Abstract：
:The objective of this study was to investigate the presence of amino acid transporters on the corneal epithelium and to enhance corneal drug absorption through prodrug modification targeted to the amino acid transporters. SIRC was used as a model cell line representing the corneal epithelium. Uptake studies were carried out using [3H] L-tyrosine at 37 degrees C. Temperature, energy and pH dependence studies were carried out. The uptake seems to be composed of a major saturable and minor non-saturable component (V(max) =2.9+/-0.62 nmoles/min/mg protein, K(m) =71+/-21 microM, K(d) =2.6+/-0.6 nl/min/mg protein). No significant inhibition of uptake was observed in the presence of metabolic inhibitors or in the absence of sodium. Competitive inhibition studies were performed in the presence of various amino acids and model tyrosine conjugates (p-nitro and p-chloro benzyl ether conjugate of L-tyrosine). Uptake was inhibited by neutral aromatic and large neutral aliphatic amino acids. L-Tyrosine uptake was inhibited by its ether conjugates in a concentration dependent manner suggesting that these compounds may be sharing the same transport mechanism. This study provides biochemical evidence of the presence of a large neutral amino acid transport system on the corneal epithelium, which may be utilized to enhance the corneal drug transport.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Balakrishnan A,Jain-Vakkalagadda B,Yang C,Pal D,Mitra AKdoi
10.1016/s0378-5173(02)00405-2keywords:
subject
Has Abstractpub_date
2002-10-24 00:00:00pages
115-25issue
1-2eissn
0378-5173issn
1873-3476pii
S0378517302004052journal_volume
247pub_type
杂志文章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
更新日期：2012-10-15 00:00:00
abstract：:Recently, we synthesized novel amphiphilic gelatin-oleic acid (GO) conjugate to prepare self-assembled nanoparticles for drug delivery. The aim of this study was to investigate pharmaceutical potentialities of self-assembled GO nanoparticles for solubility enhancement and modified release of poorly water-soluble drugs...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.07.025
更新日期：2013-10-15 00:00:00
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
更新日期：2003-06-04 00:00:00
abstract：:For effective topical delivery, a drug must cross the stratum corneum (SC) barrier into viable tissue. The use of permeation enhancers is a widespread approach for barrier modification. In the current study, flufenamic acid (FluA), a non-steroidal anti-inflammatory drug, is a model agent for investigating the influenc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.04.011
更新日期：2016-05-30 00:00:00
abstract：:A quality-by-design (QbD) principle, including process analytical technology, is becoming the principal idea in drug development and manufacturing. The implementation of QbD into product development and manufacturing requires larger resources, both human and financial, however, large-scale production can be establishe...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.01.023
更新日期：2010-04-15 00:00:00
abstract：:Streamlining the manufacturing process has been recognized as a key issue to reduce production costs and improve safety in pharmaceutical manufacturing. Although data available from earlier developmental stages are often sparse and unstructured, they can be very useful to improve the understanding about the process un...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.01.018
更新日期：2013-02-28 00:00:00
abstract：:Rhenium-188 labeled tin (Sn) microparticles were developed for pain palliation therapy in the patients suffering from synovitis with acute pain. The rhenium tin microparticles were prepared using stannous chloride and freshly eluted (188)ReO(4)(-) from (188)W/(188)Re generator. The aggregated colloidal particles, pack...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.01.014
更新日期：2007-06-29 00:00:00
abstract：:Tuberculosis (TB) remains a major global health problem as it is the second leading cause of death from an infectious disease worldwide, after the human immunodeficiency virus (HIV). Conventional treatments fail either because of poor patient compliance to the drug regimen or due to the emergence of multidrug-resistan...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2014.12.009
更新日期：2015-01-30 00:00:00
abstract：:The aim of this study was to investigate if amorphous indomethacin samples, prepared using different preparation methods, exhibit different structural and kinetic characteristics and if these differences can be correlated to their physical stability (time to crystallisation). Samples were prepared by melt quenching, s...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.12.019
更新日期：2011-09-30 00:00:00
abstract：:Liposomal formulations were made using Solvent-assisted active loading technology (SALT). Two formulations composed of HSPC:DPPG:Chol:DSPE-mPEG2000 (PG-LipCUR) and HSPC:Chol:DSPE-mPEG2000 (LipCUR) demonstrated good colloidal properties and the CUR-encapsulation of 82% and 89% for PG-LipCUR and LipCUR, respectively. Th...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119211
更新日期：2020-04-30 00:00:00
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
更新日期：2008-06-05 00:00:00
abstract：:The effects of carriers, the drug:carrier ratio and a 1 month storage period of a formulation in permeable polystyrene tube at 40 degrees C/75% RH on the in vitro pulmonary deposition of model drugs from dry powder inhaler (DPI) were evaluated. Budesonide (hydrophobic) and salbutamol sulphate (hydrophilic) were used a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00357-0
更新日期：2003-09-16 00:00:00
abstract：:Fiber-optic near infrared (NIR) spectroscopy was used to investigate several key features of the polymorphic transitions observed during the crystallization and the filtration of SaC, an Active Pharmaceutical Ingredient (API) produced by Sanofi-Synthelabo. Using few samples, the spectroscopic data were calibrated to p...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.01.003
