Comparison of the permeability of metoprolol and labetalol in rat, mouse, and Caco-2 cells: use as a reference standard for BCS classification.

abstract：:The development of cancer and fibrotic diseases has been shown to be highly dependent on disregulation of cap-dependent translation. Binding protein eIF4E to N(7)-methylated guanosine capped mRNA has been found to be the rate-limiting step governing translation initiation, and therefore represents an attractive target...

journal_title：Molecular pharmaceutics

authors： Li S,Jia Y,Jacobson B,McCauley J,Kratzke R,Bitterman PB,Wagner CR

更新日期：2013-02-04 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：:One hypothesis for persisting HIV-associated neurocognitive disorders (HAND) in effectively treated individuals is the limited permeation of antiretroviral agents (ARV) across the blood-brain barrier (BBB). However, the physicochemical factors limiting the brain entry of a given ARV and the mutual interactions of comb...

journal_title：Molecular pharmaceutics

authors： Marzolini C,Mueller R,Li-Blatter X,Battegay M,Seelig A

更新日期：2013-06-03 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

authors： Smith AJ,Kavuru P,Arora KK,Kesani S,Tan J,Zaworotko MJ,Shytle RD

更新日期：2013-08-05 00:00:00

abstract：:A redox-sensitive prodrug, octreotide(Phe)-polyethene glycol-disulfide bond-paclitaxel [OCT(Phe)-PEG-ss-PTX], was successfully developed for targeted intracellular delivery of PTX. The formulation emphasizes long-circulation-time polymer-drug conjugates, combined targeting based on EPR and OCT-receptor mediated endocy...

journal_title：Molecular pharmaceutics

authors： Yin T,Wu Q,Wang L,Yin L,Zhou J,Huo M

更新日期：2015-08-03 00:00:00

abstract：:There are an increasing number of studies showing the order of drug presentation plays a critical role in achieving optimal combination therapy. Here, a nanoparticle design is presented using ion pairing and drug-polymer conjugate for the sequential delivery of gefitinib (Gi) and doxorubicin (Dox) targeting epidermal ...

journal_title：Molecular pharmaceutics

authors： Zhou Z,Jafari M,Sriram V,Kim J,Lee JY,Ruiz-Torres SJ,Waltz SE

更新日期：2017-12-04 00:00:00

abstract：:Itraconazole is a drug of choice for the treatment of severe fungal infections and parasitic diseases, but its use is limited by its low water solubility and varying bioavailability. New self-emulsifying drug delivery systems (SEDDS) based on PEGylated bile acids (BA-PEGs) were designed and prepared, where the number ...

journal_title：Molecular pharmaceutics

authors： Le Dévédec F,Strandman S,Hildgen P,Leclair G,Zhu XX

更新日期：2013-08-05 00:00:00

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 hepatobil...

journal_title：Molecular pharmaceutics

authors： 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 D

更新日期：2018-02-05 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：:Approximately, 40-70% of active pharmaceutical ingredients (API) are severely limited by their extremely poor aqueous solubility, and consequently, there is a high demand for excipients that can be used to formulate clinically relevant doses of these drug candidates. Here, proof-of-concept studies demonstrate the pote...

journal_title：Molecular pharmaceutics

authors： Hettiarachchi G,Samanta SK,Falcinelli S,Zhang B,Moncelet D,Isaacs L,Briken V

更新日期：2016-03-07 00:00:00

abstract：:The objective of this study was to enhance oral mucosal permeation of fenretinide by coincorporation of propylene glycol (PG) and menthol in fenretinide/Eudragit RL PO mucoadhesive patches. Fenretinide is an extremely hydrophobic chemopreventive compound with poor tissue permeability. Coincorporation of 5-10 wt % PG (...

journal_title：Molecular pharmaceutics

authors： Wu X,Desai KG,Mallery SR,Holpuch AS,Phelps MP,Schwendeman SP

更新日期：2012-04-02 00:00:00

abstract：:In this paper, we investigate the release of two drugs, nicotine and caffeine, from poly epsilon-caprolactone (PCL) matrices, as a model for the delivery of highly hydrophilic drugs. Since PCL does not degrade over the period of our experiments (<30 days), drug diffusion through the matrix is expected to be the domina...

