Photolytic Labeling To Quantify Peptide-Water Interactions in Lyophilized Solids.

abstract：:The small molecule fluorescein is commonly used to guide the repair of cerebral spinal fluid leaks (CSFLs) in the clinic. We modified fluorescein so that it is also visible by positron emission tomography (PET). This probe was used to quantitatively track the fast distribution of small molecules in the CSF of rats. We...

journal_title：Molecular pharmaceutics

authors： Guo H,Kommidi H,Maachani UB,Voronina JC,Zhang W,Magge RS,Ivanidze J,Wu AP,Souweidane MM,Aras O,Ting R

更新日期：2019-08-05 00:00:00

abstract：:Genospheres are cationic lipid-nucleic acid nanoparticles prepared by the assembly of the lipids and nucleic acids from an aqueous/organic liquid monophase that independently dissolves the components, where the resultant particles are homogeneously sized (70-110 nm), with efficiently incorporated and protected DNA. In...

journal_title：Molecular pharmaceutics

authors： Hayes ME,Drummond DC,Hong K,Zheng WW,Khorosheva VA,Cohen JA,C O N 4th,Park JW,Marks JD,Benz CC,Kirpotin DB

更新日期：2006-11-01 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：: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：:We report the development of sponge Haliclona sp. spicules, referred to as SHS, and its topical application in skin delivery of hydrophilic biomacromolecules, a series of fluorescein isothiocyanate-dextrans (FDs). SHS are silicious oxeas which are sharp-edged and rod-shaped (∼120 μm in length and ∼7 μm in diameter). S...

journal_title：Molecular pharmaceutics

authors： Zhang S,Ou H,Liu C,Zhang Y,Mitragotri S,Wang D,Chen M

更新日期：2017-09-05 00:00:00

abstract：:Effective delivery is a critical issue in the use of conventional free drugs. Studies on the structure-function relationship of a therapeutic antibody-derived candidacidal decapeptide (killer peptide, KP) revealed its ability to spontaneously and reversibly self-assemble in an organized network of fibril-like structur...

journal_title：Molecular pharmaceutics

authors： Pertinhez TA,Conti S,Ferrari E,Magliani W,Spisni A,Polonelli L

更新日期：2009-05-01 00:00:00

abstract：:The wet form of age-related macular degeneration (AMD) is a leading cause of blindness among elderly Americans and is characterized by abnormal vessel growth, termed choroidal neovascularization (CNV). Integrin α5β1 is a transmembrane receptor that binds matrix macromolecules and proteinases to stimulate angiogenesis....

journal_title：Molecular pharmaceutics

authors： Wang WQ,Wang FH,Qin WX,Liu HY,Lu B,Chung C,Zhu J,Gu Q,Shi W,Wen C,Wu F,Zhang K,Sun XD

更新日期：2016-09-06 00:00:00

abstract：:In this study, dinitrosyl iron complexes (DNICs) are shown to deliver nitric oxide (NO) into the cytosol of vascular smooth muscle cells (SMCs), which play a major role in vascular relaxation and contraction. Malfunction of SMCs can lead to hypertension, asthma, and erectile dysfunction, among other disorders. For com...

journal_title：Molecular pharmaceutics

authors： Pectol DC,Khan S,Chupik RB,Elsabahy M,Wooley KL,Darensbourg MY,Lim SM

更新日期：2019-07-01 00:00:00

abstract：:In this study, transferrin (Tf)-modified poly(ethylene glycol)-phosphatidylethanolamine (mPEG-PE) micelles loaded with the poorly water-soluble drug, R547 (a potent and selective ATP-competitive cyclin-dependent kinase (CDK) inhibitor), were prepared and evaluated for their targeting efficiency and cytotoxicity in vit...

