Cyclic RGDfK Peptide Functionalized Polymeric Nanocarriers for Targeting Gemcitabine to Ovarian Cancer Cells.

abstract：:There is a great need for delivery strategies capable of efficiently localizing drugs to the damaged myocardium that do not require direct intramyocardial injection of therapeutic molecules. In the work discussed here, we exploited the myocardium-specific upregulation of matrix metalloproteinases (MMPs) that occurs du...

journal_title：Molecular pharmaceutics

authors： Nguyen J,Sievers R,Motion JP,Kivimäe S,Fang Q,Lee RJ

更新日期：2015-04-06 00:00:00

abstract：:Major obstacles in the development of new therapeutic anticancer drugs are the low bioavailability of hydrophilic substances and the nonspecific toxicity toward healthy tissues. As such, cell-targeting oligopeptides have emerged as attractive drug delivery vehicles for a variety of different types of cargo. The recent...

journal_title：Molecular pharmaceutics

authors： Liu Y,Steiniger SC,Kim Y,Kaufmann GF,Felding-Habermann B,Janda KD

更新日期：2007-05-01 00:00:00

abstract：:The need for an efficacious and safe oral anticoagulant that does not require monitoring has been largely unmet. Many efforts have centered on preparing orally available heparin to improve patient compliance. In this study, novel orally active heparin derivatives (LHD), i.e. low molecular weight heparin (LMWH) conjuga...

journal_title：Molecular pharmaceutics

authors： Park JW,Jeon OC,Kim SK,Al-Hilal TA,Moon HT,Kim CY,Byun Y

更新日期：2010-06-07 00:00:00

abstract：:The safety and efficacy of anticancer antibody-drug conjugates (ADCs) depend on the selection of tumor-targeting monoclonal antibody (mAb), linker, and drug, as well as their specific chemical arrangement and linkage chemistry. In this study, we used a heterobifunctional cross-linker to conjugate docetaxel (DX) to cet...

journal_title：Molecular pharmaceutics

authors： Glatt DM,Beckford Vera DR,Prabhu SS,Mumper RJ,Luft JC,Benhabbour SR,Parrott MC

更新日期：2018-11-05 00:00:00

abstract：:Harmane and norharmane are representative members of the large group of natural β-carboline alkaloids featured with diverse pharmacological activities. In blood, these agents are transported by human serum albumin (HSA) which has a profound impact on the pharmacokinetic and pharmacodynamic properties of many therapeut...

journal_title：Molecular pharmaceutics

authors： Domonkos C,Fitos I,Visy J,Zsila F

更新日期：2013-12-02 00:00:00

abstract：:Organic anion transporting polypeptide (OATP) 1B1 plays an important role in the hepatic uptake of various drugs. Because OATP1B1 is a site of drug-drug interactions (DDIs), evaluating the inhibitory potential of drug candidates on OATP1B1 is required during drug development. For establishing a highly sensitive, high-...

journal_title：Molecular pharmaceutics

authors： Izumi S,Nozaki Y,Komori T,Takenaka O,Maeda K,Kusuhara H,Sugiyama Y

更新日期：2016-02-01 00:00:00

abstract：:The effective delivery of bioimaging probes to a selected cancerous tissue has extensive significance for biological studies and clinical investigations. Herein, the peptide functionalized NaGdF4 nanodots (termed as, pPeptide-NaGdF4 nanodots) have been prepared for highly efficient magnetic resonance imaging (MRI) of ...

journal_title：Molecular pharmaceutics

authors： Chen H,Li X,Liu F,Zhang H,Wang Z

更新日期：2017-09-05 00:00:00

abstract：:The transfection activity and the phase behavior of two novel cationic O-alkyl-phosphatidylcholines, 1,2-dioleoyl- sn-glycero-3-hexylphosphocholine (C6-DOPC) and 1,2-dierucoyl- sn-glycero-3-ethylphosphocholine (di22:1-EPC), have been examined with the aim of more completely understanding the mechanism of lipid-mediate...

journal_title：Molecular pharmaceutics

authors： Koynova R,Wang L,Macdonald RC

更新日期：2008-09-01 00:00:00

abstract：:Structural features of lysine-conjugated antibody-drug conjugate (ADC) from humanized IgG1 were studied by small-angle X-ray scattering (SAXS). As the physicochemical properties of the cytotoxic drug (payload) and linker may impact the conformational and colloidal stabilities of the conjugated monoclonal antibody (mAb...

journal_title：Molecular pharmaceutics

authors： Law-Hine D,Rudiuk S,Bonestebe A,Ienco R,Huille S,Tribet C

更新日期：2019-12-02 00:00:00

abstract：:Design and development of amphiphilic block copolymer-based nanocarriers exhibiting enhanced colloidal stability upon dilution in the blood and cellular glutathione-responsive rapid drug release is highly desired for tumor-targeting chemotherapy. Herein, we report a novel ABA-type triblock copolymer consisting of a hy...

