Molecular interaction fields (MIFs) to predict lipophilicity and ADME profile of antitumor Pt(II) complexes.

abstract：PURPOSE:Low temperature sensitive liposome (LTSL) encapsulated docetaxel were combined with mild hyperthermia (40-42°C) to investigate in vivo biodistribution and efficacy against a castrate resistant prostate cancer. METHOD:Female athymic nude mice with human prostate PC-3 M-luciferase cells grown subcutaneously into...

journal_title：Pharmaceutical research

authors： Ranjan A,Benjamin CJ,Negussie AH,Chokshi S,Chung PH,Volkin D,Yeram N,Linehan WM,Dreher MR,Pinto PA,Wood BJ

更新日期：2016-10-01 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: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

authors： Leng HM,Syce JA

更新日期：1997-02-01 00:00:00

abstract：PURPOSE:At elevated temperatures, the rate of drug release and skin permeation from transdermal delivery systems (TDS) may be higher than at a normal skin temperature. The aim of this study was to compare the effect of heat on the transdermal delivery of two model drugs, nicotine and fentanyl, from matrix-type TDSs wit...

journal_title：Pharmaceutical research

authors： Shin SH,Ghosh P,Newman B,Hammell DC,Raney SG,Hassan HE,Stinchcomb AL

更新日期：2017-09-01 00:00:00

abstract：PURPOSE:Predicting human skin permeability of chemical compounds accurately and efficiently is useful for developing dermatological medicines and cosmetics. However, previous work have two problems; 1) quality of databases used, and 2) methods for prediction models. In this paper, we attempt to solve these two problems...

journal_title：Pharmaceutical research

authors： Baba H,Takahara J,Mamitsuka H

更新日期：2015-07-01 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

authors： Gras R,Almonacid L,Ortega P,Serramia MJ,Gomez R,de la Mata FJ,Lopez-Fernandez LA,Muñoz-Fernandez MA

更新日期：2009-03-01 00:00:00

abstract：PURPOSE:To study the use of poly (lactide-co-glycolide) (PLGA) microparticles in respirable sizes as carriers for recombinant tuberculosis (TB) antigen, TB10.4-Ag85B, with the ultimate goal of pulmonary delivery as vaccine for the prevention of TB. MATERIALS AND METHODS:Recombinant TB antigens were purified from E. co...

journal_title：Pharmaceutical research

authors： Shi S,Hickey AJ

更新日期：2010-02-01 00:00:00

abstract：PURPOSE:The main goal of this research was to assess the mechanical properties of APIs' polymorphic forms at the single-crystal level (piroxicam, famotidine, nifedipine, olanzapine) in order to predict their bulk deformational attributes, which are critical for some pharmaceutical technology processes. METHODS:The mec...

journal_title：Pharmaceutical research

authors： Egart M,Janković B,Lah N,Ilić I,Srčič S

更新日期：2015-02-01 00:00:00

abstract：:A series of multilamellar liposome dispersions was prepared from lipids of soy phosphatidylcholine or hydrogenated soy phosphatidylcholine containing from 0 to 30 mol% of either cholesterol, stearylamine, or dipalmitoyl phosphatidylglycerol. The liposome dispersions were aerosolized with a Collison nebulizer for 80 mi...

journal_title：Pharmaceutical research

authors： Niven RW,Schreier H

更新日期：1990-11-01 00:00:00

abstract：PURPOSE:Recombinant human platelet glycoprotein Ibalpha-immunoglobulin G1 chimeric proteins (GPIbalpha-Ig) have varying levels of anti-thrombotic activities based on their ability to compete for platelet mediated adhesion to von Willebrand Factor (vWF). Valine substituted GPIbalpha-Ig chimeras, at certain position, inc...

journal_title：Pharmaceutical research

authors： Wang Q,Shorten D,Xu X,Shaw GD,Schaub RG,Shea C,Brooks J,Sako D,Wiswall E,Xu J,Szklut P,Patel VS

