Physicochemical characterization of molecular assemblies of miltefosine and amphotericin B.

abstract：:Rodent models are less suitable for predicting drug-drug interactions at the level of the human intestinal mucosa, especially when nuclear receptors such as pregnane X receptor (PXR) are involved. Recently, a transgenic mouse model, expressing both human PXR and CYP3A4, was developed and shown to be a better predictor...

journal_title：Molecular pharmaceutics

authors： Holmstock N,Gonzalez FJ,Baes M,Annaert P,Augustijns P

更新日期：2013-03-04 00:00:00

abstract：:Active targeting of nanostructures containing chemotherapeutic agents can improve cancer treatment. Here, a three-way junction pocket DNA nanostructure was developed for efficient doxorubicin (Dox) delivery into cancer cells. The three-way junction pocket DNA nanostructure is composed of three strands of AS1411 aptame...

journal_title：Molecular pharmaceutics

authors： Taghdisi SM,Danesh NM,Ramezani M,Yazdian-Robati R,Abnous K

更新日期：2018-05-07 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：: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：:sec-Butylpropylacetamide (SPD) is the amide derivative of valproic acid (VPA). SPD possess a wide-spectrum anticonvulsant profile better than that of VPA and blocks status epilepticus (SE) induced by pilocarpine and organophosphates. The activity of SPD on SE is better than that of benzodiazepines (BZDs) in terms of t...

journal_title：Molecular pharmaceutics

authors： Mawasi H,Bibi D,Shekh-Ahmad T,Shaul C,Blotnik S,Bialer M

更新日期：2016-07-05 00:00:00

abstract：:Fexofenadine is a nonsedative antihistamine that exhibits good oral bioavailability despite its zwitterionic chemical structure and efflux by P-gp. Evidence exists that multiple uptake and efflux transporters play a role in hepatic disposition of fexofenadine. However, the roles of specific transporters and their inte...

journal_title：Molecular pharmaceutics

authors： Ming X,Knight BM,Thakker DR

更新日期：2011-10-03 00:00:00

abstract：:A general, easy-to-implement strategy for mapping the structure of organic phases integrated in mesoporous silica drug delivery devices is presented. The approach based on a few straightforward solid-state NMR techniques has no limitations regarding concentrations of the active compounds and enables straightforward di...

journal_title：Molecular pharmaceutics

authors： Brus J,Albrecht W,Lehmann F,Geier J,Czernek J,Urbanova M,Kobera L,Jegorov A

更新日期：2017-06-05 00:00:00

abstract：:The thermal unfolding and subsequent aggregation of the unglycosylated Fc fragment of a human IgG1 antibody (Fc) were studied in the salt solutions of Na(2)SO(4), KF, KCl and KSCN at pH 4.8 and 7.2 below and at its pI of 7.2, respectively, using differential scanning calorimetry (DSC), far ultraviolet circular dichroi...

journal_title：Molecular pharmaceutics

authors： Zhang-van Enk J,Mason BD,Yu L,Zhang L,Hamouda W,Huang G,Liu D,Remmele RL Jr,Zhang J

更新日期：2013-02-04 00:00:00

abstract：:We have identified and characterized a new solid form of trehalose, the δ form (Tδ) using (13)C solid-state NMR spectroscopy (SSNMR). Tδ is formed from dehydrations of trehalose dihydrate (T(h)) performed at or below 100 °C, and it is generated concurrently with the α form of trehalose (Tα) and amorphous trehalose (T(...

journal_title：Molecular pharmaceutics

authors： Pyszczynski SJ,Munson EJ

更新日期：2013-09-03 00:00:00

abstract：:This study describes a novel nonlinear variant of the well-known Yalkowsky general solubility equation (GSE). The modified equation can be trained with small molecules, mostly from the Lipinski Rule of 5 (Ro5) chemical space, to predict the intrinsic aqueous solubility, S0, of large molecules (MW > 800 Da) from beyond...

journal_title：Molecular pharmaceutics

authors： Avdeef A,Kansy M

更新日期：2020-10-05 00:00:00

abstract：:Current chemotherapy strategies for second-line treatment of relapsed ovarian cancer are unable to effectively treat residual disease post-cytoreduction. The findings presented herein suggest that tissue penetration of drug is not only an issue for large, unresectable tumors, but also for invisible, microscopic lesion...

journal_title：Molecular pharmaceutics

authors： Eetezadi S,De Souza R,Vythilingam M,Lessa Cataldi R,Allen C

更新日期：2015-11-02 00:00:00

abstract：:While highly efficacious in treating rheumatoid arthritis (RA), the approved Janus kinase (JAK) inhibitor, Tofacitinib (Tofa, CP-690 550), has dose-dependent toxicities that limit its clinical application. In this study, we have examined whether a prodrug design that targets arthritic joints would enhance Tofa's thera...

journal_title：Molecular pharmaceutics

authors： Wei X,Wu J,Zhao G,Galdamez J,Lele SM,Wang X,Liu Y,Soni DM,Purdue PE,Mikuls TR,Goldring SR,Wang D

更新日期：2018-08-06 00:00:00

abstract：:We investigated the feasibility and efficacy of a drug delivery strategy to vascularized cancer that combines targeting selectivity with high uptake by targeted cells and high bioexposure of cells to delivered chemotherapeutics. Targeted lipid vesicles composed of pH responsive membranes were designed to reversibly fo...

journal_title：Molecular pharmaceutics

authors： Bandekar A,Zhu C,Gomez A,Menzenski MZ,Sempkowski M,Sofou S

更新日期：2013-01-07 00:00:00

abstract：:Development of an effective and potent RNA delivery system remains a challenge for the clinical application of RNA therapeutics. Herein, we describe the development of an RNA delivery platform derived from self-assembled bicontinuous cubic lyotropic liquid crystalline phases, functionalized with zinc coordinated lipid...

