Characterizing Drug-Polymer Interactions in Aqueous Solution with Analytical Ultracentrifugation.

abstract：:Bisphosphonates (BPs) are a class of bone resorptive drug with a high affinity for the hydroxyapatite structure of bone matrices that are used for the treatment of osteoporosis. However, clinical application is limited by a common toxicity, BP-related osteonecrosis of the jaw. There is emerging evidence that BPs posse...

journal_title：Molecular pharmaceutics

authors： Massey AS,Pentlavalli S,Cunningham R,McCrudden CM,McErlean EM,Redpath P,Ali AA,Annett S,McBride JW,McCaffrey J,Robson T,Migaud ME,McCarthy HO

更新日期：2016-04-04 00:00:00

abstract：:The ultrasmall nanoparticle AGuIX is a versatile platform that tolerates a range of chemical diversity for theranostic applications. Our previous work showed that AGuIX clears rapidly from normal tissues, while durably accumulating within the tumor microenvironment. On this basis, AGuIX was used to detect tumor tissue...

journal_title：Molecular pharmaceutics

authors： Truillet C,Thomas E,Lux F,Huynh LT,Tillement O,Evans MJ

更新日期：2016-07-05 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：:Isoniazid (INH) is still one of the two most effective antitubercular drugs and is included in all recommended multitherapeutic regimens. Because of the increasing resistance of Mycobacterium tuberculosis to INH, mainly associated with mutations in the katG gene, new INH-based compounds have been proposed to circumven...

journal_title：Molecular pharmaceutics

authors： Teixeira VH,Ventura C,Leitão R,Ràfols C,Bosch E,Martins F,Machuqueiro M

更新日期：2015-03-02 00:00:00

abstract：:Lipophilic cations such as phosphonium salts can accumulate in mitochondria of heart in response to the negative inner-transmembrane potentials. Two phosphonium salts [(18)F]FMBTP and [(18)F]mFMBTP were prepared and evaluated as potential myocardial perfusion imaging (MPI) agents in this study. The cations were radiol...

journal_title：Molecular pharmaceutics

authors： Zhao Z,Yu Q,Mou T,Liu C,Yang W,Fang W,Peng C,Lu J,Liu Y,Zhang X

更新日期：2014-11-03 00:00:00

abstract：:Contrast-enhanced ultrasound imaging has shown promise in the field of molecular imaging. This technique relies upon the adhesion of ultrasound contrast agent (UCA) to targeted molecular markers of disease. This is accomplished by coating the surface of the contrast agent with a ligand that specifically binds to the i...

journal_title：Molecular pharmaceutics

authors： Rychak JJ,Li B,Acton ST,Leppänen A,Cummings RD,Ley K,Klibanov AL

更新日期：2006-09-01 00:00:00

abstract：:DEK protein is critical to the formation of neutrophil extracellular traps (NETs) in rheumatoid arthritis (RA). Blocking DEK using the aptamer DTA via articular injection has been shown to have robust anti-inflammatory efficacy in a previous study. However, DTA is prone to nuclease degradation and renal clearance in v...

journal_title：Molecular pharmaceutics

authors： Cao J,Su J,An M,Yang Y,Zhang Y,Zuo J,Zhang N,Zhao Y

更新日期：2021-01-04 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：:In the present research a salt of vincamine, a poorly bioavailable indole alkaloid derived from the leaves of Vinca minor L., was synthesized in the solid state by means of a mechanochemical process employing citric acid as a reagent. The mechanochemical process was adopted as a solvent-free alternative to classical c...

journal_title：Molecular pharmaceutics

authors： Hasa D,Perissutti B,Cepek C,Bhardwaj S,Carlino E,Grassi M,Invernizzi S,Voinovich D

更新日期：2013-01-07 00:00:00

abstract：:Cell penetrating peptides (CPPs) have been extensively studied in polyelectrolyte complexes as a means to enhance the transfection efficiency of plasmid DNA (pDNA). Increasing the molecular weight of CPPs often enhances gene expression but poses a risk of increased cytotoxicity and immunogenicity compared to low molec...

journal_title：Molecular pharmaceutics

authors： Alhakamy NA,Berkland CJ

更新日期：2013-05-06 00:00:00

abstract：:Polymer therapeutics have shown promise as tumor-targeted drug delivery systems in mice. The multivalency of polymers allows the attachment of different functional agents to a polymeric backbone, including chemotherapeutic and antiangiogenic drugs, as well as targeting moieties, such as the bone-targeting agent alendr...

journal_title：Molecular pharmaceutics

authors： Miller K,Eldar-Boock A,Polyak D,Segal E,Benayoun L,Shaked Y,Satchi-Fainaro R

