Reduced Punch Sticking Propensity of Acesulfame by Salt Formation: Role of Crystal Mechanical Property and Surface Chemistry.

abstract：:PLGA was functionalized with PEG and biotin using click chemistry to generate a biotin receptor targeted copolymer (biotinylated-PEG-PLGA) which in turn was used to fabricate ultrafine nanoparticles (BPNP) of doxorubicin hydrochloride (DOX) for effective delivery in 4T1 cell induced breast cancer. However, adequate en...

journal_title：Molecular pharmaceutics

authors： Singh Y,Durga Rao Viswanadham KK,Kumar Jajoriya A,Meher JG,Raval K,Jaiswal S,Dewangan J,Bora HK,Rath SK,Lal J,Mishra DP,Chourasia MK

更新日期：2017-08-07 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：: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：: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：: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：:Following oral administration, dabigatran etexilate (DABE) is rapidly hydrolyzed to its active form, dabigatran. DABE, but not dabigatran, presents as a P-glycoprotein (P-gp) substrate and has increasingly been used as a probe drug. Therefore, although dosed as DABE, a P-gp drug-drug interaction (DDI) is reported as a...

journal_title：Molecular pharmaceutics

authors： Shen H,Yao M,Sinz M,Marathe P,Rodrigues AD,Zhu M

更新日期：2019-09-03 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：:Many cancer therapy regimes still rely heavily on the systemic administration of toxic chemotherapeutic agents. Ultrasound contrast agents consisting of microbubbles (MBs) have emerged as a drug delivery vehicle to overcome the challenges associated with systemic chemotherapy. Here, we describe the development of non-...

journal_title：Molecular pharmaceutics

authors： Jablonowski LJ,Teraphongphom NT,Wheatley MA

更新日期：2017-10-02 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：:The molecular mechanisms of autophagy in polyethylenimine (PEI)-treated cells are not well understood because of the use of nonspecific autophagy inhibitors. Here, we applied autophagy-related gene expression analysis to pinpoint the molecular mechanisms of autophagy in PEI-treated wild-type and atg5 gene knockout (at...

journal_title：Molecular pharmaceutics

authors： Lin CW,Jan MS,Kuo JH

更新日期：2014-09-02 00:00:00

abstract：:Targeted delivery of anticancer drugs to brain tumors, especially glioblastoma multiforme, which is the most frequent and aggressive type, is one of the important objectives in nanomedicine. Vascular endothelial growth factor (VEGF) and its receptor type II (VEGFR2) are promising targets because they are overexpressed...

journal_title：Molecular pharmaceutics

authors： Shein SA,Kuznetsov II,Abakumova TO,Chelushkin PS,Melnikov PA,Korchagina AA,Bychkov DA,Seregina IF,Bolshov MA,Kabanov AV,Chekhonin VP,Nukolova NV

更新日期：2016-11-07 00:00:00

abstract：:As a chronic inflammatory and angiogenic disease with increased morbidity and mortality, rheumatoid arthritis (RA) is characterized by the proliferation of synovial tissue and the accumulation of excessive mononuclear infiltration, which always results in the joint deformity, disability, and eventually the destruction...

journal_title：Molecular pharmaceutics

authors： Wang J,Li Y,Yang Y,Du J,Zhao M,Lin F,Zhang S,Wang B

更新日期：2017-09-05 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：: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：:Lipid nanoemulsions are being investigated for the parenteral administration of poorly soluble drugs. A narrow particle size distribution in these formulations is a prerequisite for meaningful research and safe administration to patients. Autoclaving a poloxamer-stabilized trimyristin nanoemulsion resulted in moderate...

journal_title：Molecular pharmaceutics

authors： Göke K,Roese E,Bunjes H

更新日期：2018-08-06 00:00:00

abstract：:Tumor hypoxia plays a major role in radio- and chemotherapy resistance in solid tumors. Carbonic Anhydrase IX (CAIX) is an endogenous hypoxia-related protein, which is associated with poor patient outcome. The quantitative assessment of CAIX expression of tumors may steer cancer treatment by predicting therapy respons...

journal_title：Molecular pharmaceutics

authors： Huizing FJ,Hoeben BAW,Franssen GM,Boerman OC,Heskamp S,Bussink J

更新日期：2019-02-04 00:00:00

abstract：:Improving the therapeutic index of anticancer agents is an enormous challenge. Targeting decreases the side effects of the therapeutic agents by delivering the drugs to the intended destination. Nanocarriers containing the nuclear localizing peptide sequences (NLS) translocate to the cell nuclei. However, the nuclear ...

journal_title：Molecular pharmaceutics

authors： Anajafi T,Yu J,Sedigh A,Haldar MK,Muhonen WW,Oberlander S,Wasness H,Froberg J,Molla MS,Katti KS,Choi Y,Shabb JB,Srivastava DK,Mallik S

更新日期：2017-06-05 00:00:00

abstract：:Terpenoids represent a diverse class of molecules that provide a wealth of opportunities to address many human health and societal issues. The expansive array of structures and functionalities that have been evolved in nature provide an excellent pool of molecules for use in human therapeutics. While this class of mol...

