abstract：:Metastatic breast cancer is incurable. The goal of this study was to develop a positron emission tomography (PET)/near-infrared fluorescent (NIRF) probe for imaging CD105 expression in breast cancer experimental lung metastasis. TRC105, a chimeric anti-CD105 antibody, was dual-labeled with a NIRF dye (IRDye 800CW) and...

journal_title：Molecular pharmaceutics

authors： Hong H,Zhang Y,Severin GW,Yang Y,Engle JW,Niu G,Nickles RJ,Chen X,Leigh BR,Barnhart TE,Cai W

更新日期：2012-08-06 00:00:00

abstract：:Though metastasis is considered an inefficient process, over 90% of cancer related deaths are attributed to the formation of secondary tumors. Thus, eliminating circulating cancer cells could lead to improved patient survival. This study was aimed at exploiting the interactions of cancer cells with selectins under flo...

journal_title：Molecular pharmaceutics

authors： Rana K,Reinhart-King CA,King MR

更新日期：2012-08-06 00:00:00

abstract：:Porous silicon microparticles presenting pathogen-associated molecular patterns mimic pathogens, enhancing internalization of the microparticles and activation of antigen presenting dendritic cells. We demonstrate abundant uptake of microparticles bound by the TLR-4 ligands LPS and MPL by murine bone marrow-derived de...

journal_title：Molecular pharmaceutics

authors： Meraz IM,Melendez B,Gu J,Wong ST,Liu X,Andersson HA,Serda RE

更新日期：2012-07-02 00:00:00

abstract：:An ability to estimate the maximum flux of a xenobiotic across skin is desirable from the perspective of both drug delivery and toxicology. While there is an abundance of mathematical models describing the estimation of drug permeability coefficients, there are relatively few that focus on the maximum flux. This artic...

journal_title：Molecular pharmaceutics

authors： Milewski M,Stinchcomb AL

更新日期：2012-07-02 00:00:00

abstract：:Near-infrared (NIR)-to-visible upconversion nanoparticle (UCNP) has shown promising prospects in photodynamic therapy (PDT) as a drug carrier or energy donor. In this work, a photosensitizer pyropheophorbide a (Ppa) and RGD peptide c(RGDyK) comodified chitosan-wrapped NaYF(4):Yb/Er upconversion nanoparticle UCNP-Ppa-R...

journal_title：Molecular pharmaceutics

authors： Zhou A,Wei Y,Wu B,Chen Q,Xing D

更新日期：2012-06-04 00:00:00

abstract：:Due to the aging of the population, the incidence of neurodegenerative diseases, such as Parkinson's and Alzheimer's, is expected to grow and, hence, the demand for adequate treatment modalities. However, the delivery of medicines into the brain for the treatment of brain-related diseases is hampered by the presence o...

journal_title：Molecular pharmaceutics

authors： Stojanov K,Georgieva JV,Brinkhuis RP,van Hest JC,Rutjes FP,Dierckx RA,de Vries EF,Zuhorn IS

更新日期：2012-06-04 00:00:00

abstract：:Safe and effective gene delivery is essential to the success of gene therapy. We synthesized and characterized a novel nonviral gene delivery system in which folate (FA) molecules were functioned as blockers on cationic polyrotaxanes (PR) composed of poly(ethylenimine) (PEI)(600)-grafted α-cyclodextrin rings linearize...

journal_title：Molecular pharmaceutics

authors： Zhou Y,Wang H,Wang C,Li Y,Lu W,Chen S,Luo J,Jiang Y,Chen J

更新日期：2012-05-07 00:00:00

abstract：:The goal of this study was to develop a (66)Ga-based positron emission tomography (PET) tracer for noninvasive imaging of CD105 expression during tumor angiogenesis, a hallmark of cancer. (66)Ga was produced using a cyclotron with (nat)Zn or isotopically enriched (66)Zn targets. TRC105, a chimeric anti-CD105 monoclona...

journal_title：Molecular pharmaceutics

authors： Engle JW,Hong H,Zhang Y,Valdovinos HF,Myklejord DV,Barnhart TE,Theuer CP,Nickles RJ,Cai W

更新日期：2012-05-07 00:00:00

abstract：:Nonviral gene delivery has seen limited clinical application due in part to the inefficiency with which most nonviral vehicles navigate the intracellular gene delivery pathway. One key problem is the inability of most DNA-packaging materials to release DNA and enable its efficient transcription. Thus, our aim was to d...

