Doxorubicin and lapatinib combination nanomedicine for treating resistant breast cancer.

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：: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：: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：: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：: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：: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

authors： Lee SY,Tyler JY,Kim S,Park K,Cheng JX

更新日期：2013-09-03 00:00:00

abstract：:TGX-221 is a highly potent phosphoinositide 3-kinase β (PI3Kβ) inhibitor that holds great promise as a novel chemotherapeutic agent to treat prostate cancer. However, poor solubility and lack of targetability limit its therapeutic applications. The objective of this present study is to develop a peptide-drug conjugate...

journal_title：Molecular pharmaceutics

authors： Tai W,Shukla RS,Qin B,Li B,Cheng K

更新日期：2011-06-06 00:00:00

abstract：:Paracetamol has been one of the most commonly used and prescribed analgesic drugs for more than a hundred years. Despite being generally well tolerated, it can result in high liver toxicity when administered in specific conditions, such as overdose, or in vulnerable individuals. We have synthesized and characterized a...

journal_title：Molecular pharmaceutics

authors： Sodano F,Lazzarato L,Rolando B,Spyrakis F,De Caro C,Magliocca S,Marabello D,Chegaev K,Gazzano E,Riganti C,Calignano A,Russo R,Rimoli MG

更新日期：2019-10-07 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 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：:Dry powder inhalations (DPI) of microparticles containing isoniazid (INH) and rifabutin (RFB) are under preclinical development for use in pulmonary tuberculosis. Microparticles containing 0.25, 2.5, or 25 mg of each drug were administered daily for 90 days to rhesus macaques (n = 4/group). Single inhalations or intra...

journal_title：Molecular pharmaceutics

authors： Kumar Verma R,Mukker JK,Singh RS,Kumar K,Verma PR,Misra A

更新日期：2012-04-02 00:00:00

abstract：:The rate and extent of drug dissolution and absorption from solid oral dosage forms is highly dependent on the volume of liquid in the gastrointestinal tract (GIT). However, little is known about the time course of GIT liquid volumes after drinking a glass of water (8 oz), particularly in the colon, which is a targete...

journal_title：Molecular pharmaceutics

authors： Murray K,Hoad CL,Mudie DM,Wright J,Heissam K,Abrehart N,Pritchard SE,Al Atwah S,Gowland PA,Garnett MC,Amidon GE,Spiller RC,Amidon GL,Marciani L

更新日期：2017-08-07 00:00:00

abstract：:Oncolytic adenoviruses rank among the most promising innovative agents in cancer therapy. We examined the potential of boosting the efficacy of the oncolytic adenovirus dl520 by associating it with magnetic nanoparticles and magnetic-field-guided infection in multidrug-resistant (MDR) cancer cells in vitro and upon in...

journal_title：Molecular pharmaceutics

authors： Tresilwised N,Pithayanukul P,Mykhaylyk O,Holm PS,Holzmüller R,Anton M,Thalhammer S,Adigüzel D,Döblinger M,Plank C

更新日期：2010-08-02 00:00:00

abstract：:In humans, C-X-C chemokine receptor type 4 (CXCR4) is a protein that is encoded by the CXCR4 gene and binds the ligand CXCL12 (also known as SDF-1). The CXCR4-CXCL12 interaction in cancer elicits biological activities that result in tumor progression and has accordingly been the subject of significant investigation fo...

journal_title：Molecular pharmaceutics

authors： Brickute D,Braga M,Kaliszczak MA,Barnes C,Lau D,Carroll L,Stevens E,Trousil S,Alam IS,Nguyen QD,Aboagye EO

更新日期：2019-05-06 00:00:00

abstract：:p53 is a key tumor suppressor gene involved in key cellular processes and implicated in cancer therapy. However, it is inactivated in more than 50% of all cancers due to mutation or overexpression of its negative regulators. This leads to drug resistance and poor chemotherapeutic outcome as most clinical drugs act via...

journal_title：Molecular pharmaceutics

authors： Chow MJ,Babak MV,Wong DY,Pastorin G,Gaiddon C,Ang WH

更新日期：2016-07-05 00:00:00

abstract：:We report herein on the preparation of thermoresponsive hydrogels by taking advantage of the interaction of cyclodextrins (CDs) and a hydrophobically modified polymer. A hydrophobically modified hydroxypropyl methylcellulose (HM-HPMC) gel formed thermoresponsive hydrogels when small amounts of α-CD were added to the s...

journal_title：Molecular pharmaceutics

authors： Iohara D,Okubo M,Anraku M,Uramatsu S,Shimamoto T,Uekama K,Hirayama F

更新日期：2017-08-07 00:00:00

abstract：:The purpose of this study was to investigate labetalol as a potential high permeability reference standard for the application of Biopharmaceutics Classification Systems (BCS). Permeabilities of labetalol and metoprolol were investigated in animal intestinal perfusion models and Caco-2 cell monolayers. After isolating...

journal_title：Molecular pharmaceutics

authors： Incecayir T,Tsume Y,Amidon GL

更新日期：2013-03-04 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：:The ability to select patients who will respond to therapy is especially acute for autoimmune/inflammatory diseases, where the costs of therapies can be high and the progressive damage associated with ineffective treatments can be irreversible. In this article we describe a clinical test that will rapidly predict the ...

