Abstract:
:Under the heading "Methods-Synthesis of the Bioreducible Modified-PAE (mPAE)", on page 3, line 14-17, there is an error. The quantity unit of PAE and 2-iminothiolane hydrochloride needs to be corrected to mg instead of g.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Gandhi NS,Godeshala S,Koomoa-Lange DT,Miryala B,Rege K,Chougule MBdoi
10.1007/s11095-018-2488-0subject
Has Abstractpub_date
2018-09-05 00:00:00pages
202issue
11eissn
0724-8741issn
1573-904Xpii
10.1007/s11095-018-2488-0journal_volume
35pub_type
杂志文章,已发布勘误abstract:PURPOSE:Targeted delivery of aerosols could not only improve efficacy of inhaled drugs but also reduce side effects resulting from their accumulation in healthy tissue. Here we investigated the impact of magnetized aerosols on model drug accumulation and transgene expression in magnetically targeted lung regions of una...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0682-z
更新日期:2012-05-01 00:00:00
abstract:PURPOSE:We recently showed that the perfusion of isolated rat livers with perfusates containing bovine serum albumin (BSA) would significantly stimulate the release of tumor necrosis factor (TNF)-alpha. Here, we hypothesize that BSA-induced increase in the release of TNF-alpha, and possibly other cytokines, would affec...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1022202926073
更新日期:2003-01-01 00:00:00
abstract:PURPOSE:The use of dendrimers for biomedical applications has emerged with promising results. 2G-NN16 is a carbosilane dendrimer with sixteen positive charges per molecule tested to be capable to bind and release antisense oligonucleotides (ODNs) and small interference RNA (siRNA) in vitro. In spite of low cytotoxicity...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9776-z
更新日期:2009-03-01 00:00:00
abstract:PURPOSE:The aim was to replace the traditional 21-day Caco-2 permeability protocol by a more high-throughput assay. METHODS:Caco-2 cells were seeded at high density in 96-well plates in novel cell culture boxes. After 7 days, drug permeability studies were performed. Samples were analyzed by a new UV detection method....
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000008043.71001.43
更新日期:2003-12-01 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:We reported that suramin produced chemosensitization at nontoxic doses. This benefit was lost at the approximately 10-fold higher, maximally tolerated doses (MTD). The aim of the current study was to identify in patients the chemosensitizing suramin dose that delivers 10-50 microM plasma concentrations over 48 ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-0165-1
更新日期:2006-06-01 00:00:00
abstract::The binding of 1-anilino-8-naphthalenesulfonate (ANS) to bovine serum albumin (BSA), human serum albumin (HSA), and human plasma has been studied by potentiometric titration utilizing a laboratory constructed ion selective electrode (ISE) of ANS. Three classes of ANS binding sites were found on BSA, HSA, and plasma at...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015855613083
更新日期:1991-07-01 00:00:00
abstract:PURPOSE:Overexpression of hyaluronan (HA) receptors on cancer cells results in enhanced endocytotic uptake of the drug conjugate. An N-(2-hydroxypropyl)methacrylamide (HPMA)-HA polymeric drug delivery system was used for targeted delivery of doxorubicin to cancer cells. METHODS:HA-doxorubicin (DOX) bioconjugates (HA-D...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015170907274
更新日期:2002-04-01 00:00:00
abstract:PURPOSE:To study Cereport (RMP-7, bradykinin B2 agonist) effects on human brain microvascular endothelial cell (HBMEC) monolayer permeability. METHODS:HBMEC grown on transwell membranes were exposed to Cereport. The monolayer permeability was determined with [14C]-inulin (MW. 5,200) and [3H]-dextran (MW. 70,000). RES...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018938722768
更新日期:1999-09-01 00:00:00
abstract:PURPOSE:Melanoma is an aggressive neoplasm with a propensity for metastases and resistance to therapy. Previously, we showed that (-)-epigallocatechin-3-gallate (EGCG), the major polyphenolic antioxidant present in green tea, resulted in a significant decrease in the viability and growth of melanoma and induction of ap...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0054-5
更新日期:2010-06-01 00:00:00
abstract:PURPOSE:To study the influence of crystallizing and non-crystallizing cosolutes on the crystallization behavior of trehalose in frozen solutions and to monitor the phase behavior of trehalose dihydrate and mannitol hemihydrate during drying. METHODS:Trehalose (a lyoprotectant) and mannitol (a bulking agent) are widely...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0221-8
更新日期:2010-11-01 00:00:00
abstract:PURPOSE:Performance of a transdermal delivery system (TDS) can be affected by exposure to elevated temperature, which can lead to unintended safety issues. This study investigated TDS and skin temperatures and their relationship in vivo, characterized the effective thermal resistance of skin, and identified the in vitr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2171-x
更新日期:2017-07-01 00:00:00
abstract:PURPOSE:To determine the factors influencing "solid solubility" and phase separation kinetics of drugs from amorphous solid dispersions. METHODS:Solid dispersions of griseofulvin-poly(vinyl pyrrolidone) (PVP) and indoprofen-PVP were prepared using solvent evaporation technique. Dispersions demonstrating single Tg were...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-1882-y
更新日期:2005-03-01 00:00:00
abstract:PURPOSE:To examine the changes in expression levels of CYP3A4 and efflux transporters in CYP3A4-transfected Caco-2 (colon carcinoma) cells in the presence of the inducers sodium butyrate (NaB) and 12-O-tetradecanoylphorbol-13-acetate (TPA). To characterize the transport of [3H]-digoxin and the metabolism of midazolam i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1010914624111
更新日期:2001-08-01 00:00:00
abstract:PURPOSE:The heats of reaction between the enantiomers and racemates of ibuprofen and naproxen and human serum albumin (HSA) are to be measured with and without the addition of octanoic acid. The effects of octanoic acid on the free energies of interaction between the drugs and HSA is to be determined and compared to th...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016066325476
