Structural effects on the binding of amine drugs with the diphenylmethyl functionality to cyclodextrins. II. A molecular modeling study.

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:Monoamine oxidases (MAOs) are non-CYP enzymes that contribute to systemic elimination of therapeutic agents, and localized on mitochondrial membranes. The aim of the present study was to validate quantitative estimation of metabolic clearance of MAO substrate drugs using human liver microsomes (HLMs). METHODS:...

journal_title：Pharmaceutical research

authors： Masuo Y,Nagamori S,Hasegawa A,Hayashi K,Isozumi N,Nakamichi N,Kanai Y,Kato Y

更新日期：2017-06-01 00:00:00

abstract：PURPOSE:Cell penetrating peptides (CPPs) were widely used as motifs for drug delivery to tumor. In former study, an RGD reverse sequence dGR was used to develop active-targeting liposome R8dGR-Lip, which showed well penetrating ability and treatment efficiency on glioma model. However, recurrence after tumor resection ...

journal_title：Pharmaceutical research

authors： Qiu Y,Yu Q,Liu Y,Tang J,Wang X,Lu Z,Xu Z,He Q

更新日期：2018-04-26 00:00:00

abstract：:Transport studies using intestinal brush-border membrane vesicles isolated from rats and rabbits have failed to demonstrate proton- or Na(+)-dependent carrier-mediated transport of thyrotropin-releasing hormone (TRH), despite a pharmacologically relevant oral bioavailability. To examine the hypothesis that reported le...

journal_title：Pharmaceutical research

authors： Thwaites DT,Hirst BH,Simmons NL

更新日期：1993-05-01 00:00:00

abstract：PURPOSE:To study the role of unsaturated fatty acid ester substituents in the autoxidation of polysorbate 80 using quantitative kinetics. METHODS:Oxidation kinetics were monitored at 40 degrees C in aqueous solution by tracking head space oxygen consumption using a fiber optic oxygen sensor with phase shift fluorescen...

journal_title：Pharmaceutical research

authors： Yao J,Dokuru DK,Noestheden M,Park SS,Kerwin BA,Jona J,Ostovic D,Reid DL

更新日期：2009-10-01 00:00:00

abstract：PURPOSE:To evaluate the mechanism of renal transport of quinolone antibacterial drugs, we examined the interaction of levofloxacin with p-aminohippurate (PAH) transport systems and the transport of levofloxacin in renal epithelial cells. METHODS:Transport of [14C]PAH or [14C]levofloxacin was measured using OK cell mon...

journal_title：Pharmaceutical research

authors： Matsuo Y,Yano I,Habu Y,Katsura T,Hashimoto Y,Inui K

更新日期：2001-05-01 00:00:00

abstract：PURPOSE:The aim of the study is to determine the effect of experimental parameters on microinfusion through hollow microneedles into skin to optimize drug delivery protocols and identify rate-limiting barriers to flow. METHODS:Glass microneedles were inserted to a depth of 720-1080 microm into human cadaver skin to mi...

journal_title：Pharmaceutical research

authors： Martanto W,Moore JS,Kashlan O,Kamath R,Wang PM,O'Neal JM,Prausnitz MR

更新日期：2006-01-01 00:00:00

abstract：PURPOSE:This study aims to develop a characterization method for coating structure based on image analysis, which is particularly promising for the rational design of coated particles in the pharmaceutical industry. METHODS:The method applies the MATLAB image processing toolbox to images of coated particles taken with...

journal_title：Pharmaceutical research

authors： Laksmana FL,Van Vliet LJ,Hartman Kok PJ,Vromans H,Frijlink HW,Van der Voort Maarschalk K

更新日期：2009-04-01 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:To investigate the influence of primary crystallization conditions on the mechanical properties and secondary processing behaviour of fluticasone propionate (FP) for carrier based dry powder inhaler (DPI) formulations. METHODS:Young's modulus of FP crystals produced using different anti-solvents was determined...

journal_title：Pharmaceutical research

authors： Kubavat HA,Shur J,Ruecroft G,Hipkiss D,Price R

更新日期：2012-04-01 00:00:00

abstract：PURPOSE:The in-situ particle size of delavirdine mesylate in dry mix and tablets was determined. METHODS:Optical microscopy and fluorescence microscopy combined with image analysis were used for qualitative and quantitative measurements. RESULTS:Using optical microscopy, it was demonstrated qualitatively that fragmen...

