A Mechanistic Study on Nanoparticle-Mediated Glucagon-Like Peptide-1 (GLP-1) Secretion from Enteroendocrine L Cells.

abstract：:BCS classification is a vital tool in the development of both generic and innovative drug products. The purpose of this work was to provisionally classify the world's top selling oral drugs according to the BCS, using in silico methods. Three different in silico methods were examined: the well-established group contri...

journal_title：Molecular pharmaceutics

authors： Dahan A,Wolk O,Kim YH,Ramachandran C,Crippen GM,Takagi T,Bermejo M,Amidon GL

更新日期：2013-11-04 00:00:00

abstract：:The objective of this study is to synthesize and evaluate acute toxicity of the bacterial cellulose (BC)/acrylamide (Am) hydrogels as noncytotoxic and biocompatible oral drug delivery vehicles. A novel series of solubilized BC/Am hydrogels were synthesized using a microwave irradiation method. The hydrogels were chara...

journal_title：Molecular pharmaceutics

authors： Pandey M,Mohamad N,Amin MC

更新日期：2014-10-06 00:00:00

abstract：:In this study, transferrin (Tf)-modified poly(ethylene glycol)-phosphatidylethanolamine (mPEG-PE) micelles loaded with the poorly water-soluble drug, R547 (a potent and selective ATP-competitive cyclin-dependent kinase (CDK) inhibitor), were prepared and evaluated for their targeting efficiency and cytotoxicity in vit...

journal_title：Molecular pharmaceutics

authors： Sawant RR,Jhaveri AM,Koshkaryev A,Zhu L,Qureshi F,Torchilin VP

更新日期：2014-02-03 00:00:00

abstract：:The impact of OATP drug uptake transporters in drug-drug interactions (DDIs) is increasingly recognized. OATP1B1 and OATP1B3 are human hepatic uptake transporters that can mediate liver uptake of a wide variety of drugs. Recently, we generated transgenic mice with liver-specific expression of human OATP1B1 or OATP1B3 ...

journal_title：Molecular pharmaceutics

authors： Durmus S,Lozano-Mena G,van Esch A,Wagenaar E,van Tellingen O,Schinkel AH

更新日期：2015-12-07 00:00:00

abstract：:Two-phase gas-liquid microfluidic reactors provide shear processing control of SN-38-loaded polymer nanoparticles (SN-38-PNPs). We prepare SN-38-PNPs from the block copolymer poly(methyl caprolactone- co-caprolactone)- block-poly(ethylene oxides) (P(MCL- co-CL)- b-PEO) using bulk and microfluidic methods and at differ...

journal_title：Molecular pharmaceutics

authors： Cao Y,Silverman L,Lu C,Hof R,Wulff JE,Moffitt MG

更新日期：2019-01-07 00:00:00

abstract：:The impact of the chain length or dispersity of polymers in controlling the crystallization of amorphous active pharmaceutical ingredients (APIs) has been discussed for a long time. However, because of the weak control of these parameters in the majority of macromolecules used in pharmaceutical formulations, the above...

journal_title：Molecular pharmaceutics

authors： Minecka A,Tarnacka M,Jurkiewicz K,Hachuła B,Wrzalik R,Kamiński K,Paluch M,Kamińska E

更新日期：2021-01-04 00:00:00

abstract：:Studies were conducted to develop antibody- and fluorescence-labeled superparamagnetic iron oxide nanoparticle (SPIO) nanotheranostics for magnetic resonance imaging (MRI) and fluorescence imaging of cancer cells and pH-dependent intracellular drug release. SPIO nanoparticles (10 nm) were coated with amphiphilic polym...

journal_title：Molecular pharmaceutics

authors： Zou P,Yu Y,Wang YA,Zhong Y,Welton A,Galbán C,Wang S,Sun D

更新日期：2010-12-06 00:00:00

abstract：:It is highly demanded and still a big challenge to develop an effective formulation for immunochemotherapy against advanced tumors. We have previously reported a PEG-NLG-based immunostimulatory nanocarrier (PEG2k-Fmoc-NLG919) for co-delivery of an IDO1 inhibitor (NLG919) and a chemotherapeutic agent (paclitaxel, PTX)....

