Combination Chemotherapy of L1210 Tumors in Mice with Pretubulysin and Methotrexate Lipo-Oligomer Nanoparticles.

abstract：:Alkylphosphocholine (APC) analogs are a novel class of broad-spectrum tumor-targeting agents that can be used for both diagnosis and treatment of cancer. The potential for clinical translation for APC analogs will strongly depend on their pharmacokinetic (PK) profiles. The aim of this work was to understand how the ch...

journal_title：Molecular pharmaceutics

authors： Zhang RR,Grudzinksi JJ,Mehta TI,Burnette RR,Hernandez R,Clark PA,Lubin JA,Pinchuk AN,Jeffrey J,Longino M,Kuo JS,Weichert JP

更新日期：2019-08-05 00:00:00

abstract：:Heart transplantation (HT) is an effective treatment for end-stage heart disease. However, acute rejection (AR) is still the main cause of death within one year after HT. AR is an acute immune response mediated by T lymphocytes, mainly CD4+ T lymphocytes. This study innovatively develops a radiolabeled probe 99mTc-HYN...

journal_title：Molecular pharmaceutics

authors： Li H,Chen Y,Jin Q,Wu Y,Deng C,Gai Y,Sun Z,Li Y,Wang J,Yang Y,Lv Q,Zhang Y,An R,Lan X,Zhang L,Xie M

更新日期：2021-01-28 00:00:00

abstract：:Process-induced phase transformations (PIPTs) of active pharmaceutical ingredients (APIs) can alter APIs' physicochemical properties and impact performance of pharmaceutical drug products. In this study, we investigated compression-induced amorphization of crystalline posaconazole (POSA), where the impact of mechanica...

journal_title：Molecular pharmaceutics

authors： Huang C,Klinzing G,Procopio A,Yang F,Ren J,Burlage R,Zhu L,Su Y

更新日期：2019-02-04 00:00:00

abstract：:We have developed a macromolecular prodrug platform based on poly(l-lysine succinylated) (PLS) that targets scavenger receptor A1 (SR-A1), a receptor expressed by myeloid and endothelial cells. We demonstrate the selective uptake of PLS by murine macrophage, RAW 264.7 cells, which was eliminated upon cotreatment with ...

journal_title：Molecular pharmaceutics

authors： Stevens DM,Adiseshaiah P,Dasa SSK,Potter TM,Skoczen SL,Snapp KS,Cedrone E,Patel N,Busman-Sahay K,Rosen EP,Sykes C,Cottrell M,Dobrovolskaia MA,Estes JD,Kashuba ADM,Stern ST

更新日期：2020-10-05 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：:Solvation of drugs in the core (C) and headgroup (H) strata of phospholipid bilayers affects their physiological transport rates and accumulation. These characteristics, especially a complete drug distribution profile across the bilayer strata, are tedious to obtain experimentally, to the point that even simplified pr...

journal_title：Molecular pharmaceutics

authors： Natesan S,Lukacova V,Peng M,Subramaniam R,Lynch S,Wang Z,Tandlich R,Balaz S

更新日期：2014-10-06 00:00:00

abstract：:Photodynamic therapy, a procedure that uses a photosensitizer to enable light therapy selectively at diseased sites, remains underutilized in oncological clinic. To further improve its cancer selectivity, we developed a polymeric nanosystem by conjugating a photosensitizer IRDye 700DX (IR700) and cancer targeting RGD ...

journal_title：Molecular pharmaceutics

authors： Zhao Y,Li F,Mao C,Ming X

更新日期：2018-07-02 00:00:00

abstract：:Amorphous solids and crystalline salts are both of interest as a means of improving the dissolution characteristics and apparent solubility of poorly water soluble active pharmaceutical ingredients which have low bioavailability in humans. The theory and selection of both crystalline drug substance salt forms and amor...