journal_title：Molecular pharmaceutics

authors： Larsen JD,Reilly MJ,Sullivan MO

更新日期：2012-05-07 00:00:00

abstract：:Amphotericin B (AmB) is a lifesaving polyene antibiotic used widely to treat deep-seated mycoses. Both the pharmaceutical effectiveness as well as toxic side effects depend on molecular organization of the drug. In the present study, we analyzed steady-state fluorescence, fluorescence anisotropy spectra, fluorescence ...

journal_title：Molecular pharmaceutics

authors： Wasko P,Luchowski R,Tutaj K,Grudzinski W,Adamkiewicz P,Gruszecki WI

更新日期：2012-05-07 00:00:00

abstract：:The objective of this study was to enhance oral mucosal permeation of fenretinide by coincorporation of propylene glycol (PG) and menthol in fenretinide/Eudragit RL PO mucoadhesive patches. Fenretinide is an extremely hydrophobic chemopreventive compound with poor tissue permeability. Coincorporation of 5-10 wt % PG (...

journal_title：Molecular pharmaceutics

authors： Wu X,Desai KG,Mallery SR,Holpuch AS,Phelps MP,Schwendeman SP

更新日期：2012-04-02 00:00:00

abstract：:The present work investigates the influence of electrostatic surface potential distribution of monoclonal antibodies (MAbs) on intermolecular interactions and viscosity. Electrostatic models suggest MAb-1 has a less uniform surface charge distribution than MAb-2. The patches of positive and negative potential on MAb-1...

journal_title：Molecular pharmaceutics

authors： Yadav S,Laue TM,Kalonia DS,Singh SN,Shire SJ

更新日期：2012-04-02 00:00:00

abstract：:The human organic anion-transporting polypeptides OATP1B1 (SLCO1B1) and OATP1B3 (SLCO1B3) are liver-enriched membrane transporters of major importance to hepatic uptake of numerous endogenous compounds, including bile acids, steroid conjugates, hormones, and drugs, including the 3-hydroxy-3-methylglutaryl Co-A reducta...

journal_title：Molecular pharmaceutics

authors： DeGorter MK,Ho RH,Leake BF,Tirona RG,Kim RB

更新日期：2012-04-02 00:00:00

abstract：:Solid-state hydrogen-deuterium exchange with mass spectrometric analysis (ssHDX) is a promising method for characterizing proteins in amorphous solids. Though analysis of HDX kinetics is informative and well-established in solution, application of these methods to solid samples is complicated by possible heterogeneiti...

journal_title：Molecular pharmaceutics

authors： Sophocleous AM,Topp EM

更新日期：2012-04-02 00:00:00

abstract：:Dry powder inhalations (DPI) of microparticles containing isoniazid (INH) and rifabutin (RFB) are under preclinical development for use in pulmonary tuberculosis. Microparticles containing 0.25, 2.5, or 25 mg of each drug were administered daily for 90 days to rhesus macaques (n = 4/group). Single inhalations or intra...

journal_title：Molecular pharmaceutics

authors： Kumar Verma R,Mukker JK,Singh RS,Kumar K,Verma PR,Misra A

更新日期：2012-04-02 00:00:00

abstract：:Biophysical tools have been invaluable in formulating therapeutic proteins. These tools characterize protein stability rapidly in a variety of solution conditions, but in general, the techniques lack the ability to discern site-specific information to probe how solution environment acts to stabilize or destabilize the...

journal_title：Molecular pharmaceutics

authors： Krause ME,Martin TT,Laurence JS

更新日期：2012-04-02 00:00:00

abstract：:Indocyanine green (ICG) is a conventional dye that can be used in clinical near-infrared (NIR) imaging, and it is also an effective light absorber for laser-mediated photothermal therapy. However, applications of ICG were limited due to its fast degradation in aqueous media and quick clearance from the body. Herein, a...

journal_title：Molecular pharmaceutics

authors： Zheng X,Zhou F,Wu B,Chen WR,Xing D

更新日期：2012-03-05 00:00:00

abstract：:Cancer is a leading cause of death within developed nations, and part of this morbidity is due to difficulties associated with its treatment. Currently, anticancer therapy relies heavily upon the administration of small molecule cytotoxic drugs that attack both cancerous and noncancerous cells due to limited selectivi...

journal_title：Molecular pharmaceutics

authors： Kaminskas LM,McLeod VM,Porter CJ,Boyd BJ

更新日期：2012-03-05 00:00:00

abstract：:The killing efficacy of doxorubicin from liposome-based delivery carriers has been shown to correlate strongly with its intracellular trafficking and, in particular, its fast and extensive release from the delivery carrier. However, previously explored pH-triggered mechanisms that were designed to become activated dur...