journal_title：Molecular pharmaceutics

authors： Chen Y,Sun J,Huang Y,Lu B,Li S

更新日期：2018-11-05 00:00:00

abstract：:The present study explores the potential of polyelectrolyte-coated liposomes for improving the oral deliverability of doxorubicin (Dox). As a part of formulation strategy, stearyl amine was selected as a formulation component to provide positive charge to liposomes, which were subsequently coated with anionic poly(acr...

journal_title：Molecular pharmaceutics

authors： Jain S,Patil SR,Swarnakar NK,Agrawal AK

更新日期：2012-09-04 00:00:00

abstract：:Alkylphosphocholine (APC) analogs are a novel class of broad-spectrum tumor-targeting agents that can be used for both diagnosis and treatment of cancer. The potential for clinical translation for APC analogs will strongly depend on their pharmacokinetic (PK) profiles. The aim of this work was to understand how the ch...

journal_title：Molecular pharmaceutics

authors： Zhang RR,Grudzinksi JJ,Mehta TI,Burnette RR,Hernandez R,Clark PA,Lubin JA,Pinchuk AN,Jeffrey J,Longino M,Kuo JS,Weichert JP

更新日期：2019-08-05 00:00:00

abstract：:Particle size distribution and stability are key attributes for the evaluation of the safety and efficacy profile of medical nanoparticles (Med-NPs). Measuring particle average size and particle size distribution is a challenging task which requires the combination of orthogonal high-resolution sizing techniques, espe...

journal_title：Molecular pharmaceutics

authors： Caputo F,Arnould A,Bacia M,Ling WL,Rustique E,Texier I,Mello AP,Couffin AC

更新日期：2019-02-04 00:00:00

abstract：:Polymeric nanoparticles (NPs) are extremely attractive vaccine adjuvants, able to promote antigen delivery and in some instances, exert intrinsic immunostimulatory properties that enhance antigen specific humoral and cellular immune responses. The poly-ε-caprolactone (PCL)/chitosan NPs were designed with the aim of be...

journal_title：Molecular pharmaceutics

authors： Jesus S,Soares E,Borchard G,Borges O

更新日期：2018-01-02 00:00:00

abstract：:Because of its biocompatibility and ability to accommodate a variety of payloads from poorly soluble drugs to biomolecules, porous silicon (PSi) is a lucrative material for the development of carriers for particle-mediated drug delivery. We report a successful direct one-step (18)F-radiolabeling of three types of PSi ...

journal_title：Molecular pharmaceutics

authors： Sarparanta M,Mäkilä E,Heikkilä T,Salonen J,Kukk E,Lehto VP,Santos HA,Hirvonen J,Airaksinen AJ

更新日期：2011-10-03 00:00:00

abstract：:Rodent models are less suitable for predicting drug-drug interactions at the level of the human intestinal mucosa, especially when nuclear receptors such as pregnane X receptor (PXR) are involved. Recently, a transgenic mouse model, expressing both human PXR and CYP3A4, was developed and shown to be a better predictor...

journal_title：Molecular pharmaceutics

authors： Holmstock N,Gonzalez FJ,Baes M,Annaert P,Augustijns P

更新日期：2013-03-04 00:00:00

abstract：:The αvβ3-integrin addressing cyclic pentapeptide cyclo(RGDfK) was conjugated to NOPO, 1,4,7-triazacyclononane-1,4-bis[methylene(hydroxymethyl)phosphinic acid]-7-[methylene(2-carboxyethyl)phosphinic acid], a bifunctional chelator with exceptional gallium-68 labeling properties. NOPO-c(RGDfK) and its Ga(III) and Cu(II) ...

