activity of a pharmaceutical microemulsion.

    abstract::The characterization of a pharmaceutical microemulsion system with glycerol monolaurate as oil, ethanol as cosurfactant, Tween 40 as surfactant, sodium diacetate and water, and the antimicrobial activities against Escherichia coli, Staphylococcus aureus, Bacillus subtilis, Candida albicans, Aspergillus niger and Penic...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.05.022

    authors: Zhang H,Cui Y,Zhu S,Feng F,Zheng X

    更新日期:2010-08-16 00:00:00

  • Polymeric nanoparticles encapsulating betamethasone phosphate with different release profiles and stealthiness.

    abstract::The purpose of this study was to engineer nanoparticles with various sustained profiles of drug release and prolonged circulation by blending poly(D,L-lactic acid)/poly(D,L-lactic/glycolic acid) (PLA/PLGA) homopolymers and poly(ethylene glycol) (PEG)-block-PLA/PLGA copolymers encapsulating betamethasone disodium 21-ph...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.04.001

    authors: Ishihara T,Kubota T,Choi T,Takahashi M,Ayano E,Kanazawa H,Higaki M

    更新日期:2009-06-22 00:00:00

  • The progress on sulfhydryl modified polymers with regard to synthesis, characterization and mucoadhesion.

    abstract::The concepts of mucoadhesion and mucoadhesive polymers were introduced in the 20th century, leading to several advantages. These included enhanced drug absorption and extended residence at specific site of action. Polymeric excipients underwent chemical modification with sulfhydryl groups on the polymeric backbone so ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2020.120016

    authors: Sanchez Armengol E,Laffleur F

    更新日期:2021-01-05 00:00:00

  • Multifunctional nanogels with dual temperature and pH responsiveness.

    abstract::Over the last 10 years, the development of intelligent biomaterials for medical and pharmaceutical applications has attracted growing interest by combining interdisciplinary efforts. Between them nanogels represent one of the most attractive carriers for innovative drug delivery systems. In the present investigation n...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.10.017

    authors: Nita LE,Chiriac AP,Diaconu A,Tudorachi N,Mititelu-Tartau L

    更新日期:2016-12-30 00:00:00

  • Physicochemical and biopharmaceutical characterization of BTA-243, a diacidic drug with low oral bioavailability.

    abstract::This investigation has examined possible causes of the poor bioavailability of the beta(3)-adrenoceptor agonist BTA-243. The aqueous solubility of BTA-243 is pH dependent with a solubility minimum at pH 1.5. However, the dissolution rate of the disodium salt of BTA-243 is similar at both pH 2.0 and 7.4 indicating that...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(00)00657-8

    authors: Brown JR,Collett JH,Attwood D,Ley RW,Sims EE

    更新日期:2001-02-01 00:00:00

  • Enhanced stability of rubbery amylose-rich maize starch films plasticized with a combination of sorbitol and glycerol.

    abstract::Well known aging problems with rubbery starch films are the migration of plasticizer and increased crystallinity leading to embrittlement. The effects of a combination of sorbitol and glycerol used as plasticizers on mechanical, moisture permeability and solid-state properties of rubbery amylose maize starch (Hylon VI...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00585-9

    authors: Krogars K,Heinämäki J,Karjalainen M,Niskanen A,Leskelä M,Yliruusi J

    更新日期:2003-01-30 00:00:00

  • Combination of microneedles and microemulsions to increase celecoxib topical delivery for potential application in chemoprevention of breast cancer.

    abstract::In spite of the high incidence of breast cancer worldwide, there are few strategies for its chemoprevention, and they have limited adherence mainly due to their serious adverse effects. As a new approach for local breast cancer chemoprevention, we developed and optimized microemulsions for topical delivery of celecoxi...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.02.011

    authors: Mojeiko G,de Brito M,Salata GC,Lopes LB

    更新日期:2019-04-05 00:00:00

  • Preparation and evaluation of agglomerated crystals by crystallo-co-agglomeration: an integrated approach of principal component analysis and Box-Behnken experimental design.

    abstract::Poor mechanical properties of crystalline drug particles require wet granulation technique for tablet production which is uneconomical, laborious, and tedious. The present investigation was aimed to improve flow and mechanical properties of racecadotril (RCD), a poorly water soluble antidiarrheal agent, by a crystallo...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.04.073

    authors: Garala KC,Patel JM,Dhingani AP,Dharamsi AT

    更新日期:2013-08-16 00:00:00

  • A therapeutic dose of primaquine can be delivered across excised human skin from simple transdermal patches.

    abstract::This work investigated the permeation of primaquine across full-thickness excised human skin from two acrylate transdermal adhesives. Primaquine base was formulated with National Starch 387-2516 and 387-2287 to provide aluminium foil-backed 1-cm diameter patches, each loaded with 10 mg drug. Other patches were prepare...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(99)00215-x

    authors: Jeans CW,Heard CM

    更新日期:1999-10-28 00:00:00

  • Enhanced transdermal delivery of low molecular weight heparin by barrier perturbation.

    abstract::The purpose of this work was to investigate the in vitro transdermal delivery of low molecular weight heparin (LMWH). Hairless rat skin was mounted on Franz diffusion cells and treated with various enhancement strategies. Passive flux was essentially zero and remained low even after iontophoresis (0.065 U cm(-2) h(-1)...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.08.028

    authors: Lanke SS,Kolli CS,Strom JG,Banga AK

    更新日期:2009-01-05 00:00:00