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“Clicking” Gene Therapeutics: A Successful Union of Chemistry and Biomedicine for New Solutions
10.1021/acs.molpharmaceut.7b00765 2018-02-26 The use of nucleic acid, DNA and RNA, based strategies to disrupt gene expression as a therapeutic is quickly emerging. Indeed, synthetic oligonucleotides represent a major component of modern gene therapeutics. However, the efficiency and specificity of intr... |
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Computational Modeling of Antiviral Drug Diffusion from Poly(lactic-co-glycolic-acid) Fibers and Multicompartment Pharmacokinetics for Application to the Female Reproductive Tract
10.1021/acs.molpharmaceut.7b01089 2018-02-26 The need for more versatile technologies to deliver antiviral agents to the female reproductive tract (FRT) has spurred the development of on-demand and sustained-release platforms. Electrospun fibers (EFs), in particular, have recently been applied to FRT de... |
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Drug Clearance from Cerebrospinal Fluid Mediated by Organic Anion Transporters 1 (Slc22a6) and 3 (Slc22a8) at Arachnoid Membrane of Rats
10.1021/acs.molpharmaceut.7b00852 2018-02-21 Although arachnoid mater epithelial cells form the blood–arachnoid barrier (BAB), acting as a blood–CSF interface, it has been generally considered that the BAB is impermeable to water-soluble substances and plays a largely passive role. Here, we aimed to cla... |
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Polysaccharide Submicrocarrier for Improved Pulmonary Delivery of Poorly Soluble Anti-infective Ciprofloxacin: Preparation, Characterization, and Influence of Size on Cellular Uptake
10.1021/acs.molpharmaceut.7b00967 2018-02-21 The majority of the currently used and developed anti-infectives are poorly water-soluble molecules. The poor solubility might lead to limited bioavailability and pharmacological action of the drug. Novel pharmaceutical materials have thus been designed to so... |
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Importance of Net Hydrophobicity in the Cellular Uptake of All-Hydrocarbon Stapled Peptides
10.1021/acs.molpharmaceut.7b01130 2018-02-21 All-hydrocarbon stapled peptides make up a promising class of protein–protein interaction regulators; their potential therapeutic benefit arises because they have a high binding affinity and specificity for intracellular molecules. The cell permeation efficac... |
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Near Infrared Photoimmunotherapy with Combined Exposure of External and Interstitial Light Sources
10.1021/acs.molpharmaceut.8b00002 2018-02-21 Near infrared photoimmunotherapy (NIR-PIT) is a new target-cell-specific cancer treatment that induces highly selective necrotic/immunogenic cell death after systemic administration of a photoabsorber antibody conjugate and subsequent NIR light exposure. Howe... |
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Antioxidative Nanoparticles Significantly Enhance Therapeutic Efficacy of an Antibacterial Therapy against Listeria monocytogenes Infection
10.1021/acs.molpharmaceut.7b00995 2018-02-20 Acute inflammatory conditions such as sepsis lead to fatal conditions, including multiple organ failure. Several treatments such as steroidal anti-inflammatory drugs are currently being investigated in order to decrease the blood cytokine level, which increas... |
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Isosteric Substitution of 4H-1,2,4-Triazole by 1H-1,2,3-Triazole in Isophthalic Derivative Enabled Hydrogel Formation for Controlled Drug Delivery
10.1021/acs.molpharmaceut.7b01049 2018-02-20 In this work, we demonstrated that the simple substitution of the 1,2,4-triazole moiety in 5-(4H-1,2,4-triazol-4-yl)isophthalic acid (5-TIA) by the 1H-1,2,3-triazol-5-yl unit enables the preparation of a hydrogelator (click-TIA). In sharp contrast to 5-TIA, i... |
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Role of Hepatic Organic Anion Transporter 2 in the Pharmacokinetics of R- and S-Warfarin: In Vitro Studies and Mechanistic Evaluation
10.1021/acs.molpharmaceut.7b01108 2018-02-20 Interindividual variability in warfarin dose requirement demands personalized medicine approaches to balance its therapeutic benefits (anticoagulation) and bleeding risk. Cytochrome P450 2C9 (CYP2C9) genotype-guided warfarin dosing is recommended in the clini... |
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Enhancing the Spreading Behavior on Pulmonary Mucus Mimicking Subphase via Catanionic Surfactant Solutions: Toward Effective Drug Delivery through the Lungs
10.1021/acs.molpharmaceut.8b00086 2018-02-20 Effective and efficient spreading of drug formulations on the pulmonary mucosal layer is key to successful delivery of therapeutics through the lungs. The pulmonary mucus layer, which covers the airway surface, acts as a barrier against therapeutic agents, es... |