更新日期：2011-08-01 00:00:00

abstract：:Selective ligands to the peripheral benzodiazepine receptor (PBR) may induce apoptosis and cell cycle arrest. An overexpression of PBR in certain cancers allowed us to consider the use of highly selective ligands to PBR for receptor-mediated drug targeting to tumors. With this in mind, we prepared PBR-targeted nanopar...

journal_title：Molecular pharmaceutics

authors： Musacchio T,Laquintana V,Latrofa A,Trapani G,Torchilin VP

更新日期：2009-03-01 00:00:00

abstract：:Targeted delivery system would be an interesting platform to enhance the therapeutic effect and to reduce the side effects of anticancer drugs. In this study, we have developed lactobionic acid (LA)-modified chitosan-stearic acid (CS-SA) (CSS-LA) to deliver doxorubicin (DOX) to hepatic cancer cells. The average partic...

journal_title：Molecular pharmaceutics

authors： Yang Y,Yuan SX,Zhao LH,Wang C,Ni JS,Wang ZG,Lin C,Wu MC,Zhou WP

更新日期：2015-02-02 00:00:00

abstract：:Constitutive activation of signal transducer and activator of transcription 3 (STAT3) in tumor cells and tumor associated dendritic cells (DCs) plays a major role in the progression of cancer. JSI-124 (cucurbitacin I) is a potent inhibitor of STAT3; however, its poor solubility and nonspecificity limit its effectivene...

journal_title：Molecular pharmaceutics

authors： Garg SM,Vakili MR,Molavi O,Lavasanifar A

更新日期：2017-08-07 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：:A novel design of anticancer drug delivery system, based on an electrostatic binding of negatively charged liposomes and cationic metalloporphyrins under physiological conditions, is reported. A lack of cytotoxicity of the iron(III) porphyrin-loaded liposomes and an efficient generation of a toxic hydroxyl radical (OH...

journal_title：Molecular pharmaceutics

authors： Yuasa M,Oyaizu K,Horiuchi A,Ogata A,Hatsugai T,Yamaguchi A,Kawakami H

更新日期：2004-09-01 00:00:00

abstract：:An artificial stomach duodenum (ASD) model has been used to demonstrate the performance difference between two formulations of LY2300559, a low-solubility acidic developmental drug. The two formulations investigated were a conventional high-shear wet granulation (HSWG) formulation and a solid dispersion formulation. A...

journal_title：Molecular pharmaceutics

authors： Polster CS,Wu SJ,Gueorguieva I,Sperry DC

更新日期：2015-04-06 00:00:00

abstract：:Helicobacter pylori inhabits the gastric epithelium and can promote the development of gastric disorders, such as peptic ulcers, acute and chronic gastritis, mucosal lymphoid tissue (MALT), and gastric adenocarcinomas. To use nanotechnology as a tool to increase the antibacterial activity of silver I [Ag(I)] compounds...

journal_title：Molecular pharmaceutics

authors： Almeida Furquim de Camargo B,Soares Silva DE,Noronha da Silva A,Campos DL,Machado Ribeiro TR,Mieli MJ,Borges Teixeira Zanatta M,Bento da Silva P,Pavan FR,Gallina Moreira C,Resende FA,Menegário AA,Chorilli M,Vieira de Godoy Nett

更新日期：2020-07-06 00:00:00

abstract：:The objectives of this study were as follows: (i) To develop an in silico technique, based on molecular dynamics (MD) simulations, to predict glass transition temperatures (Tg) of amorphous pharmaceuticals. (ii) To computationally study the effect of plasticizer on Tg. (iii) To investigate the intermolecular interacti...

journal_title：Molecular pharmaceutics

authors： Gupta J,Nunes C,Jonnalagadda S

更新日期：2013-11-04 00:00:00

abstract：:Influenza viruses cause seasonal epidemics and represent a pandemic risk. With current vaccine methods struggling to protect populations against emerging strains, there is a demand for a next-generation flu vaccine capable of providing broad protection. Recombinant biotechnology, combined with nanomedicine techniques,...

journal_title：Molecular pharmaceutics

authors： Sia ZR,Miller MS,Lovell JF

更新日期：2021-02-01 00:00:00

abstract：:Novel strategy has been developed for fabricating the biocompatible reduction and pH dual-responsive core cross-linked (CCL) micelles as drug delivery system (DDS) for the controlled anticancer drug delivery, via the atom transfer radical polymerization (ATRP) of tert-butyl acrylate (tBA) with N,N'-bis(acryloyl)cystam...