journal_title：Pharmaceutical research

authors： White JG

更新日期：1999-04-01 00:00:00

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

authors： Hasenpusch G,Geiger J,Wagner K,Mykhaylyk O,Wiekhorst F,Trahms L,Heidsieck A,Gleich B,Bergemann C,Aneja MK,Rudolph C

更新日期：2012-05-01 00:00:00

abstract：PURPOSE:Phase II metabolism involves the conjugation of a polar moiety, such as sulfate or glucuronic acid, to a (relatively) nonpolar xenobiotic. Although it might be expected that such conjugates may exhibit amphiphilic character (e.g., surface activity and potential to form micelles), no detailed study of the micell...

journal_title：Pharmaceutical research

authors： Shackleford DM,Prankerd RJ,Scanlon MJ,Charman WN

更新日期：2003-03-01 00:00:00

abstract：:Chemoembolization using microspheres of 100- to 200-microns is a useful way to treat primary and secondary hepatic tumors. In a search for a better embolic material, we described in detail the preparation and characterization of a poly(benzyl l-glutamate) (PBLG) microspheres containing cisplatin (CDDP). We determined ...

journal_title：Pharmaceutical research

authors： Li C,Yang DJ,Nikiforow S,Tansey W,Kuang LR,Wright KC,Wallace S

更新日期：1994-12-01 00:00:00

abstract：:Nucleic acids are increasingly being considered for therapeutic uses, either to interfere with the function of specific nucleic acids or to bind specific proteins. Three types of nucleic acid drugs are discussed in this review: aptamers, compounds which bind specific proteins; triplex forming (antigene) compounds; whi...

journal_title：Pharmaceutical research

authors： Stull RA,Szoka FC Jr

更新日期：1995-04-01 00:00:00

abstract：:Primaquine (I), a 6-methoxy-8-aminoqumoline derivative used for the treatment of malaria has previously been shown to be metabolized to 8-(3-carboxy-l-methyl-propylamino)-6-methoxyquinoline by both micro-organisms and laboratory rats. Reported herein is the synthesis of this novel metabolite. ...

journal_title：Pharmaceutical research

authors： McChesney JD,Sarangan S

更新日期：1984-03-01 00:00:00

abstract：PURPOSE:The amphiphilic block copolymer Pluronic P85 (P85) increases the permeability of the blood-brain barrier (BBB) with respect to a broad spectrum of drugs by inhibiting the drug efflux transporter, P-glycoprotein (Pgp). In this regard, P85 serves as a promising component for CNS drug delivery systems. To assess t...

journal_title：Pharmaceutical research

authors： Batrakova EV,Zhang Y,Li Y,Li S,Vinogradov SV,Persidsky Y,Alakhov VY,Miller DW,Kabanov AV

更新日期：2004-11-01 00:00:00

abstract：:Knowledge of comparative solubility profiles of a base and its hydrochloride salt is important in selecting one form over the other for dosage form design. The studies with two model bases, namely, tiaramide and papaverine, showed that, except during phase transition from a base to a salt or vice versa, the pH-solubil...

journal_title：Pharmaceutical research

authors： Serajuddin AT,Mufson D

更新日期：1985-03-01 00:00:00

abstract：PURPOSE:The acne skin is characteristic of a relatively lower pH microenvironment compared to the healthy skin. The aim of this work was to utilize such pH discrepancy as a site-specific trigger for on-demand topical adapalene delivery. METHODS:The anti-acne agent, adapalene, was encapsulated in acid-responsive polyme...

journal_title：Pharmaceutical research

authors： Guo C,Khengar RH,Sun M,Wang Z,Fan A,Zhao Y

更新日期：2014-11-01 00:00:00

abstract：:Over the last few decades, intraperitoneal (IP) local drug delivery, providing high drug concentrations with prolonged retention in the peritoneal cavity, has opened a new horizon for the management of life-threatening peritoneal disorders, such as peritoneal carcinomatosis (PC). However, clinical translation of this ...

