Delivering siRNA and Chemotherapeutic Molecules Across BBB and BTB for Intracranial Glioblastoma Therapy.

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：:Colistin has been increasingly used for the treatment of respiratory infections caused by Gram-negative bacteria. Unfortunately parenteral administration of colistin can cause severe adverse effects. This study aimed to develop an inhaled combination dry powder formulation of colistin and rifapentine for the treatment...

journal_title：Molecular pharmaceutics

authors： Zhou QT,Sun SP,Chan JG,Wang P,Barraud N,Rice SA,Wang J,Li J,Chan HK

更新日期：2015-08-03 00:00:00

abstract：:We report on the fabrication and characterization of dry hybrid lipid-silica nanoparticle based microcapsules with an internal porous matrix structure for encapsulation of poorly soluble drugs, and their delivery properties (in vitro release and lipolysis and in vivo pharmacokinetics demonstrated for indomethacin as a...

journal_title：Molecular pharmaceutics

authors： Simovic S,Heard P,Hui H,Song Y,Peddie F,Davey AK,Lewis A,Rades T,Prestidge CA

更新日期：2009-05-01 00:00:00

abstract：:Selective ligands to the peripheral benzodiazepine receptor (PBR) may induce apoptosis and cell cycle arrest. An overexpression of PBR in certain cancers allowed us to consider the use of highly selective ligands to PBR for receptor-mediated drug targeting to tumors. With this in mind, we prepared PBR-targeted nanopar...

journal_title：Molecular pharmaceutics

authors： Musacchio T,Laquintana V,Latrofa A,Trapani G,Torchilin VP

更新日期：2009-03-01 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：: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：:Currently, the most prominent barrier to the success of orally delivered paclitaxel (PTX) is the extremely limited bioavailability of delivered therapeutic. In light of this issue, an amphiphilic sulfhydrylated N-deoxycholic acid-N,O-hydroxyethyl chitosan (TGA-DHC) was synthesized to improve the oral bioavailability o...

journal_title：Molecular pharmaceutics

authors： Yu Y,Huo M,Fu Y,Xu W,Cai H,Yao L,Chen Q,Mu Y,Zhou J,Yin T

更新日期：2017-12-04 00:00:00

abstract：:Hydrophilic matrices are an effective option for oral controlled release but can face challenges in terms of bioavailability and efficacy when used in conjunction with poorly soluble, weakly basic drugs. Attenuated total reflectance Fourier transform infrared (ATR-FTIR) imaging provides dynamic information relating to...

journal_title：Molecular pharmaceutics

authors： Zahoor FD,Mader KT,Timmins P,Brown J,Sammon C

更新日期：2020-04-06 00:00:00

abstract：:The ATP-binding cassette (ABC) drug transporter ABCG2 can actively efflux a wide variety of chemotherapeutic agents out of cancer cells and subsequently reduce the intracellular accumulation of these drugs. Therefore, the overexpression of ABCG2 often contributes to the development of multidrug resistance (MDR) in can...

journal_title：Molecular pharmaceutics

authors： Wu CP,Hsiao SH,Murakami M,Lu YJ,Li YQ,Huang YH,Hung TH,Ambudkar SV,Wu YS

更新日期：2017-08-07 00:00:00

abstract：:The use of adult stem cells for therapeutic purposes has met with great success in recent years. Among several types of adult stem cells, mesenchymal stem cells (MSCs) derived from bone marrow (BM) and other sources have gained popularity for basic research and clinical applications because of their therapeutic potent...

journal_title：Molecular pharmaceutics

authors： Wu H,Ye Z,Mahato RI

更新日期：2011-10-03 00:00:00

abstract：:Stably transfected MDCK/hPepT1-V5&His clonal cell lines expressing varying levels of epitope-tagged hPepT1 protein were established to quantify the relationship between transgene hPepT1 expression levels and its functional kinetics in facilitating peptide and peptide-like drug uptake and transport in vitro. The hPepT1...