更新日期：2004-04-01 00:00:00
abstract：:Genetic immunization through skin is highly desirable as skin has plenty of antigen presenting cells (APCs) and is easily accessible. The purpose of this study was to investigate the effects of electroporation pulse amplitude, pulse length and number of pulses on cutaneous plasmid DNA vaccine delivery and immune respo...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.12.014
更新日期：2005-04-27 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.04.068
更新日期：2019-06-10 00:00:00
abstract：:Subcutaneous vaccination of C57bl/6 mice with irradiated B16 melanoma cells supplemented with liposomal interleukin-2 (IL2) or murine interferon-gamma (mIFNgamma), resulted in systemic protection in 50% of the animals, against a subsequent tumor cell challenge in a dose dependent manner. The protective efficacy was co...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00039-3
更新日期：1999-06-10 00:00:00
abstract：:The objective of this investigation was to evaluate phenobarbital transdermal delivery for possible use in paediatric care. In vitro experiments were performed using intact pig skin and barriers from which the stratum corneum had been stripped to different extents to model the less resistant skin of premature babies. ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.02.026
更新日期：2012-10-01 00:00:00
abstract：:Solid dispersions were prepared with the extremely poorly water soluble drug, probucol and the water soluble polymers, polyvinyl pyrrolidone (PVP), polyacrylic acid (PAA) or polyethylene oxide (PEO) and blends of these polymers. The solid dispersions were prepared either by the solvent evaporation method, or by compre...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00709-8
更新日期：2001-07-03 00:00:00
abstract：:Herein we investigate the efficiency of various biomimetic coatings for localized drug delivery, using vancomycin as key therapeutic drug, which is a widely used antibiotic for the treatment of strong infections caused by positive Gram bacteria. We evaluate classical hydroxyapatite and biomimetic hydroxyapatite-collag...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.11.062
更新日期：2017-01-30 00:00:00
abstract：:Aristotelia chilensis (Mol.) Stuntz (A. chilensis), also known as maqui, is a plant of the Elaeocarpaceae family that grows in central and southern Chile as well as southwestern Argentina. Infusions of its leaves have long been used in the traditional native herbal medicine to treat different ailments. Phytochemical s...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.07.005
更新日期：2008-11-03 00:00:00
abstract：:The high incidence of degenerative tears and prevalence of retears (20-95%) after surgical repair makes rotator cuff injuries a significant health problem. This high retear rate is attributed to the failure of the repaired tissue to regenerate the native tendon-to-bone insertion (enthesis). Biological augmentation of ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2018.01.006
更新日期：2018-06-15 00:00:00
abstract：:The objective of the study was to assess the effect of enhanced mucoadhesion of a cationic mucoadhesive nanostructured lipid carrier (NLC) on its ocular disposition after topical administration. The NLC was made mucoadhesive by surface coating with chitosan oligosaccharide (COS), a low molecular weight derivate of chi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119095
更新日期：2020-03-15 00:00:00
abstract：:The bioavailability of ibuprofen from matrix mini-tablets based on microcrystalline wax and a starch derivative was tested. An oral dose of 300 mg of ibuprofen was administered to healthy volunteers (n=8) in a randomized cross-over study design either as a commercial matrix formulation (Ibu-Slow 600) or as mini-tablet...
journal_title：International journal of pharmaceutics
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1016/s0378-5173(00)00549-4
更新日期：2000-11-04 00:00:00
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
更新日期：2019-04-05 00:00:00
abstract：:This study aimed to investigate the following factors affecting the cytotoxicity of Capmul®MCM (C8/10MD) in self-emulsified nanoemulsions (SENs): concentration, triglycerides, and droplet size, and how these factors influence permeability of lipid droplets. Two triglycerides (C8T and C18T) and six formulations were us...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.03.010
更新日期：2019-04-20 00:00:00
abstract：:This paper reports measurements of the release characteristics of the model drug salbutamol from a liquid crystalline vehicle across both human and hairless murine skin in vitro. The use of oleic acid and iontophoresis as penetration enhancement techniques, used separately and simultaneously, was also investigated. Ov...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.04.004
更新日期：2007-08-16 00:00:00
abstract：:Topical poultices of ketoprofen were prepared using deionized water, propylene glycol (X1), and glycerin (X2) as the vehicle in combination with hydrophilic matrix materials, including gelatin (X3) and sodium polyacrylate. A mixture design was utilized to evaluate the influence of these constituents (X1-X3) on the adh...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00919-x
更新日期：2002-02-21 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 release properties of steroids from a combined contraceptive vaginal ring have been investigated. The product design is based on a coaxial fiber consisting of two types of polyethylene vinylacetate copolymers. Inside the core of the fiber, two steroids are present in a molecularly dissolved state. In order to desi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00900-0
更新日期：2002-01-31 00:00:00
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 everte...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00343-5
更新日期：2002-10-01 00:00:00
