Modulation of pyridinium cationic lipid-DNA complex properties by pyridinium gemini surfactants and its impact on lipoplex transfection properties.

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：:Three different types of atom accessibility descriptors are investigated in relation to site of metabolism predictions. To enable the integration of local accessibility we have constructed 2DSASA, a method for the calculation of the atomic solvent accessible surface area that is independent of 3D coordinates. The meth...

journal_title：Molecular pharmaceutics

authors： Rydberg P,Rostkowski M,Gloriam DE,Olsen L

更新日期：2013-04-01 00:00:00

abstract：:Photodynamic therapy (PDT) is promising for clinical cancer therapy; however, the efficacy was limited as an individual treatment regimen. Here, an approach synergistically combining PDT and nitric oxide (NO) gas therapy along with destruction of the tumor extracellular matrix (ECM) was presented to eliminate cancer. ...

journal_title：Molecular pharmaceutics

authors： Sun Z,Wang X,Liu J,Wang Z,Wang W,Kong D,Leng X

更新日期：2021-01-11 00:00:00

abstract：:In the current study, nanoparticles containing the antimetabolite drug methotrexate (MTX) and the novel tubulin-binding drug pretubulysin (PT) were developed for combination chemotherapy. Polyelectrolyte complexes were formed based on ∼20 nm cationic nanomicelles of lipo-oligomer 454 with the anionic MTX at the molar ...

journal_title：Molecular pharmaceutics

authors： Truebenbach I,Kern S,Loy DM,Höhn M,Gorges J,Kazmaier U,Wagner E

更新日期：2019-06-03 00:00:00

abstract：:Myeloid differentiation primary response 88 (MyD88) is an intracellular adaptor protein central to the signaling of multiple receptors involved in inflammation. Since innate immune inflammation promotes autoimmunity, MyD88 is an attractive target in autoimmune disease. We previously developed c(MyD 4-4), a novel cycli...

journal_title：Molecular pharmaceutics

authors： Dishon S,Schumacher-Klinger A,Gilon C,Hoffman A,Nussbaum G

更新日期：2019-04-01 00:00:00

abstract：:Doxorubicin (DOX) is one of the most commonly used antineoplastic agents, but its clinical application is oftentimes coupled with severe side effects. Selective delivery of DOX to tumors via nanosized drug carrier represents an attractive approach to this problem. Previously, we developed a dual functional nanomicella...

journal_title：Molecular pharmaceutics

authors： Lu J,Zhao W,Huang Y,Liu H,Marquez R,Gibbs RB,Li J,Venkataramanan R,Xu L,Li S,Li S

更新日期：2014-11-03 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：:An artificial stomach duodenum (ASD) model has been used to demonstrate the performance difference between two formulations of LY2300559, a low-solubility acidic developmental drug. The two formulations investigated were a conventional high-shear wet granulation (HSWG) formulation and a solid dispersion formulation. A...

journal_title：Molecular pharmaceutics

authors： Polster CS,Wu SJ,Gueorguieva I,Sperry DC

更新日期：2015-04-06 00:00:00

abstract：:A novel design of anticancer drug delivery system, based on an electrostatic binding of negatively charged liposomes and cationic metalloporphyrins under physiological conditions, is reported. A lack of cytotoxicity of the iron(III) porphyrin-loaded liposomes and an efficient generation of a toxic hydroxyl radical (OH...

journal_title：Molecular pharmaceutics

authors： Yuasa M,Oyaizu K,Horiuchi A,Ogata A,Hatsugai T,Yamaguchi A,Kawakami H

更新日期：2004-09-01 00:00:00

abstract：:The applicability of the computational docking approach was investigated to create a novel method for quick additive screening to inhibit the crystallization taking place in amorphous drugs. Surface energy and attachment energy were utilized to recognize the morphologically most important crystal faces. The surfaces (...

journal_title：Molecular pharmaceutics

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

更新日期：2012-10-01 00:00:00

abstract：:Our work has focused on defining the utility of fluorine (19F)-labeled bile acid analogues and magnetic resonance imaging (MRI) to identify altered bile acid transport in vivo. In the current study, we explored the ability of this approach to differentiate fibroblast growth factor-15 (FGF15)-deficient from wild-type (...