journal_title：Molecular pharmaceutics

authors： Kelderhouse LE,Robins MT,Rosenbalm KE,Hoylman EK,Mahalingam S,Low PS

更新日期：2015-10-05 00:00:00

abstract：:Polymer therapeutics has emerged as a new clinical option for the treatment of human diseases. However, little is known about pharmacogenetic responses to drugs formulated with polymers. In this study, we demonstrate that a formulation containing the block copolymer Pluronic P85 and antineoplastic drug doxorubicin (Do...

journal_title：Molecular pharmaceutics

authors： Batrakova EV,Kelly DL,Li S,Li Y,Yang Z,Xiao L,Alakhova DY,Sherman S,Alakhov VY,Kabanov AV

更新日期：2006-03-01 00:00:00

abstract：:2-Methoxyestradiol (2MeO-E2) is an endogenous metabolite of estrogen which was initially considered to be inactive. During the last few decades it has been shown that 2MeO-E2 is a promising anticancer drug. In vitro experiments have demonstrated that it has several anticancer activities, and potential to alleviate hyp...

journal_title：Molecular pharmaceutics

authors： Verenich S,Gerk PM

更新日期：2010-12-06 00:00:00

abstract：:Modifying nanoparticles with targeting peptides which can specifically bind to intestinal epithelium was recently suggested as a strategy to further enhance their ability for the oral delivery of macromolecular drugs. However, few studies were focused on comprehensive understanding of the uptake and transport processe...

journal_title：Molecular pharmaceutics

authors： Zhang J,Zhu X,Jin Y,Shan W,Huang Y

更新日期：2014-05-05 00:00:00

abstract：:Poly(ethylcyanoacrylate) (PECA) nanoparticles containing the bioactive d-Lys(6)-GnRH were manufactured by an in situ interfacial polymerization process using a w/o-microemulsion template containing the peptide in the dispersed aqueous pseudophase of the microemulsion. Polymeric nanoparticles were characterized using P...

journal_title：Molecular pharmaceutics

authors： Kafka AP,Kleffmann T,Rades T,McDowell A

更新日期：2009-09-01 00:00:00

abstract：:The purpose of this study was to determine the effect of PEGylation on the interaction of poly(amidoamine) (PAMAM) dendrimer nanocarriers (DNCs) with in vitro and in vivo models of the pulmonary epithelium. Generation-3 PAMAM dendrimers with varying surface densities of PEG 1000 Da were synthesized and characterized. ...

journal_title：Molecular pharmaceutics

authors： Bharatwaj B,Mohammad AK,Dimovski R,Cassio FL,Bazito RC,Conti D,Fu Q,Reineke J,da Rocha SR

更新日期：2015-03-02 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：:Rho-GTPases are small GTP-binding proteins that contribute to the epithelial-to-mesenchymal transition by regulating several cellular processes including organization of the actin cytoskeleton, cell motility, transcription, and cell proliferation. Overexpression of RhoC-GTPases (RhoC) in breast cancer has been implica...

journal_title：Molecular pharmaceutics

authors： Kaushal N,Durmaz YY,Bao L,Merajver SD,ElSayed ME

更新日期：2015-07-06 00:00:00

abstract：:Simvastatin is one of the most widely used active pharmaceutical ingredients for the treatment of hyperlipidemias. Because the compound is employed as a solid in drug formulations, particular attention should be given to the characterization of different polymorphs, their stability domains, and the nature of the phase...

journal_title：Molecular pharmaceutics

authors： Simões RG,Bernardes CES,Joseph A,M Piedade MF,Kraus W,Emmerling F,Diogo HP,Minas da Piedade ME

更新日期：2018-11-05 00:00:00

abstract：:To develop a radioactive metal complex platform for tumor theranostics, we introduced three radiopharmaceutical derivatives of 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic acid-benzothiazole aniline (DO3A-BTA, L1) labeled with medical radioisotopes for diagnosis (68Ga/64Cu) and therapy (177Lu). The tumor-targeting ...

journal_title：Molecular pharmaceutics

authors： Park JA,Lee JW,Kim HK,Shin UC,Lee KC,Kim TJ,Chang Y,Kim KM,Kim JY,Lee YJ

更新日期：2018-03-05 00:00:00

abstract：:The amorphization of the readily crystallizable therapeutic ingredient and food additive, menthol, was successfully achieved by inclusion of neat menthol in mesoporous silica matrixes of 3.2 and 5.9 nm size pores. Menthol amorphization was confirmed by the calorimetric detection of a glass transition. The respective g...

journal_title：Molecular pharmaceutics

authors： Cordeiro T,Castiñeira C,Mendes D,Danède F,Sotomayor J,Fonseca IM,Gomes da Silva M,Paiva A,Barreiros S,Cardoso MM,Viciosa MT,Correia NT,Dionisio M

更新日期：2017-09-05 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

authors： Myint KZ,Wang L,Tong Q,Xie XQ

更新日期：2012-10-01 00:00:00