Sulfation patterns determine cellular internalization of heparin-like polysaccharides.

abstract：:The purpose of this study was to examine and compare the melanoma targeting and imaging properties of (64)Cu-NOTA-GGNle-CycMSH(hex) {(64)Cu-1,4,7-triazacyclononane-1,4,7-triacetic acid-Gly-Gly-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-CONH2} and (64)Cu-DOTA-GGNle-CycMSH(hex) {(64)Cu-1,4,7,10-tetraazacyclononane-1,4,7,10-tetraac...

journal_title：Molecular pharmaceutics

authors： Guo H,Miao Y

更新日期：2012-08-06 00:00:00

abstract：:Although tumor-targeting nanovehicles for hepatocellular carcinoma (HCC) chemotherapy have attracted great research and clinic interest, the poor cancer penetration, inefficient cellular uptake, and slow intracellular drug release greatly compromise their therapeutic outcomes. In this work, a multifunctional mixed mic...

journal_title：Molecular pharmaceutics

authors： Zhang J,Zheng Y,Xie X,Wang L,Su Z,Wang Y,Leong KW,Chen M

更新日期：2017-11-06 00:00:00

abstract：:This paper develops a structure-activity relationship understanding of the way in which surfactant-like dendrons with hydrophilic spermine surface groups and a variety of lipophilic units at their focal points can self-assemble and subsequently bind to DNA with high affinity. The choice of functional group at the foca...

journal_title：Molecular pharmaceutics

authors： Jones SP,Gabrielson NP,Wong CH,Chow HF,Pack DW,Posocco P,Fermeglia M,Pricl S,Smith DK

更新日期：2011-04-04 00:00:00

abstract：:Simvastatin is one of the most widely used active pharmaceutical ingredients for the treatment of hyperlipidemias. Because the compound is employed as a solid in drug formulations, particular attention should be given to the characterization of different polymorphs, their stability domains, and the nature of the phase...

journal_title：Molecular pharmaceutics

authors： Simões RG,Bernardes CES,Joseph A,M Piedade MF,Kraus W,Emmerling F,Diogo HP,Minas da Piedade ME

更新日期：2018-11-05 00:00:00

abstract：BACKGROUND:For the development of novel buccoadhesive formulations, their physicochemical properties, strength of the interfacial joint, and residence time on the buccal mucosa are considered as a measure for their in vivo mucoadhesive properties. Focusing on these parameters, the predictive power of established in vit...

journal_title：Molecular pharmaceutics

authors： Baus RA,Haug MF,Leichner C,Jelkmann M,Bernkop-Schnürch A

更新日期：2019-06-03 00:00:00

abstract：:Recently we characterized an unusual switch in the internalization mechanism of the monomeric and dimeric forms of the cell-penetrating peptide RDLWEMMMVSLACQY. Here, we observed both energy-dependent and energy-independent modes of peptide uptake by the target B-lymphocytes WI-L2-729HF2, suggesting that higher-order ...

journal_title：Molecular pharmaceutics

authors： Kim Y,Lillo A,Moss JA,Janda KD

更新日期：2005-11-01 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：:We investigated the effect of polymer composition on nifedipine (NIF) dissolution through molecular-level characterization of NIF/hypromellose (HPMC)/Eudragit S (EUD-S) ternary solid dispersions. The dissolution rates and molecular states of NIF and polymers were evaluated in NIF/HPMC/EUD-S spray-dried samples (SPDs) ...

journal_title：Molecular pharmaceutics

authors： Ueda K,Yamazoe C,Yasuda Y,Higashi K,Kawakami K,Moribe K

更新日期：2018-09-04 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：:We developed a modular multifunctional nonviral gene delivery system by targeting the overexpressed cancer surface receptor α5β1 integrin and the upregulated transcriptional activity of the cancer resistance mediating transcription factor NF-κB, thereby introducing a new form of transcriptional targeting. NF-κB regula...

journal_title：Molecular pharmaceutics

authors： Adil MM,Levine RM,Kokkoli E

更新日期：2014-03-03 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：:Organic anion transporting polypeptide (OATP) 1B1 plays an important role in the hepatic uptake of various drugs. Because OATP1B1 is a site of drug-drug interactions (DDIs), evaluating the inhibitory potential of drug candidates on OATP1B1 is required during drug development. For establishing a highly sensitive, high-...

