Gene expression profiling of transporters in the solute carrier and ATP-binding cassette superfamilies in human eye substructures.

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：:Block copolymer micelles (BCMs) have been employed as effective drug delivery systems to solid tumors by virtue of their capacity to transport large therapeutic payloads and passively target tumor sites. Active targeting of nanoparticles (NPs) has been exploited as a means to increase the therapeutic efficacy of NP-ba...

journal_title：Molecular pharmaceutics

authors： Hoang B,Ekdawi SN,Reilly RM,Allen C

更新日期：2013-11-04 00:00:00

abstract：:Robust deposition of extracellular matrix is a significant barrier for delivery of nanotherapeutics and small-molecule anticancer drugs to different tumors including pancreatic ductal adenocarcinoma. Here, we investigated permeation and total uptake of polystyrene nanoparticles of different diameters in 3D multicellul...

journal_title：Molecular pharmaceutics

authors： Durymanov M,Kroll C,Permyakova A,Reineke J

更新日期：2019-03-04 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：:This work aims to elucidate the mechanism by which N-methylpyrrolidone (NMP) enhances the skin permeation of a compound by combining experimental data with molecular dynamic (MD) simulations. The addition of 10% NMP significantly increased the propranolol (PR) permeation through the human epidermis (∼ 15 μg/cm(2) vs ∼...

journal_title：Molecular pharmaceutics

authors： Cilurzo F,Vistoli G,Selmin F,Gennari CG,Musazzi UM,Franzé S,Lo Monte M,Minghetti P

更新日期：2014-03-03 00:00:00

abstract：:Solubility limited compounds require enabling formulations such as amorphous solid dispersions (ASDs) to increase the apparent solubility by dissolving to a concentration higher than the equilibrium solubility of the drug. This may lead to subsequent precipitation and thus the loss of the solubility advantage. Althoug...

journal_title：Molecular pharmaceutics

authors： Han YR,Lee PI

更新日期：2017-01-03 00:00:00

abstract：:meta-Tetra(hydroxyphenyl)chlorin (mTHPC) is one of the most potent second-generation photosensitizers, clinically used for photodynamic therapy (PDT) of head and neck squamous cell carcinomas. However, improvements are still required concerning its present formulation (i.e., Foscan, a solution of mTHPC in ethanol/prop...

journal_title：Molecular pharmaceutics

authors： Liu Y,Scrivano L,Peterson JD,Fens MHAM,Hernández IB,Mesquita B,Toraño JS,Hennink WE,van Nostrum CF,Oliveira S

更新日期：2020-04-06 00:00:00

abstract：:Cytochrome c (Cyt c) is a small mitochondrial heme protein involved in the intrinsic apoptotic pathway. Once Cyt c is released into the cytosol, the caspase mediated apoptosis cascade is activated resulting in programmed cell death. Herein, we explore the covalent immobilization of Cyt c into mesoporous silica nanopar...

journal_title：Molecular pharmaceutics

authors： Méndez J,Morales Cruz M,Delgado Y,Figueroa CM,Orellano EA,Morales M,Monteagudo A,Griebenow K

更新日期：2014-01-06 00:00:00

abstract：:The synthesis and biodistribution of three triazine dendrimers differing in PEGylation are described. Dendrimers 1, 2, and 3 are derived from a common intermediate, dendrimer 4, and vary in molecular mass from 11 to 73 kDa as a result of PEGylation with multiple (theoretically, 16) PEG groups of 0.6, 2, and 5 kDa, res...

journal_title：Molecular pharmaceutics

authors： Lim J,Guo Y,Rostollan CL,Stanfield J,Hsieh JT,Sun X,Simanek EE

更新日期：2008-07-01 00:00:00

abstract：:Aerosol glucocorticoid medications have become more and more important in treating BA (bronchial asthma). Although these agents are dosed to directly target airway inflammation, adrenocortical suppression and other systematic effects are still seen. To tackle this problem in a novel way, two L-carnitine ester derivati...

journal_title：Molecular pharmaceutics

authors： Mo JX,Shi SJ,Zhang Q,Gong T,Sun X,Zhang ZR

更新日期：2011-10-03 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：:The purpose of the present study was to investigate the effect of seed particles on the precipitation behavior of weak base drugs in the small intestine. A simple in vitro infusion method was used to mimic in vivo processes. Dipyridamole, pioglitazone, topiroxostat, chlorpromazine, cinnarizine, and ketoconazole were u...

journal_title：Molecular pharmaceutics

authors： Koyama H,Ito M,Terada K,Sugano K

更新日期：2016-08-01 00:00:00

abstract：:A novel design of anticancer drug delivery system, based on an electrostatic binding of negatively charged liposomes and cationic metalloporphyrins under physiological conditions, is reported. A lack of cytotoxicity of the iron(III) porphyrin-loaded liposomes and an efficient generation of a toxic hydroxyl radical (OH...

journal_title：Molecular pharmaceutics

authors： Yuasa M,Oyaizu K,Horiuchi A,Ogata A,Hatsugai T,Yamaguchi A,Kawakami H

更新日期：2004-09-01 00:00:00

abstract：:Generation 5 poly(amidoamine) (G5 PAMAM) methotrexate (MTX) conjugates employing two small molecular linkers, G5-(COG-MTX)n, G5-(MFCO-MTX)n were prepared along with the conjugates of the G5-G5 (D) dimer, D-(COG-MTX)n, D-(MFCO-MTX)n. The monomer G5-(COG-MTX)n conjugates exhibited only a weak, rapidly reversible binding...

