Abstract:
:A physiologically pertinent in vitro model is urgently needed for probing interactions between inhaled drugs and the organic cation transporters (OCT) in the bronchial epithelium. This study evaluated OCT expression, functionality, inhibition by common inhaled drugs and impact on formoterol transepithelial transport in layers of human bronchial epithelial Calu-3 cells grown at an air-liquid interface. 21 day old Calu-3 layers expressed OCT1, OCT3, OCTN1 and OCTN2 whereas OCT2 could not be detected. Quantification of the cellular uptake of the OCT substrate ASP(+) in presence of inhibitors suggested several OCT were functional at the apical side of the cell layers. ASP(+) uptake was reduced by the bronchodilators formoterol, salbutamol (albuterol), ipratropium and the glucocorticoid budesonide. However, the OCT inhibitory properties of the two β(2)-mimetics were suppressed at therapeutically relevant concentrations. The absorptive permeability of formoterol across the cell layers was enhanced at a high drug concentration shown to decrease ASP(+) uptake by ∼50% as well as in presence of the OCT inhibitor tetraethylammonium (TEA). Secretory transport was unaffected by the drug concentration but was reduced by TEA. Our data indicate air-interfaced Calu-3 layers offer a low-cost in vitro model suitable for assessing inhaled drug-OCT interactions in the bronchial epithelium.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Mukherjee M,Pritchard DI,Bosquillon Cdoi
10.1016/j.ijpharm.2011.12.036subject
Has Abstractpub_date
2012-04-15 00:00:00pages
7-14issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(11)01162-8journal_volume
426pub_type
杂志文章abstract::In this study, the antibacterial bionanocomposites of poly(ε-caprolactone) (PCL) with different concentrations of triclosan (TC) loaded polylactic acid (PLA) nanoparticles (30wt% triclosan) (LATC30) were fabricated via a melt mixing process in order to lower the burst release of PCL and to extend the antibacterial act...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.05.009
更新日期:2016-07-11 00:00:00
abstract::Gold nanoparticle (AuNP) interaction with the blood compartment as a function of their charge and the binding energy of their surface ligand was explored. Citrate, polyallylamine and cysteamine stabilized AuNP along with dihydrolipoic acid and polyethylene glycol capped AuNP were synthesized and fully characterized. T...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119244
更新日期:2020-04-30 00:00:00
abstract::The purpose of this study was to synthesize and characterize biodegradable and thermosensitive triblock copolymers for delivering protein at controlled rate in biologically active form for longer duration of time. A series of thermosensitive triblock copolymers with different block lengths (PLGA-PEG-PLGA) were synthes...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.09.026
更新日期:2005-01-20 00:00:00
abstract::Lipid-based liquid crystalline nanoparticles (LCNPs) have attracted growing interest as a new drug nanocarrier system for improving bioavailability for both hydrophilic and hydrophobic drugs. In this study, self-assembled LCNPs based on soy phosphatidyl choline and glycerol dioleate, which was known possessing low tox...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.12.058
更新日期:2012-03-15 00:00:00
abstract::Chronic non-healing wounds tender a great challenge to patients, physicians, and wound care professionals. In view of the increasing prevalence of chronic wounds due to ischemia, diabetic foot, venous, and pressure ulcers, their appropriate management requires significant attention. Along with the basic techniques of ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2021.120270
更新日期:2021-01-21 00:00:00
abstract::The purpose of this study was to develop the correlation of cycle parameters between a laboratory and a production freeze-dryer. With the established correlation, key cycle parameters obtained using a laboratory dryer may be converted to those for a production dryer with minimal experimental efforts. In order to devel...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.06.022
更新日期:2005-09-30 00:00:00
abstract::Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely prescribed drugs. Debilitating diseases such as rheumatoid arthritis and osteoarthritis are commonly managed by NSAIDs. However, NSAIDs pharmacological mechanism is often associated with the presence of gastrointestinal side effects. NSAIDs encap...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2016.11.002
更新日期:2016-12-30 00:00:00
abstract::Although several in vitro models have been reported to predict the ability of drug candidates to cross the blood-brain barrier, their real in vivo relevance has rarely been evaluated. The present study demonstrates the in vivo relevance of simple unidirectional permeability coefficient (P(app)) determined in three in ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.09.016
