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：:In this paper, we investigate the release of two drugs, nicotine and caffeine, from poly epsilon-caprolactone (PCL) matrices, as a model for the delivery of highly hydrophilic drugs. Since PCL does not degrade over the period of our experiments (<30 days), drug diffusion through the matrix is expected to be the domina...

journal_title：Molecular pharmaceutics

authors： Rosenberg R,Devenney W,Siegel S,Dan N

更新日期：2007-11-01 00:00:00

abstract：:Macromolecules with defined nanosizes--nanoglobules--were synthesized and characterized as novel drug carriers with precise molecular architectures. Poly-L-lysine dendrimers with a cubic octa(3-aminopropyl)silsesquioxane (OAS) core, (L-lysine 8-OAS, (L-lysine) 16-(L-lysine) 8-OAS, (L-lysine) 32-(L-lysine) 16-(L-lysine...

journal_title：Molecular pharmaceutics

authors： Kaneshiro TL,Wang X,Lu ZR

更新日期：2007-09-01 00:00:00

abstract：:Hydrophobic single-wall carbon nanohorns (SWNHs) were dispersed in aqueous media by noncovalently modifying their surfaces with conjugate molecules comprised of polyethylene glycol (PEG) and a peptide aptamer (NHBP-1) that specifically bind to the surfaces of the SWNHs. The conjugates were synthesized by coupling PEG ...

journal_title：Molecular pharmaceutics

authors： Matsumura S,Ajima K,Yudasaka M,Iijima S,Shiba K

更新日期：2007-09-01 00:00:00

abstract：:Major obstacles in the development of new therapeutic anticancer drugs are the low bioavailability of hydrophilic substances and the nonspecific toxicity toward healthy tissues. As such, cell-targeting oligopeptides have emerged as attractive drug delivery vehicles for a variety of different types of cargo. The recent...

journal_title：Molecular pharmaceutics

authors： Liu Y,Steiniger SC,Kim Y,Kaufmann GF,Felding-Habermann B,Janda KD

更新日期：2007-05-01 00:00:00

abstract：:This study describes the interactions between two amphiphilic molecules with antileishmanial activity, amphotericin B (AmB) and miltefosine [hexadecylphosphocholine (HePC)], the latter being effective by the oral route. The effect of HePC on the aggregation state of AmB in aqueous solution and the interactions between...

journal_title：Molecular pharmaceutics

authors： Ménez C,Legrand P,Rosilio V,Lesieur S,Barratt G

更新日期：2007-03-01 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：:Genospheres are cationic lipid-nucleic acid nanoparticles prepared by the assembly of the lipids and nucleic acids from an aqueous/organic liquid monophase that independently dissolves the components, where the resultant particles are homogeneously sized (70-110 nm), with efficiently incorporated and protected DNA. In...

journal_title：Molecular pharmaceutics

authors： Hayes ME,Drummond DC,Hong K,Zheng WW,Khorosheva VA,Cohen JA,C O N 4th,Park JW,Marks JD,Benz CC,Kirpotin DB

更新日期：2006-11-01 00:00:00

abstract：:Contrast-enhanced ultrasound imaging has shown promise in the field of molecular imaging. This technique relies upon the adhesion of ultrasound contrast agent (UCA) to targeted molecular markers of disease. This is accomplished by coating the surface of the contrast agent with a ligand that specifically binds to the i...

journal_title：Molecular pharmaceutics

authors： Rychak JJ,Li B,Acton ST,Leppänen A,Cummings RD,Ley K,Klibanov AL

更新日期：2006-09-01 00:00:00

abstract：:Cationic poly-L-lysine 3H-dendrimers with either 16 or 32 surface amine groups (BHALys [Lys]4 [3H-Lys]8 [NH2]16 and BHALys [Lys]8 [3H-Lys]16 [NH2]32, generation 3 and 4, respectively) have been synthesized and their pharmacokinetics and biodistribution investigated after intravenous administration to rats. The species...