journal_title：Molecular pharmaceutics

authors： Izumi S,Nozaki Y,Komori T,Takenaka O,Maeda K,Kusuhara H,Sugiyama Y

更新日期：2016-02-01 00:00:00

abstract：:To synergistically enhance the selectivity and efficiency of anticancer copper drugs, we proposed and built a model to develop anticancer copper pro-drugs based on the nature of human serum albumin (HSA) IIA subdomain and cancer cells. Three copper(II) compounds of a 2-hydroxy-1-naphthaldehyde benzoyl hydrazone Schiff...

journal_title：Molecular pharmaceutics

authors： Gou Y,Qi J,Ajayi JP,Zhang Y,Zhou Z,Wu X,Yang F,Liang H

更新日期：2015-10-05 00:00:00

abstract：:Folate receptor (FR) targeting is an attractive strategy for nuclear imaging of cancer and activated macrophages through application of folic acid radioconjugates. However, significant renal accumulation of folate radioconjugates and hence exceedingly high emission of radiation from the kidneys may mask uptake of radi...

journal_title：Molecular pharmaceutics

authors： Müller C,Reber J,Schlup C,Leamon CP,Schibli R

更新日期：2013-03-04 00:00:00

abstract：:The formulation of drug/polymer amorphous solid dispersions (ASDs) is one of the most successful strategies for improving the oral bioavailability of poorly soluble active pharmaceutical ingredients (APIs). Hot-melt extrusion (HME) is one method for preparing ASDs that is growing in importance in the pharmaceutical in...

journal_title：Molecular pharmaceutics

authors： Pisa E,Hughes LP,Wren SAC,Booth J,McCabe JF,Whittaker DTE,Mantle MD

更新日期：2020-06-01 00:00:00

abstract：:In this paper the preparation of magnetic nanocarriers (MNCs), containing superparamagnetic domains, is reported, useful as potential magnetically targeted drug delivery systems. The preparation of MNCs was performed by using the PHEA-IB-p(BMA) graft copolymer as coating material through the homogenization-solvent eva...

journal_title：Molecular pharmaceutics

authors： Licciardi M,Scialabba C,Fiorica C,Cavallaro G,Cassata G,Giammona G

更新日期：2013-12-02 00:00:00

abstract：:In this study, the polymer-free electrospinning was performed in order to produce cyclodextrin/ibuprofen inclusion complex nanofibers, which could have potential as the fast dissolving oral drug delivery system. Ibuprofen is a poorly water-soluble nonsteroidal anti-inflammatory drug; however, the water solubility of i...

journal_title：Molecular pharmaceutics

authors： Celebioglu A,Uyar T

更新日期：2019-10-07 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：:Gemcitabine, a clinically effective nucleoside anticancer agent, is a polar drug with low membrane permeability and is administered intravenously. Further, extensive degradation of gemcitabine by cytidine deaminase to an inactive metabolite in the liver affects its activity adversely. Thus, strategies that provide bot...

journal_title：Molecular pharmaceutics

authors： Song X,Lorenzi PL,Landowski CP,Vig BS,Hilfinger JM,Amidon GL

更新日期：2005-03-01 00:00:00

abstract：:The need for an efficacious and safe oral anticoagulant that does not require monitoring has been largely unmet. Many efforts have centered on preparing orally available heparin to improve patient compliance. In this study, novel orally active heparin derivatives (LHD), i.e. low molecular weight heparin (LMWH) conjuga...

journal_title：Molecular pharmaceutics

authors： Park JW,Jeon OC,Kim SK,Al-Hilal TA,Moon HT,Kim CY,Byun Y

更新日期：2010-06-07 00:00:00

abstract：:Retinal pigment epithelium, which forms the outer blood-retinal barrier, is a critical barrier for transport of drugs to the retina. The purpose of this study was to develop a pigmented MDCK (P-MDCK) cell line as a rapidly established in vitro model for the outer blood-retinal barrier to assess the influence of melani...

journal_title：Molecular pharmaceutics

authors： Kadam RS,Scheinman RI,Kompella UB

更新日期：2012-11-05 00:00:00

abstract：:Today, about 50% of men and 15-30% of women suffer from hair loss as well as the associated psychological impact. Drug therapy, especially through topical administration, is the main treatment strategy for stimulating hair regrowth. However, challenges exist due to the skin barrier that hinders drug penetration. To th...

