Abstract:
:The biodistribution of dendronized iron oxides, NPs10@D1_DOTAGA and melanin-targeting NPs10@D1_ICF_DOTAGA, was studied in vivo using magnetic resonance imaging (MRI) and planar scintigraphy through [177Lu]Lu-radiolabeling. MRI experiments showed high contrast power of both dendronized nanoparticles (DPs) and hepatobiliary and urinary excretions. Little tumor uptake could be highlighted after intravenous injection probably as a consequence of the negatively charged DOTAGA-derivatized shell, which reduces the diffusion across the cells' membrane. Planar scintigraphy images demonstrated a moderate specific tumor uptake of melanoma-targeted [177Lu]Lu-NPs10@D1_ICF_DOTAGA at 2 h post-intravenous injection (pi), and the highest tumor uptake of the control probe [177Lu]Lu-NPs10@D1_DOTAGA at 30 min pi, probably due to the enhanced permeability and retention effect. In addition, ex vivo confocal microscopy studies showed a high specific targeting of human melanoma samples impregnated with NPs10@D1_ICF_Alexa647_ DOTAGA.
journal_name
Mol Pharmjournal_title
Molecular pharmaceuticsauthors
Bordeianu C,Parat A,Piant S,Walter A,Zbaraszczuk-Affolter C,Meyer F,Begin-Colin S,Boutry S,Muller RN,Jouberton E,Chezal JM,Labeille B,Cinotti E,Perrot JL,Miot-Noirault E,Laurent S,Felder-Flesch Ddoi
10.1021/acs.molpharmaceut.7b00904subject
Has Abstractpub_date
2018-02-05 00:00:00pages
536-547issue
2eissn
1543-8384issn
1543-8392journal_volume
15pub_type
杂志文章abstract::Delta-like ligand 4 (Dll4) expressed in tumor cells plays a key role to promote tumor growth of numerous cancer types. Based on a novel antihuman Dll4 monoclonal antibody (61B), we developed a (64)Cu-labeled probe for positron emission tomography (PET) imaging of tumor Dll4 expression. In this study, 61B was conjugate...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.5b00105
更新日期:2015-10-05 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
pub_type: 杂志文章
doi:10.1021/mp049936v
更新日期:2004-09-01 00:00:00
abstract::In women with human epidermal growth factor 2 (HER2)-positive breast cancer, the improved control of systemic disease with new therapies has unmasked brain metastases that historically would have remained clinically silent. The efficacy of therapeutic agents against brain metastases is limited by their inability to pe...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.9b01167
更新日期:2020-02-03 00:00:00
abstract::We present a new approach for characterizing drug-polymer interactions in aqueous media, using sedimentation velocity analytical ultracentrifugation (AUC). We investigated the potential interaction of ketoconazole (KTZ), a poorly water-soluble drug, with polyacrylic acid (PAA) and a polyvinyl caprolactam-polyvinyl ace...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.0c00849
更新日期:2021-01-04 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
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.7b00068
更新日期:2017-05-01 00:00:00
abstract::We have identified and characterized a new solid form of trehalose, the δ form (Tδ) using (13)C solid-state NMR spectroscopy (SSNMR). Tδ is formed from dehydrations of trehalose dihydrate (T(h)) performed at or below 100 °C, and it is generated concurrently with the α form of trehalose (Tα) and amorphous trehalose (T(...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp400104b
更新日期:2013-09-03 00:00:00
abstract::Molecular imaging of programmed cell death (apoptosis) in vivo is an innovative strategy for early assessment of treatment response and treatment efficacy in cancer patients. Externalization of phosphatidylserine (PS) to the cell membrane surface of dying cells makes this phospholipid an attractive molecular target fo...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.6b00666
更新日期:2016-10-03 00:00:00
abstract::The most abundant polyphenol in green tea, epigallocatechin-3-gallate (EGCg), has recently received considerable attention due to the discovery of numerous health-promoting bioactivities. Despite reports of its poor oral bioavailability, EGCg has been included in many dietary supplement formulations. Conventional pref...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp4000794
更新日期:2013-08-05 00:00:00
abstract::Most anticancer drugs are poorly soluble and nonspecific, which restricts their clinical application. Drug conjugates, as a prodrug strategy, provide the possibility to overcome these shortcomings, especially combined with nanotechnology. Drug conjugate nanoparticles possess the advantages of high drug loading capacit...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.5b00631
更新日期:2016-01-04 00:00:00
abstract::As a result of its higher molecular mobility, the surface of an amorphous drug can grow crystals much more rapidly than the bulk, causing poor stability and slow dissolution of drug products. We show that a nanocoating of chitosan (a pharmaceutically acceptable polymer) can be deposited on the surface of amorphous ind...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.8b01237
更新日期:2019-03-04 00:00:00
abstract::A big hurdle for the use of protein-based drugs is that they are easily degraded by proteases in the human body. In an attempt to solve this problem, we show the possibility to functionalize TM encapsulin nanoparticles with an mEETI-II knottin miniprotein from the cysteine-stabilized knot class. The resulting particle...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.8b00630
更新日期:2018-08-06 00:00:00
abstract::Lipid-based drug delivery systems have been vastly investigated as a pharmaceutical method to enhance oral absorption of lipophilic drugs. However, these vehicles not only affect drug bioavailability but may also have an impact on gastric emptying, drug disposition, lymphatic absorption and be affected by lipid digest...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.0c00141