journal_title：Molecular pharmaceutics

authors： Herrera-Ruiz D,Faria TN,Bhardwaj RK,Timoszyk J,Gudmundsson OS,Moench P,Wall DA,Smith RL,Knipp GT

更新日期：2004-03-01 00:00:00

abstract：:The effect of a lipidated prodrug of mitomycin C (MLP) on the membrane of a pegylated liposome formulation (PL-MLP), also known as Promitil, was characterized through high-sensitivity differential scanning calorimetry (DSC) and cryo-TEM. The thermodynamic analysis demonstrated that MLP led to the formation of heteroge...

journal_title：Molecular pharmaceutics

authors： Wei X,Patil Y,Ohana P,Amitay Y,Shmeeda H,Gabizon A,Barenholz Y

更新日期：2017-12-04 00:00:00

abstract：:Positron emission tomography (PET) imaging using 68Ga-labeled bisphosphonates to target bone metastasis could be a valuable tool in cancer diagnosis and monitoring therapeutic treatment. A 68Ga labeled ligand, N,N'-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N'-diacetic acid (HBED-CC) containing one bisphos...

journal_title：Molecular pharmaceutics

authors： Zha Z,Wu Z,Choi SR,Ploessl K,Smith M,Alexoff D,Zhu L,Kung HF

更新日期：2020-05-04 00:00:00

abstract：:Fluid bed coating has been shown to be a suitable manufacturing technique to formulate poorly soluble drugs in glass solutions. Layering inert carriers with a drug-polymer mixture enables these beads to be immediately filled into capsules, thus avoiding additional, potentially destabilizing, downstream processing. In ...

journal_title：Molecular pharmaceutics

authors： Dereymaker A,Scurr DJ,Steer ED,Roberts CJ,Van den Mooter G

更新日期：2017-04-03 00:00:00

abstract：:Our previous studies have shown that multidrug resistance protein 2 (MRP2) is overexpressed in tamoxifen-resistant MCF-7 breast cancer cells (TAMR-MCF-7 cells) and forkhead box-containing protein, O subfamily1 (FoxO1), functions as a key regulator of multidrug resistance 1 (MDR1) gene transcription. This study aimed t...

journal_title：Molecular pharmaceutics

authors： Choi HK,Cho KB,Phuong NT,Han CY,Han HK,Hien TT,Choi HS,Kang KW

更新日期：2013-07-01 00:00:00

abstract：:Targeting of drugs administered systemically relies on the higher affinity of ligands for specific receptors to obtain selectivity in drug response. However, achieving the same goal inside the bladder is much easier with an intelligent pharmaceutical approach that restricts drug effects by exploiting the pelvic anatom...

journal_title：Molecular pharmaceutics

authors： Tyagi P,Wu PC,Chancellor M,Yoshimura N,Huang L

更新日期：2006-07-01 00:00:00

abstract：:Abnormal tumor vessels impede the transport and distribution of chemotherapeutics, resulting in low drug concentration at tumor sites and compromised drug efficacy. Normalizing tumor vessels can modulate tumor vascular permeability, alleviate tumor hypoxia, increase blood perfusion, attenuate interstitial fluid pressu...

journal_title：Molecular pharmaceutics

authors： Xiao W,Ruan S,Yu W,Wang R,Hu C,Liu R,Gao H

更新日期：2017-10-02 00:00:00

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：:The formation mechanism of drug nanoparticles was investigated using solid-state nuclear magnetic resonance (NMR) techniques for the efficient discovery of an optimized nanoparticle formulation. The cogrinding of nifedipine (NIF) with polymers, including hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (P...

journal_title：Molecular pharmaceutics

authors： Ueda K,Higashi K,Moribe K

更新日期：2016-03-07 00:00:00

abstract：:It is highly demanded and still a big challenge to develop an effective formulation for immunochemotherapy against advanced tumors. We have previously reported a PEG-NLG-based immunostimulatory nanocarrier (PEG2k-Fmoc-NLG919) for co-delivery of an IDO1 inhibitor (NLG919) and a chemotherapeutic agent (paclitaxel, PTX)....