journal_title：Molecular pharmaceutics

authors： Towler CS,Li T,Wikström H,Remick DM,Sanchez-Felix MV,Taylor LS

更新日期：2008-11-01 00:00:00

abstract：:Gene therapy represents a potential efficient approach of disease prevention and therapy. However, due to their poor in vivo stability, gene molecules need to be associated with delivery systems to overcome extracellular and intracellular barriers and allow access to the site of action. Cationic polymeric nanoparticle...

journal_title：Molecular pharmaceutics

authors： Navarro G,Pan J,Torchilin VP

更新日期：2015-02-02 00:00:00

abstract：:Some of the most significant therapeutic leads and agents used for the treatment of cancer target microtubule dynamics. Paclitaxel is an exceptional example that is currently used for treating a wide range of tumors. New, non-taxane microtubule stabilizers, including several epothilones, are advancing through clinical...

journal_title：Molecular pharmaceutics

authors： Clark EA,Hills PM,Davidson BS,Wender PA,Mooberry SL

更新日期：2006-07-01 00:00:00

abstract：:Lipophilic cations such as phosphonium salts can accumulate in mitochondria of heart in response to the negative inner-transmembrane potentials. Two phosphonium salts [(18)F]FMBTP and [(18)F]mFMBTP were prepared and evaluated as potential myocardial perfusion imaging (MPI) agents in this study. The cations were radiol...

journal_title：Molecular pharmaceutics

authors： Zhao Z,Yu Q,Mou T,Liu C,Yang W,Fang W,Peng C,Lu J,Liu Y,Zhang X

更新日期：2014-11-03 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 study presents the effects of blending a cationic gemini surfactant into cationic lipid bilayers and its impact on the plasmid DNA compaction and delivery process. Using nanoDSC, dynamic light scattering, zeta potential, and electrophoretic mobility measurements, together with transfection (2D- and 3D-) and viabil...

journal_title：Molecular pharmaceutics

authors： Sharma VD,Lees J,Hoffman NE,Brailoiu E,Madesh M,Wunder SL,Ilies MA

更新日期：2014-02-03 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：:Low molecular weight nucleoside gelators hold great promise in drug delivery and particularly for the delivery of biologics because of their excellent biocompatibility. However, the influence of these gelators on protein aggregation inhibition has not yet been studied. Protein aggregation is the most significant cause...

journal_title：Molecular pharmaceutics

authors： Johnson L,Faidra Angelerou MG,Surikutchi BT,Allen S,Zelzer M,Marlow M

更新日期：2019-01-07 00:00:00

abstract：:Metallacarborane moieties have been identified as promising pharmacophores. The pharmaceutical use of such compounds is, however, complicated by their low solubility and tendency to self-assemble in aqueous solution. In this work, we estimated the solubilities of a vast series of metallacarboranes [cobalt bis(dicarbol...

journal_title：Molecular pharmaceutics

authors： Rak J,Dejlová B,Lampová H,Kaplánek R,Matějíček P,Cígler P,Král V

更新日期：2013-05-06 00:00:00

abstract：:Tumor endothelial marker 8 (TEM8) is a cell surface receptor that is highly expressed in a variety of human tumors and promotes tumor angiogenesis and cell growth. Antibodies targeting TEM8 block tumor angiogenesis in a manner distinct from the VEGF receptor pathway. Development of a TEM8 imaging agent could aid in pa...

journal_title：Molecular pharmaceutics

authors： Kuo F,Histed S,Xu B,Bhadrasetty V,Szajek LP,Williams MR,Wong K,Wu H,Lane K,Coble V,Vasalatiy O,Griffiths GL,Paik CH,Elbuluk O,Szot C,Chaudhary A,St Croix B,Choyke P,Jagoda EM

更新日期：2014-11-03 00:00:00

abstract：:BCS classification is a vital tool in the development of both generic and innovative drug products. The purpose of this work was to provisionally classify the world's top selling oral drugs according to the BCS, using in silico methods. Three different in silico methods were examined: the well-established group contri...

journal_title：Molecular pharmaceutics

authors： Dahan A,Wolk O,Kim YH,Ramachandran C,Crippen GM,Takagi T,Bermejo M,Amidon GL