journal_title：Molecular pharmaceutics

authors： Rosenberg R,Devenney W,Siegel S,Dan N

更新日期：2007-11-01 00:00:00

abstract：:Some of the most significant therapeutic leads and agents used for the treatment of cancer target microtubule dynamics. Paclitaxel is an exceptional example that is currently used for treating a wide range of tumors. New, non-taxane microtubule stabilizers, including several epothilones, are advancing through clinical...

journal_title：Molecular pharmaceutics

authors： Clark EA,Hills PM,Davidson BS,Wender PA,Mooberry SL

更新日期：2006-07-01 00:00:00

abstract：:Recent developments in pharmaceutical technology have facilitated the design and production of modified release formulas for drugs whose physical, chemical or biological properties impede release and thus might compromise their efficacy or safety. One such drug is morphine, whose short half-life requires repeated dose...

journal_title：Molecular pharmaceutics

authors： Morales ME,López G,Gallardo V,Ruiz MA

更新日期：2011-04-04 00:00:00

abstract：:For aggressive brain glioblastoma, the therapy is significantly impaired by blood-brain barrier (BBB) and blood-tumor barrier (BTB). Choosing more than one target from the pool of tumor-stroma interactions is profoundly beneficial to therapeutic approaches. Thus, a multifunctional liposomal system based on anchoring t...

journal_title：Molecular pharmaceutics

authors： Yang ZZ,Gao W,Liu YJ,Pang N,Qi XR

更新日期：2017-04-03 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：:Whether luteolin inhibits HBV replication has not been validated and the underlying mechanism of which has never been elucidated. In this study, we show that luteolin reduces HBV DNA replication in HepG2.2.15 cells. Luteolin effectively inhibited the expression of hepatocyte nuclear factor 4α (HNF4α) and its binding t...

journal_title：Molecular pharmaceutics

authors： Bai L,Nong Y,Shi Y,Liu M,Yan L,Shang J,Huang F,Lin Y,Tang H

更新日期：2016-02-01 00:00:00

abstract：:Antibody-based near-infrared photoimmunotherapy (NIR-PIT) is an attractive strategy for cancer treatment. Tumor cells can be selectively and efficiently killed by the targeted delivery of an antibody-photoabsorber complex followed by exposure to NIR light. Glycoprotein A33 antigen (GPA33) is highly expressed in most h...

journal_title：Molecular pharmaceutics

authors： Wei D,Tao Z,Shi Q,Wang L,Liu L,She T,Yi Q,Wen X,Liu L,Li S,Yang H,Jiang X

更新日期：2020-07-06 00:00:00

abstract：:In the drug discovery setting, the ability to rapidly identify drug absorption risk in preclinical species at high doses from easily measured physical properties is desired. This is due to the large number of molecules being evaluated and their high attrition rate, which make resource-intensive in vitro and in silico ...

journal_title：Molecular pharmaceutics

authors： Wuelfing WP,Daublain P,Kesisoglou F,Templeton A,McGregor C

更新日期：2015-04-06 00:00:00

abstract：:The transfer of genetic material into cells using nonviral vectors offers unique potential for therapeutics; however, the efficacy of delivery depends upon a poorly understood, multistep pathway, limiting the prospects for successful gene delivery. Mechanistic insight into DNA association and release has been hampered...

journal_title：Molecular pharmaceutics

authors： Prevette LE,Nikolova EN,Al-Hashimi HM,Banaszak Holl MM

更新日期：2012-09-04 00:00:00

abstract：:Major obstacles in the development of new therapeutic anticancer drugs are the low bioavailability of hydrophilic substances and the nonspecific toxicity toward healthy tissues. As such, cell-targeting oligopeptides have emerged as attractive drug delivery vehicles for a variety of different types of cargo. The recent...

