Sustained release of transgenic human factor IX: preparation, characterization, and in vivo efficacy.

abstract：:Gemcitabine (GEM), a first-line chemotherapy for pancreatic cancer undergoes rapid metabolism and develops chemoresistance after repeated administration. We previously demonstrated that the combination of GEM and miR-205 provides an effective therapeutic strategy to sensitize GEM-resistant pancreatic cancer cells. Sin...

journal_title：Molecular pharmaceutics

authors： Mondal G,Almawash S,Chaudhary AK,Mahato RI

更新日期：2017-09-05 00:00:00

abstract：:Boron neutron capture therapy (BNCT) has received extensive attention as noninvasive cell-level oncotherapy for treating solid cancer tumors. However, boron-containing drugs such as l-boronophenylalanine (BPA) and sodium borocaptate have low boron content and/or poor tumor-targeting ability, limiting their application...

journal_title：Molecular pharmaceutics

authors： Li R,Zhang J,Guo J,Xu Y,Duan K,Zheng J,Wan H,Yuan Z,Chen H

更新日期：2020-01-06 00:00:00

abstract：:The synthesis of a dendrimer based on melamine that displays multiple copies of four orthogonally reactive groups, three on the surface and one on the interior, is described. The three groups on the surface are nucleophilic and include four free hydroxyl groups, four hydroxyl groups masked as tert-butyldiphenylsilyl (...

journal_title：Molecular pharmaceutics

authors： Lim J,Simanek EE

更新日期：2005-07-01 00:00:00

abstract：:Saquinavir mesylate (SQV) is the first-in-class and prototypical HIV protease inhibitor (PI) used in the treatment of HIV infection. SQV undergoes extensive hepatic metabolism and intestinal and bile secretion, and has poor and variable oral bioavailability. In previous studies, our group and others have described the...

journal_title：Molecular pharmaceutics

authors： Su Y,Zhang X,Sinko PJ

更新日期：2004-01-12 00:00:00

abstract：:Antibody-coupled photosensitive molecules can achieve an ideal tumor-specific photodynamic therapy (PDT) and show strong clinical application potential. However, some inherent disadvantages, such as long circulation half-life, poor permeation into solid tumors, and difficulty in obtaining uniform coupling products, pr...

journal_title：Molecular pharmaceutics

authors： Li S,Jin Y,Su Y,Li W,Xing Y,Wang F,Hong Z

更新日期：2020-05-04 00:00:00

abstract：:The drug-induced accumulation of phospholipids in lysosomes of various tissues is predominantly observed in regular repeat dose studies, often after prolonged exposure, and further investigated in mechanistic studies prior to candidate nomination. The finding can cause delays in the discovery process inflicting high c...

journal_title：Molecular pharmaceutics

authors： Fusani L,Brown M,Chen H,Ahlberg E,Noeske T

更新日期：2017-12-04 00:00:00

abstract：:OATP1B3 is a member of the OATP (organic anion transporting polypeptides) superfamily, responsible for mediating the transport of numerous endogenous and xenobiotic substances. Although initially reported to be exclusively expressed in the liver, several studies reported that OATP1B3 is frequently expressed in multipl...

journal_title：Molecular pharmaceutics

authors： Thakkar N,Kim K,Jang ER,Han S,Kim K,Kim D,Merchant N,Lockhart AC,Lee W

更新日期：2013-01-07 00:00:00

abstract：:Near-infrared (NIR)-to-visible upconversion nanoparticle (UCNP) has shown promising prospects in photodynamic therapy (PDT) as a drug carrier or energy donor. In this work, a photosensitizer pyropheophorbide a (Ppa) and RGD peptide c(RGDyK) comodified chitosan-wrapped NaYF(4):Yb/Er upconversion nanoparticle UCNP-Ppa-R...

journal_title：Molecular pharmaceutics

authors： Zhou A,Wei Y,Wu B,Chen Q,Xing D

更新日期：2012-06-04 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

authors： Song Q,Wang X,Wang Y,Liang Y,Zhou Y,Song X,He B,Zhang H,Dai W,Wang X,Zhang Q

更新日期：2016-01-04 00:00:00

abstract：:Indocyanine green (ICG) is a conventional dye that can be used in clinical near-infrared (NIR) imaging, and it is also an effective light absorber for laser-mediated photothermal therapy. However, applications of ICG were limited due to its fast degradation in aqueous media and quick clearance from the body. Herein, a...

journal_title：Molecular pharmaceutics

authors： Zheng X,Zhou F,Wu B,Chen WR,Xing D

更新日期：2012-03-05 00:00:00

abstract：:The systemic pharmacokinetics and pharmacodynamics of small molecules are determined by subcellular transport phenomena. Although approaches used to study the subcellular distribution of small molecules have gradually evolved over the past several decades, experimental analysis and prediction of cellular pharmacokinet...

journal_title：Molecular pharmaceutics

authors： Zheng N,Tsai HN,Zhang X,Rosania GR

更新日期：2011-10-03 00:00:00

abstract：:Cancer stem cells (CSCs) are a subpopulation of cancer cells that have stem cell-like properties and are thought to be responsible for tumor drug resistance and relapse. Therapies that can effectively eliminate CSCs will, therefore, likely inhibit tumor recurrence. The objective of our study was to determine the susce...

journal_title：Molecular pharmaceutics

authors： Sadhukha T,Niu L,Wiedmann TS,Panyam J

更新日期：2013-04-01 00:00:00

abstract：:The mechanism of cell death in A2780 human ovarian carcinoma cells induced by free doxorubicin (DOX) and N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-bound DOX [P-(GFLG)-DOX] was investigated. In particular, the involvement of the Fas receptor system in drug-induced apoptosis was evaluated. P-(GFLG)-DOX was show...