更新日期：2006-08-01 00:00:00

abstract：PURPOSE:The intratumoral heterogeneity observed in breast cancer (BC), in particular with regard to cell surface receptor expression, can hinder the success of many targeted cancer therapies. The development of novel therapeutic agents that target more than one receptor can overcome this inherent property of tumors and...

journal_title：Pharmaceutical research

authors： Houdaihed L,Evans JC,Allen C

更新日期：2020-01-21 00:00:00

abstract：PURPOSE:To investigate differences in the cellular uptake and intracellular distribution of protein-bound doxorubicin in comparison to free doxorubicin and a liposomal formulation (CAELYX) METHODS: LXFL 529 lung carcinoma cells were incubated with an acid-sensitive transferrin and albumin conjugate of doxorubicin, a st...

journal_title：Pharmaceutical research

authors： Beyer U,Rothern-Rutishauser B,Unger C,Wunderli-Allenspach H,Kratz F

更新日期：2001-01-01 00:00:00

abstract：PURPOSE:The effect of the molecular weight of dextran on the molecular mobility and protein stability of freeze-dried serum gamma-globulin (BGG) formulations was studied. The stabilizing effect of higher molecular weight dextran is discussed in relation to the molecular mobility of the formulations. METHODS:The molecu...

journal_title：Pharmaceutical research

authors： Yoshioka S,Aso Y,Kojima S

更新日期：1997-06-01 00:00:00

abstract：PURPOSE:Propofol is a widely used anesthetic agent with highly desirable fast "on" and "off" effects. It is currently formulated as lipid emulsions, which are known to support microbial growth. In this study, a novel, lipid-free nanodispersion formulation of propofol was characterized. METHODS:The formulation was eval...

journal_title：Pharmaceutical research

authors： Chen H,Zhang Z,Almarsson O,Marier JF,Berkovitz D,Gardner CR

更新日期：2005-03-01 00:00:00

abstract：:Although much effort has been devoted to opioid research since the identification of enkephalins, understanding of the physiological importance and mechanisms of action of endogenous opioids lags behind understanding of opiate alkaloids such as morphine. In recent years, several novel approaches have been refined with...

journal_title：Pharmaceutical research

authors： Rapaka RS,Porreca F

更新日期：1991-01-01 00:00:00

abstract：:Indomethacin microspheres based on a combination of ethylcellulose and polyethyleneglycol were prepared using the solvent evaporation process. Release profiles of ensemble and individual microspheres were measured. Both were found to follow first-order kinetics, in contrast to what was expected. This was attributed to...

journal_title：Pharmaceutical research

authors： Benita S,Babay D,Hoffman A,Donbrow M

更新日期：1988-03-01 00:00:00

abstract：PURPOSE:To investigate the feasibility of using the Aerosol Solvent Extraction System (ASES) to produce fine powders of recombinant human deoxyribonuclease (rhDNase), lysozyme-lactose and rhDNase-lactose powders from aqueous based solutions. METHODS:The ASES technique using high pressure carbon dioxide modified with e...

journal_title：Pharmaceutical research

authors： Bustami RT,Chan HK,Sweeney T,Dehghani F,Foster NR

更新日期：2003-12-01 00:00:00

abstract：:The interaction between several marker solutes and a polyolefin laminate polymer was studied in several solutions. Solutions studied included mixtures of sodium chloride and dextrose (at concentrations more less typical of i.v. administration solutions) and several actual i.v. products [lactated Ringer's injection, Di...

journal_title：Pharmaceutical research

authors： Jenke DR

更新日期：1991-06-01 00:00:00

abstract：PURPOSE:A series of studies was conducted to evaluate the preclinical pharmacokinetics of SB-239063 (trans-1-(4-hydroxycyclohexyl)-4-(4-fluorophenyl)-5-[(2-methoxy)pyrimidin-4-yl] imidazole), a potent and selective p38 MAP kinase inhibitor. METHODS:SB-239063 was administered both i.v. and p.o. in the rat, dog, cynomol...

journal_title：Pharmaceutical research

authors： Ward KW,Proksch JW,Azzarano LM,Salyers KL,McSurdy-Freed JE,Molnar TM,Levy MA,Smith BR