journal_title：Molecular pharmaceutics

authors： Metry M,Felton J,Cheng K,Xu S,Ai Y,Xue F,Raufman JP,Polli JE

更新日期：2018-11-05 00:00:00

abstract：:Targeting of drugs administered systemically relies on the higher affinity of ligands for specific receptors to obtain selectivity in drug response. However, achieving the same goal inside the bladder is much easier with an intelligent pharmaceutical approach that restricts drug effects by exploiting the pelvic anatom...

journal_title：Molecular pharmaceutics

authors： Tyagi P,Wu PC,Chancellor M,Yoshimura N,Huang L

更新日期：2006-07-01 00:00:00

abstract：:Targeted delivery of anticancer drugs to brain tumors, especially glioblastoma multiforme, which is the most frequent and aggressive type, is one of the important objectives in nanomedicine. Vascular endothelial growth factor (VEGF) and its receptor type II (VEGFR2) are promising targets because they are overexpressed...

journal_title：Molecular pharmaceutics

authors： Shein SA,Kuznetsov II,Abakumova TO,Chelushkin PS,Melnikov PA,Korchagina AA,Bychkov DA,Seregina IF,Bolshov MA,Kabanov AV,Chekhonin VP,Nukolova NV

更新日期：2016-11-07 00:00:00

abstract：:Boron neutron capture therapy (BNCT) has received extensive attention as noninvasive cell-level oncotherapy for treating solid cancer tumors. However, boron-containing drugs such as l-boronophenylalanine (BPA) and sodium borocaptate have low boron content and/or poor tumor-targeting ability, limiting their application...

journal_title：Molecular pharmaceutics

authors： Li R,Zhang J,Guo J,Xu Y,Duan K,Zheng J,Wan H,Yuan Z,Chen H

更新日期：2020-01-06 00:00:00

abstract：:Two-phase gas-liquid microfluidic reactors provide shear processing control of SN-38-loaded polymer nanoparticles (SN-38-PNPs). We prepare SN-38-PNPs from the block copolymer poly(methyl caprolactone- co-caprolactone)- block-poly(ethylene oxides) (P(MCL- co-CL)- b-PEO) using bulk and microfluidic methods and at differ...

journal_title：Molecular pharmaceutics

authors： Cao Y,Silverman L,Lu C,Hof R,Wulff JE,Moffitt MG

更新日期：2019-01-07 00:00:00

abstract：:In the postprandial stomach, processes such as secretion, digestion, and gastric emptying all occur simultaneously. Therefore, the system is highly heterogeneous and dynamically changing, for instance, in terms of various physicochemical parameters such as pH value or viscosity. Thus, the administration of a drug toge...

journal_title：Molecular pharmaceutics

authors： Schick P,Sager M,Wegner F,Wiedmann M,Schapperer E,Weitschies W,Koziolek M

更新日期：2019-11-04 00:00:00

abstract：:As microRNAs (miRNAs) have been reported to be a type of novel high-value small molecule (SM) drug targets for disease treatments, many researchers are engaged in the field of exploring new SM-miRNA associations. Nevertheless, because of the high cost, adopting traditional biological experiments constrains the efficie...

journal_title：Molecular pharmaceutics

authors： Yin J,Chen X,Wang CC,Zhao Y,Sun YZ

更新日期：2019-07-01 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：:Stably transfected MDCK/hPepT1-V5&His clonal cell lines expressing varying levels of epitope-tagged hPepT1 protein were established to quantify the relationship between transgene hPepT1 expression levels and its functional kinetics in facilitating peptide and peptide-like drug uptake and transport in vitro. The hPepT1...

journal_title：Molecular pharmaceutics

authors： Herrera-Ruiz D,Faria TN,Bhardwaj RK,Timoszyk J,Gudmundsson OS,Moench P,Wall DA,Smith RL,Knipp GT

