Abstract：
PURPOSE:The aim of this study was to test the ability of paclitaxel-loaded poly(butylcyanoacrylate) (PBCA) nanoparticles to overcome multidrug resistance (MDR) in human ovarian resistant cells (A2780/T) and investigate its possible mechanism. METHODS:We prepared paclitaxel-loaded PBCA nanoparticles by interfacial polymerization method. The physicochemistry of the nanoparticles was characterized. The cytotoxicity of paclitaxel-loaded PBCA nanoparticles was measured by MTT assay. Calcein-AM assay was used to analyze the P-glycoprotein (P-gp) function, and the expression of MDR-1 mRNA in A2780/T cells treated with drug-loaded nanoparticles was defined by QRT-PCR. RESULTS:The nanoparticles were approximately spherical in shape with an average diameter of 224.5 ± 5.7 nm. The encapsulation efficiency was 99.23%. The in vitro drug release profile exhibited a biphasic pattern. The drug formulated in PBCA nanoparticles showed a greater cytotoxicity than paclitaxel against A2780/T cells. Paclitaxel-loaded PBCA as well as blank PBCA nanoparticles decreased P-gp function in a dose-dependent manner, suggesting the efficacy of the drug-loaded nanoparticle system on overcoming MDR. There was no significant effect on inhibition to the expression of MDR1 mRNA. CONCLUSIONS:Paclitaxel-loaded PBCA nanoparticles can enhance cytotoxicity and overcome MDR through a mechanism of the inhibition of P-gp function caused by the nanoparticles system.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Ren F,Chen R,Wang Y,Sun Y,Jiang Y,Li Gdoi
10.1007/s11095-010-0346-9subject
Has Abstractpub_date
2011-04-01 00:00:00pages
897-906issue
4eissn
0724-8741issn
1573-904Xjournal_volume
28pub_type
杂志文章abstract：:Colonic absorption of recombinant human insulin-like growth factor I (rhIGF-I) was measured in vitro using both rat and minipig colon. The permeability coefficients were 8.03 +/- 1.03 and 4.75 +/- 0.43 x 10(-8) cm sec-1 in the rat and minipig, respectively. The steady-state flux in rat colon was linearly related to th...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018999106684
更新日期：1994-02-01 00:00:00
abstract：:A sensitive radioreceptor assay (RRA) to determine the serum concentrations of fentanyl, pentazocine and morphine was developed on the basis of the drug's competition with a labeled tracer ((3)H-naloxone) for the membrane bound opioid receptor in rat brain homogenates. The binding data were computer-fitted to a standa...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016369229440
更新日期：1984-09-01 00:00:00
abstract：PURPOSE:Relatively large (>5 microm) and porous (mass density <0.4 g/cm3) particles present advantages for the delivery of drugs to the lungs, e.g., excellent aerosolization properties. The aim of this study was, first, to formulate such particles with excipients that are either FDA-approved for inhalation or endogenou...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018910200420
更新日期：1999-11-01 00:00:00
abstract：:Nanobiosensors with high sensitivity and specificity have shown great potential in the detection of diseases. The incorporation of therapeutic agents with nanobiosensors allows the simultaneous diagnosis and therapy of diseases. The delivery of nanobiosensors and therapeutic agents using polymers is a common strategy ...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-016-1944-y
更新日期：2016-10-01 00:00:00
abstract：:A method for determination of absorption rate and bioavailability was developed to reduce the influence of intraindividual variability and applied to the absolute intraperitoneal availability of lithium in the rat. In this method the test and the reference doses are given with a few hours' interval, and the resulting ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015939917646
更新日期：1989-09-01 00:00:00
abstract：PURPOSE:To develop an isolated perfused rat liver (IPRL) model with low baseline levels of tumor necrosis factor (TNF)-alpha in the outlet perfusate to study the effects of immunostimulants and immunosuppressants on the release of TNF-alpha from this organ. METHODS:Isolated rat livers were perfused with a buffer conta...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1013603331899
更新日期：2002-01-01 00:00:00
abstract：:The mechanism of release from sustained-release adinazolam mesylate tablets was assessed by the Higuchi equation and by analysis of drug release profiles through 60% released using the Peppas equation. Computed values of the diffusional exponent, n, ranged from 0.59 to 0.66. Values of n in this range are consistent wi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015834114359
更新日期：1991-12-01 00:00:00
abstract：PURPOSE:The purpose of this investigation was to determine the influence on the antimicrobial activity of cetylpyridinium chloride of the various components of the formulation of each of six candy based lozenges. METHODS:In vivo activity was investigated using six volunteers by determining the reduction in colony form...
