Natural and synthetic polymers as inhibitors of drug efflux pumps.

abstract：PURPOSE:E-selectin is a cell adhesion molecule that is specifically expressed in the inflammatory vascular endothelium in response to cytokines such as IL-1 beta and TNF-alpha, and interacts with specific ligands containing sialyl Lewis X (Neu5Ac alpha 2-3Gal beta 1-4(Fuc alpha 1-3)GlcNAc-, SLex). In order to investiga...

journal_title：Pharmaceutical research

authors： Horie K,Sakagami M,Kuramochi K,Hanasaki K,Hamana H,Ito T

更新日期：1999-02-01 00:00:00

abstract：PURPOSE:Generalizations based upon behavior of small molecules have established that a crystalline solid is generally much more stable toward chemical degradation than is the amorphous solid. This study examines the validity of this generalization for proteins using biosynthetic human insulin as the model protein. MET...

journal_title：Pharmaceutical research

authors： Pikal MJ,Rigsbee DR

更新日期：1997-10-01 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

authors： Alsenz J,Haenel E

更新日期：2003-12-01 00:00:00

abstract：:Solution calorimetry has been employed to evaluate the stability constants and enthalpy changes associated with complex formation between alpha-, beta, or gamma-cyclodextrin (CD) and a group of amine compounds having the diphenylmethyl functionality. Data from thermal titrations of the compounds were analyzed using no...

journal_title：Pharmaceutical research

authors： Tong WQ,Lach JL,Chin TF,Guillory JK

更新日期：1991-07-01 00:00:00

abstract：PURPOSE:A polysaccharide-flavonoid conjugate was developend and proposed for the treatment of pancreatic ductal adenocarcinoma (PDAC). METHODS:The conjugate was synthesized by free radical grafting reaction between catechin and dextran. The chemical characterization of the conjugate was obtained by UV-Vis, 1H-NMR, FT-...

journal_title：Pharmaceutical research

authors： Vittorio O,Cirillo G,Iemma F,Di Turi G,Jacchetti E,Curcio M,Barbuti S,Funel N,Parisi OI,Puoci F,Picci N

更新日期：2012-09-01 00:00:00

abstract：PURPOSE:β-Hydroxy-β-methylbutyrate (HMB), a nutritional supplement, elicits anabolic activity in muscle. Here we investigated the mechanism of HMB uptake in muscle cells. METHODS:Murine muscle cells (C2C12) and human mammary epithelial cells (MCF7) were used for uptake. As HMB is a monocarboxylate, focus was on monoca...

journal_title：Pharmaceutical research

authors： Ogura J,Sato T,Higuchi K,Bhutia YD,Babu E,Masuda M,Miyauchi S,Rueda R,Pereira SL,Ganapathy V

更新日期：2019-04-17 00:00:00

abstract：PURPOSE:Indocyanine green (ICG), an FDA-approved near infrared (NIR) dye, has potential application as a contrast agent for tumor detection. Because ICG binds strongly to plasma proteins and exhibits aqueous, photo, and thermal instability, its current applications are largely limited to monitoring blood flow. To addre...

journal_title：Pharmaceutical research

authors： Kim TH,Chen Y,Mount CW,Gombotz WR,Li X,Pun SH

更新日期：2010-09-01 00:00:00

abstract：PURPOSE:The purpose of this human intestinal perfusion study was to investigate the transport and metabolism of R/S-verapamil in the human jejunum (in vivo). METHODS:A regional single-pass perfusion of the jejunum was performed using a Loc-I-Gut perfusion tube in 12 healthy volunteers. Each perfusion lasted for 200 mi...

journal_title：Pharmaceutical research

authors： Sandström R,Karlsson A,Knutson L,Lennernäs H

更新日期：1998-06-01 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

authors： Akula MR,Matowe WC,Wolowyk MW,Knaus EE

更新日期：1990-09-01 00:00:00

abstract：:The Office of Generic Drugs has ensured the high quality of generic products based upon two requirements: pharmaceutical equivalence and bioequivalence to the reference listed drug (RLD). This paradigm has been used with success toward ensuring quality generic drug products that provide the same therapeutic benefit as...