更新日期：2001-09-01 00:00:00

abstract：PURPOSE:The aim of this work was to investigate the influence of the oily nucleus composition on physico-chemical properties and anesthetic activity of poly (lactide-co-glycolide) nanocapsules with benzocaine. METHODS:Nanocapsules containing benzocaine were prepared with three different oily nucleus composition and ch...

journal_title：Pharmaceutical research

authors： de Melo NF,Grillo R,Guilherme VA,de Araujo DR,de Paula E,Rosa AH,Fraceto LF

更新日期：2011-08-01 00:00:00

abstract：PURPOSE:The purpose of this study was to determine the existence of insulin-degrading enzyme (EC 3.4.22.11) (IDE) in rat intestinal enterocytes. METHODS:Subcellular fractionation, biochemical characterization, immunoprecipitation, and western blots were employed. RESULTS:Insulin-degrading activity was localized in th...

journal_title：Pharmaceutical research

authors： Bai JP,Chang LL

更新日期：1995-08-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate the specific changes in body distribution of camptothecin (CA) through incorporation into solid lipid nanoparticles (SLN) by peroral route. METHODS:Camptothecin loaded solid lipid nanoparticles (CA-SLN) coated with poloxamer 188 were produced by high pressure homogeniza...

journal_title：Pharmaceutical research

authors： Yang S,Zhu J,Lu Y,Liang B,Yang C

更新日期：1999-05-01 00:00:00

abstract：PURPOSE:To examine the transport characteristics of the multidrug resistance-associated protein (MRP) substrate fluorescein across the isolated rat small intestinal segments. METHODS:The transport of fluorescein was studied in side-by-side diffusion chambers under short-circuited conditions at physiological pH. RESUL...

journal_title：Pharmaceutical research

authors： Legen I,Kristl A

更新日期：2004-04-01 00:00:00

abstract：PURPOSE:To prepare a thermoreversible gel system able to work as a medium for crystallization at around 20°C, allowing easy retrieval of crystals by simply decreasing the gel temperature. Lactose was selected has model substance for crystallization. METHODS:Water solutions with different% of poloxamer 407, α-Lactose m...

journal_title：Pharmaceutical research

authors： Cespi M,Bonacucina G,Casettari L,Mencarelli G,Palmieri GF

更新日期：2012-03-01 00:00:00

abstract：:For the last 50 years we have known of a broad-spectrum agent tilorone dihydrochloride (Tilorone). This is a small-molecule orally bioavailable drug that was originally discovered in the USA and is currently used clinically as an antiviral in Russia and the Ukraine. Over the years there have been numerous clinical and...

journal_title：Pharmaceutical research

authors： Ekins S,Lane TR,Madrid PB

更新日期：2020-03-25 00:00:00

abstract：PURPOSE:Multidrug and toxin extrusion proteins (MATEs) are multispecific organic cation transporters mediating the efflux of various cationic drugs into the urine. The present study aimed at identifying endogenous compounds in human plasma and urine specimens as biomarkers to evaluate drug interactions involving MATEs ...

journal_title：Pharmaceutical research

authors： Kato K,Mori H,Kito T,Yokochi M,Ito S,Inoue K,Yonezawa A,Katsura T,Kumagai Y,Yuasa H,Moriyama Y,Inui K,Kusuhara H,Sugiyama Y

更新日期：2014-01-01 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

authors： Lee WR,Shen SC,Sun CK,Aljuffali IA,Suen SY,Lin YK,Wang JJ,Fang JY

更新日期：2015-05-01 00:00:00

abstract：PURPOSE:The aim of the present study was to design a new mucosal drug delivery system composed of liposomes dispersed within a bioadhesive hydrogel containing methyl-beta-cyclodextrin (Me(beta)CD) for controlled drug release. METHODS:A hydrophilic model molecule, inulin, was encapsulated within positively charged and ...

journal_title：Pharmaceutical research

authors： Boulmedarat L,Piel G,Bochot A,Lesieur S,Delattre L,Fattal E

更新日期：2005-06-01 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

authors： Langguth P,Spahn H,Mutschler E

更新日期：1986-02-01 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