journal_title：Molecular pharmaceutics

authors： Biswas D,An SY,Li Y,Wang X,Oh JK

更新日期：2017-08-07 00:00:00

abstract：:A promising strategy to enable patient stratification for targeted therapies is to monitor the target expression in a tumor by radionuclide molecular imaging. Affibody molecules (7 kDa) are nonimmunoglobulin scaffold proteins with a 25-fold smaller size than intact antibodies. They have shown an apparent potential as ...

journal_title：Molecular pharmaceutics

authors： Westerlund K,Honarvar H,Norrström E,Strand J,Mitran B,Orlova A,Eriksson Karlström A,Tolmachev V

更新日期：2016-05-02 00:00:00

abstract：:The rapid absorptive clearance of drugs delivered to the airways of the lungs means that many inhaled medicines have a short duration of action. The aim of this study was to investigate whether forming polar ion-pairs can modify drug absorption to slow down clearance from the airways. Salbutamol was used as a model dr...

journal_title：Molecular pharmaceutics

authors： Dutton B,Woods A,Sadler R,Prime D,Barlow DJ,Forbes B,Jones SA

更新日期：2020-05-04 00:00:00

abstract：:The encapsulation of glucocorticoids, such as dexamethasone, in nanoparticles (NPs) faces two main issues: a low drug loading and the destabilization of the nanoparticle suspension due to drug crystallization. Here, we successfully formulated a prodrug of dexamethasone, dexamethasone palmitate (DXP), into nanoparticle...

journal_title：Molecular pharmaceutics

authors： Lorscheider M,Tsapis N,Simón-Vázquez R,Guiblin N,Ghermani N,Reynaud F,Canioni R,Abreu S,Chaminade P,Fattal E

更新日期：2019-07-01 00:00:00

abstract：:We have developed a macromolecular prodrug platform based on poly(l-lysine succinylated) (PLS) that targets scavenger receptor A1 (SR-A1), a receptor expressed by myeloid and endothelial cells. We demonstrate the selective uptake of PLS by murine macrophage, RAW 264.7 cells, which was eliminated upon cotreatment with ...

journal_title：Molecular pharmaceutics

authors： Stevens DM,Adiseshaiah P,Dasa SSK,Potter TM,Skoczen SL,Snapp KS,Cedrone E,Patel N,Busman-Sahay K,Rosen EP,Sykes C,Cottrell M,Dobrovolskaia MA,Estes JD,Kashuba ADM,Stern ST

更新日期：2020-10-05 00:00:00

abstract：:The aim of this work was to develop a phosphate buffer based dissolution method for enteric-coated formulations with improved biopredictivity for fasted conditions. Two commercially available enteric-coated aspirin products were used as model formulations (Aspirin Protect 300 mg, and Walgreens Aspirin 325 mg). The dis...

journal_title：Molecular pharmaceutics

authors： Al-Gousous J,Amidon GL,Langguth P

更新日期：2016-06-06 00:00:00

abstract：:Targeted gene delivery using nonviral vectors is a highly touted scheme to reduce the potential for toxic or immunological side effects by reducing dose. In previous reports, TAT polyplexes with DNA have shown relatively poor gene delivery. The transfection efficiency has been enhanced by condensing TAT/DNA complexes ...

journal_title：Molecular pharmaceutics

authors： Khondee S,Baoum A,Siahaan TJ,Berkland C

更新日期：2011-06-06 00:00:00

abstract：:In previous studies, we developed a new technique (ionic gelation vibrational jet flow; IGVJF) in order to encapsulate pancreatic β-cells, for insulin in vivo delivery, and diabetes treatment. The fabricated microcapsules showed good morphology but limited cell functions. Thus, this study aimed to optimize the IGVJF t...

journal_title：Molecular pharmaceutics

authors： Mooranian A,Negrulj R,Takechi R,Jamieson E,Morahan G,Al-Salami H

更新日期：2017-08-07 00:00:00

abstract：:We have recently reported that by converting a perforin inhibitor into an l-type amino acid transporter 1 (LAT1)-utilizing prodrug its cellular uptake can be greatly increased. The aim of the present study was to determine the in vivo and brain pharmacokinetics of two perforin inhibitors and their LAT1-utilizing prodr...

journal_title：Molecular pharmaceutics

authors： Gynther M,Pickering DS,Spicer JA,Denny WA,Huttunen KM

更新日期：2016-07-05 00:00:00

abstract：:Dry powders from aqueous dispersions, formed by antisolvent precipitation, dissolved to form solutions with supersaturation values up to 12 in 10 min at pH 6.8 with sodium dodecyl sulfate micelles. Itraconazole/hydroxypropylmethylcellulose (HPMC) aqueous particle dispersions were salt flocculated and filtered to produ...

journal_title：Molecular pharmaceutics

authors： Matteucci ME,Paguio JC,Miller MA,Williams RO 3rd,Johnston KP

更新日期：2009-03-01 00:00:00

abstract：:The molecular mechanisms of autophagy in polyethylenimine (PEI)-treated cells are not well understood because of the use of nonspecific autophagy inhibitors. Here, we applied autophagy-related gene expression analysis to pinpoint the molecular mechanisms of autophagy in PEI-treated wild-type and atg5 gene knockout (at...