journal_title：Molecular pharmaceutics

authors： Simeček J,Notni J,Kapp TG,Kessler H,Wester HJ

更新日期：2014-05-05 00:00:00

abstract：:The purpose of this work was to elucidate the molecular interactions leading to monoclonal antibody self-association and precipitation and utilize biophysical measurements to predict solubility behavior at high protein concentration. Two monoclonal antibodies (mAb-G and mAb-R) binding to overlapping epitopes were inve...

journal_title：Molecular pharmaceutics

authors： Pindrus M,Shire SJ,Kelley RF,Demeule B,Wong R,Xu Y,Yadav S

更新日期：2015-11-02 00:00:00

abstract：:Stably transfected MDCK/hPepT1-V5&His clonal cell lines expressing varying levels of epitope-tagged hPepT1 protein were established to quantify the relationship between transgene hPepT1 expression levels and its functional kinetics in facilitating peptide and peptide-like drug uptake and transport in vitro. The hPepT1...

journal_title：Molecular pharmaceutics

authors： Herrera-Ruiz D,Faria TN,Bhardwaj RK,Timoszyk J,Gudmundsson OS,Moench P,Wall DA,Smith RL,Knipp GT

更新日期：2004-03-01 00:00:00

abstract：:Achieving effective gene therapy for glioma depends on gene delivery systems. The gene delivery system should be able to cross the blood-brain barrier (BBB) and further target glioma at its early stage. Active brain tumor targeted delivery can be achieved using the "Trojan horse" technology, which involves either endo...

journal_title：Molecular pharmaceutics

authors： Liu Y,He X,Kuang Y,An S,Wang C,Guo Y,Ma H,Lou J,Jiang C

更新日期：2014-10-06 00:00:00

abstract：:Drug repositioning is an important drug development strategy as it saves the time and efforts exerted in drug discovery. Since reepithelization of the cornea is a critical problem, we envisioned that the anticonvulsant phenytoin sodium can promote reepithelization of corneal ulcers as it was repurposed for skin wound ...

journal_title：Molecular pharmaceutics

authors： Mahmoud DB,Afifi SA,El Sayed NS

更新日期：2020-10-05 00:00:00

abstract：:Small interfering RNA (siRNA) is a novel therapeutic modality that benefits from nanoparticle mediated delivery. The most clinically advanced siRNA-containing nanoparticles are polymer-coated supramolecular assemblies of siRNA and lipids (lipid nanoparticles or LNPs), which protect the siRNA from nucleases, modulate p...

journal_title：Molecular pharmaceutics

authors： Wilson SC,Baryza JL,Reynolds AJ,Bowman K,Keegan ME,Standley SM,Gardner NP,Parmar P,Agir VO,Yadav S,Zunic A,Vargeese C,Lee CC,Rajan S

更新日期：2015-02-02 00:00:00

abstract：:In developing targeted probes for positron emission tomography (PET) based on (64)Cu, stable complexation of the radiometal is key, and a flexible handle for bioconjugation is highly advantageous. Here, we present the synthesis and characterization of the chelator pycup and four derivatives. Pycup is a cross-bridged c...

journal_title：Molecular pharmaceutics

authors： Boros E,Rybak-Akimova E,Holland JP,Rietz T,Rotile N,Blasi F,Day H,Latifi R,Caravan P

更新日期：2014-02-03 00:00:00

abstract：:By the combined use of powder and single-crystal X-ray diffraction, solid-state NMR, and molecular modeling, the crystal structures of two systems containing the unusually large tenapanor drug molecule have been determined: the free form, ANHY, and a dihydrochloride salt form, 2HCl. Dynamic nuclear polarization (DNP) ...

journal_title：Molecular pharmaceutics

authors： Nilsson Lill SO,Widdifield CM,Pettersen A,Svensk Ankarberg A,Lindkvist M,Aldred P,Gracin S,Shankland N,Shankland K,Schantz S,Emsley L

更新日期：2018-04-02 00:00:00

abstract：:Generation 5 poly(amidoamine) (G5 PAMAM) methotrexate (MTX) conjugates employing two small molecular linkers, G5-(COG-MTX)n, G5-(MFCO-MTX)n were prepared along with the conjugates of the G5-G5 (D) dimer, D-(COG-MTX)n, D-(MFCO-MTX)n. The monomer G5-(COG-MTX)n conjugates exhibited only a weak, rapidly reversible binding...

