Targeted delivery of doxorubicin by HPMA copolymer-hyaluronan bioconjugates.

abstract：PURPOSE:To describe a computational tool to calculate molecular descriptors of potential application in ADME virtual screening of antitumor Pt(II) drug candidates. METHODS:The multistep computational procedure consists in (a) building and optimization (PM3) of the 3D structures of the investigated complexes, (b) param...

journal_title：Pharmaceutical research

authors： Caron G,Ravera M,Ermondi G

更新日期：2011-03-01 00:00:00

abstract：PURPOSE:Using monolayers of human pancreatic adenocarcinoma cells (Panc-1) that express multidrug resistance-associated protein (MRP), the present work investigates the effects of Pluronic block copolymers on the functional activity of MRP. METHODS:The studies examined the accumulation and efflux of the MRP selective ...

journal_title：Pharmaceutical research

authors： Miller DW,Batrakova EV,Kabanov AV

更新日期：1999-03-01 00:00:00

abstract：PURPOSE:Orthorhombic crystals of paracetamol exhibit good technological properties during compression. The purpose of this study was to investigate the compression behavior of this substance and to compare it to that of monoclinic paracetamol. From the crystal structure, it could be hypothesized that sliding planes are...

journal_title：Pharmaceutical research

authors： Joiris E,Di Martino P,Berneron C,Guyot-Hermann AM,Guyot JC

更新日期：1998-07-01 00:00:00

abstract：:The present review discusses drugs and counter ions suitable for ion pair transport (IPT). Ion pairing is shown to effectively increase the lipophilicity and transport rate of polar drugs across lipid membranes. The proposed mechanisms of IPT are discussed in detail. A marked change in drug properties upon ion pair fo...

journal_title：Pharmaceutical research

authors： Neubert R

更新日期：1989-09-01 00:00:00

abstract：PURPOSE:The objective of the present work was to prepare safe and effective Ciclosporin A Lipid nanocapsule (CsA-LNC) eye-drops for the treatment of DED. METHODS:The phase-inversion method was used to prepared different sizes CsA-LNC. CsA biodistribution in ocular after topical administration in rabbits was analyzed b...

journal_title：Pharmaceutical research

authors： Zhang A,Sun R,Ran M,Deng Y,Ge Y,Zhu Y,Tao X,Shang L,Gou J,He H,Yin T,Wang Y,Zhang Y,Tang X

更新日期：2020-07-14 00:00:00

abstract：PURPOSE:To identify High Molecular Weight Products (HMWP) formed in human insulin formulation during storage. METHODS:Commercial formulation of human insulin was stored at 37°C for 1 year and HMWP was isolated using preparative size exclusion chromatography (SEC) and reverse phase (RP) chromatography. The primary stru...

journal_title：Pharmaceutical research

authors： Hjorth CF,Hubálek F,Andersson J,Poulsen C,Otzen D,Naver H

更新日期：2015-06-01 00:00:00

abstract：:Apigenin, a naturally occurring plant flavone, abundantly present in common fruits and vegetables, is recognized as a bioactive flavonoid shown to possess anti-inflammatory, antioxidant and anticancer properties. Epidemiologic studies suggest that a diet rich in flavones is related to a decreased risk of certain cance...

journal_title：Pharmaceutical research

authors： Shukla S,Gupta S

更新日期：2010-06-01 00:00:00

abstract：PURPOSE:A patient was denoted to be generic brittle (GB) if they had a negative opinion about generics (e.g. prior history of a switch problem) or took the innovator brand of their most problematic anti-epileptic drug (AED) when generic was available. The aim of this hypothesis-generating study was to assess possible g...

journal_title：Pharmaceutical research

authors： Das S,Guo D,Jiang X,Jiang W,Shu Y,Ting TY,Polli JE

更新日期：2020-02-26 00:00:00

abstract：PURPOSE:This study was aimed to investigate the effects of a phenolic antioxidant, butylated hydroxyanisole (BHA) and its metabolite, tert-butylhydroquinone (tBHQ) on the induction of HO-1, NQO1 and Nrf2 proteins and their regulatory mechanisms in primary-cultured hepatocytes. METHODS:After exposure of BHA and tBHQ to...