journal_title：Pharmaceutical research

authors： Raw AS,Lionberger R,Yu LX

更新日期：2011-07-01 00:00:00

abstract：PURPOSE:To devise experimental and computational models to predict aqueous drug solubility. METHODS:A simple and reliable modification of the shake flask method to a small-scale format was devised, and the intrinsic solubilities of 17 structurally diverse drugs were determined. The experimental solubility data were us...

journal_title：Pharmaceutical research

authors： Bergström CA,Norinder U,Luthman K,Artursson P

更新日期：2002-02-01 00:00:00

abstract：PURPOSE:To assess the efficacy of lipid-protein-sugar particles (LPSPs) in providing prolonged duration local anesthesia by percutaneous injection. METHODS:Bupivacaine-containing LPSPs were characterized and optimized in vitro. Male Sprague-Dawley rats were given sciatic nerve blocks with bupivacaine-containing LPSPs....

journal_title：Pharmaceutical research

authors： Kohane DS,Lipp M,Kinney RC,Lotan N,Langer R

更新日期：2000-10-01 00:00:00

abstract：:Physiologically-based pharmacokinetic (PBPK) models explicitly incorporate tissue-specific blood flows, partition coefficients, and metabolic processes. Since PBPK models are derived using physiologic parameters and interactions of the compound with tissue components, these models are considered to be "bottom up" as o...

journal_title：Pharmaceutical research

authors： Korzekwa K,Nagar S

更新日期：2017-03-01 00:00:00

abstract：PURPOSE:To develop novel biomineral-binding liposomes (BBL) for the prevention of orthopedic implant associated osteomyelitis. METHODS:A biomineral-binding lipid, alendronate-tri(ethyleneglycol)-cholesterol conjugate (ALN-TEG-Chol), was synthesized through Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition (a versatile...

journal_title：Pharmaceutical research

authors： Liu XM,Zhang Y,Chen F,Khutsishvili I,Fehringer EV,Marky LA,Bayles KW,Wang D

更新日期：2012-11-01 00:00:00

abstract：:Short-lived gamma emitting radioisotopes can be incorporated into polylactide/glycolide polymeric microspheres with various specific activities for possible use in understanding the in-vivo deposition, distribution and clearance of microparticulate drug carrier systems. The incorporated radiolabel is stable with negli...

journal_title：Pharmaceutical research

authors： Thanoo BC,Doll WJ,Mehta RC,Digenis GA,DeLuca PP

更新日期：1995-12-01 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

authors： Valsami GN,Macheras PE,Koupparis MA

更新日期：1991-07-01 00:00:00

abstract：:The effects of tertiary amine-containing basic drugs on the enzymes located in the mitochondria and the effect of monoamine oxidase inhibitors (MAOIs) on drug accumulation in lung mitochondria have been studied. Various basic drugs inhibited MAO activity but not other mitochondrial marker enzymes. The potency of MAO i...

journal_title：Pharmaceutical research

authors： Yoshida H,Kamiya A,Okumura K,Hori R

更新日期：1989-10-01 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:Modulating sialylation of therapeutic glycoproteins may be used to influence their clearance and systemic exposure. We studied the effect of low and high sialylated IL4-10 fusion protein (IL4-10 FP) on in vitro and in vivo bioactivity and evaluated the effect of differential sialylation on pharmacokinetic param...

journal_title：Pharmaceutical research

authors： Steen-Louws C,Boross P,Prado J,Meeldijk J,Langenhorst JB,Huitema ADR,den Hartog MT,Boon L,Lafeber FPJG,Hack CE,Eijkelkamp N,Popov-Celeketic J