journal_title：Molecular pharmaceutics

authors： Liu Y,Steiniger SC,Kim Y,Kaufmann GF,Felding-Habermann B,Janda KD

更新日期：2007-05-01 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：:Therapeutic monoclonal antibody (mAb) candidates that form highly viscous solutions at concentrations above 100 mg/mL can lead to challenges in bioprocessing, formulation development, and subcutaneous drug delivery. Earlier studies of mAbs with concentration-dependent high viscosity have indicated that mAbs with negat...

journal_title：Molecular pharmaceutics

authors： Buck PM,Chaudhri A,Kumar S,Singh SK

更新日期：2015-01-05 00:00:00

abstract：:The formulation of drug/polymer amorphous solid dispersions (ASDs) is one of the most successful strategies for improving the oral bioavailability of poorly soluble active pharmaceutical ingredients (APIs). Hot-melt extrusion (HME) is one method for preparing ASDs that is growing in importance in the pharmaceutical in...

journal_title：Molecular pharmaceutics

authors： Pisa E,Hughes LP,Wren SAC,Booth J,McCabe JF,Whittaker DTE,Mantle MD

更新日期：2020-06-01 00:00:00

abstract：:In order to gain molecular level understanding of drug dissolution into aqueous media, we report the first molecular dynamics (MD) simulation of a drug crystal dissolving. The simulation was performed for acetaminophen crystal Form I dissolving in 0.15 M aqueous NaCl solution at 37 °C. The 10 ns simulation revealed in...

journal_title：Molecular pharmaceutics

authors： Gao Y,Olsen KW

更新日期：2013-03-04 00:00:00

abstract：:This study determined intraluminal ethanol concentrations (stomach and duodenum) in fed healthy volunteers after the consumption of common alcoholic beverages (beer, wine, and whisky). The results of this study were compared with a previous study in fasted volunteers. Five healthy volunteers were recruited in a crosso...

journal_title：Molecular pharmaceutics

authors： Rubbens J,Riethorst D,Brouwers J,Wolfs K,Adams E,Tack J,Augustijns P

更新日期：2017-12-04 00:00:00

abstract：:The thermal unfolding and subsequent aggregation of the unglycosylated Fc fragment of a human IgG1 antibody (Fc) were studied in the salt solutions of Na(2)SO(4), KF, KCl and KSCN at pH 4.8 and 7.2 below and at its pI of 7.2, respectively, using differential scanning calorimetry (DSC), far ultraviolet circular dichroi...

journal_title：Molecular pharmaceutics

authors： Zhang-van Enk J,Mason BD,Yu L,Zhang L,Hamouda W,Huang G,Liu D,Remmele RL Jr,Zhang J

更新日期：2013-02-04 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：:In this work, we have developed covalent and low molecular weight docetaxel delivery systems based on conjugation with N-acetyl-d-galactosamine and studied their properties related to hepatocellular carcinoma cells. The resulting glycoconjugates have an excellent affinity to the asialoglycoprotein receptor (ASGPR) in ...

journal_title：Molecular pharmaceutics

authors： Petrov RA,Mefedova SR,Yamansarov EY,Maklakova SY,Grishin DA,Lopatukhina EV,Burenina OY,Lopukhov AV,Kovalev SV,Timchenko YV,Ondar EE,Ivanenkov YA,Evteev SA,Vaneev AN,Timoshenko RV,Klyachko NL,Erofeev AS,Gorelkin PV,Bel

更新日期：2021-01-04 00:00:00

abstract：:In vitro antibody discovery and/or affinity maturation are often performed using antibody fragments (Fabs), but most monovalent Fabs are reformatted as bivalent IgGs (monoclonal antibodies, mAbs) for therapeutic applications. One problem related to reformatting antibodies is that the bivalency of mAbs can lead to incr...

journal_title：Molecular pharmaceutics

authors： Alam ME,Geng SB,Bender C,Ludwig SD,Linden L,Hoet R,Tessier PM

更新日期：2018-01-02 00:00:00