Application of Nitroimidazole-Carbobane-Modified Phenylalanine Derivatives as Dual-Target Boron Carriers in Boron Neutron Capture Therapy.

abstract：:A wide variety of chemotherapy and radiotherapy agents are available for treating cancer, but a critical challenge is to deliver these agents locally to cancer cells and tumors while minimizing side effects from systemic delivery. Nanomedicine uses nanoparticles with diameters in the range of ∼1-100 nm to encapsulate ...

journal_title：Molecular pharmaceutics

authors： Moore T,Chen H,Morrison R,Wang F,Anker JN,Alexis F

更新日期：2014-01-06 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：:Nerve damage during surgery is a common morbidity experienced by patients that leaves them with chronic pain and/or loss of function. Currently, no clinically approved imaging technique exists to enhance nerve visualization in the operating room. Fluorescence image-guided surgery has gained in popularity and clinical ...

journal_title：Molecular pharmaceutics

authors： Hackman KM,Doddapaneni BS,Barth CW,Wierzbicki IH,Alani AW,Gibbs SL

更新日期：2015-12-07 00:00:00

abstract：:The caveolin scaffolding domain peptide (CSP) is being developed for the therapeutic intervention of a lethal lung disease, idiopathic pulmonary fibrosis. While direct respiratory delivery of CSP7 (a 7-mer fragment of CSP) is considered an effective route, proper formulation and processing of the peptide are required....

journal_title：Molecular pharmaceutics

authors： Zhang Y,MacKenzie B,Koleng JJ,Maier E,Warnken ZN,Williams RO 3rd

更新日期：2020-02-03 00:00:00

abstract：:Approximately, 40-70% of active pharmaceutical ingredients (API) are severely limited by their extremely poor aqueous solubility, and consequently, there is a high demand for excipients that can be used to formulate clinically relevant doses of these drug candidates. Here, proof-of-concept studies demonstrate the pote...

journal_title：Molecular pharmaceutics

authors： Hettiarachchi G,Samanta SK,Falcinelli S,Zhang B,Moncelet D,Isaacs L,Briken V

更新日期：2016-03-07 00:00:00

abstract：:Rodent models are less suitable for predicting drug-drug interactions at the level of the human intestinal mucosa, especially when nuclear receptors such as pregnane X receptor (PXR) are involved. Recently, a transgenic mouse model, expressing both human PXR and CYP3A4, was developed and shown to be a better predictor...

journal_title：Molecular pharmaceutics

authors： Holmstock N,Gonzalez FJ,Baes M,Annaert P,Augustijns P

更新日期：2013-03-04 00:00:00

abstract：:Dual variable domain immunoglobulin proteins (DVD-Ig proteins) are large molecules (MW ∼ 200 kDa) with increased asymmetry because of their extended Y-like shape, which results in increased formulation challenges. Liquid-liquid phase separation (LLPS) of protein solutions into protein-rich and protein-poor phases redu...

journal_title：Molecular pharmaceutics

authors： Raut AS,Kalonia DS

更新日期：2015-09-08 00:00:00

abstract：:The objective was to determine the disposition of polymer nanoparticles and an associated, lipophilic, model "active" component on and within the skin following topical application. Polystyrene and poly(methyl methacrylate) nanoparticles containing covalently bound fluorescein methacrylate and dispersed Nile Red were ...

journal_title：Molecular pharmaceutics

authors： Wu X,Price GJ,Guy RH

更新日期：2009-09-01 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：:The biodistribution of dendronized iron oxides, NPs10@D1_DOTAGA and melanin-targeting NPs10@D1_ICF_DOTAGA, was studied in vivo using magnetic resonance imaging (MRI) and planar scintigraphy through [177Lu]Lu-radiolabeling. MRI experiments showed high contrast power of both dendronized nanoparticles (DPs) and hepatobil...

journal_title：Molecular pharmaceutics

authors： Bordeianu C,Parat A,Piant S,Walter A,Zbaraszczuk-Affolter C,Meyer F,Begin-Colin S,Boutry S,Muller RN,Jouberton E,Chezal JM,Labeille B,Cinotti E,Perrot JL,Miot-Noirault E,Laurent S,Felder-Flesch D

更新日期：2018-02-05 00:00:00

abstract：:Although nitric oxide (NO) is a bactericidal component of the macrophage's innate response to intracellular infections such as tuberculosis (TB), prolonged inhalation of NO gas has little benefit in chemotherapy of TB. The impact of controlled release of NO through intracellular delivery of NO donors to macrophages in...

journal_title：Molecular pharmaceutics

authors： Verma RK,Singh AK,Mohan M,Agrawal AK,Verma PR,Gupta A,Misra A

更新日期：2012-11-05 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：:It is well-known that renal cell carcinomas (RCCs) are resistant to classical cytotoxic anticancer drugs. Therefore, facilitating the impact of anticancer drugs by altering the cell phenotype should be a useful strategy for circumventing this. We developed a multifunctional envelope-type nanodevice (MEND) as an in viv...

journal_title：Molecular pharmaceutics

authors： Sakurai Y,Hatakeyama H,Akita H,Harashima H

更新日期：2014-08-04 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：:It is difficult to predict the first-pass effect in the human intestine due to a lack of scaling factors for correlating in vitro and in vivo data. We have quantified cytochrome P450/3A4 (CYP3A4) and two ABC transporters, P-glycoprotein (P-gp, ABCB1) and the breast cancer resistant protein BCRP (ABCG2), throughout the...

