Post-PEGylation of siRNA Lipo-oligoamino Amide Polyplexes Using Tetra-glutamylated Folic Acid as Ligand for Receptor-Targeted Delivery.

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：: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：:Here, we report the antiproliferative/cytotoxic properties of 8-hydroxyquinoline (8-HQ) derivatives on HeLa cells in the presence of transition metal ions (Cu(2+), Fe(3+), Co(2+), Ni(2+)). Two series of ligands were tested, the arylvinylquinolinic L1-L8 and the arylethylenequinolinic L9-L16, which can all interact wit...

journal_title：Molecular pharmaceutics

authors： Barilli A,Atzeri C,Bassanetti I,Ingoglia F,Dall'Asta V,Bussolati O,Maffini M,Mucchino C,Marchiò L

更新日期：2014-04-07 00:00:00

abstract：:Liposomes are representative lipid nanoparticles widely used for delivering anticancer drugs, DNA fragments, or siRNA to cancer cells. Upon targeting, various internal and external triggers have been used to increase the rate for contents release from the liposomes. Among the internal triggers, decreased pH within the...

journal_title：Molecular pharmaceutics

authors： Nahire R,Hossain R,Patel R,Paul S,Meghnani V,Ambre AH,Gange KN,Katti KS,Leclerc E,Srivastava DK,Sarkar K,Mallik S

更新日期：2014-11-03 00:00:00

abstract：:The interaction with cervicovaginal mucus presents the potential to impact the performance of drug nanocarriers. These systems must migrate through this biological fluid in order to deliver their drug payload to the underlying mucosal surface. We studied the ability of dapivirine-loaded polycaprolactone (PCL)-based na...

journal_title：Molecular pharmaceutics

authors： das Neves J,Rocha CM,Gonçalves MP,Carrier RL,Amiji M,Bahia MF,Sarmento B

更新日期：2012-11-05 00:00:00

abstract：:Solid-state NMR (SSNMR) (1)H T1 and T1ρ relaxation times were used to evaluate the miscibility of amorphous solid dispersions of nifedipine (NIF) and polyvinylpyrrolidone (PVP) prepared by three different methods: melt quenching in the typical lab setting, spray drying and melt quenching in the NMR rotor while spinnin...

journal_title：Molecular pharmaceutics

authors： Yuan X,Sperger D,Munson EJ

更新日期：2014-01-06 00:00:00

abstract：:In this study, the polymer-free electrospinning was performed in order to produce cyclodextrin/ibuprofen inclusion complex nanofibers, which could have potential as the fast dissolving oral drug delivery system. Ibuprofen is a poorly water-soluble nonsteroidal anti-inflammatory drug; however, the water solubility of i...

journal_title：Molecular pharmaceutics

authors： Celebioglu A,Uyar T

更新日期：2019-10-07 00:00:00

abstract：:Recently, increased interest in drug transporters and research in this area has revealed that drug transporters play an important role in modulating drug absorption, distribution, and elimination. Acting alone or in concert with drug metabolizing enzymes they can affect the pharmacokinetics and pharmacodynamics of a d...

journal_title：Molecular pharmaceutics

authors： Zhang L,Strong JM,Qiu W,Lesko LJ,Huang SM

更新日期：2006-01-01 00:00:00

abstract：:Nonviral transfections of six low passage human colon cancer cell lines using the artificial beta-catenin/TCF-dependent promoter CTP4 demonstrated a high promoter activity which was 1000- to 70000-fold higher than in HeLa control cells. Luciferase gene expression levels obtained with CTP4 in epithelial-like tumor cell...

journal_title：Molecular pharmaceutics

authors： Gaedtke L,Pelisek J,Lipinski KS,Wrighton CJ,Wagner E

更新日期：2007-01-01 00:00:00

abstract：:Our primary objective is to characterize the self-association of rafoxanide in alkaline media. The second objective is to illustrate the feasibility of using rafoxanide micellar solution as the feed solution to prepare amorphous solid dispersion via spray drying. Rafoxanide is a poorly water-soluble drug. It is a weak...