journal_title：Molecular pharmaceutics

authors： Sawant RR,Jhaveri AM,Koshkaryev A,Zhu L,Qureshi F,Torchilin VP

更新日期：2014-02-03 00:00:00

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：:New bifunctional hexa- and octadentate analogues of the hydroxamate-containing siderophore desferrichrome (DFC) have been synthesized and evaluated as 89Zr-chelating agents for immunoPET applications. The in vitro and in vivo inertness of these new ligands, Orn3-hx (hexadentate) and Orn-4hx derivatives (octadentate), ...

journal_title：Molecular pharmaceutics

authors： Adams CJ,Wilson JJ,Boros E

更新日期：2017-08-07 00:00:00

abstract：:In this study, a facile strategy for efficient codelivery of gene and drug was developed. Using a coprecipitation method, doxorubicin hydrochloride (DOX), an antitumor drug, and p53 expression plasmid were encapsulated in alginate/CaCO(3)/DNA/DOX nanoparticles with high encapsulation efficiency. The in vitro cell inhi...

journal_title：Molecular pharmaceutics

authors： Zhao D,Liu CJ,Zhuo RX,Cheng SX

更新日期：2012-10-01 00:00:00

abstract：:The human apical sodium-dependent bile acid transporter (hASBT) is a potential target for drug delivery, but an understanding of hASBT substrate requirements is limited. The objective of this study was to evaluate the influence of ionic character and steric bulk in the C-24 region of bile acid conjugates in governing ...

journal_title：Molecular pharmaceutics

authors： Balakrishnan A,Wring SA,Coop A,Polli JE

更新日期：2006-05-01 00:00:00

abstract：:The impact of OATP drug uptake transporters in drug-drug interactions (DDIs) is increasingly recognized. OATP1B1 and OATP1B3 are human hepatic uptake transporters that can mediate liver uptake of a wide variety of drugs. Recently, we generated transgenic mice with liver-specific expression of human OATP1B1 or OATP1B3 ...

journal_title：Molecular pharmaceutics

authors： Durmus S,Lozano-Mena G,van Esch A,Wagenaar E,van Tellingen O,Schinkel AH

更新日期：2015-12-07 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：:Two coamorphous drug-amino acid systems, indomethacin-tryptophan (Ind-Trp) and furosemide-tryptophan (Fur-Trp), were analyzed toward their ease of amorphization and mechanism of coamorphization during ball milling. The two mixtures were compared to the corresponding amorphization of the pure drug without amino acid. P...

journal_title：Molecular pharmaceutics

authors： Jensen KT,Larsen FH,Cornett C,Löbmann K,Grohganz H,Rades T

更新日期：2015-07-06 00:00:00

abstract：:Recently we characterized an unusual switch in the internalization mechanism of the monomeric and dimeric forms of the cell-penetrating peptide RDLWEMMMVSLACQY. Here, we observed both energy-dependent and energy-independent modes of peptide uptake by the target B-lymphocytes WI-L2-729HF2, suggesting that higher-order ...

journal_title：Molecular pharmaceutics

authors： Kim Y,Lillo A,Moss JA,Janda KD

更新日期：2005-11-01 00:00:00

abstract：:Our previous studies have demonstrated that a generation 5 dendrimer (G5) conjugated with both folic acid (FA) and methotrexate (MTX) has a higher chemotherapeutic index than MTX alone. Despite this, batch-to-batch inconsistencies in the number of FA and MTX molecules linked to each dendrimer led to conjugate batches ...

journal_title：Molecular pharmaceutics

authors： Thomas TP,Huang B,Choi SK,Silpe JE,Kotlyar A,Desai AM,Zong H,Gam J,Joice M,Baker JR Jr

更新日期：2012-09-04 00:00:00

abstract：:Although tumor-targeting nanovehicles for hepatocellular carcinoma (HCC) chemotherapy have attracted great research and clinic interest, the poor cancer penetration, inefficient cellular uptake, and slow intracellular drug release greatly compromise their therapeutic outcomes. In this work, a multifunctional mixed mic...