更新日期:2010-12-15 00:00:00
abstract::The incomplete release of Endostar from PLGA microspheres was observed in our previous study. In the present study, we focused on the effect of medium-chain triglycerides (MCT) on the in vitro/in vivo release behavior of Endostar encapsulated PLGA microspheres, which were prepared by a water-in-oil-in-water (W/O/W) do...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.07.018
更新日期:2010-09-15 00:00:00
abstract::This work aims to study the biophysical interactions of rifampicin (RIF) with three-dimensional macrophage membrane models, under environments with physiological and pathological relevance. The interaction of RIF with liposomes formed by 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) in different pH values (i.e., ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.03.005
更新日期:2014-05-15 00:00:00
abstract::Native low-density lipoproteins (LDL) naturally accumulate at atherosclerotic lesions and are thought to be among the main drivers of atherosclerosis progression. Numerous nanoparticular systems making use of recombinant lipoproteins have been developed for targeting atherosclerotic plaque. These innovative formulatio...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119282
更新日期:2020-05-15 00:00:00
abstract::Polyurethane polymers and poly(ether urethane) copolymers were chosen as drug carriers for alpha-tocopherol. This active ingredient is widely used as a strong antioxidant in many medical and cosmetic applications, but is rapidly degraded, because of its light, heat and oxygen sensitivity. Polyurethane and poly(ether u...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2003.09.025
更新日期:2004-01-09 00:00:00
abstract::Naked plasmid DNA is a powerful tool for gene therapy, but it is rapidly eliminated from the circulation after intravenous administration. Therefore, the development of optimized DNA delivery systems is necessary for its successful clinical use. Solid lipid nanoparticles (SLNs) have demonstrated transfection capacity ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.10.020
更新日期:2010-01-29 00:00:00
abstract::In this work, the sizing of microemulsion droplets of a lipid-based pharmaceutical excipient (Labrasol® ALF) is performed by Taylor dispersion analysis (TDA) using fluorescent detection. An hydrophobic fluorescent marker is used to tag the microemulsion droplet and to increase the sensitivity of detection (compared to...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.09.016
更新日期:2016-11-20 00:00:00
abstract::The aim of this study was to investigate how a selection of formulation variables affects the in vitro transfection efficiency and physicochemical properties (particle size, zetapotential and chitosan-plasmid association) of chitosan-based polyplexes. Experimental designs in combination with multivariate data analysis...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(03)00301-6
更新日期:2003-08-11 00:00:00
abstract::A mechanistic particle scale model is proposed for bilayer tablet compaction. Making bilayer tablets involves the application of first layer compaction pressure on the first layer powder and a second layer compaction pressure on entire powder bed. The bonding formed between the first layer and the second layer particl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.07.032
更新日期:2017-08-30 00:00:00
abstract::Several classes of antifungal have been employed in candidiasis treatment, but patients with advanced immunodeficiency can present unsatisfactory results after therapy. In these cases, high doses of drugs or the use of multiple agents are sometimes used, and hence increasing the risk of serious side effects. Consideri...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.08.002
更新日期:2008-02-12 00:00:00
abstract::This investigation is a contribution to standardization in in vitro drug penetration measurements using excised human skin and to statistical treatment of the observations. The wide variations observed in measurements of drug accumulation in and drug permeation through the stratum corneum are caused not only by analyt...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00558-5
更新日期:2000-11-19 00:00:00
abstract::The aim of this study was to introduce a fast and reliable differential scanning calorimetry (DSC)-based method to determine the monomolecular loading capacity of drugs with good glass-forming ability in mesoporous silica (MS). The proposed method is based on a solvent-free melting/fusion of drug into the MS during a ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.04.035
更新日期:2018-06-10 00:00:00
abstract::Phenoporlamine hydrochloride is a novel compound that is used for the treatment of hypertension. The purpose of this study was to develop a sustained release tablet for phenoporlamine hydrochloride because of its short biological half-life. Three floating matrix formulations of phenoporlamine hydrochloride based on ga...