journal_title：Pharmaceutical research
pub_type： 临床试验,杂志文章
doi：10.1023/a:1016002322692
更新日期：1996-04-01 00:00:00
abstract：:The three-dimensional structures and molecular electrostatic potentials of the cis(Z) and trans(E)-isomers of flupenthixol and clopenthixol were examined by computer graphics and molecular mechanical and quantum mechanical calculations, and their internal molecular motions were studied by molecular dynamics simulation...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015842926345
更新日期：1991-04-01 00:00:00
abstract：PURPOSE:To investigate the ability of various polymers to inhibit the crystallization of amorphous felodipine from amorphous molecular dispersions in the presence of absorbed moisture. METHODS:Spin coated films of felodipine with poly(vinylpyrrolidone) (PVP), hydroxypropylmethylcellulose acetate succinate (HPMCAS) and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9331-3
更新日期：2008-04-01 00:00:00
abstract：PURPOSE:To evaluate the use of an in vitro intestinal permeability model to predict rat and human absorption as well as to evaluate the use of an internal standard to control for intra- and inter-rat variability. METHODS:In vivo peroral absorption and in vitro steady-state intestinal permeability coefficients were det...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012148300807
更新日期：1997-12-01 00:00:00
abstract：PURPOSE:To develop a statistical model for predicting effect of food on the extent of absorption (area under the curve of time-plasma concentration profile, AUC) of drugs based on physicochemical properties. MATERIALS AND METHODS:Logistic regression was applied to establish the relationship between the effect of food ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9236-1
更新日期：2007-06-01 00:00:00
abstract：:Unsymmetrical aryl(heteroaryl)methyl isopropyl ester analogues of nifedipine, in which the 2-nitrophenyl group at C-4 is replaced by a 2- or 3-pyridyl substituent, were synthesized and evaluated as calcium-channel antagonists using guinea pig ileal longitudinal smooth muscle. The point of attachment of the C-4 pyridyl...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015941706008
更新日期：1990-09-01 00:00:00
abstract：PURPOSE:This study seeks to develop fiber membranes for local sustained delivery of 25-hydroxyvitamin D3 to induce the expression and secretion of LL-37 at or near the surgical site, which provides a novel therapeutic approach to minimize the risk of infections. METHODS:25-hydroxyvitamin D3 loaded poly(L-lactide) (PLA...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1667-5
更新日期：2015-09-01 00:00:00
abstract：PURPOSE:Stable transformants expressing human multidrug resistance 1 (MDR1), monkey MDR1, canine MDR1, rat MDR1a, rat MDR1b, mouse mdr1a, and mouse mdr1b in LLC-PK1 were established to investigate species differences in P-glycoprotein (P-gp, ABCB1) mediated efflux activity. METHODS:The seven cDNAs of MDR1 from five an...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-0285-7
更新日期：2006-07-01 00:00:00
abstract：PURPOSE:To analyze the mechanics of some pharmaceutical agglomerates during uniaxial confined compression by using compression parameters derived from the Heckel, Kawakita and Adams equations, and to study the influence of these compression parameters on the tablet-forming ability of agglomerates. METHODS:Force and di...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007575120817
更新日期：2000-08-01 00:00:00
abstract：PURPOSE:The purpose of this work was to determine the jejunal permeability of cyclosporin A (CsA) in humans and whether formulation variables modulate the effects of P-glycoprotein (P-gp) on the permeability of CsA in Caco-2 cells. METHODS:A solution containing CsA, phenylalanine, propranolol, polyethyleneglycol (PEG)...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1023481418576
更新日期：2003-05-01 00:00:00
abstract：:Chimeric L6 is a mouse-human monoclonal antibody specific for tumor cell-associated antigens. The factors affecting the physical and chemical stability of chimeric L6 were assessed at elevated temperatures (30-60 degrees C) and by multiple freezing and thawing. Three routes of degradation were observed: chemical degra...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018948901599
更新日期：1994-05-01 00:00:00