journal_title：Pharmaceutical research

authors： Alavi S,Haeri A,Mahlooji I,Dadashzadeh S

更新日期：2020-06-03 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：:The efficacy of topical formulations of acidic fibroblast growth factor (aFGF) in healing of full-thickness wounds has been studied in a diabetic db+/db+ mouse model. The effect of several formulation variables, dose, and application frequency was examined. It was found that wound healing in diabetic animals treated w...

journal_title：Pharmaceutical research

authors： Matuszewska B,Keogan M,Fisher DM,Soper KA,Hoe CM,Huber AC,Bondi JV

更新日期：1994-01-01 00:00:00

abstract：PURPOSE:A theoretical study was performed to generate a pharmacophore model for chemically diverse structures that specifically interact with the diltiazem binding site of L-type calcium channels. METHODS:Via molecular mechanics and quantum chemical methods solvation energies, logP values, conformational and electroni...

journal_title：Pharmaceutical research

authors： Schleifer KJ,Tot E

更新日期：1999-10-01 00:00:00

abstract：PURPOSE:To elucidate the catalytic mechanism of the esterase-like activity of serum albumin (SA), the reactivity of SA from six species was investigated using p-nitrophenyl esters as model substrates. METHODS:The effect of pH and the energetic and thermodynamic profiles of SA were determined for all species for p-nitr...

journal_title：Pharmaceutical research

authors： Sakurai Y,Ma SF,Watanabe H,Yamaotsu N,Hirono S,Kurono Y,Kragh-Hansen U,Otagiri M

更新日期：2004-02-01 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

authors： Luo Y,Bernshaw NJ,Lu ZR,Kopecek J,Prestwich GD

更新日期：2002-04-01 00:00:00

abstract：:An oral formulation of controlled-release isosorbide-5-nitrate pellets has been used to investigate the location of pellets in the gastrointestinal (GI) tract and, in parallel, to measure the drug absorption from these locations. Using the method of gamma scintigraphy the transit times and spreading of pellets in the ...

journal_title：Pharmaceutical research

authors： Fischer W,Boertz A,Davis SS,Khosla R,Cawello W,Sandrock K,Cordes G

更新日期：1987-12-01 00:00:00

abstract：PURPOSE:The aim of this work is to design new chitosan conjugates able to self-organize in aqueous solution in the form of micrometer-size platelets. When mixed with amphotericin B deoxycholate (AmB-DOC), micro-platelets act as a drug booster allowing further improvement in AmB-DOC anti-Candida albicans activity. METH...

journal_title：Pharmaceutical research

authors： Grisin T,Bories C,Bombardi M,Loiseau PM,Rouffiac V,Solgadi A,Mallet JM,Ponchel G,Bouchemal K

更新日期：2017-05-01 00:00:00

abstract：PURPOSE:The purpose of the current study is to evaluate the solubility advantage offered by celecoxib (CEL) amorphous systems and to characterize and correlate the physical and thermodynamic properties of CEL and its amorphous molecular dispersions containing poly(vinylpyrrolidone) (PVP). METHODS:The measurement of cr...

journal_title：Pharmaceutical research

authors： Gupta P,Kakumanu VK,Bansal AK

更新日期：2004-10-01 00:00:00

abstract：:A liposomal formulation of methylprednisolone (L-MPL) was developed to improve localization of this immunosuppressant in lymphatic tissues. Liposomes containing MPL were formulated from a mixture of phosphatydylcholine and phosphatydylglycerol (molar ratio, 9:1) and sized by extrusion through a 0.1-micron membrane. Ma...

journal_title：Pharmaceutical research

authors： Mishina EV,Straubinger RM,Pyszczynski NA,Jusko WJ

更新日期：1993-10-01 00:00:00

abstract：PURPOSE:To monitor the biodistribution of IgG1 aggregates upon subcutaneous (SC) and intravenous (IV) administration in mice and measure their propensity to stimulate an early immune response. METHODS:A human mAb (IgG1) was fluorescently labeled, aggregated by agitation stress and injected in SKH1 mice through SC and ...

journal_title：Pharmaceutical research

authors： Filipe V,Que I,Carpenter JF,Löwik C,Jiskoot W

更新日期：2014-01-01 00:00:00