journal_title：Molecular pharmaceutics

authors： Yang G,Chen G,Gu Z

更新日期：2021-02-01 00:00:00

abstract：:Nonviral transfections of six low passage human colon cancer cell lines using the artificial beta-catenin/TCF-dependent promoter CTP4 demonstrated a high promoter activity which was 1000- to 70000-fold higher than in HeLa control cells. Luciferase gene expression levels obtained with CTP4 in epithelial-like tumor cell...

journal_title：Molecular pharmaceutics

authors： Gaedtke L,Pelisek J,Lipinski KS,Wrighton CJ,Wagner E

更新日期：2007-01-01 00:00:00

abstract：:Peptide nucleic acids have a number of features that make them an ideal platform for the development of in vitro biological probes and tools. Unfortunately, their inability to pass through membranes has limited their in vivo application as diagnostic and therapeutic agents. Herein, we describe the development of catio...

journal_title：Molecular pharmaceutics

authors： Fang H,Zhang K,Shen G,Wooley KL,Taylor JS

更新日期：2009-03-01 00:00:00

abstract：:We have recently reported that by converting a perforin inhibitor into an l-type amino acid transporter 1 (LAT1)-utilizing prodrug its cellular uptake can be greatly increased. The aim of the present study was to determine the in vivo and brain pharmacokinetics of two perforin inhibitors and their LAT1-utilizing prodr...

journal_title：Molecular pharmaceutics

authors： Gynther M,Pickering DS,Spicer JA,Denny WA,Huttunen KM

更新日期：2016-07-05 00:00:00

abstract：:The reaction of singlet oxygen with water to form hydrogen peroxide was catalyzed by antibodies and has been termed as the antibody catalyzed water oxidation pathway (ACWOP) (Nieva and Wentworth, Trends Biochem. Sci. 2004, 29, 274-278; Nieva et al. Immunol. Lett. 2006, 103, 33-38). While conserved and buried tryptopha...

journal_title：Molecular pharmaceutics

authors： Sreedhara A,Lau K,Li C,Hosken B,Macchi F,Zhan D,Shen A,Steinmann D,Schöneich C,Lentz Y

更新日期：2013-01-07 00:00:00

abstract：:The ultrasmall nanoparticle AGuIX is a versatile platform that tolerates a range of chemical diversity for theranostic applications. Our previous work showed that AGuIX clears rapidly from normal tissues, while durably accumulating within the tumor microenvironment. On this basis, AGuIX was used to detect tumor tissue...

journal_title：Molecular pharmaceutics

authors： Truillet C,Thomas E,Lux F,Huynh LT,Tillement O,Evans MJ

更新日期：2016-07-05 00:00:00

abstract：:Polysorbate 20 (PS20) is a commonly used surfactant in biopharmaceutical formulations. It is a heterogeneous surfactant containing a distribution of fatty acid esters, which are subject to hydrolytic degradation, generating free fatty acids (FFAs). The FFAs can form visible or subvisible particles in drug product on s...

journal_title：Molecular pharmaceutics

authors： Doshi N,Martin J,Tomlinson A

更新日期：2020-11-02 00:00:00

abstract：:Viral nanotechnology is an emerging and highly interdisciplinary field in which viral nanoparticles (VNPs) are applied in diverse areas such as electronics, energy and next-generation medical devices. VNPs have been developed as candidates for novel materials, and are often described as "programmable" because they can...

journal_title：Molecular pharmaceutics

authors： Pokorski JK,Steinmetz NF

更新日期：2011-02-07 00:00:00

abstract：:The amorphization of the readily crystallizable therapeutic ingredient and food additive, menthol, was successfully achieved by inclusion of neat menthol in mesoporous silica matrixes of 3.2 and 5.9 nm size pores. Menthol amorphization was confirmed by the calorimetric detection of a glass transition. The respective g...

journal_title：Molecular pharmaceutics

authors： Cordeiro T,Castiñeira C,Mendes D,Danède F,Sotomayor J,Fonseca IM,Gomes da Silva M,Paiva A,Barreiros S,Cardoso MM,Viciosa MT,Correia NT,Dionisio M

更新日期：2017-09-05 00:00:00