Probing phase transitions in simvastatin with terahertz time-domain spectroscopy.

abstract：:Similar to glycolysis, glutaminolysis acts as a vital energy source in tumor cells, providing building blocks for the metabolic needs of tumor cells. To capture glutaminolysis in tumors, 18F-(2S,4R)4-fluoroglutamine ([18F]FGln) and 18F-fluoroboronoglutamine ([18F]FBQ) have been successfully developed for positron emis...

journal_title：Molecular pharmaceutics

authors： Chen J,Li C,Hong H,Liu H,Wang C,Xu M,Han Y,Liu Z

更新日期：2019-12-02 00:00:00

abstract：:Hydrophilic peptides constitute most of the active peptides. They mostly permeate via tight junctions (paracellular pathway) in the intestine. This permeability mechanism restricts the magnitude of their oral absorption and bioavailability. We hypothesized that concealing the hydrophilic residues of the peptide using ...

journal_title：Molecular pharmaceutics

authors： Schumacher-Klinger A,Fanous J,Merzbach S,Weinmüller M,Reichart F,Räder AFB,Gitlin-Domagalska A,Gilon C,Kessler H,Hoffman A

更新日期：2018-08-06 00:00:00

abstract：:This paper develops a structure-activity relationship understanding of the way in which surfactant-like dendrons with hydrophilic spermine surface groups and a variety of lipophilic units at their focal points can self-assemble and subsequently bind to DNA with high affinity. The choice of functional group at the foca...

journal_title：Molecular pharmaceutics

authors： Jones SP,Gabrielson NP,Wong CH,Chow HF,Pack DW,Posocco P,Fermeglia M,Pricl S,Smith DK

更新日期：2011-04-04 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

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：: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：:Current cancer chemotherapies commonly suffer from nonspecificity, drug resistance, poor bioavailability, and narrow therapeutic indices. To achieve the optimum drug efficacy, we designed a polymeric drug delivery system for targeted intracellular delivery of a clinically approved, water-soluble anticancer drug, gemci...

journal_title：Molecular pharmaceutics

authors： Kulhari H,Pooja D,Kota R,Reddy TS,Tabor RF,Shukla R,Adams DJ,Sistla R,Bansal V

更新日期：2016-05-02 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

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：:Hydrophobic single-wall carbon nanohorns (SWNHs) were dispersed in aqueous media by noncovalently modifying their surfaces with conjugate molecules comprised of polyethylene glycol (PEG) and a peptide aptamer (NHBP-1) that specifically bind to the surfaces of the SWNHs. The conjugates were synthesized by coupling PEG ...

journal_title：Molecular pharmaceutics

authors： Matsumura S,Ajima K,Yudasaka M,Iijima S,Shiba K

更新日期：2007-09-01 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：:The killing efficacy of doxorubicin from liposome-based delivery carriers has been shown to correlate strongly with its intracellular trafficking and, in particular, its fast and extensive release from the delivery carrier. However, previously explored pH-triggered mechanisms that were designed to become activated dur...

journal_title：Molecular pharmaceutics

authors： Mamasheva E,O'Donnell C,Bandekar A,Sofou S

更新日期：2011-12-05 00:00:00

abstract：:How genotypic variation results in phenotypic differences is still a challenge for biology. In the field of drug metabolism, the means by which specific cytochrome P4502D6 (CYP2D6) genotypes yield different phenotypes at various levels (molecular, cellular, and organismal) is an important question, as differences in C...

journal_title：Molecular pharmaceutics

authors： Gao J,Tian X,Zhou J,Cui MZ,Zhang HF,Gao N,Wen Q,Qiao HL

更新日期：2017-03-06 00:00:00

abstract：:Therapeutic efficacy of nanocarriers can be amplified by active targeting and overcoming the extracellular matrix associated barriers of tumors. The aim of the present study was to investigate the effect of oral antifibrotic agent (telmisartan) on tumor uptake and anticancer efficacy of EphA2 receptor targeted liposom...

journal_title：Molecular pharmaceutics

authors： Patel K,Doddapaneni R,Sekar V,Chowdhury N,Singh M

更新日期：2016-06-06 00:00:00

abstract：:5P12-RANTES is a recently developed chemokine analogue that has shown high level protection from SHIV infection in macaques. However, the feasibility of using 5P12-RANTES as a long-term HIV prevention agent has not been explored partially due to the lack of available delivery devices that can easily be modified for lo...

journal_title：Molecular pharmaceutics

authors： Wang NX,Sieg SF,Lederman MM,Offord RE,Hartley O,von Recum HA

更新日期：2013-10-07 00:00:00

abstract：:We examined the inhibitory effect of hydroxypropyl methylcellulose acetate succinate (HPMC-AS) on drug recrystallization from a supersaturated solution using carbamazepine (CBZ) and phenytoin (PHT) as model drugs. HPMC-AS HF grade (HF) inhibited the recrystallization of CBZ more strongly than that by HPMC-AS LF grade ...

journal_title：Molecular pharmaceutics

authors： Ueda K,Higashi K,Yamamoto K,Moribe K

更新日期：2013-10-07 00:00:00

abstract：:Gold nanoparticles (AuNPs) have a number of physical properties that make them appealing for medical applications. For example, the attenuation of X-rays by gold nanoparticles has led to their use in computed tomography imaging and as adjuvants for radiotherapy. AuNPs have numerous other applications in imaging, thera...