更新日期：2004-03-01 00:00:00

abstract：:5-Fluorocytosine (FC), an antifungal drug and a cytosine derivative, has a complex solid-state landscape that challenges its development into a drug product. A total of eight new FC salts, both cytosinium and hemicytosinium, with four strong acids were prepared by controlling acid concentration in the crystallization ...

journal_title：Molecular pharmaceutics

authors： Perumalla SR,Pedireddi VR,Sun CC

更新日期：2013-06-03 00:00:00

abstract：:The Biopharmaceutical Classification System (BCS) guidance issued by the FDA allows waivers for in vivo bioavailability and bioequivalence studies for immediate-release (IR) solid oral dosage forms only for BCS class I drugs. However, a number of drugs within BCS class III have been proposed to be eligible for biowaiv...

journal_title：Molecular pharmaceutics

authors： Tsume Y,Amidon GL

更新日期：2010-08-02 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：:Terpenoids represent a diverse class of molecules that provide a wealth of opportunities to address many human health and societal issues. The expansive array of structures and functionalities that have been evolved in nature provide an excellent pool of molecules for use in human therapeutics. While this class of mol...

journal_title：Molecular pharmaceutics

authors： Ajikumar PK,Tyo K,Carlsen S,Mucha O,Phon TH,Stephanopoulos G

更新日期：2008-03-01 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：:Fenretinide, a chemotherapeutic agent for cancer, is water-insoluble and has a very low oral bioavailability. Hence, the objective was to deliver it as an injectable depot and improve the drug solubility and release behavior from poly(lactide-co-glycolide) (PLGA) microspheres by incorporating nonionic surfactants with...

journal_title：Molecular pharmaceutics

authors： Zhang Y,Wischke C,Mittal S,Mitra A,Schwendeman SP

更新日期：2016-08-01 00:00:00

abstract：:For the purpose of improving the tumor delivery of doxorubicin (DOX), a kind of peptide-DOXO conjugate was designed and prepared, in which the peptide composed of an albumin-binding domain (ABD) and a tumor-specific internalizing sequence (RGDK or RPARPAR) was conjugated to a (6-maleimidocaproyl) hydrazone derivative ...

journal_title：Molecular pharmaceutics

authors： Liu L,Zhang C,Li Z,Wang C,Bi J,Yin S,Wang Q,Yu R,Liu Y,Su Z

更新日期：2017-11-06 00:00:00

abstract：:Electrostatic potential (ESP) is a useful physicochemical property of a molecule that provides insights into inter- and intramolecular associations, as well as prediction of likely sites of electrophilic and nucleophilic metabolic attack. Knowledge of sites of metabolic attack is of paramount importance in DMPK resear...

journal_title：Molecular pharmaceutics

authors： Ford KA

更新日期：2013-04-01 00:00:00

abstract：:A highly versatile and step-economical route to a new class of guanidinium-rich molecular transporters and evaluation of their ability to complex, deliver, and release siRNA are described. These new drug/probe delivery systems are prepared in only two steps, irrespective of length or composition, using an organocataly...

journal_title：Molecular pharmaceutics

authors： Wender PA,Huttner MA,Staveness D,Vargas JR,Xu AF

更新日期：2015-03-02 00:00:00

abstract：:The tumor microenvironments are often acidic and overexpress specific enzymes. In this work, we synthesized a poly(AA-b-NIPAAm) copolymer (PAA-b-PNIPAAm) using a reversible addition-fragmentation chain transfer (RAFT) polymerization method. PAA-b-PNIPAAm and a cationic protein (protamine) were self-assembled into nano...

journal_title：Molecular pharmaceutics

authors： Don TM,Lu KY,Lin LJ,Hsu CH,Wu JY,Mi FL

更新日期：2017-12-04 00:00:00

abstract：:Conventional drug solubilization strategies limit the understanding of the full potential of poorly water-soluble drugs during drug screening. Here, we propose a screening approach in which poorly water-soluble drugs are entrapped in poly(2-(methacryloyloxyethyl phosphorylcholine)-poly(2-(diisopropylaminoethyl methacr...

journal_title：Molecular pharmaceutics

authors： Sola-Barrado B,M Leite D,Scarpa E,Duro-Castano A,Battaglia G

更新日期：2020-12-07 00:00:00