Pharmacokinetics in Vitro and in Vivo of Two Novel Prodrugs of Oleanolic Acid in Rats and Its Hepatoprotective Effects against Liver Injury Induced by CCl4.

abstract：:We report the development of sponge Haliclona sp. spicules, referred to as SHS, and its topical application in skin delivery of hydrophilic biomacromolecules, a series of fluorescein isothiocyanate-dextrans (FDs). SHS are silicious oxeas which are sharp-edged and rod-shaped (∼120 μm in length and ∼7 μm in diameter). S...

journal_title：Molecular pharmaceutics

authors： Zhang S,Ou H,Liu C,Zhang Y,Mitragotri S,Wang D,Chen M

更新日期：2017-09-05 00:00:00

abstract：:Secondary macrophage cytotoxicity induced by nanoparticles was described before. The study aim was to investigate the role of secondary cytotoxic effect in a macrophage-lung cancer coculture model after nanoparticle treatment in the presence and absence of anti-inflammatory drugs. An in vitro coculture model composed ...

journal_title：Molecular pharmaceutics

authors： Sarfraz M,Roa W,Bou-Chacra N,Löbenberg R

更新日期：2016-09-06 00:00:00

abstract：:Deep generative adversarial networks (GANs) are the emerging technology in drug discovery and biomarker development. In our recent work, we demonstrated a proof-of-concept of implementing deep generative adversarial autoencoder (AAE) to identify new molecular fingerprints with predefined anticancer properties. Another...

journal_title：Molecular pharmaceutics

authors： Kadurin A,Nikolenko S,Khrabrov K,Aliper A,Zhavoronkov A

更新日期：2017-09-05 00:00:00

abstract：:Engineered superparamagnetic iron oxide nanoparticles (SPIONs) have been studied extensively for their localized homogeneous heat generation in breast cancer therapy. However, challenges such as aggregation and inability to produce sub-10 nm SPIONs limit their potential in magnetothermal ablation. We report a facile, ...

journal_title：Molecular pharmaceutics

authors： Alhasan AH,Fardous RS,Alsudir SA,Majrashi MA,Alghamdi WM,Alsharaeh EH,Almalik AM

更新日期：2019-08-05 00:00:00

abstract：:The antiviral drug tenofovir (TFV) is orally administered as the fumarate salt of its disoproxil prodrug (TFV disoproxil fumarate (TDF)). TFV is a dianion at physiological pH and, as a result, has poor lipid membrane permeability. Administration of the lipophilic and cell-permeable prodrug, TFV disoproxil, enhances th...

journal_title：Molecular pharmaceutics

authors： Durand-Gasselin L,Van Rompay KK,Vela JE,Henne IN,Lee WA,Rhodes GR,Ray AS

更新日期：2009-07-01 00:00:00

abstract：:Following oral administration, dabigatran etexilate (DABE) is rapidly hydrolyzed to its active form, dabigatran. DABE, but not dabigatran, presents as a P-glycoprotein (P-gp) substrate and has increasingly been used as a probe drug. Therefore, although dosed as DABE, a P-gp drug-drug interaction (DDI) is reported as a...

journal_title：Molecular pharmaceutics

authors： Shen H,Yao M,Sinz M,Marathe P,Rodrigues AD,Zhu M

更新日期：2019-09-03 00:00:00

abstract：:The rapid absorptive clearance of drugs delivered to the airways of the lungs means that many inhaled medicines have a short duration of action. The aim of this study was to investigate whether forming polar ion-pairs can modify drug absorption to slow down clearance from the airways. Salbutamol was used as a model dr...

journal_title：Molecular pharmaceutics

authors： Dutton B,Woods A,Sadler R,Prime D,Barlow DJ,Forbes B,Jones SA

更新日期：2020-05-04 00:00:00

abstract：:Erythropoietin (EPO), a hematopoietic growth factor and a promising therapy for Alzheimer's disease, has low permeability across the blood-brain barrier. The transferrin receptor antibody fused to EPO (TfRMAb-EPO) is a chimeric monoclonal antibody that ferries EPO into the brain via the transvascular route. However, T...

journal_title：Molecular pharmaceutics

authors： Yang J,Sun J,Castellanos DM,Pardridge WM,Sumbria RK

更新日期：2020-08-03 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：:L cells have attracted particular interest because of the pleiotropic effects of their secreted peptides (i.e., glucagon-like peptide (GLP) 1 and 2, peptide YY (PYY)). L cells express different G-protein-coupled receptors (GPCRs) that can be activated by endogenous ligands found in the gut lumen. We herein hypothesize...

journal_title：Molecular pharmaceutics

authors： Beloqui A,Alhouayek M,Carradori D,Vanvarenberg K,Muccioli GG,Cani PD,Préat V

更新日期：2016-12-05 00:00:00

abstract：:The effect of a lipidated prodrug of mitomycin C (MLP) on the membrane of a pegylated liposome formulation (PL-MLP), also known as Promitil, was characterized through high-sensitivity differential scanning calorimetry (DSC) and cryo-TEM. The thermodynamic analysis demonstrated that MLP led to the formation of heteroge...

journal_title：Molecular pharmaceutics

authors： Wei X,Patil Y,Ohana P,Amitay Y,Shmeeda H,Gabizon A,Barenholz Y

更新日期：2017-12-04 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：: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：:Dissolution is a crucial process for the oral delivery of drug products. Before being absorbed through epithelial cell membranes to reach the systemic circulation, drugs must first dissolve in the human gastrointestinal (GI) tract. In vivo and in vitro dissolutions are complex because of their dependency upon the drug...