更新日期：2019-12-26 00:00:00

abstract：PURPOSE:To investigate the effect of γ-irradiation of poly(lactic-co-glycolic acid) (PLGA)/Al(OH)₃/0 or 5 wt% diethyl phthalate (DEP) microspheres for active self-healing encapsulation of vaccine antigens. METHODS:Microspheres were irradiated with ⁶⁰Co at 2.5 and 1.8 MRad and 0.37 and 0.20 MRad/h. Encapsulation of tet...

journal_title：Pharmaceutical research

authors： Desai KG,Kadous S,Schwendeman SP

更新日期：2013-07-01 00:00:00

abstract：:The delivery of therapeutic nucleic acids to neurons has the potential to treat neurological disease and spinal cord injury. While select viral vectors have shown promise as gene carriers to neurons, their potential as therapeutic agents is limited by their toxicity and immunogenicity, their broad tropism, and the cos...

journal_title：Pharmaceutical research

authors： Bergen JM,Park IK,Horner PJ,Pun SH

更新日期：2008-05-01 00:00:00

abstract：:We studied the effects of two verapamil analogs, anipamil and ronipamil, in traumatic shock. Noble-Collip drum trauma produced a shock state characterized by an eight-fold increase in plasma cathepsin D activity, a 13-fold increase in the rate of plasma myocardial depressant factor (MDF) accumulation, and a survival t...

journal_title：Pharmaceutical research

authors： Hock CE,Daitch JS,Lefer AM

更新日期：1985-05-01 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

authors： Jiang J,Chen G,Shuler FD,Wang CH,Xie J

更新日期：2015-09-01 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:The clinical utility of anthracyclines like idarubicin (IDA) is limited by the occurrence of multidrug resistance and cardiotoxicity. Previous studies have demonstrated that the multidrug transporter P-glycoprotein (P-gp) is present in the heart and have suggested that it exerts a protective function. We sought...

journal_title：Pharmaceutical research

authors： Kang W,Weiss M

更新日期：2001-11-01 00:00:00

abstract：PURPOSE:Nanocrystalline drug-polymer dispersions are of significant interest in pharmaceutical delivery. The purpose of this work is to demonstrate the applicability of methods based on two-dimensional (2D) and multinuclear solid-state NMR (SSNMR) to a novel nanocrystalline pharmaceutical dispersion of ebselen with pol...

journal_title：Pharmaceutical research

authors： Vogt FG,Williams GR

更新日期：2012-07-01 00:00:00

abstract：:Fibers were spun by the downward configuration of the wet spinning technique. This configuration is capable of encapsulating nonspherical and/or coarse particles. We examined encapsulation of propranolol hydrochloride and the ability of the fibers to act as a sustained-release delivery system for propranolol hydrochlo...

journal_title：Pharmaceutical research

authors： Hussain MA,DiLuccio RC,Shefter E,Hurwitz AR

更新日期：1989-12-01 00:00:00

abstract：:The physicochemical properties and crystal structures of the crystalline salts formed by the interaction of an achiral anion, salicylate, with homochiral and racemic ephedrinium and pseudoephedrinium cations were determined. The interaction of ephedrinium or pseudoephedrinium with salicylate in aqueous solution yielde...

journal_title：Pharmaceutical research

authors： Duddu SP,Grant DJ

更新日期：1994-11-01 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

authors： Takeda M,Maeda T,Ishihara T,Sakamoto H,Yuki K,Takasaki N,Nishimura F,Yamashita T,Tanaka K,Takenaga M,Igarashi R,Higaki M,Yamakawa N,Okamoto Y,Ogawa H,Otsuka M,Mizushima Y,Mizushima T

更新日期：2009-07-01 00:00:00

abstract：PURPOSE:For selective inhibition of endothelial cell activation in chronic inflammation, we have developed a dexamethasone-anti-E-selectin immunoconjugate. The present study was performed to evaluate the cellular handling of this immunoconjugate by activated primary endothelial cells and to compare its drug delivery ca...

journal_title：Pharmaceutical research

authors： Kok RJ,Everts M,Asgeirsdóttir SA,Meijer DK,Molema G

更新日期：2002-11-01 00:00:00