journal_title：Molecular pharmaceutics

authors： van Dongen MA,Rattan R,Silpe J,Dougherty C,Michmerhuizen NL,Van Winkle M,Huang B,Choi SK,Sinniah K,Orr BG,Banaszak Holl MM

更新日期：2014-11-03 00:00:00

abstract：:In women with human epidermal growth factor 2 (HER2)-positive breast cancer, the improved control of systemic disease with new therapies has unmasked brain metastases that historically would have remained clinically silent. The efficacy of therapeutic agents against brain metastases is limited by their inability to pe...

journal_title：Molecular pharmaceutics

authors： Wyatt EA,Davis ME

更新日期：2020-02-03 00:00:00

abstract：:An important aspect to ensure progress in biomedicine is the fundamental understanding of the interaction of cells and tissue with (bio)materials. The consideration of shear stress in drug delivery and/or tissue engineering remains largely unexplored. To illustrate the fundamental relevance, we employ a microfluidic s...

journal_title：Molecular pharmaceutics

authors： Hosta-Rigau L,Städler B

更新日期：2013-07-01 00:00:00

abstract：:Influenza viruses cause seasonal epidemics and represent a pandemic risk. With current vaccine methods struggling to protect populations against emerging strains, there is a demand for a next-generation flu vaccine capable of providing broad protection. Recombinant biotechnology, combined with nanomedicine techniques,...

journal_title：Molecular pharmaceutics

authors： Sia ZR,Miller MS,Lovell JF

更新日期：2021-02-01 00:00:00

abstract：:Resveratrol (RES) is a nutraceutical with promising anti-inflammatory properties for the treatment of inflammatory bowel diseases (IBD). However, the clinical effectiveness of resveratrol as an oral anti-inflammatory agent is hindered by its extremely poor solubility and poor stability. In this study, we encapsulated ...

journal_title：Molecular pharmaceutics

authors： Pujara N,Wong KY,Qu Z,Wang R,Moniruzzaman M,Rewatkar P,Kumeria T,Ross BP,McGuckin M,Popat A

更新日期：2021-02-01 00:00:00

abstract：:The drug-induced accumulation of phospholipids in lysosomes of various tissues is predominantly observed in regular repeat dose studies, often after prolonged exposure, and further investigated in mechanistic studies prior to candidate nomination. The finding can cause delays in the discovery process inflicting high c...

journal_title：Molecular pharmaceutics

authors： Fusani L,Brown M,Chen H,Ahlberg E,Noeske T

更新日期：2017-12-04 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：:Powder adhesion or sticking onto punches is one of the outstanding issues in pharmaceutical tablet manufacturing. We show in this work that, at comparable particle sizes, the acesulfame potassium exhibited pronouncedly reduced propensity to punch sticking than acesulfame. Detailed analyses revealed strong correlation ...

journal_title：Molecular pharmaceutics

authors： Paul S,Wang C,Wang K,Sun CC

更新日期：2019-06-03 00:00:00

abstract：:Nucleic acid biopharmaceuticals are being investigated as potential therapeutics. They need to be incorporated into a biocompatible carrier so as to overcome several biological barriers. Rational development of suitable nanocarriers requires high-quality characterization techniques. While size, concentration, and stab...

journal_title：Molecular pharmaceutics

authors： Zagato E,Vermeulen L,Dewitte H,Van Imschoot G,Vandenbroucke RE,Demeester J,De Smedt SC,Neyts K,Remaut K,Braeckmans K

更新日期：2018-03-05 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：: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：:Amino acids derivative are well established molecular probes for diagnosis of a variety of cancer using positron emission tomography (PET). Recently, boramino acid (BAAs) was found as a prospective molecular platform for developing PET tracer. The objective of this study was to develop a 18F-labeled alanine derivative...

journal_title：Molecular pharmaceutics

authors： Liu H,Han Y,Li J,Qin M,Fu Q,Wang C,Liu Z

更新日期：2018-03-05 00:00:00

abstract：:Dual-targeted imaging agents have shown improved targeting efficiencies in comparison to single-targeted entities. The purpose of this study was to quantitatively assess the tumor accumulation of a dual-labeled heterobifunctional imaging agent, targeting two overexpressed biomarkers in pancreatic cancer, using positro...

journal_title：Molecular pharmaceutics

authors： Luo H,England CG,Goel S,Graves SA,Ai F,Liu B,Theuer CP,Wong HC,Nickles RJ,Cai W

更新日期：2017-05-01 00:00:00

abstract：:Isoniazid (INH) is still one of the two most effective antitubercular drugs and is included in all recommended multitherapeutic regimens. Because of the increasing resistance of Mycobacterium tuberculosis to INH, mainly associated with mutations in the katG gene, new INH-based compounds have been proposed to circumven...

journal_title：Molecular pharmaceutics

authors： Teixeira VH,Ventura C,Leitão R,Ràfols C,Bosch E,Martins F,Machuqueiro M

更新日期：2015-03-02 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：: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：:Most anticancer drugs are poorly soluble and nonspecific, which restricts their clinical application. Drug conjugates, as a prodrug strategy, provide the possibility to overcome these shortcomings, especially combined with nanotechnology. Drug conjugate nanoparticles possess the advantages of high drug loading capacit...

journal_title：Molecular pharmaceutics

authors： Song Q,Wang X,Wang Y,Liang Y,Zhou Y,Song X,He B,Zhang H,Dai W,Wang X,Zhang Q

更新日期：2016-01-04 00:00:00