abstract：PURPOSE:Models to predict membrane-water partition coefficients (Kp) as a function of drug structure, membrane composition, and solution properties would be useful. This study explores the partitioning of dexamethasone (Dex) and its ionizable 21-phosphate (Dex-P) in liposomes varying in acyl chain length, physical stat...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1143-z
更新日期：2013-12-01 00:00:00
abstract：PURPOSE:The purpose of this study was (i) to develop glancing angle x-ray powder diffractometry (XRD) as a method for profiling phase transformations as a function of tablet depth; and (ii) to apply this technique to (a) study indomethacin crystallization during dissolution of partially amorphous indomethacin tablets a...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000012163.89163.f8
更新日期：2004-01-01 00:00:00
abstract：:Effects of protease inhibitors and absorption enhancers on the absorption of salmon calcitonin (sCT) were evaluated after intratracheal coadministration to rats using the plasma Ca level as an index. Remarkable absorption enhancement could be attained with unsaturated fatty acids such as oleic acid and polyoxyethylene...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018926007902
更新日期：1994-09-01 00:00:00
abstract：PURPOSE:The aim of the present study was to improve the dry powder inhalation behavior of steroid KSR-592 with lactose by altering the crystal shape and the particle size of the drug for use in a newly designed inhalation device, Jethaler. METHOD:The shape of the crystals was changed by polymorphic transformation of o...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1020492213172
更新日期：2002-10-01 00:00:00
abstract：PURPOSE:The objective of this study was to elucidate the different mechanisms of action of different excipients on the oxidation of Met1, Met122, Met127, and Met138 in granulocyte colony-stimulating factor (G-CSF) by using hydrogen peroxide as the oxidant. METHODS:The oxidation of Met1, Met127, and Met138 was quantifi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-004-9019-x
更新日期：2005-01-01 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
abstract：PURPOSE:To show, using a model study, how electronic structure theory can be applied in combination with LC/UV/MS/MS for the prediction and identification of oxidative degradants. METHODS:The benzyloxazole 1, was used to represent an active pharmaceutical ingredient for oxidative forced degradation studies. Bond disso...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000041469.96466.12
更新日期：2004-09-01 00:00:00
abstract：PURPOSE:Novel therapeutics are greatly needed that target specific pathological receptors and pathways involved in Neuropathic Pain (NP). Extending our previous work published in this Journal on Group I metabotropic glutamate receptor (mGluR) modulators, we now investigate the therapeutic potential of niclosamide in mo...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2027-9
更新日期：2016-12-01 00:00:00
abstract：PURPOSE:The aim of the study was to investigate whether dopamine is transferred along the olfactory pathway to the brain following nasal administration to mice. METHODS:[3H]-Dopamine was administered nasally or intravenously to female mice. Brain tissue samples were excised and the radioactive content was measured. Th...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007542618378
更新日期：2000-06-01 00:00:00
abstract：PURPOSE:Prostaglandin E(1) (PGE(1)) is an effective treatment for peripheral vascular diseases. The encapsulation of PGE(1) in nanoparticles for its sustained-release would improve its therapeutic effect and quality of life (QOL) of patients. METHODS:In order to encapsulate PGE(1) in nanoparticles prepared with a poly...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9891-5
更新日期：2009-07-01 00:00:00
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
更新日期：2014-10-01 00:00:00
abstract：PURPOSE:The aim of this study is to investigate the effects of 50% ethyl acetate extracts of grapefruit juice (GFJ) and orange juice (OJ) on the transport activity of P-glycoprotein (P-gp) in the rat small intestine. METHODS:The efflux of P-gp substrates from rat everted sac in the absence or presence of verapamil, GF...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016100715125
更新日期：2002-06-01 00:00:00
