Abstract:
PURPOSE:To investigate the effect of polyelectrolytes on the formation and physicochemical properties of chitosan nanoparticles (CS-NPs) used for the delivery of an anticancer drug, doxorubicin (DOX). METHOD:Three DOX-loaded CS-NPs were formulated with tripolyphosphate (CS-TP/DOX NPs), dextran sulfate (CS-DS/DOX NPs), and hyaluronic acid (CS-HA/DOX NPs) by using ionotropic gelation or complex coacervation. RESULTS:CS-TP/DOX NPs were the smallest, with an average size of ~100 nm and a narrow size distribution, while CS-DS/DOX and CS-HA/DOX NPs were ~200 nm in size. Transmission electron microscopy clearly showed a spherical shape for all the NPs. The strong binding affinity of DOX for the multiple sulfate groups in DS resulted in a sustained release profile from CS-DS/DOX NPs at pH 7.4, while CS-HA/DOX NPs exhibited faster DOX release. This trend was also present under acidic conditions, where release of DOX was significantly augmented because of polymer protonation. Compared to CS-TP/DOX or CS-DS/DOX NPs, CS-HA/DOX NPs showed superior cellular uptake and cytotoxicity in MCF-7 and A-549 cells, because of their ability to undergo CD44-mediated endocytosis. Pharmacokinetic studies clearly showed that all CS-NPs tested significantly improved DOX plasma circulation time and decreased its elimination rate constant. Consistent with the in vitro release data, CS-DS/DOX NPs exhibited a relatively better DOX plasma profile and enhanced blood circulation, compared to CS-HA/DOX or CS-TP/DOX NPs. Overall, these results demonstrated how NP design can influence their function. CONCLUSIONS:Taken together, CS-based polyelectrolyte complexes could provide a versatile delivery system with enormous potential in the pharmaceutical and biomedical sectors.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Ramasamy T,Tran TH,Cho HJ,Kim JH,Kim YI,Jeon JY,Choi HG,Yong CS,Kim JOdoi
10.1007/s11095-013-1251-9subject
Has Abstractpub_date
2014-05-01 00:00:00pages
1302-14issue
5eissn
0724-8741issn
1573-904Xjournal_volume
31pub_type
杂志文章abstract:PURPOSE:To characterize temporal exposure and elimination of 5 gold/dendrimer composite nanodevices (CNDs) (5 nm positive, negative, and neutral, 11 nm negative, 22 nm positive) in mice using a physiologically based mathematical model. METHODS:400 ug of CNDs is injected intravenously to mice bearing melanoma cell line...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0784-7
更新日期:2012-09-01 00:00:00
abstract::Coprecipitates of fluorescein and magnesium hydroxide demonstrate delayed absorption relative to fluorescein solutions when administered to the airways of the isolated perfused rat lung (IPRL). Perfusate concentration vs time profiles showed that dissolution and not epithelial permeability was the rate-controlling fac...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015942013413
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abstract:PURPOSE:In pharmacokinetic (PK)/pharmacodynamic (PD) modelling and simulations (M&S), omitting dropouts can cause inaccuracies in parameter estimation and clinical trial simulations (CTS). This study examines the impact of different imputation methods for missing data on the interpretation of model results, as well as ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1380-9
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015917023949
更新日期:1988-03-01 00:00:00
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journal_title:Pharmaceutical research
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doi:10.1007/s11095-005-2486-x
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doi:10.1007/s11095-007-9301-9
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015843811150
更新日期:1990-01-01 00:00:00
abstract::One thousand milligrams of aspirin, as its lysine salt was administered intravenously, orally, and intramuscularly to nine male and nine female young healthy adult volunteers. After intravenous injection mean (+/- SD) values of clearance, steady-state volume of distribution, and terminal half-life were 12.2 +/- 2.2 ml...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章
doi:10.1023/a:1015978104017
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011032502097
更新日期:2001-02-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015880327911
更新日期:1992-07-01 00:00:00
abstract::Polymeric biomaterials have extensively been used in medicinal applications. However, factors that determine their biocompatibility are still not very clear. This article reviews various effects of the chemical structure and the surface properties of polymeric biomaterials on their biocompatibility, including protein ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/b:pham.0000036909.41843.18
更新日期:2004-08-01 00:00:00
abstract::The fluxes of nitroglycerine (NG) through human abdominal epidermis from different individuals were measured in vitro at 32°C. The mean NG flux for the entire group was 16.9 µg/cm(2) × hr, with a standard deviation of 47.7%. There are no significant differences in the means and the variances of NG fluxes between males...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016381017357
更新日期:1986-02-01 00:00:00
abstract:PURPOSE:Cell-based permeability screens are widely used to identify drug-P-glycoprotein (PGP) interaction in vitro. However, their reliability in predicting the impact of PGP on human drug pharmacokinetics is poorly defined. The aim was to determine whether a quantitative relationship exists between PGP-mediated altera...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000026434.82855.69