journal_title：Molecular pharmaceutics

authors： Tian K,Jia X,Zhao X,Liu P

更新日期：2017-03-06 00:00:00

abstract：:The purpose of this study was to investigate the role of P-gp efflux in the in vivo intestinal absorption process of BCS class III P-gp substrates, i.e. high-solubility low-permeability drugs. The in vivo permeability of two H (2)-antagonists, cimetidine and famotidine, was determined by the single-pass intestinal per...

journal_title：Molecular pharmaceutics

authors： Dahan A,Amidon GL

更新日期：2009-01-01 00:00:00

abstract：:This research determined the uptake of individual components of topically applied microemulsions into the stratum corneum (SC) and assessed their molecular effects on skin barrier function. The microemulsions comprised oleic acid, Tween20, Transcutol and water. The effects of selected formulations, and of the individu...

journal_title：Molecular pharmaceutics

authors： Hathout RM,Mansour S,Mortada ND,Geneidi AS,Guy RH

更新日期：2010-08-02 00:00:00

abstract：:The bicarbonate buffer capacity is usually considered in a phase-homogeneous system, at equilibrium, with no CO2 transfer between the liquid buffer phase and another phase. However, typically, an in vitro bicarbonate buffer-based system is a phase-heterogeneous system, as it entails continuously sparging (bubbling) th...

journal_title：Molecular pharmaceutics

authors： Al-Gousous J,Sun KX,McNamara DP,Hens B,Salehi N,Langguth P,Bermejo M,Amidon GE,Amidon GL

更新日期：2018-11-05 00:00:00

abstract：:As microRNAs (miRNAs) have been reported to be a type of novel high-value small molecule (SM) drug targets for disease treatments, many researchers are engaged in the field of exploring new SM-miRNA associations. Nevertheless, because of the high cost, adopting traditional biological experiments constrains the efficie...

journal_title：Molecular pharmaceutics

authors： Yin J,Chen X,Wang CC,Zhao Y,Sun YZ

更新日期：2019-07-01 00:00:00

abstract：:Nucleic acid biopharmaceuticals are being investigated as potential therapeutics. They need to be incorporated into a biocompatible carrier so as to overcome several biological barriers. Rational development of suitable nanocarriers requires high-quality characterization techniques. While size, concentration, and stab...

journal_title：Molecular pharmaceutics

authors： Zagato E,Vermeulen L,Dewitte H,Van Imschoot G,Vandenbroucke RE,Demeester J,De Smedt SC,Neyts K,Remaut K,Braeckmans K

更新日期：2018-03-05 00:00:00

abstract：:An effective short interfering RNA (siRNA) delivery system protects the siRNA from degradation, facilitates its cellular uptake, and promotes its release into the cytoplasm. Local administration of siRNA presents advantages over systemic administration, such as the possibility to use lower doses and allow local and su...

journal_title：Molecular pharmaceutics

authors： Borgheti-Cardoso LN,Kooijmans SAA,Fens MHAM,van der Meel R,Vicentini FTMC,Fantini MCA,Bentley MVLB,Schiffelers RM

更新日期：2017-05-01 00:00:00

abstract：:Metastatic breast cancer is incurable. The goal of this study was to develop a positron emission tomography (PET)/near-infrared fluorescent (NIRF) probe for imaging CD105 expression in breast cancer experimental lung metastasis. TRC105, a chimeric anti-CD105 antibody, was dual-labeled with a NIRF dye (IRDye 800CW) and...

journal_title：Molecular pharmaceutics

authors： Hong H,Zhang Y,Severin GW,Yang Y,Engle JW,Niu G,Nickles RJ,Chen X,Leigh BR,Barnhart TE,Cai W

更新日期：2012-08-06 00:00:00

abstract：:Diabetic wounds are a worldwide health problem causing extremely heavy public health burden and require effective treatment. Optimal strategies for treating nonhealing diabetic wounds include stem-cell-based therapy and delivery of novel drug substances, such as functional microRNAs (miRNAs); however, miRNA easily deg...

journal_title：Molecular pharmaceutics

authors： Lv Q,Deng J,Chen Y,Wang Y,Liu B,Liu J

更新日期：2020-05-04 00:00:00

abstract：:Two coamorphous drug-amino acid systems, indomethacin-tryptophan (Ind-Trp) and furosemide-tryptophan (Fur-Trp), were analyzed toward their ease of amorphization and mechanism of coamorphization during ball milling. The two mixtures were compared to the corresponding amorphization of the pure drug without amino acid. P...

journal_title：Molecular pharmaceutics

authors： Jensen KT,Larsen FH,Cornett C,Löbmann K,Grohganz H,Rades T

更新日期：2015-07-06 00:00:00