journal_title：Molecular pharmaceutics

authors： Bruyère A,Declèves X,Bouzom F,Ball K,Marques C,Treton X,Pocard M,Valleur P,Bouhnik Y,Panis Y,Scherrmann JM,Mouly S

更新日期：2010-10-04 00:00:00

abstract：: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 1 H-1,2,3-triazol-5-yl unit enables the preparation of a hydrogelator (click-TIA). In sharp contrast to 5-TIA, its isostere click-TIA undergoes self-assembly in water upo...

journal_title：Molecular pharmaceutics

authors： Häring M,Rodríguez-López J,Grijalvo S,Tautz M,Eritja R,Martín VS,Díaz Díaz D

更新日期：2018-08-06 00:00:00

abstract：:Hydrophilic peptides constitute most of the active peptides. They mostly permeate via tight junctions (paracellular pathway) in the intestine. This permeability mechanism restricts the magnitude of their oral absorption and bioavailability. We hypothesized that concealing the hydrophilic residues of the peptide using ...

journal_title：Molecular pharmaceutics

authors： Schumacher-Klinger A,Fanous J,Merzbach S,Weinmüller M,Reichart F,Räder AFB,Gitlin-Domagalska A,Gilon C,Kessler H,Hoffman A

更新日期：2018-08-06 00:00:00

abstract：:Antiviral drugs often suffer from poor intestinal permeability, preventing their delivery via the oral route. The goal of this work was to enhance the intestinal absorption of the low-permeability antiviral agents zanamivir heptyl ester (ZHE) and guanidino oseltamivir (GO) utilizing an ion-pairing approach, as a criti...

journal_title：Molecular pharmaceutics

authors： Miller JM,Dahan A,Gupta D,Varghese S,Amidon GL

更新日期：2010-08-02 00:00:00

abstract：:Recent developments in pharmaceutical technology have facilitated the design and production of modified release formulas for drugs whose physical, chemical or biological properties impede release and thus might compromise their efficacy or safety. One such drug is morphine, whose short half-life requires repeated dose...

journal_title：Molecular pharmaceutics

authors： Morales ME,López G,Gallardo V,Ruiz MA

更新日期：2011-04-04 00:00:00

abstract：:Effective penetration of drug-carrying nanoparticles into solid tumors is a major challenge in cancer therapy. Exploration of the physicochemical properties of nanoparticles that affect penetration efficiency is required to achieve maximum therapeutic effects. Here, we used confocal laser scanning microscopy to evalua...

journal_title：Molecular pharmaceutics

authors： Takechi-Haraya Y,Goda Y,Sakai-Kato K

更新日期：2017-06-05 00:00:00

abstract：:Recently, increased interest in drug transporters and research in this area has revealed that drug transporters play an important role in modulating drug absorption, distribution, and elimination. Acting alone or in concert with drug metabolizing enzymes they can affect the pharmacokinetics and pharmacodynamics of a d...

journal_title：Molecular pharmaceutics

authors： Zhang L,Strong JM,Qiu W,Lesko LJ,Huang SM

更新日期：2006-01-01 00:00:00

abstract：:The encapsulation of glucocorticoids, such as dexamethasone, in nanoparticles (NPs) faces two main issues: a low drug loading and the destabilization of the nanoparticle suspension due to drug crystallization. Here, we successfully formulated a prodrug of dexamethasone, dexamethasone palmitate (DXP), into nanoparticle...

journal_title：Molecular pharmaceutics

authors： Lorscheider M,Tsapis N,Simón-Vázquez R,Guiblin N,Ghermani N,Reynaud F,Canioni R,Abreu S,Chaminade P,Fattal E

更新日期：2019-07-01 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：:The toxicity of Amphotericin B (AmB) is contributed by the small, water-soluble aggregates of the drug. Hence, AmB lipid polymer hybrid nanoparticles (LIPOMER), comprising stearate lipids with a hydrophilic polymer Gantrez (GZ), and solid lipid nanoparticles (SLN), comprising only stearates, were prepared with the obj...

journal_title：Molecular pharmaceutics

authors： Das S,Devarajan PV

更新日期：2020-06-01 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：: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：:As the hearts of tumor cells, the nucleus is the ultimate target of many chemotherapeutic agents and genes. However, nuclear drug delivery is always hampered by multiple intracellular obstacles, such as low efficiency of lysosome escape and insufficient nuclear trafficking. Herein, an N-(2-hydroxypropyl) methacrylamid...

journal_title：Molecular pharmaceutics

authors： Zhong J,Zhu X,Luo K,Li L,Tang M,Liu Y,Zhou Z,Huang Y

更新日期：2016-09-06 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：:Superoxide dismutase 1 (SOD1) efficiently catalyzes dismutation of superoxide, but its poor delivery to the target sites in the body, such as brain, hinders its use as a therapeutic agent for superoxide-associated disorders. Here to enhance the delivery of SOD1 across the blood-brain barrier (BBB) and in neurons the e...

journal_title：Molecular pharmaceutics

authors： Tong J,Yi X,Luxenhofer R,Banks WA,Jordan R,Zimmerman MC,Kabanov AV

更新日期：2013-01-07 00:00:00

abstract：:Conjugation with a cell penetrating peptide such as Tat presents an effective approach to improve the intracellular accumulation of molecules with low membrane permeability. This strategy, however, leads to a reduced cellular entry of molecules that can cross cell membrane effectively. We report here that covalent lin...

journal_title：Molecular pharmaceutics

authors： Zhang P,Lock LL,Cheetham AG,Cui H

更新日期：2014-03-03 00:00:00