journal_title:International journal of pharmaceutics
pub_type: 临床试验,杂志文章
doi:10.1016/j.ijpharm.2005.12.003
更新日期:2006-03-09 00:00:00
abstract::The terahertz region of the electromagnetic spectrum spans the frequency range between the infrared and the microwave. Traditionally the exploitation of this spectral region has been difficult owing to the lack of suitable source and detector. Over the last ten years or so, terahertz technology has advanced considerab...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2011.01.012
更新日期:2011-09-30 00:00:00
abstract::Formulations of ultra-deformable liposomes containing bleomycin (Bleosome) have previously been described and proposed for topical treatment of skin cancer [Lau, K.G., Chopra, S., Maitani, Y., 2003. Entrapment of bleomycin in ultra-deformable liposomes. S. T. P. Pharm. Sci. 13, 237-239]. In this study, the stability o...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.04.019
更新日期:2005-08-26 00:00:00
abstract::Epidermal growth factor receptor (EGFR) is an important anti-cancer therapy target that is applicable to many cancer types. We had previously reported the screening and discovery of a novel peptide ligand against EGFR named GE11. It was shown to bind to EGFR competitively with EGF and mediate gene delivery to cancer c...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2008.07.012
更新日期:2008-11-03 00:00:00
abstract::Danshen (Salvia miltiorrhiza) contains tanshinones, which inhibit P-glycoprotein (P-gp) and the cytochrome P450 (CYP) system. In the present study, we evaluated the possible pharmacokinetic interactions of Danshen extract with docetaxel and clopidogrel in rats. Docetaxel (5 mg/kg intravenously and 40 mg/kg orally) or ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.03.031
更新日期:2011-05-30 00:00:00
abstract::The effect of nicotinamide on the properties of aqueous hydroxypropylmethylcellulose (HPMC) solutions was studied. Rheological studies showed that solutions of HPMC of concentration less than 3.0 w/v.% did not form gels and exhibited Newtonian flow patterns at 25 degrees C. The inclusion of nicotinamide increased the ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(01)00770-0
更新日期:2001-09-11 00:00:00
abstract::This paper describes a systematic approach to select optimum stabilizer for the preparation of nano-crystalline suspensions of an active pharmaceutical ingredient (API). The stabilizer can be either a dispersant or a combination of dispersant and wetting agent. The proposed screening method is a quick and efficient wa...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.09.048
更新日期:2014-12-10 00:00:00
abstract::A novel method to include poorly water-soluble substances into the polyelectrolyte capsules of defined size, stability, composition and affinity properties is proposed. Encapsulation explores the polarity gradient across the capsule wall. Capsules creation makes use of electrostatic interaction and can involve many su...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(02)00161-8
更新日期:2002-08-21 00:00:00
abstract::Gamma-oryzanol, a phytosteryl ferulate mixture extracted from rice bran oil, has a wide spectrum of biological activities; in particular, it has antioxidant properties and is often used in cosmetic formulations as a sunscreen. The first objective of the present investigation was to elucidate the molecular mechanism(s)...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.05.018
更新日期:2005-08-11 00:00:00
abstract::The physico-chemical behaviour of trehalose dihydrate during storage at low relative humidity and ambient temperature was investigated, using a combination of techniques commonly employed in pharmaceutical research. Weight loss, water content determinations, differential scanning calorimetry and X-ray powder diffracti...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.01.026
更新日期:2006-04-26 00:00:00
abstract::The aim of the current study is to explore the potential of PEG-30-dipolyhydroxystearate (Cithrol(®) DPHS) and Soluplus(®) as ingredients in novel semisolid self-nanoemulsifying drug delivery systems (SNEDDS). Semisolid SNEDDS consisting of Cithrol(®) DPHS, Capmul(®) MCM and Kolliphor(®) HS 15 were successfully prepar...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.10.063
更新日期:2014-12-30 00:00:00