更新日期:1996-01-01 00:00:00
abstract:PURPOSE:Modulation of 5-HT3 receptor in the central nervous system (CNS) is a promising approach for treatment of neuropathic pain. The goal was to evaluate the role of P-glycoprotein (Pgp) in limiting exposure of different parts of the CNS to ondansetron (5-HT3 receptor antagonist) using wild-type and genetic knockout...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02929-2
更新日期:2020-09-28 00:00:00
abstract:PURPOSE:Tissue partitioning is an important component of drug distribution and half-life. Protein binding and lipid partitioning together determine drug distribution. METHODS:Two structure-based models to predict partitioning into microsomal membranes are presented. An orientation-based model was developed using a mem...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2085-z
更新日期:2017-03-01 00:00:00
abstract:PURPOSE:To determine the effect of Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate (SNAC) on the permeation of cromolyn across Caco-2 cell monolayers and explore the molecular basis for the enhanced absorption. METHODS:Transport studies of cromolyn across Caco-2 cell monolayers were conducted in the presence of various ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-7671-9
更新日期:2004-12-01 00:00:00
abstract::We report the chemical and enzymatic hydrolysis of two hydrophobic prodrugs of ganciclovir (3 = dipropionate ester; 4 = diadamantoate ester). Both prodrugs undergo hydrolysis showing a pH dependence of kobs = kH+aH+ + ko + kHO-aHO- and a pH of maximum stability near pH 5. Only 4 exhibited a shelf life (t90) greater th...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015809408908
更新日期:1991-11-01 00:00:00
abstract:PURPOSE:The purpose of the study was to examine the suitability of using laser diffraction to measure the fine particle fraction (FPF) of drugs emitted from carrier-free dry powder aerosol formulations. MATERIALS AND METHODS:Particle size distribution of terbutaline sulphate from Bricanyl Turbohaler, which contained l...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9056-8
更新日期:2006-09-01 00:00:00
abstract:PURPOSE:This study focuses on the formulation optimization, in vitro and in vivo performance of differently sized nano-crystalline liquid suspensions and spray-dried powders of a poorly soluble BCS class II compound i.e. Danazol. METHODS:A DoE approach was utilized to optimize stabilizer concentration and formulate da...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1567-0
更新日期:2015-05-01 00:00:00
abstract::Interogan variation in tissue distribution of weakly basic drugs such as quinidine, propranolol, and imipramine was investigated as a function of binding to phosphatidylserine (PhS) in tissues. Tissue distributions of these drugs were determined using 10 different tissues at a steady-state plasma concentration and wer...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015935031933
更新日期:1990-10-01 00:00:00
abstract::Porcine pancreatic elastase, a well-characterized serine protease, has been used as a model to assess the effects of excessive humidity on solid-state stability of the lyophilized protein. Elastase lyophilized without excipients retained full activity immediately after freeze-drying but became denatured upon continued...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018979410338
更新日期:1993-10-01 00:00:00
abstract:PURPOSE:A thermodynamic analysis of the binding to rat cortex adenosine A1 receptor of N6-substituted (full agonists) and N6-substituted-deoxyribose (partial agonists) adenosine derivatives was performed. The intrinsic activity of the compounds was evaluated by measurements of the inhibition of forskolin stimulated 3',...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018987816891
更新日期:1999-07-01 00:00:00
abstract:PURPOSE:To evaluate and classify the hydrolases of the primate lung. METHODS:Homologous series of aromatic, aliphatic, and choline ester substrates were assayed with the pH-stat method to obtain the Michaelis-Menten kinetic constants, Vmax and K(m), for the enzymes in pulmonary alveolar tissue with esterase activity. ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012004911942
更新日期:1997-02-01 00:00:00
abstract:PURPOSE:This work investigated the effect of relative humidity (RH) on bipolar electrostatic charge profiles of dry powder inhaler aerosols using the Bipolar Charge Analyzer (BOLAR). METHODS:Two commercial products, Pulmicort® (400 μg, budesonide) and Bricanyl® (500 μg, terbutaline sulfate) Turbuhaler®, were used as m...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2178-3
更新日期:2017-08-01 00:00:00
abstract:PURPOSE:The objective of this study was to investigate the possible influence of probenecid on morphine transport across the blood-brain barrier (BBB) in rats. METHODS:Microdialysis probes, calibrated using retrodialysis by drug, were placed into the striatum and jugular vein of seven Sprague-Dawley rats. Morphine was...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023250900462
更新日期:2003-04-01 00:00:00
abstract::5'-Ester derivatives of 5-iodo-2'-deoxyuridine (IDU) with varying degrees of lipophilicity were examined to evaluate the effectiveness of lipophilic ester prodrugs for enhanced and sustained delivery of IDU to the brain parenchyma. Approximately 1.0% (1.0 +/- 0.19; n = 4) of the total radioactivity was found in the br...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015803922401
更新日期:1992-09-01 00:00:00
abstract::A novel method of dipeptide synthesis is described that can be carried out in aqueous solution and does not require complicated protecting and deprotecting procedures. An analgesic neuropeptide named kyotorphin, H-Tyr-Arg-OH, was synthesized from unprotected tyrosine and arginine in a new enzymatic reaction catalyzed ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016479305603
更新日期:1987-04-01 00:00:00
abstract:PURPOSE:Previous literature has suggested the absence of an effective barrier between the nasal mucosa and the brain for compounds administered via the nasal route. These experiments were conducted to elucidate the role of the blood-brain barrier efflux transporter P-glycoprotein (P-gp) in attenuating delivery of P-gp ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1025053115583
更新日期:2003-08-01 00:00:00