journal_title：Molecular pharmaceutics

authors： Meng F,Liu T,Schneider E,Alzobaidi S,Gil M,Zhang F

更新日期：2017-05-01 00:00:00

abstract：:Metallacarborane moieties have been identified as promising pharmacophores. The pharmaceutical use of such compounds is, however, complicated by their low solubility and tendency to self-assemble in aqueous solution. In this work, we estimated the solubilities of a vast series of metallacarboranes [cobalt bis(dicarbol...

journal_title：Molecular pharmaceutics

authors： Rak J,Dejlová B,Lampová H,Kaplánek R,Matějíček P,Cígler P,Král V

更新日期：2013-05-06 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：:Photodynamic therapy (PDT) is a light-induced chemical reaction that produces localized tissue damage for the treatment of cancers and other nonmalignant conditions. The activation of photosensitizers in a target tissue is accomplished with a specific light source in the presence of molecular oxygen. In the clinic, pa...

journal_title：Molecular pharmaceutics

authors： Shieh MJ,Peng CL,Chiang WL,Wang CH,Hsu CY,Wang SJ,Lai PS

更新日期：2010-08-02 00:00:00

abstract：:Folate receptor (FR) targeting is an attractive strategy for nuclear imaging of cancer and activated macrophages through application of folic acid radioconjugates. However, significant renal accumulation of folate radioconjugates and hence exceedingly high emission of radiation from the kidneys may mask uptake of radi...

journal_title：Molecular pharmaceutics

authors： Müller C,Reber J,Schlup C,Leamon CP,Schibli R

更新日期：2013-03-04 00:00:00

abstract：:Heparin is a widely used anticoagulant due to its ability to inhibit key components in the coagulation cascade such as Factor Xa and thrombin (Factor IIa). Its potential to preferentially bind to antithrombin (ATIII) results in a conformational change and activation that leads to the prevention of fibrin formation fro...

journal_title：Molecular pharmaceutics

authors： Suchyta DJ,Handa H,Meyerhoff ME

更新日期：2014-02-03 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：: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：:The purpose of the present study was to investigate the effect of seed particles on the precipitation behavior of weak base drugs in the small intestine. A simple in vitro infusion method was used to mimic in vivo processes. Dipyridamole, pioglitazone, topiroxostat, chlorpromazine, cinnarizine, and ketoconazole were u...

journal_title：Molecular pharmaceutics

authors： Koyama H,Ito M,Terada K,Sugano K

更新日期：2016-08-01 00:00:00

abstract：:The objective of this work was to investigate the feasibility of using a novel granulation technique, namely, fluidized hot melt granulation (FHMG), to prepare gastroretentive extended-release floating granules. In this study we have utilized FHMG, a solvent free process in which granulation is achieved with the aid o...

journal_title：Molecular pharmaceutics

authors： Zhai H,Jones DS,McCoy CP,Madi AM,Tian Y,Andrews GP

更新日期：2014-10-06 00:00:00

abstract：:Gemcitabine, a clinically effective nucleoside anticancer agent, is a polar drug with low membrane permeability and is administered intravenously. Further, extensive degradation of gemcitabine by cytidine deaminase to an inactive metabolite in the liver affects its activity adversely. Thus, strategies that provide bot...

journal_title：Molecular pharmaceutics

authors： Song X,Lorenzi PL,Landowski CP,Vig BS,Hilfinger JM,Amidon GL

更新日期：2005-03-01 00:00:00

abstract：:The antiviral drug tenofovir (TFV) is orally administered as the fumarate salt of its disoproxil prodrug (TFV disoproxil fumarate (TDF)). TFV is a dianion at physiological pH and, as a result, has poor lipid membrane permeability. Administration of the lipophilic and cell-permeable prodrug, TFV disoproxil, enhances th...

journal_title：Molecular pharmaceutics

authors： Durand-Gasselin L,Van Rompay KK,Vela JE,Henne IN,Lee WA,Rhodes GR,Ray AS