journal_title：Molecular pharmaceutics

authors： Lin CW,Jan MS,Kuo JH

更新日期：2014-09-02 00:00:00

abstract：:Sodium lauryl sulfate (SLS), as an effective surfactant, is often used as a solubilizer and/or wetting agent in various dosage forms for the purpose of improving the solubility and dissolution of lipophilic, poorly water-soluble drugs. This study aims to understand the impact of SLS on the solution behavior and bioava...

journal_title：Molecular pharmaceutics

authors： Chen Y,Wang S,Wang S,Liu C,Su C,Hageman M,Hussain M,Haskell R,Stefanski K,Qian F

更新日期：2016-08-01 00:00:00

abstract：:Oral chemotherapy with SN38 is restricted by its poor solubility in gastrointestinal (GI) fluids and low permeability. Here we report the oral delivery of SN38 by a combined lipophilic prodrug and lipid-based formulation strategy. A lead lipophilic prodrug of SN38, SN38-undecanoate (SN38-unde20), was incorporated into...

journal_title：Molecular pharmaceutics

authors： Bala V,Rao S,Bateman E,Keefe D,Wang S,Prestidge CA

更新日期：2016-10-03 00:00:00

abstract：:This work was designed to clarify the absolute abundances of transporters and receptors at different cerebral regions of the blood-brain barriers (BBB) and blood-spinal cord barrier (BSCB) in humans and rats, using physiologically relevant units (pmol/g tissue and fmol/cm2); 39 and 29 proteins including tight-junction...

journal_title：Molecular pharmaceutics

authors： Uchida Y,Yagi Y,Takao M,Tano M,Umetsu M,Hirano S,Usui T,Tachikawa M,Terasaki T

更新日期：2020-06-01 00:00:00

abstract：:In this study, dinitrosyl iron complexes (DNICs) are shown to deliver nitric oxide (NO) into the cytosol of vascular smooth muscle cells (SMCs), which play a major role in vascular relaxation and contraction. Malfunction of SMCs can lead to hypertension, asthma, and erectile dysfunction, among other disorders. For com...

journal_title：Molecular pharmaceutics

authors： Pectol DC,Khan S,Chupik RB,Elsabahy M,Wooley KL,Darensbourg MY,Lim SM

更新日期：2019-07-01 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：:Herein, we report on the role of endocytosis in the selective chemotherpeutic toxicity of rhodamine 6G (R6G) based nanomaterials, i.e., nanoGUMBOS, that are derived from a group of uniform materials based on organic salts (GUMBOS). Evaluation of cellular uptake in the presence and absence of endocytosis inhibitors sug...

journal_title：Molecular pharmaceutics

authors： Bhattarai N,Mathis JM,Chen M,Pérez RL,Siraj N,Magut PKS,McDonough K,Sahasrabudhe G,Warner IM

更新日期：2018-09-04 00:00:00

abstract：:For efficient and receptor-specific siRNA delivery, a new post-PEGylation strategy was established to provide siRNA polyplexes with targeting and shielding agents. For this purpose, core nanoparticles were formed by complexing siRNA with sequence-defined cationic lipo-oligomers. The T-shaped bis-oleoyl-oligoethanamino...

journal_title：Molecular pharmaceutics

authors： Müller K,Kessel E,Klein PM,Höhn M,Wagner E

更新日期：2016-07-05 00:00:00

abstract：:Recent studies on aqueous supersaturated lipophilic drug solutions prepared by methods including antisolvent addition, pH swing, or dissolution of amorphous solid dispersions (ASDs) have demonstrated that when crystallization is slow, these systems undergo liquid-liquid phase separation (LLPS) when the concentration o...

journal_title：Molecular pharmaceutics

authors： Indulkar AS,Gao Y,Raina SA,Zhang GG,Taylor LS

更新日期：2016-06-06 00:00:00

abstract：:Our objective was to design a polymeric micelle-based doxorubicin and lapatinib combination therapy for treating multidrug resistant (MDR) breast cancers. Poly(ethylene glycol)-block-poly(2-methyl-2-benzoxycarbonylpropylene carbonate) (PEG-PBC) polymers were synthesized for preparing doxorubicin and lapatinib loaded m...

journal_title：Molecular pharmaceutics

authors： Wang H,Li F,Du C,Wang H,Mahato RI,Huang Y

更新日期：2014-08-04 00:00:00

abstract：:Safe and effective gene delivery is essential to the success of gene therapy. We synthesized and characterized a novel nonviral gene delivery system in which folate (FA) molecules were functioned as blockers on cationic polyrotaxanes (PR) composed of poly(ethylenimine) (PEI)(600)-grafted α-cyclodextrin rings linearize...

journal_title：Molecular pharmaceutics

authors： Zhou Y,Wang H,Wang C,Li Y,Lu W,Chen S,Luo J,Jiang Y,Chen J

更新日期：2012-05-07 00:00:00