journal_title：Molecular pharmaceutics

authors： Zhang J,Zheng Y,Xie X,Wang L,Su Z,Wang Y,Leong KW,Chen M

更新日期：2017-11-06 00:00:00

abstract：:Metastasis is the primary cause resulting in the high mortality of breast cancer. The inherent antimetastasis bioactivity of Pluronic copolymers with a wide range of hydrophilic-lipophilic balance (HLB) including Pluronic L61, P85, P123, F127, F68, and F108 was first explored on metastatic 4T1 breast cancer cells. The...

journal_title：Molecular pharmaceutics

authors： Sun H,Meng Q,Tang S,Su J,Yin Q,Chen L,Gu W,Yu H,Zhang Z,Wang S,Li Y

更新日期：2015-09-08 00:00:00

abstract：:Lipid-based nanoparticles are considered as promising candidates for delivering siRNA into the cytoplasm of targeted cells. However, in vivo efficiency of these nanoparticles is critically dependent on formulation strategies of lipid-siRNA complexes. Adsorption of serum proteins to lipid-siRNA complexes and its charge...

journal_title：Molecular pharmaceutics

authors： Dar GH,Gopal V,Rao NM

更新日期：2015-02-02 00:00:00

abstract：:The most promising F508del-CFTR corrector, VX-809, has been unsuccessful as an effective, stand-alone treatment for CF patients, but the rescue effect in combination with other drugs may confer an acceptable level of therapeutic benefit. Targeting cellular factors that modify trafficking may act to enhance the cell su...

journal_title：Molecular pharmaceutics

authors： Perkins LA,Fisher GW,Naganbabu M,Schmidt BF,Mun F,Bruchez MP

更新日期：2018-03-05 00:00:00

abstract：:Stereoregularity of polymers is known to influence their physicochemical and functional properties in the bulk form. Recent studies have also provided evidence for the effect of polymer stereoregularity on the physicochemical and functional properties of their self-assembled nanostructures. Research in this area has w...

journal_title：Molecular pharmaceutics

authors： Soleymani Abyaneh H,Vakili MR,Shafaati A,Lavasanifar A

更新日期：2017-08-07 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：:This research determined the uptake of individual components of topically applied microemulsions into the stratum corneum (SC) and assessed their molecular effects on skin barrier function. The microemulsions comprised oleic acid, Tween20, Transcutol and water. The effects of selected formulations, and of the individu...

journal_title：Molecular pharmaceutics

authors： Hathout RM,Mansour S,Mortada ND,Geneidi AS,Guy RH

更新日期：2010-08-02 00:00:00

abstract：:Milk has been used as a vehicle for the delivery of antimalarial drugs during clinical trials to test for a food effect and artefenomel (OZ439) showed enhanced oral bioavailability with milk. However, the nature of the interaction between milk and OZ439 in the gastrointestinal tract remains poorly understood. To under...

journal_title：Molecular pharmaceutics

authors： Salim M,Khan J,Ramirez G,Clulow AJ,Hawley A,Ramachandruni H,Boyd BJ

更新日期：2018-08-06 00:00:00

abstract：:Photodynamic therapy (PDT) has been shown to kill cancer cells and improve survival and quality of life in cancer patients, and numerous new approaches have been considered for maximizing the efficacy of PDT. In this study, a new multifunctional nanophotosensitizer Ce6/GE11-(pH)micelle was developed to target epiderma...

journal_title：Molecular pharmaceutics

authors： Chu WY,Tsai MH,Peng CL,Shih YH,Luo TY,Yang SJ,Shieh MJ

更新日期：2018-04-02 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：:We report on tailored lipid-polymer hybrid nanoparticles (NPs) delivering nitric oxide (NO) under the control of visible light as a tool for overcoming doxorubicin (DOX) resistance. The NPs consist of a polymeric core and a coating. They are appropriately designed to entrap DOX in the poly(lactide-co-glycolide) core a...

journal_title：Molecular pharmaceutics

authors： Fraix A,Conte C,Gazzano E,Riganti C,Quaglia F,Sortino S

更新日期：2020-06-01 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