更新日期:2020-06-01 00:00:00
abstract::Our previous studies have demonstrated that a generation 5 dendrimer (G5) conjugated with both folic acid (FA) and methotrexate (MTX) has a higher chemotherapeutic index than MTX alone. Despite this, batch-to-batch inconsistencies in the number of FA and MTX molecules linked to each dendrimer led to conjugate batches ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp3002232
更新日期:2012-09-04 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
pub_type: 杂志文章
doi:10.1021/mp900319k
更新日期:2010-06-07 00:00:00
abstract::The adenosine triphosphate-binding cassette transporter P-glycoprotein (ABCB1/Abcb1a) restricts at the blood-brain barrier (BBB) brain distribution of many drugs. ABCB1 may be involved in drug-drug interactions (DDIs) at the BBB, which may lead to changes in brain distribution and central nervous system side effects o...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.5b00168
更新日期:2015-09-08 00:00:00
abstract::Understanding in vivo drug release kinetics is critical for the development of nanoparticle-based delivery systems. In this study, we developed a fluorescence resonance energy transfer (FRET) imaging approach to noninvasively monitor in vitro and in vivo cargo release from polymeric nanoparticles. The FRET donor dye (...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp4002393
更新日期:2013-11-04 00:00:00
abstract::Although nanocarriers hold promise for cancer chemotherapy, their intracellular drug delivery pathways are not fully understood. In particular, the influence of nanocarrier stability on cellular uptake is still uncertain. By physically loading hydrophobic FRET probes, we revealed different intracellular drug delivery ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp4003333
更新日期:2013-09-03 00:00:00
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
pub_type: 杂志文章
doi:10.1021/mp400485k
更新日期:2013-11-04 00:00:00
abstract::P-glycoprotein (Pgp) is highly expressed on blood-brain barrier (BBB) and glioblastoma (GB) cells, particularly on cancer stem cells (SC). Pgp recognizes a broad spectrum of substrates, limiting the therapeutic efficacy of several chemotherapeutic drugs in eradicating GB SC. Finding effective and safe inhibitors of Pg...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.9b00018
更新日期:2019-08-05 00:00:00
abstract::It is likely that drug resistance evolves after transformation. Exactly how these resistant cells arise is uncertain. This review outlines how the evolution of individual human cancers may be inferred by comparing genomic variation from different parts of the same tumor. The past of a tumor may help predict its respon...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章,评审
doi:10.1021/mp200256n
更新日期:2011-12-05 00:00:00
abstract::Porous silicon microparticles presenting pathogen-associated molecular patterns mimic pathogens, enhancing internalization of the microparticles and activation of antigen presenting dendritic cells. We demonstrate abundant uptake of microparticles bound by the TLR-4 ligands LPS and MPL by murine bone marrow-derived de...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp3001292
更新日期:2012-07-02 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
pub_type: 杂志文章
doi:10.1021/mp100060v
更新日期:2010-08-02 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
pub_type: 杂志文章,随机对照试验
doi:10.1021/acs.molpharmaceut.6b00077
更新日期:2016-06-06 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
pub_type: 杂志文章
doi:10.1021/mp5006036
更新日期:2015-04-06 00:00:00
abstract::An important aspect to ensure progress in biomedicine is the fundamental understanding of the interaction of cells and tissue with (bio)materials. The consideration of shear stress in drug delivery and/or tissue engineering remains largely unexplored. To illustrate the fundamental relevance, we employ a microfluidic s...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp4001298
更新日期:2013-07-01 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
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.9b01166
更新日期:2020-05-04 00:00:00
abstract::Abnormal tumor vessels impede the transport and distribution of chemotherapeutics, resulting in low drug concentration at tumor sites and compromised drug efficacy. Normalizing tumor vessels can modulate tumor vascular permeability, alleviate tumor hypoxia, increase blood perfusion, attenuate interstitial fluid pressu...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.7b00475
更新日期:2017-10-02 00:00:00
abstract::The objective was to determine the disposition of polymer nanoparticles and an associated, lipophilic, model "active" component on and within the skin following topical application. Polystyrene and poly(methyl methacrylate) nanoparticles containing covalently bound fluorescein methacrylate and dispersed Nile Red were ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp9001188
更新日期:2009-09-01 00:00:00
abstract::Ratiometric fluorescence and cellular fractionation studies were employed to characterize the intracellular trafficking dynamics of antibody-poly(propylacrylic acid) (PPAA) conjugates in CD22+ RAMOS-AW cells. The HD39 monoclonal antibody (mAb) directs CD22-dependent, receptor-mediated uptake in human B-cell lymphoma c...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp300338s
更新日期:2012-12-03 00:00:00
abstract::In this manuscript, we have reported a novel 2D fingerprint-based artificial neural network QSAR (FANN-QSAR) method in order to effectively predict biological activities of structurally diverse chemical ligands. Three different types of fingerprints, namely, ECFP6, FP2 and MACCS, were used in FANN-QSAR algorithm devel...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp300237z
更新日期:2012-10-01 00:00:00