journal_title：Molecular pharmaceutics

authors： Malugin A,Kopecková P,Kopecek J

更新日期：2004-05-01 00:00:00

abstract：:Organic anion-transporting polypeptides (OATPs) mediate the uptake of various drugs from blood into the liver in the basolateral membrane of hepatocytes. Positron emission tomography (PET) is a potentially powerful tool to assess the activity of hepatic OATPs in vivo, but its utility critically depends on the availabi...

journal_title：Molecular pharmaceutics

authors： Bauer M,Traxl A,Matsuda A,Karch R,Philippe C,Nics L,Klebermass EM,Wulkersdorfer B,Weber M,Poschner S,Tournier N,Jäger W,Wadsak W,Hacker M,Wanek T,Zeitlinger M,Langer O

更新日期：2018-10-01 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：:Polysorbate 20 (PS20) is a commonly used surfactant in biopharmaceutical formulations. It is a heterogeneous surfactant containing a distribution of fatty acid esters, which are subject to hydrolytic degradation, generating free fatty acids (FFAs). The FFAs can form visible or subvisible particles in drug product on s...

journal_title：Molecular pharmaceutics

authors： Doshi N,Martin J,Tomlinson A

更新日期：2020-11-02 00:00:00

abstract：:Breast cancer is the second most common cause of cancer-related deaths in women. Chemotherapy is an important treatment modality, and paclitaxel (PTX) is often the first-line therapy for its metastatic form. The two most notable limitations related to PTX-based treatment are the poor hydrophilicity of the drug and the...

journal_title：Molecular pharmaceutics

authors： Satsangi A,Roy SS,Satsangi RK,Vadlamudi RK,Ong JL

更新日期：2014-06-02 00:00:00

abstract：:As the hearts of tumor cells, the nucleus is the ultimate target of many chemotherapeutic agents and genes. However, nuclear drug delivery is always hampered by multiple intracellular obstacles, such as low efficiency of lysosome escape and insufficient nuclear trafficking. Herein, an N-(2-hydroxypropyl) methacrylamid...

journal_title：Molecular pharmaceutics

authors： Zhong J,Zhu X,Luo K,Li L,Tang M,Liu Y,Zhou Z,Huang Y

更新日期：2016-09-06 00:00:00

abstract：:The pharmacological exploitation of resveratrol is hindered by rapid phase-II conjugative metabolism in enterocytes and hepatocytes. One approach to the solution of this problem relies on prodrugs. We report the synthesis and characterization as well as the assessment of in vivo absorption and metabolism of a set of p...

journal_title：Molecular pharmaceutics

authors： Mattarei A,Azzolini M,Carraro M,Sassi N,Zoratti M,Paradisi C,Biasutto L

更新日期：2013-07-01 00:00:00

abstract：:Powder adhesion or sticking onto punches is one of the outstanding issues in pharmaceutical tablet manufacturing. We show in this work that, at comparable particle sizes, the acesulfame potassium exhibited pronouncedly reduced propensity to punch sticking than acesulfame. Detailed analyses revealed strong correlation ...

journal_title：Molecular pharmaceutics

authors： Paul S,Wang C,Wang K,Sun CC

更新日期：2019-06-03 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：: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：: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：:This study describes a novel nonlinear variant of the well-known Yalkowsky general solubility equation (GSE). The modified equation can be trained with small molecules, mostly from the Lipinski Rule of 5 (Ro5) chemical space, to predict the intrinsic aqueous solubility, S0, of large molecules (MW > 800 Da) from beyond...

journal_title：Molecular pharmaceutics

authors： Avdeef A,Kansy M

更新日期：2020-10-05 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：: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：:The formation of a gel coat around xanthan (Xan) tablets, empty or loaded with pentoxifylline (PF), and its release in media differing in pH and ionic strength by NMR, MR imaging, and two release methods were studied. The T1 and T2 NMR relaxation times in gels depend predominantly on Xan concentration; the presence of...

journal_title：Molecular pharmaceutics

authors： Mikac U,Sepe A,Baumgartner S,Kristl J

更新日期：2016-03-07 00:00:00

abstract：:Active targeting of nanostructures containing chemotherapeutic agents can improve cancer treatment. Here, a three-way junction pocket DNA nanostructure was developed for efficient doxorubicin (Dox) delivery into cancer cells. The three-way junction pocket DNA nanostructure is composed of three strands of AS1411 aptame...

journal_title：Molecular pharmaceutics

authors： Taghdisi SM,Danesh NM,Ramezani M,Yazdian-Robati R,Abnous K

更新日期：2018-05-07 00:00:00

abstract：:In this paper the preparation of magnetic nanocarriers (MNCs), containing superparamagnetic domains, is reported, useful as potential magnetically targeted drug delivery systems. The preparation of MNCs was performed by using the PHEA-IB-p(BMA) graft copolymer as coating material through the homogenization-solvent eva...

journal_title：Molecular pharmaceutics

authors： Licciardi M,Scialabba C,Fiorica C,Cavallaro G,Cassata G,Giammona G

更新日期：2013-12-02 00:00:00

abstract：:Conventional drug solubilization strategies limit the understanding of the full potential of poorly water-soluble drugs during drug screening. Here, we propose a screening approach in which poorly water-soluble drugs are entrapped in poly(2-(methacryloyloxyethyl phosphorylcholine)-poly(2-(diisopropylaminoethyl methacr...

journal_title：Molecular pharmaceutics

authors： Sola-Barrado B,M Leite D,Scarpa E,Duro-Castano A,Battaglia G

更新日期：2020-12-07 00:00:00