journal_title：Molecular pharmaceutics

authors： Boyd BJ,Kaminskas LM,Karellas P,Krippner G,Lessene R,Porter CJ

更新日期：2006-09-01 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：: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：:The human apical sodium-dependent bile acid transporter (hASBT) is a potential target for drug delivery, but an understanding of hASBT substrate requirements is limited. The objective of this study was to evaluate the influence of ionic character and steric bulk in the C-24 region of bile acid conjugates in governing ...

journal_title：Molecular pharmaceutics

authors： Balakrishnan A,Wring SA,Coop A,Polli JE

更新日期：2006-05-01 00:00:00

abstract：:Polymer therapeutics has emerged as a new clinical option for the treatment of human diseases. However, little is known about pharmacogenetic responses to drugs formulated with polymers. In this study, we demonstrate that a formulation containing the block copolymer Pluronic P85 and antineoplastic drug doxorubicin (Do...

journal_title：Molecular pharmaceutics

authors： Batrakova EV,Kelly DL,Li S,Li Y,Yang Z,Xiao L,Alakhova DY,Sherman S,Alakhov VY,Kabanov AV

更新日期：2006-03-01 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：: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：:We studied the molecular mechanism of greater efficacy of paclitaxel-loaded nanoparticles (Tx-NPs) following conjugation to transferrin (Tf) ligand in breast cancer cell line. NPs were formulated using biodegradable polymer, poly(lactic-co-glycolide) (PLGA), with encapsulated Tx and conjugated to Tf ligand via an epox...

journal_title：Molecular pharmaceutics

authors： Sahoo SK,Labhasetwar V

更新日期：2005-09-01 00:00:00

abstract：:The synthesis of a dendrimer based on melamine that displays multiple copies of four orthogonally reactive groups, three on the surface and one on the interior, is described. The three groups on the surface are nucleophilic and include four free hydroxyl groups, four hydroxyl groups masked as tert-butyldiphenylsilyl (...

journal_title：Molecular pharmaceutics

authors： Lim J,Simanek EE

更新日期：2005-07-01 00:00:00

abstract：:We have developed a novel water-dispersible oleic acid (OA)-Pluronic-coated iron oxide magnetic nanoparticle formulation that can be loaded easily with high doses of water-insoluble anticancer agents. Drug partitions into the OA shell surrounding iron oxide nanoparticles, and the Pluronic that anchors at the OA-water ...

journal_title：Molecular pharmaceutics

authors： Jain TK,Morales MA,Sahoo SK,Leslie-Pelecky DL,Labhasetwar V

更新日期：2005-05-01 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：:Delivery of antigenic protein to the cytosol of antigen-presenting cells (APCs), such as macrophages (MPhi) and dendritic cells (DCs), is required for an efficient CD8 T-cell-mediated immune response. We have previously shown that co-encapsulation of antigenic protein inside pH-sensitive liposomes with listeriolysin O...

journal_title：Molecular pharmaceutics

authors： Stier EM,Mandal M,Lee KD

更新日期：2005-01-01 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：:Delivery of plasmid DNA for protein production in mammalian cells is not an efficient process. In this study, the theory that cellular localization of plasmid DNA increases transfection efficiency is examined with an emphasis on the understanding of the cellular association of the components of a ternary transfection ...

journal_title：Molecular pharmaceutics

authors： Guo C,Gemeinhart RA

更新日期：2004-07-01 00:00:00

abstract：:The mechanism of cell death in A2780 human ovarian carcinoma cells induced by free doxorubicin (DOX) and N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-bound DOX [P-(GFLG)-DOX] was investigated. In particular, the involvement of the Fas receptor system in drug-induced apoptosis was evaluated. P-(GFLG)-DOX was show...

journal_title：Molecular pharmaceutics

authors： Malugin A,Kopecková P,Kopecek J

更新日期：2004-05-01 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：:Saquinavir mesylate (SQV) is the first-in-class and prototypical HIV protease inhibitor (PI) used in the treatment of HIV infection. SQV undergoes extensive hepatic metabolism and intestinal and bile secretion, and has poor and variable oral bioavailability. In previous studies, our group and others have described the...

journal_title：Molecular pharmaceutics

authors： Su Y,Zhang X,Sinko PJ

更新日期：2004-01-12 00:00:00