journal_title：Pharmaceutical research

authors： Keum YS,Han YH,Liew C,Kim JH,Xu C,Yuan X,Shakarjian MP,Chong S,Kong AN

更新日期：2006-11-01 00:00:00

abstract：PURPOSE:To evaluate the effect of re-directing the uptake mechanism of polyplexes containing oligodeoxynucleotide (ODN) decoys to nuclear factor kappa B (NF-kappaB) from absorptive-mediated to receptor-mediated endocytosis. MATERIALS AND METHODS:Complexes of ODNs and a co-polymer of biotin-polyethylenglycol and polyet...

journal_title：Pharmaceutical research

authors： Bhattacharya R,Osburg B,Fischer D,Bickel U

更新日期：2008-03-01 00:00:00

abstract：PURPOSE:A plasmid-based gene expression system was complexed with protective, interactive, and non-condensing (PINC) polymer system and administered with Medi-Jector, a needle-free injection device (NFID), to achieve high and sustained levels of antigen-specific antibodies in blood circulation. METHODS:Human growth ho...

journal_title：Pharmaceutical research

authors： Anwer K,Earle KA,Shi M,Wang J,Mumper RJ,Proctor B,Jansa K,Ledebur HC,Davis S,Eaglstein W,Rolland AP

更新日期：1999-06-01 00:00:00

abstract：PURPOSE:To determine of the pharmacokinetic profile of methotrexate (MTX) in blood and extracellular fluid (ECF) of VX2 tumor and muscle in rabbits. METHODS:Microdialysis probes were inserted into VX2 tumor and in muscle tissue. Following intravenous administration of MTX (30 mg/kg), serial collection of arterial bloo...

journal_title：Pharmaceutical research

authors： Dukic S,Kaltenbach ML,Gourdier B,Marty H,Vistelle R

更新日期：1998-01-01 00:00:00

abstract：:Penetration of various compounds through shed snake skin was measured in vitro to examine the effect of lipophilicity and molecular size of a compound on permeability through this model membrane. The permeabilities were found to be controlled by the lipophilicity and the molecular size of the permeant. The smaller and...

journal_title：Pharmaceutical research

authors： Itoh T,Magavi R,Casady RL,Nishihata T,Rytting JH

更新日期：1990-12-01 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

authors： Vuppugalla R,Shah RB,Chimalakonda AP,Fisher CW,Mehvar R

更新日期：2003-01-01 00:00:00

abstract：:Leucine enkephalin (YGGFL) undergoes rapid degradation in sheep nasal mucosa to yield GGFL which is further degraded to FL. The activity of the nasal mucosal homogenate against YGGFL and GGFL (t1/2 12 and 7 min) was significantly greater than that observed with a nasal wash fluid (t1/2 40 and 13 min). The effect of cy...

journal_title：Pharmaceutical research

authors： Irwin WJ,Dwivedi AK,Holbrook PA,Dey MJ

更新日期：1994-12-01 00:00:00

abstract：PURPOSE:To elucidate the apical and basolateral components of the total unstirred water layer in regular permeability experiment. METHODS:A novel stirring apparatus was constructed to remove the basolateral unstirred water layer. Caco-2 cells were used as the permeability barrier both in Transwell-type and side-by-sid...

journal_title：Pharmaceutical research

authors： Korjamo T,Heikkinen AT,Waltari P,Mönkkönen J

更新日期：2008-07-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate transepithelial ionic permeation via the paracellular pathway of human Caco-2 epithelial monolayers and its contribution to absorption of the base guanidine. METHODS:Confluent monolayers of Caco-2 epithelial cells were mounted in Ussing chambers and the transepithelial ...

journal_title：Pharmaceutical research

authors： Carr G,Haslam IS,Simmons NL

更新日期：2006-03-01 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

authors： Mackic JB,Stins M,Jovanovic S,Kim KS,Bartus RT,Zlokovic BV

更新日期：1999-09-01 00:00:00

abstract：PURPOSE:To investigate the potential of a novel lipid carrier, comprising beads of alpha-cyclodextrin and soybean oil, for topical drug delivery. Adapalene was chosen as a model drug to explore the ability of the beads to encapsulate and release a highly lipophilic compound. MATERIALS AND METHODS:Adapalene-loaded bead...

journal_title：Pharmaceutical research

authors： Trichard L,Delgado-Charro MB,Guy RH,Fattal E,Bochot A

更新日期：2008-02-01 00:00:00

abstract：PURPOSE:There is evidence that cholesterol affects the ATPase and transport functions of P-glycoprotein (P-gp). To study the influence of cholesterol on P-gp in a well defined lipid environment, we reconstituted P-gp in egg phosphatidylcholine (PhC) and PhC/cholesterol proteoliposomes with negligible residual amounts o...