journal_title：Molecular pharmaceutics

authors： Mieszawska AJ,Mulder WJ,Fayad ZA,Cormode DP

更新日期：2013-03-04 00:00:00

abstract：:This work demonstrates the way to achieve efficient and target specific delivery of a graphene quantum dot (GQD) using hyaluronic acid (HA) (GQD-HA) as a targeting agent. HA has been anchored to a GQD that accepts the fascinating adhesive properties of the catechol moiety, dopamine hydrochloride, conjugated to HA, whi...

journal_title：Molecular pharmaceutics

authors： Abdullah-Al-Nahain,Lee JE,In I,Lee H,Lee KD,Jeong JH,Park SY

更新日期：2013-10-07 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：:Tablets which were binary mixtures of pioglitazone hydrochloride (PioHCl) with magnesium stearate (MgSt), croscarmellose sodium (CCS), microcrystalline cellulose, or lactose monohydrate were prepared. Two sets of experiments, using intact tablets, were performed. (i) Tablets containing PioHCl (90% w/w) and MgSt were e...

journal_title：Molecular pharmaceutics

authors： Koranne S,Govindarajan R,Suryanarayanan R

更新日期：2017-04-03 00:00:00

abstract：:Lipid-core nanocapsules (LCNs) have been proposed as drug carriers to improve brain delivery by modulating drug pharmacokinetics (PK). However, it is not clear whether the LCNs carry the drug through the blood-brain barrier or increase free drug penetration due to changes in the barrier permeability. Quetiapine (QTP) ...

journal_title：Molecular pharmaceutics

authors： Carreño F,Paese K,Silva CM,Guterres SS,Dalla Costa T

更新日期：2016-04-04 00:00:00

abstract：:Progesterone receptor (PR) is a significant biomarker in diseases such as endometriosis and breast, ovarian, and uterine cancers that is associated with disease prognosis and therapeutic efficacy. While receptor status is currently determined by immunohistochemistry assays, the development of noninvasive PR imaging ag...

journal_title：Molecular pharmaceutics

authors： Sukerkar PA,MacRenaris KW,Meade TJ,Burdette JE

更新日期：2011-08-01 00:00:00

abstract：:It is well-known that renal cell carcinomas (RCCs) are resistant to classical cytotoxic anticancer drugs. Therefore, facilitating the impact of anticancer drugs by altering the cell phenotype should be a useful strategy for circumventing this. We developed a multifunctional envelope-type nanodevice (MEND) as an in viv...

journal_title：Molecular pharmaceutics

authors： Sakurai Y,Hatakeyama H,Akita H,Harashima H

更新日期：2014-08-04 00:00:00

abstract：:In the postprandial stomach, processes such as secretion, digestion, and gastric emptying all occur simultaneously. Therefore, the system is highly heterogeneous and dynamically changing, for instance, in terms of various physicochemical parameters such as pH value or viscosity. Thus, the administration of a drug toge...

journal_title：Molecular pharmaceutics

authors： Schick P,Sager M,Wegner F,Wiedmann M,Schapperer E,Weitschies W,Koziolek M

更新日期：2019-11-04 00:00:00

abstract：:Cancer research regarding near-infrared (NIR) agents for chemothermal therapy (CTT) has shown that agents with specific functions are able to inhibit tumor growth. The aim of current study was to optimize CTT efficacy for treatment of colorectal cancer (CRC) by exploring strategies which can localize high temperature ...

journal_title：Molecular pharmaceutics

authors： Tsai MH,Peng CL,Yang SJ,Shieh MJ

更新日期：2017-08-07 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：: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：:To overcome the P-glycoprotein (P-gp)-induced multidrug resistance (MDR) of cancer cells, a novel copolymer, chitosan-graft-D-α-tocopheryl polyethylene glycol 1000 (TPGS) (CT) was synthesized for doxorubicin (DOX) delivery by the P-gp inhibiting virtue of TPGS. DOX-loaded CT nanoparticles (NPs) were fabricated by a mo...

journal_title：Molecular pharmaceutics

authors： Guo Y,Chu M,Tan S,Zhao S,Liu H,Otieno BO,Yang X,Xu C,Zhang Z

更新日期：2014-01-06 00:00:00

abstract：:Two-phase gas-liquid microfluidic reactors provide shear processing control of SN-38-loaded polymer nanoparticles (SN-38-PNPs). We prepare SN-38-PNPs from the block copolymer poly(methyl caprolactone- co-caprolactone)- block-poly(ethylene oxides) (P(MCL- co-CL)- b-PEO) using bulk and microfluidic methods and at differ...

journal_title：Molecular pharmaceutics

authors： Cao Y,Silverman L,Lu C,Hof R,Wulff JE,Moffitt MG

更新日期：2019-01-07 00:00:00

abstract：:Dual variable domain immunoglobulin proteins (DVD-Ig proteins) are large molecules (MW ∼ 200 kDa) with increased asymmetry because of their extended Y-like shape, which results in increased formulation challenges. Liquid-liquid phase separation (LLPS) of protein solutions into protein-rich and protein-poor phases redu...

journal_title：Molecular pharmaceutics

authors： Raut AS,Kalonia DS

更新日期：2015-09-08 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