journal_title：Molecular pharmaceutics

authors： Ajikumar PK,Tyo K,Carlsen S,Mucha O,Phon TH,Stephanopoulos G

更新日期：2008-03-01 00:00:00

abstract：:We investigated the effects of the hot-melt extrusion (HME) process on the properties of itraconazole (ITZ) amorphous solid dispersions made by thin film freezing (TFF) technology. The ITZ-HPMCAS L (1:2) TFF composition exhibited limited drug release in acidic media. HME of the ITZ-HPMCAS TFF composition with hydrophi...

journal_title：Molecular pharmaceutics

authors： Lang B,McGinity JW,Williams RO 3rd

更新日期：2014-01-06 00:00:00

abstract：:Process-induced phase transformations (PIPTs) of active pharmaceutical ingredients (APIs) can alter APIs' physicochemical properties and impact performance of pharmaceutical drug products. In this study, we investigated compression-induced amorphization of crystalline posaconazole (POSA), where the impact of mechanica...

journal_title：Molecular pharmaceutics

authors： Huang C,Klinzing G,Procopio A,Yang F,Ren J,Burlage R,Zhu L,Su Y

更新日期：2019-02-04 00:00:00

abstract：:The purpose of this study was to examine the melanoma targeting and imaging properties of two new (99m)Tc-labeled Arg-X-Asp-conjugated α-melanocyte stimulating hormone (α-MSH) peptides. RTD-Lys-(Arg(11))CCMSH {c[Asp-Arg-Thr-Asp-DTyr]-Lys-Cys-Cys-Glu-His-DPhe-Arg-Trp-Cys-Arg-Pro-Val-NH2} and RVD-Lys-(Arg(11))CCMSH pept...

journal_title：Molecular pharmaceutics

authors： Flook AM,Yang J,Miao Y

更新日期：2013-09-03 00:00:00

abstract：:Ipratropium bromide, an anticholinergic drug used for the treatment of asthma and chronic obstructive pulmonary disease, has low oral bioavailability, but systemic exposure, superior to oral administration, can be achieved by inhalation. Therefore, we investigated the pulmonary absorption mechanism of ipratropium usin...

journal_title：Molecular pharmaceutics

authors： Nakamura T,Nakanishi T,Haruta T,Shirasaka Y,Keogh JP,Tamai I

更新日期：2010-02-01 00:00:00

abstract：:The study presents the effects of blending a cationic gemini surfactant into cationic lipid bilayers and its impact on the plasmid DNA compaction and delivery process. Using nanoDSC, dynamic light scattering, zeta potential, and electrophoretic mobility measurements, together with transfection (2D- and 3D-) and viabil...

journal_title：Molecular pharmaceutics

authors： Sharma VD,Lees J,Hoffman NE,Brailoiu E,Madesh M,Wunder SL,Ilies MA

更新日期：2014-02-03 00:00:00

abstract：:Due to the aging of the population, the incidence of neurodegenerative diseases, such as Parkinson's and Alzheimer's, is expected to grow and, hence, the demand for adequate treatment modalities. However, the delivery of medicines into the brain for the treatment of brain-related diseases is hampered by the presence o...

journal_title：Molecular pharmaceutics

authors： Stojanov K,Georgieva JV,Brinkhuis RP,van Hest JC,Rutjes FP,Dierckx RA,de Vries EF,Zuhorn IS

更新日期：2012-06-04 00:00:00

abstract：:Recent studies on aqueous supersaturated lipophilic drug solutions prepared by methods including antisolvent addition, pH swing, or dissolution of amorphous solid dispersions (ASDs) have demonstrated that when crystallization is slow, these systems undergo liquid-liquid phase separation (LLPS) when the concentration o...

journal_title：Molecular pharmaceutics

authors： Indulkar AS,Gao Y,Raina SA,Zhang GG,Taylor LS

更新日期：2016-06-06 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：:Formulation of a cocrystal into a solid pharmaceutical dosage form entails numerous processing steps during which there is risk of dissociation. In an effort to reduce the number of unit operations, we have attempted the in situ formation of an indomethacin-saccharin (INDSAC) cocrystal during high-shear wet granulatio...

journal_title：Molecular pharmaceutics

authors： Tanaka R,Duggirala NK,Hattori Y,Otsuka M,Suryanarayanan R

更新日期：2020-01-06 00:00:00

abstract：:In the present age of pharmaceutical research and development, focused delivery of decision making data is more imperative than ever before. Resulting from several years' success, failure and consequential learning, this article also proffers advice and guidance on which in vitro and in vivo experiments to perform to ...

journal_title：Molecular pharmaceutics

authors： Grime KH,Barton P,McGinnity DF

更新日期：2013-04-01 00:00:00

abstract：:The antiviral drug tenofovir (TFV) is orally administered as the fumarate salt of its disoproxil prodrug (TFV disoproxil fumarate (TDF)). TFV is a dianion at physiological pH and, as a result, has poor lipid membrane permeability. Administration of the lipophilic and cell-permeable prodrug, TFV disoproxil, enhances th...

journal_title：Molecular pharmaceutics

authors： Durand-Gasselin L,Van Rompay KK,Vela JE,Henne IN,Lee WA,Rhodes GR,Ray AS

更新日期：2009-07-01 00:00:00

abstract：:Delivery of plasmid DNA for protein production in mammalian cells is not an efficient process. In this study, the theory that cellular localization of plasmid DNA increases transfection efficiency is examined with an emphasis on the understanding of the cellular association of the components of a ternary transfection ...

journal_title：Molecular pharmaceutics

authors： Guo C,Gemeinhart RA

更新日期：2004-07-01 00:00:00