journal_title：Pharmaceutical research

authors： Bucher K,Belli S,Wunderli-Allenspach H,Krämer SD

更新日期：2007-11-01 00:00:00

abstract：PURPOSE:SN-38, a potent chemotherapeutic drug, has not been used clinically because of its severe side effects and poor solubility. In this work, we aimed to evaluate the effect of dose and multiple injections of SN-38-loaded polymeric depots on antitumor efficacy and toxicity in vivo. METHODS:Preparation and characte...

journal_title：Pharmaceutical research

authors： Manaspon C,Nasongkla N,Chaimongkolnukul K,Nittayacharn P,Vejjasilpa K,Kengkoom K,Boongird A,Hongeng S

更新日期：2016-12-01 00:00:00

abstract：:Antibody drug conjugates (ADCs) are a class of therapeutics that combine the target specificity of an antibody with the potency of a chemotherapeutic. This therapeutic strategy can significantly expand the therapeutic index of a chemotherapeutic by minimizing the systemic exposure and associated toxicity of the chemot...

journal_title：Pharmaceutical research

authors： Lin K,Tibbitts J

更新日期：2012-09-01 00:00:00

abstract：PURPOSE:Chemically modified heparin-DOCA was prepared and found to have markedly lower anticoagulant activity than heparin. In the present study, we elucidated the antiangiogenic and antitumoral activities of heparin-DOCA derivative. METHODS:To evaluate the antiangiogenic and antitumoral effects of heparin-DOCA, capil...

journal_title：Pharmaceutical research

authors： Park K,Kim YS,Lee GY,Nam JO,Lee SK,Park RW,Kim SY,Kim IS,Byun Y

更新日期：2007-01-01 00:00:00

abstract：:Various carboxylic acid esters of the N-hydroxymethyl derivative of N-benzyloxycarbonylglycine benzylamide, used as a peptide-like model, were prepared and their decomposition kinetics studied in aqueous solution and in human plasma solutions. These N-acyloxymethylamide derivatives were found to undergo a facile decom...

journal_title：Pharmaceutical research

authors： Bundgaard H,Rasmussen GJ

更新日期：1991-10-01 00:00:00

abstract：PURPOSE:To improve the delivery of liposomes to tumors using P-selectin glycoprotein ligand 1 (PSGL1) mediated binding to selectin molecules, which are upregulated on tumorassociated endothelium. METHODS:PSGL1 was orientated and presented on the surface of liposomes to achieve optimal selectin binding using a novel st...

journal_title：Pharmaceutical research

authors： Carlisle R,Seymour LW,Coussios CC

更新日期：2013-02-01 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

authors： Grevel J,Thomas J,Richards ML,Sadée W

更新日期：1984-09-01 00:00:00

abstract：PURPOSE:Permeation studies, with near infrared (NIR) light and anti-aggregation antibody formulation, were used to investigate the in vitro permeation of bevacizumab, ranibizumab and aflibercept through human sclera. METHODS:A vertical, spherical Franz cell diffusion apparatus was used for this scleral tissue permeati...

journal_title：Pharmaceutical research

authors： Giannos SA,Kraft ER,Zhao ZY,Merkley KH,Cai J

更新日期：2018-03-29 00:00:00

abstract：PURPOSE:Our previous studies showed that the mRNA level of human organic anion transporter (hOAT) 3 in the kidney was correlated with the rate of elimination of an anionic antibiotic cefazolin. However, the correlation coefficient was not so high. In the present study, therefore, we enrolled more patients to examine wh...

journal_title：Pharmaceutical research

authors： Sakurai Y,Motohashi H,Ogasawara K,Terada T,Masuda S,Katsura T,Mori N,Matsuura M,Doi T,Fukatsu A,Inui K

更新日期：2005-12-01 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

authors： Jerremalm E,Hedeland M,Wallin I,Bondesson U,Ehrsson H

更新日期：2004-05-01 00:00:00

abstract：PURPOSE:To examine the iontophoretic delivery of ALA as a function of pH and to determine the principal mechanisms responsible for its electrotransport. METHODS:Anodal iontophoretic transport of ALA was measured as a function of its concentration and pH of the donor solution. Experiments were performed in vitro using ...

journal_title：Pharmaceutical research

authors： Lopez RF,Bentley MV,Delgado-Charro MB,Guy RH

更新日期：2001-03-01 00:00:00