journal_title：Molecular pharmaceutics

authors： Mamasheva E,O'Donnell C,Bandekar A,Sofou S

更新日期：2011-12-05 00:00:00

abstract：:It is likely that drug resistance evolves after transformation. Exactly how these resistant cells arise is uncertain. This review outlines how the evolution of individual human cancers may be inferred by comparing genomic variation from different parts of the same tumor. The past of a tumor may help predict its respon...

journal_title：Molecular pharmaceutics

authors： Shibata D

更新日期：2011-12-05 00:00:00

abstract：:Encapsulation and release behavior of a water-insoluble drug, magnolol, using a core-shell polysaccharide-based nanoparticle, manipulating the cellular internalization and controlled cytotoxic effect of magnolol-loaded nanoparticles over the A10 vascular smooth muscle cells (VSMCs) was reported. A magnolol-polyvinylpy...

journal_title：Molecular pharmaceutics

authors： Wang YJ,Chien YC,Wu CH,Liu DM

更新日期：2011-12-05 00:00:00

abstract：:The current regimen of factor IX (FIX) injection is of an episodic format, which leads to limited efficacy. A sustained release dosage form is beneficial in terms of reducing the injection frequency and improving the therapeutic effectiveness. The aim of this study was to formulate a new microsphere form of a FIX-cont...

journal_title：Molecular pharmaceutics

authors： Chang LC,Yang CY,Chua AC,Lin YJ,Lai SM

更新日期：2011-10-03 00:00:00

abstract：:The systemic pharmacokinetics and pharmacodynamics of small molecules are determined by subcellular transport phenomena. Although approaches used to study the subcellular distribution of small molecules have gradually evolved over the past several decades, experimental analysis and prediction of cellular pharmacokinet...

journal_title：Molecular pharmaceutics

authors： Zheng N,Tsai HN,Zhang X,Rosania GR

更新日期：2011-10-03 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：:Fexofenadine is a nonsedative antihistamine that exhibits good oral bioavailability despite its zwitterionic chemical structure and efflux by P-gp. Evidence exists that multiple uptake and efflux transporters play a role in hepatic disposition of fexofenadine. However, the roles of specific transporters and their inte...

journal_title：Molecular pharmaceutics

authors： Ming X,Knight BM,Thakker DR

更新日期：2011-10-03 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：:Because of its biocompatibility and ability to accommodate a variety of payloads from poorly soluble drugs to biomolecules, porous silicon (PSi) is a lucrative material for the development of carriers for particle-mediated drug delivery. We report a successful direct one-step (18)F-radiolabeling of three types of PSi ...

journal_title：Molecular pharmaceutics

authors： Sarparanta M,Mäkilä E,Heikkilä T,Salonen J,Kukk E,Lehto VP,Santos HA,Hirvonen J,Airaksinen AJ

更新日期：2011-10-03 00:00:00

abstract：:Poly(ethylene glycol)-block-poly(D,L-lactic acid) (PEG-b-PLA) micelles have a proven capacity for drug solubilization and have entered phase III clinical trials as a substitute for Cremophor EL in the delivery of paclitaxel in cancer therapy. PEG-b-PLA is less toxic than Cremophor EL, enabling a doubling of paclitaxel...

journal_title：Molecular pharmaceutics

authors： Shin HC,Alani AW,Cho H,Bae Y,Kolesar JM,Kwon GS

更新日期：2011-08-01 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：:In this study, the dissolution properties of celecoxib (CX) solid dispersions manufactured from Eudragit 4155F and polyvinylpyrrolidone (PVP) were evaluated. Hot-melt extrusion (HME) technology was used to prepare amorphous solid dispersions of drug/polymer binary systems at different mass ratios. The drug concentrati...

journal_title：Molecular pharmaceutics

authors： Abu-Diak OA,Jones DS,Andrews GP

更新日期：2011-08-01 00:00:00

abstract：:Hyaluronan (HA) is a biocompatible and biodegradable linear polysaccharide which is of interest for tumor targeting through cell surface CD44 receptors. HA binds with high affinity to CD44 receptors, which are overexpressed in many tumors and involved in cancer metastasis. In the present study, we investigated the imp...