更新日期:2004-05-01 00:00:00
abstract:PURPOSE:In this study, we aimed to illustrate the utility of fractional radiofrequency (RF) that generated microchannels in the skin, allowing delivery of peptide and siRNA via the skin. The mechanisms involved in the correlation between macromolecule permeation and skin structure were also elucidated. METHODS:The mor...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1568-z
更新日期:2015-05-01 00:00:00
abstract::Loracarbef is an oral 1-carba-1-dethiacephalosporin antibiotic structurally related to cefaclor. Like many beta-lactam antibiotics, loracarbef exists in several hydrated crystalline forms. The pH-solubility profile curve for loracarbef monohydrate is U-shaped, resembling those of other zwitterionic cephalosporins. Lor...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018949709797
更新日期:1992-02-01 00:00:00
abstract::To achieve time-controlled or site-specific drug delivery in the gastrointestinal tract, a sigmoidal release system (SRS) was developed, which achieved a prolonged lag time, followed by rapid release. The theophylline beads with a thick Eudragit RS film coating showed very low drug release in water, whereas the releas...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018910114436
更新日期:1994-01-01 00:00:00
abstract:PURPOSE:To develop a new bionic system from an existing drug dissolution/absorption simulating system (DDASS) to simultaneously predict the release and absorption of enteric-coated formulations. METHODS:In accordance with the pH-dependent characteristics of enteric-coated formulations, the modified DDASS was designed ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0905-3
更新日期:2013-02-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007570030368
更新日期:2000-11-01 00:00:00
abstract::Primaquine (I), a 6-methoxy-8-aminoqumoline derivative used for the treatment of malaria has previously been shown to be metabolized to 8-(3-carboxy-l-methyl-propylamino)-6-methoxyquinoline by both micro-organisms and laboratory rats. Reported herein is the synthesis of this novel metabolite. ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016311616719
更新日期:1984-03-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011935222652
更新日期:1998-02-01 00:00:00
abstract::The molecular environment of sucrose and mineral oil within sucrose and mineral oil solid state emulsions was investigated by NMR techniques. The 13C and 1H chemical shifts of sucrose and mineral oil to those observed in solid state emulsions (comprised of sucrose and mineral oil) were equivalent, indicating that the ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018946512445
更新日期:1994-09-01 00:00:00
abstract:PURPOSE:It was the aim of this study to synthesize and characterize a novel chitosan-glutathione (GSH) conjugate providing improved mucoadhesive and permeation-enhancing properties. METHODS:Mediated by carbodiimide and N-hydroxysuccinimide, glutathione was covalently attached to chitosan via the formation of an amide ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-6248-6
更新日期:2005-09-01 00:00:00
abstract:PURPOSE:To study the degradation of oxaliplatin in chloride media and evaluate the cytotoxicity of oxaliplatin in normal and chloride-deficient medium. METHODS:The products of the reaction of oxaliplatin with chloride were separated on a Hypercarb S column with a mobile phase containing 40% methanol in 0.05 M ammonia ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000026444.67883.83
更新日期:2004-05-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1693-3
更新日期:2015-10-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9139-6
更新日期:2007-01-01 00:00:00
abstract::Nanotechnology has continuously contributed to the fast development of diagnostic and therapeutic agents. Theranostic nanomedicine has encompassed the ongoing efforts on concurrent molecular imaging of biomarkers, delivery of therapeutic agents, and monitoring of therapy response. Among these formulations, polymer-bas...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-013-1103-7
更新日期:2014-06-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9586-3
更新日期:2008-09-01 00:00:00
abstract:PURPOSE:To determine the pharmacokinetics of GS-522, an oligodeoxynucleotide (GGTTGGTGTGGTTGG) inhibitor of thrombin, after constant infusion and bolus administration in the cynomolgus monkey. METHODS:Using a stability indicating HPLC method, the GS-522 plasma concentration versus time data were obtained after constan...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016295907266
更新日期:1995-12-01 00:00:00
abstract:PURPOSE:To elucidate the catalytic mechanism of the esterase-like activity of serum albumin (SA), the reactivity of SA from six species was investigated using p-nitrophenyl esters as model substrates. METHODS:The effect of pH and the energetic and thermodynamic profiles of SA were determined for all species for p-nitr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000016241.84630.06
更新日期:2004-02-01 00:00:00
abstract:PURPOSE:To explore the application of scanning ion occlusion sensing (SIOS) as a novel technology for characterization of nanoparticles. METHODS:Liposomes were employed as model nanoparticles. The size distribution of the liposomes was measured by both SIOS and dynamic light scattering (DLS). Particle number concentra...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0788-3
更新日期:2012-09-01 00:00:00