更新日期：2013-11-04 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：:Constitutive activation of signal transducer and activator of transcription 3 (STAT3) in tumor cells and tumor associated dendritic cells (DCs) plays a major role in the progression of cancer. JSI-124 (cucurbitacin I) is a potent inhibitor of STAT3; however, its poor solubility and nonspecificity limit its effectivene...

journal_title：Molecular pharmaceutics

authors： Garg SM,Vakili MR,Molavi O,Lavasanifar A

更新日期：2017-08-07 00:00:00

abstract：:This study determined intraluminal ethanol concentrations (stomach and duodenum) in fed healthy volunteers after the consumption of common alcoholic beverages (beer, wine, and whisky). The results of this study were compared with a previous study in fasted volunteers. Five healthy volunteers were recruited in a crosso...

journal_title：Molecular pharmaceutics

authors： Rubbens J,Riethorst D,Brouwers J,Wolfs K,Adams E,Tack J,Augustijns P

更新日期：2017-12-04 00:00:00

abstract：:To develop a radioactive metal complex platform for tumor theranostics, we introduced three radiopharmaceutical derivatives of 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic acid-benzothiazole aniline (DO3A-BTA, L1) labeled with medical radioisotopes for diagnosis (68Ga/64Cu) and therapy (177Lu). The tumor-targeting ...

journal_title：Molecular pharmaceutics

authors： Park JA,Lee JW,Kim HK,Shin UC,Lee KC,Kim TJ,Chang Y,Kim KM,Kim JY,Lee YJ

更新日期：2018-03-05 00:00:00

abstract：:Integrin αvβ3 is a cell adhesion molecule involved in the progression and invasion of glioblastoma, making it an attractive target for the diagnosis of glioblastoma. Although some integrin αvβ3 specific ligands, such as RGD and its mimetic peptides (Cilengitide), have been devoted in detecting glioblastoma, their clin...

journal_title：Molecular pharmaceutics

authors： Zhang L,Shan X,Meng X,Gu T,Guo L,An X,Jiang Q,Ge H,Ning X

更新日期：2019-09-03 00:00:00

abstract：:Pyropheophorbide-a (Pyro) is a highly promising photosensitizer for tumor photodynamic therapy (PDT), although its very limited tumor-accumulation ability seriously restricts its clinical applications. A higher accumulation of photosensitizers is very important for the treatment of deeply seated and larger tumors. The...

journal_title：Molecular pharmaceutics

authors： Li W,Tan S,Xing Y,Liu Q,Li S,Chen Q,Yu M,Wang F,Hong Z

更新日期：2018-04-02 00:00:00

abstract：:"Nano" drug delivery carriers are established technologies for improving the therapeutic index of chemotherapeutic drugs and overcoming formulation challenges of poorly water-soluble compounds. Two important remaining challenges, however, are the need to formulate drugs on a case-by-case basis (due to the specific che...

journal_title：Molecular pharmaceutics

authors： Fuhrmann K,Gauthier MA,Leroux JC

更新日期：2014-06-02 00:00:00

abstract：:Combinatorial chemistry has enabled the production of very potent drugs that might otherwise suffer from poor solubility and low oral bioavailability. One approach to increase solubility is to make the drug amorphous, which leads to problems associated with drug stability. To improve stability, one option is to molecu...

journal_title：Molecular pharmaceutics

authors： Pajula K,Wittoek L,Lehto VP,Ketolainen J,Korhonen O

更新日期：2014-07-07 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 impact of the chain length or dispersity of polymers in controlling the crystallization of amorphous active pharmaceutical ingredients (APIs) has been discussed for a long time. However, because of the weak control of these parameters in the majority of macromolecules used in pharmaceutical formulations, the above...

journal_title：Molecular pharmaceutics

authors： Minecka A,Tarnacka M,Jurkiewicz K,Hachuła B,Wrzalik R,Kamiński K,Paluch M,Kamińska E

更新日期：2021-01-04 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：: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