journal_title：Molecular pharmaceutics

authors： Qhattal HS,Liu X

更新日期：2011-08-01 00:00:00

abstract：:Polymer therapeutics have shown promise as tumor-targeted drug delivery systems in mice. The multivalency of polymers allows the attachment of different functional agents to a polymeric backbone, including chemotherapeutic and antiangiogenic drugs, as well as targeting moieties, such as the bone-targeting agent alendr...

journal_title：Molecular pharmaceutics

authors： Miller K,Eldar-Boock A,Polyak D,Segal E,Benayoun L,Shaked Y,Satchi-Fainaro R

更新日期：2011-08-01 00:00:00

abstract：:This study investigated the role of the prostaglandin (PG) pathway in locally applied, simvastatin-induced oral bone growth. The possibility of enhancing long-term bone augmentation with an alendronate-based carrier was initiated. Mandibles of 44 mature female rats were treated bilaterally with the following combinati...

journal_title：Molecular pharmaceutics

authors： Lee Y,Liu X,Nawshad A,Marx DB,Wang D,Reinhardt RA

更新日期：2011-08-01 00:00:00

abstract：:Targeted gene delivery using nonviral vectors is a highly touted scheme to reduce the potential for toxic or immunological side effects by reducing dose. In previous reports, TAT polyplexes with DNA have shown relatively poor gene delivery. The transfection efficiency has been enhanced by condensing TAT/DNA complexes ...

journal_title：Molecular pharmaceutics

authors： Khondee S,Baoum A,Siahaan TJ,Berkland C

更新日期：2011-06-06 00:00:00

abstract：:Cholestasis is a significant risk factor for immediate hepatic failure due to ischemia reperfusion (I/R) injury in patients undergoing liver surgery or transplantation. We recently demonstrated that inhibition of Hedgehog (Hh) signaling with cyclopamine (CYA) before I/R prevents liver injury. In this study we hypothes...

journal_title：Molecular pharmaceutics

authors： Pratap A,Panakanti R,Yang N,Lakshmi R,Modanlou KA,Eason JD,Mahato RI

更新日期：2011-06-06 00:00:00

abstract：:TGX-221 is a highly potent phosphoinositide 3-kinase β (PI3Kβ) inhibitor that holds great promise as a novel chemotherapeutic agent to treat prostate cancer. However, poor solubility and lack of targetability limit its therapeutic applications. The objective of this present study is to develop a peptide-drug conjugate...

journal_title：Molecular pharmaceutics

authors： Tai W,Shukla RS,Qin B,Li B,Cheng K

更新日期：2011-06-06 00:00:00

abstract：:Tumor-associated inflammation has been linked to angiogenesis, metastasis and poor prognosis. The 18 kDa translocator protein (TSPO), also known as the peripheral benzodiazepine receptor (PBR), is expressed in activated immune cells such as macrophages, but also in a number of cancer cell lines such as those of breast...

journal_title：Molecular pharmaceutics

authors： Zheng J,Boisgard R,Siquier-Pernet K,Decaudin D,Dollé F,Tavitian B

更新日期：2011-06-06 00:00:00

abstract：:Noninvasive measurement of human islet cell mass in pancreas or following islet transplantation by nuclear imaging has yet to be achieved. It has been shown using mouse tumor models that pretargeting imaging strategies are sensitive and can greatly increase target to nontarget signal ratios. The objective now is to de...

journal_title：Molecular pharmaceutics

authors： Liu G,Dou S,Cheng D,Leif J,Rusckowski M,Streeter PR,Shultz LD,Hnatowich DJ,Greiner DL

更新日期：2011-06-06 00:00:00

abstract：:Efficient drug delivery to the skin is essential for the treatment of major dermatologic diseases, such as eczema, psoriasis and acne. However, many compounds penetrate the skin barrier poorly and require optimized formulations to ensure their bioavailability. Here, stimulated Raman scattering (SRS) microscopy, a rece...

journal_title：Molecular pharmaceutics

authors： Saar BG,Contreras-Rojas LR,Xie XS,Guy RH

更新日期：2011-06-06 00:00:00

abstract：:Despite being widely used in the clinical setting for sentinel lymph node detection (SLND), (99m)Tc-based colloids (e.g., (99m)Tc-human serum albumin colloids) present a set of properties that are far from ideal. Aiming to design novel compounds with improved biological properties, we describe herein the first class o...

journal_title：Molecular pharmaceutics

authors： Morais M,Subramanian S,Pandey U,Samuel G,Venkatesh M,Martins M,Pereira S,Correia JD,Santos I

更新日期：2011-04-04 00:00:00