更新日期：2009-07-01 00:00:00

abstract：:This paper develops a structure-activity relationship understanding of the way in which surfactant-like dendrons with hydrophilic spermine surface groups and a variety of lipophilic units at their focal points can self-assemble and subsequently bind to DNA with high affinity. The choice of functional group at the foca...

journal_title：Molecular pharmaceutics

authors： Jones SP,Gabrielson NP,Wong CH,Chow HF,Pack DW,Posocco P,Fermeglia M,Pricl S,Smith DK

更新日期：2011-04-04 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：:The toxicity of Amphotericin B (AmB) is contributed by the small, water-soluble aggregates of the drug. Hence, AmB lipid polymer hybrid nanoparticles (LIPOMER), comprising stearate lipids with a hydrophilic polymer Gantrez (GZ), and solid lipid nanoparticles (SLN), comprising only stearates, were prepared with the obj...

journal_title：Molecular pharmaceutics

authors： Das S,Devarajan PV

更新日期：2020-06-01 00:00:00

abstract：:Interactions of a lyophilized peptide with water and excipients in a solid matrix were explored using photolytic labeling. A model peptide "KLQ" (Ac-QELHKLQ-NHCH3) was covalently labeled with NHS-diazirine (succinimidyl 4,4'-azipentanoate), and the labeled peptide (KLQ-SDA) was formulated and exposed to UV light in bo...

journal_title：Molecular pharmaceutics

authors： Chen Y,Topp EM

更新日期：2019-03-04 00:00:00

abstract：:Graphene-based tumor cell nuclear targeting fluorescent nanoprobes (GTTNs) were synthesized in our laboratory as a kind of nanomaterial and showed good performance for both in vivo and in vitro imaging. GTTNs directly cross the cell membrane and specifically target the tumor cell nucleus via a cell membrane permeabili...

journal_title：Molecular pharmaceutics

authors： Gao W,Zhang J,Xue Q,Yin X,Yin X,Li C,Wang Y

更新日期：2020-07-06 00:00:00

abstract：:A number of folate-based radioconjugates have been synthesized and evaluated for nuclear imaging purposes of folate receptor (FR)-positive tumors and potential therapeutic application. A common shortcoming of radiofolates is, however, a significant accumulation of radioactivity in the kidneys. This situation has been ...

journal_title：Molecular pharmaceutics

authors： Farkas R,Siwowska K,Ametamey SM,Schibli R,van der Meulen NP,Müller C

更新日期：2016-06-06 00:00:00

abstract：:Macromolecules with defined nanosizes--nanoglobules--were synthesized and characterized as novel drug carriers with precise molecular architectures. Poly-L-lysine dendrimers with a cubic octa(3-aminopropyl)silsesquioxane (OAS) core, (L-lysine 8-OAS, (L-lysine) 16-(L-lysine) 8-OAS, (L-lysine) 32-(L-lysine) 16-(L-lysine...

journal_title：Molecular pharmaceutics

authors： Kaneshiro TL,Wang X,Lu ZR

更新日期：2007-09-01 00:00:00

abstract：:Following oral administration, dabigatran etexilate (DABE) is rapidly hydrolyzed to its active form, dabigatran. DABE, but not dabigatran, presents as a P-glycoprotein (P-gp) substrate and has increasingly been used as a probe drug. Therefore, although dosed as DABE, a P-gp drug-drug interaction (DDI) is reported as a...

journal_title：Molecular pharmaceutics

authors： Shen H,Yao M,Sinz M,Marathe P,Rodrigues AD,Zhu M

更新日期：2019-09-03 00:00:00

abstract：:The bladder is an important tissue in which to evaluate xenobiotic drug interactions and toxicities due to the concentration of parent drug and hepatic/enteric-derived metabolites in the urine as a result of renal excretion. Breaching of the barrier provided by the bladder epithelial lining (the urothelium) can expose...

journal_title：Molecular pharmaceutics

authors： Baker SC,Shabir S,Southgate J

更新日期：2014-07-07 00:00:00