journal_title：Molecular pharmaceutics

authors： van Dongen MA,Rattan R,Silpe J,Dougherty C,Michmerhuizen NL,Van Winkle M,Huang B,Choi SK,Sinniah K,Orr BG,Banaszak Holl MM

更新日期：2014-11-03 00:00:00

abstract：:Simvastatin is known to exist in at least three polymorphic forms. The nature of polymorphism in simvastatin is ambiguous, as the crystal structures of the polymorphs do not show any significant change in crystal packing or molecular conformation. We utilize terahertz time-domain spectroscopy to characterize each of t...

journal_title：Molecular pharmaceutics

authors： Tan NY,Zeitler JA

更新日期：2015-03-02 00:00:00

abstract：:Encapsulation and release behavior of a water-insoluble drug, magnolol, using a core-shell polysaccharide-based nanoparticle, manipulating the cellular internalization and controlled cytotoxic effect of magnolol-loaded nanoparticles over the A10 vascular smooth muscle cells (VSMCs) was reported. A magnolol-polyvinylpy...

journal_title：Molecular pharmaceutics

authors： Wang YJ,Chien YC,Wu CH,Liu DM

更新日期：2011-12-05 00:00:00

abstract：:The endothelial cells lining the capillaries supplying the brain with oxygen and nutrients form a formidable barrier known as the blood-brain barrier (BBB), which exhibits selective permeability to small drug molecules and virtually impermeable to macromolecular therapeutics. Current in vitro BBB models fail to replic...

journal_title：Molecular pharmaceutics

authors： Wang JD,Khafagy el-S,Khanafer K,Takayama S,ElSayed ME

更新日期：2016-03-07 00:00:00

abstract：:In this paper, we investigate the release of two drugs, nicotine and caffeine, from poly epsilon-caprolactone (PCL) matrices, as a model for the delivery of highly hydrophilic drugs. Since PCL does not degrade over the period of our experiments (<30 days), drug diffusion through the matrix is expected to be the domina...

journal_title：Molecular pharmaceutics

authors： Rosenberg R,Devenney W,Siegel S,Dan N

更新日期：2007-11-01 00:00:00

abstract：:The goal of this study was to develop a (66)Ga-based positron emission tomography (PET) tracer for noninvasive imaging of CD105 expression during tumor angiogenesis, a hallmark of cancer. (66)Ga was produced using a cyclotron with (nat)Zn or isotopically enriched (66)Zn targets. TRC105, a chimeric anti-CD105 monoclona...

journal_title：Molecular pharmaceutics

authors： Engle JW,Hong H,Zhang Y,Valdovinos HF,Myklejord DV,Barnhart TE,Theuer CP,Nickles RJ,Cai W

更新日期：2012-05-07 00:00:00

abstract：:The current regimen of factor IX (FIX) injection is of an episodic format, which leads to limited efficacy. A sustained release dosage form is beneficial in terms of reducing the injection frequency and improving the therapeutic effectiveness. The aim of this study was to formulate a new microsphere form of a FIX-cont...

journal_title：Molecular pharmaceutics

authors： Chang LC,Yang CY,Chua AC,Lin YJ,Lai SM

更新日期：2011-10-03 00:00:00

abstract：:Novel multivalent copper(II)-conjugated phosphorus dendrimers and their corresponding mononuclear copper(II) complexes were synthesized, characterized, and screened for antiproliferative activity against human cancer cell lines. Selected copper ligands were grafted on the surface of phosphorus dendrimers of generation...

journal_title：Molecular pharmaceutics

authors： El Brahmi N,El Kazzouli S,Mignani SM,Essassi el M,Aubert G,Laurent R,Caminade AM,Bousmina MM,Cresteil T,Majoral JP

更新日期：2013-04-01 00:00:00