journal_title：Molecular pharmaceutics

authors： Salehi N,Al-Gousous J,Mudie DM,Amidon GL,Ziff RM,Amidon GE

更新日期：2020-10-05 00:00:00

abstract：:Oncolytic adenoviruses rank among the most promising innovative agents in cancer therapy. We examined the potential of boosting the efficacy of the oncolytic adenovirus dl520 by associating it with magnetic nanoparticles and magnetic-field-guided infection in multidrug-resistant (MDR) cancer cells in vitro and upon in...

journal_title：Molecular pharmaceutics

authors： Tresilwised N,Pithayanukul P,Mykhaylyk O,Holm PS,Holzmüller R,Anton M,Thalhammer S,Adigüzel D,Döblinger M,Plank C

更新日期：2010-08-02 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：:Novel multivalent copper(II)-conjugated phosphorus dendrimers and their corresponding mononuclear copper(II) complexes were synthesized, characterized, and screened for antiproliferative activity against human cancer cell lines. Selected copper ligands were grafted on the surface of phosphorus dendrimers of generation...

journal_title：Molecular pharmaceutics

authors： El Brahmi N,El Kazzouli S,Mignani SM,Essassi el M,Aubert G,Laurent R,Caminade AM,Bousmina MM,Cresteil T,Majoral JP

更新日期：2013-04-01 00:00:00

abstract：:The present study explores the potential of polyelectrolyte-coated liposomes for improving the oral deliverability of doxorubicin (Dox). As a part of formulation strategy, stearyl amine was selected as a formulation component to provide positive charge to liposomes, which were subsequently coated with anionic poly(acr...

journal_title：Molecular pharmaceutics

authors： Jain S,Patil SR,Swarnakar NK,Agrawal AK

更新日期：2012-09-04 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：:For efficient and receptor-specific siRNA delivery, a new post-PEGylation strategy was established to provide siRNA polyplexes with targeting and shielding agents. For this purpose, core nanoparticles were formed by complexing siRNA with sequence-defined cationic lipo-oligomers. The T-shaped bis-oleoyl-oligoethanamino...

journal_title：Molecular pharmaceutics

authors： Müller K,Kessel E,Klein PM,Höhn M,Wagner E

更新日期：2016-07-05 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：: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：:Recent progress in peptide synthesis simplified the synthesis of multiple N-methylation of peptides. To evaluate how multiple N-methylation affects the bioavailability of peptides, a poly alanine cyclic hexapeptide library (n = 54), varying in the number of N-methyl (N-Me) groups (1-5 groups) and their position, was s...

journal_title：Molecular pharmaceutics

authors： Ovadia O,Greenberg S,Chatterjee J,Laufer B,Opperer F,Kessler H,Gilon C,Hoffman A

更新日期：2011-04-04 00:00:00

abstract：:The rate and extent of drug dissolution and absorption from solid oral dosage forms is highly dependent on the volume of liquid in the gastrointestinal tract (GIT). However, little is known about the time course of GIT liquid volumes after drinking a glass of water (8 oz), particularly in the colon, which is a targete...

journal_title：Molecular pharmaceutics

authors： Murray K,Hoad CL,Mudie DM,Wright J,Heissam K,Abrehart N,Pritchard SE,Al Atwah S,Gowland PA,Garnett MC,Amidon GE,Spiller RC,Amidon GL,Marciani L

更新日期：2017-08-07 00:00:00

abstract：:This study aims to investigate the crystallization behavior and molecular dynamics of amorphous griseofulvin (GSF) in the presence of low-concentration poly(ethylene oxide) (PEO). We observe that the addition of 3% w/w PEO remarkably increases the crystal growth rate of GSF by two orders of magnitude in both the super...

journal_title：Molecular pharmaceutics

authors： Shi Q,Zhang C,Su Y,Zhang J,Zhou D,Cai T

更新日期：2017-07-03 00:00:00

abstract：:In this study, transferrin (Tf)-modified poly(ethylene glycol)-phosphatidylethanolamine (mPEG-PE) micelles loaded with the poorly water-soluble drug, R547 (a potent and selective ATP-competitive cyclin-dependent kinase (CDK) inhibitor), were prepared and evaluated for their targeting efficiency and cytotoxicity in vit...

journal_title：Molecular pharmaceutics

authors： Sawant RR,Jhaveri AM,Koshkaryev A,Zhu L,Qureshi F,Torchilin VP

更新日期：2014-02-03 00:00:00

abstract：:Most anticancer drugs are poorly soluble and nonspecific, which restricts their clinical application. Drug conjugates, as a prodrug strategy, provide the possibility to overcome these shortcomings, especially combined with nanotechnology. Drug conjugate nanoparticles possess the advantages of high drug loading capacit...

journal_title：Molecular pharmaceutics

authors： Song Q,Wang X,Wang Y,Liang Y,Zhou Y,Song X,He B,Zhang H,Dai W,Wang X,Zhang Q

更新日期：2016-01-04 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：: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：:Polymeric nanoparticles (NPs) are extremely attractive vaccine adjuvants, able to promote antigen delivery and in some instances, exert intrinsic immunostimulatory properties that enhance antigen specific humoral and cellular immune responses. The poly-ε-caprolactone (PCL)/chitosan NPs were designed with the aim of be...

journal_title：Molecular pharmaceutics

authors： Jesus S,Soares E,Borchard G,Borges O

更新日期：2018-01-02 00:00:00