journal_title：Molecular pharmaceutics

authors： Chen Y,Sun J,Huang Y,Lu B,Li S

更新日期：2018-11-05 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：: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：:Graphene-based tumor cell nuclear targeting fluorescent nanoprobes (GTTNs) were synthesized in our laboratory as a kind of nanomaterial and showed good performance for both in vivo and in vitro imaging. GTTNs directly cross the cell membrane and specifically target the tumor cell nucleus via a cell membrane permeabili...

journal_title：Molecular pharmaceutics

authors： Gao W,Zhang J,Xue Q,Yin X,Yin X,Li C,Wang Y

更新日期：2020-07-06 00:00:00

abstract：:We report herein on the preparation of thermoresponsive hydrogels by taking advantage of the interaction of cyclodextrins (CDs) and a hydrophobically modified polymer. A hydrophobically modified hydroxypropyl methylcellulose (HM-HPMC) gel formed thermoresponsive hydrogels when small amounts of α-CD were added to the s...

journal_title：Molecular pharmaceutics

authors： Iohara D,Okubo M,Anraku M,Uramatsu S,Shimamoto T,Uekama K,Hirayama F

更新日期：2017-08-07 00:00:00

abstract：:Iron oxide nanoparticles have great potential as diagnostic and therapeutic agents in cancer and other diseases; however, biological aggregation severely limits their function in vivo. Aggregates can cause poor biodistribution, reduced heating capability, and can confound their visualization and quantification by magn...

journal_title：Molecular pharmaceutics

authors： Hurley KR,Ring HL,Etheridge M,Zhang J,Gao Z,Shao Q,Klein ND,Szlag VM,Chung C,Reineke TM,Garwood M,Bischof JC,Haynes CL

更新日期：2016-07-05 00:00:00

abstract：:Engineered superparamagnetic iron oxide nanoparticles (SPIONs) have been studied extensively for their localized homogeneous heat generation in breast cancer therapy. However, challenges such as aggregation and inability to produce sub-10 nm SPIONs limit their potential in magnetothermal ablation. We report a facile, ...

journal_title：Molecular pharmaceutics

authors： Alhasan AH,Fardous RS,Alsudir SA,Majrashi MA,Alghamdi WM,Alsharaeh EH,Almalik AM

更新日期：2019-08-05 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：:There is a great need for delivery strategies capable of efficiently localizing drugs to the damaged myocardium that do not require direct intramyocardial injection of therapeutic molecules. In the work discussed here, we exploited the myocardium-specific upregulation of matrix metalloproteinases (MMPs) that occurs du...

journal_title：Molecular pharmaceutics

authors： Nguyen J,Sievers R,Motion JP,Kivimäe S,Fang Q,Lee RJ

更新日期：2015-04-06 00:00:00

abstract：:Water-insoluble anticancer drugs, including paclitaxel, present severe clinical side effects when administered to patients, primarily associated with the toxicity of reagents used to solubilize the drugs. In efforts to develop alternative formulations of water-insoluble anticancer drugs suitable for intravenous admini...

journal_title：Molecular pharmaceutics

authors： Kim JH,Kim Y,Bae KH,Park TG,Lee JH,Park K

更新日期：2015-04-06 00:00:00

abstract：:HEPES has been widely employed as an organic buffer agent in cell culture medium as well as uptake and transport experiments in vitro. However, concentrations of HEPES used in such studies vary from one laboratory to another. In this study, we investigated the effect of HEPES on the uptake and bidirectional transport ...

journal_title：Molecular pharmaceutics

authors： Luo S,Pal D,Shah SJ,Kwatra D,Paturi KD,Mitra AK

更新日期：2010-04-05 00:00:00