journal_title：Molecular pharmaceutics

authors： Tajik-Ahmadabad B,Chollet L,White J,Separovic F,Polyzos A

更新日期：2019-03-04 00:00:00

abstract：:The acetylcholinesterase inhibitor, acotiamide, improves gastric motility and is clinically used to treat functional dyspepsia. The present study aimed to identify the transporters involved in the distribution of acotiamide in stomach tissue. Acotiamide uptake by the gastric cancer-derived model cell line, Hs746 T, wa...

journal_title：Molecular pharmaceutics

authors： Hirayama M,Hoshino Y,Yoshii K,Toda R,Kawabata Y,Nakanishi T,Tamai I

更新日期：2020-04-06 00:00:00

abstract：:Within the immune system there is an exquisite ability to discriminate between "self" and "non-self" that is orchestrated by antigen-specific T lymphocytes. Genomic plasticity enables differentiation of naive CD4+ T lymphocytes into either regulatory cells (Treg) that express the transcription factor Foxp3 and activel...

journal_title：Molecular pharmaceutics

authors： Park J,Gao W,Whiston R,Strom TB,Metcalfe S,Fahmy TM

更新日期：2011-02-07 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) can inhibit cell growth and metastasis, and induce cell apoptosis in cancerous cells. They have been shown to reduce incidence and mortality of gastric cancer by an unknown mechanism. NSAIDs often exert their effects by Cox-2 inhibition, and Cox-2 is overexpressed in gastr...

journal_title：Molecular pharmaceutics

authors： Jin H,Wang Z,Liu L,Gao L,Sun L,Li X,Zhao H,Pan Y,Shi H,Liu N,Hong L,Liang J,Wu Q,Yang Z,Wu K,Fan D

更新日期：2010-02-01 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：:A big hurdle for the use of protein-based drugs is that they are easily degraded by proteases in the human body. In an attempt to solve this problem, we show the possibility to functionalize TM encapsulin nanoparticles with an mEETI-II knottin miniprotein from the cysteine-stabilized knot class. The resulting particle...

journal_title：Molecular pharmaceutics

authors： Klem R,de Ruiter MV,Cornelissen JJLM

更新日期：2018-08-06 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：:High-functionality and -quality (HFQ) lipids have a discrete molecular weight and good water dispersibility and can be produced by solid-phase peptide synthesis. Therefore, HFQ lipids are a promising material for the preparation of ligand-grafted PEGylated liposomes. Recently, we have reported serine-glycine repeated ...

journal_title：Molecular pharmaceutics

authors： Suga T,Kato N,Hagimori M,Fuchigami Y,Kuroda N,Kodama Y,Sasaki H,Kawakami S

更新日期：2018-10-01 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：:Bacterial capsular polysaccharides are components of many modern vaccines, but they are weakly immunogenic. Herein, we describe the delivery of pneumococcal capsular polysaccharide serotype-1 (PCP-1) in polylactide polymeric particles to enhance its immunogenicity. Immunization with PCP-1-entrapped particles elicited ...

journal_title：Molecular pharmaceutics

authors： Anish C,Khan N,Upadhyay AK,Sehgal D,Panda AK

更新日期：2014-03-03 00:00:00

abstract：:There is a great need for delivery strategies capable of efficiently localizing drugs to the damaged myocardium that do not require direct intramyocardial injection of therapeutic molecules. In the work discussed here, we exploited the myocardium-specific upregulation of matrix metalloproteinases (MMPs) that occurs du...

journal_title：Molecular pharmaceutics

authors： Nguyen J,Sievers R,Motion JP,Kivimäe S,Fang Q,Lee RJ

更新日期：2015-04-06 00:00:00

abstract：:In this study, dinitrosyl iron complexes (DNICs) are shown to deliver nitric oxide (NO) into the cytosol of vascular smooth muscle cells (SMCs), which play a major role in vascular relaxation and contraction. Malfunction of SMCs can lead to hypertension, asthma, and erectile dysfunction, among other disorders. For com...

journal_title：Molecular pharmaceutics

authors： Pectol DC,Khan S,Chupik RB,Elsabahy M,Wooley KL,Darensbourg MY,Lim SM

更新日期：2019-07-01 00:00:00

abstract：:Mouse laser-induced choroidal neovascularization (mouse LCNV) recapitulates the "wet" form of human age-related macular degeneration (AMD). Vascular cell adhesion molecule-1 (VCAM-1) is a known inflammatory biomarker, and it increases in the choroidal neovascular tissues characteristic of this experimental model. We h...

journal_title：Molecular pharmaceutics

authors： Uddin MI,Kilburn TC,Yang R,McCollum GW,Wright DW,Penn JS

更新日期：2018-12-03 00:00:00

abstract：:Lipoplexes, composed of Lipofectamine and mRNA encoding HIV Gag protein, were shown to be internalized by dendritic cells (DCs) and promote antigen presentation to stimulate HIV-specific T cell responses. Using confocal microscopy, we showed that one-third of fluorescently labeled mRNA containing lipoplexes are coloca...

journal_title：Molecular pharmaceutics

authors： De Haes W,Van Mol G,Merlin C,De Smedt SC,Vanham G,Rejman J

更新日期：2012-10-01 00:00:00

abstract：:Our previous studies have shown that multidrug resistance protein 2 (MRP2) is overexpressed in tamoxifen-resistant MCF-7 breast cancer cells (TAMR-MCF-7 cells) and forkhead box-containing protein, O subfamily1 (FoxO1), functions as a key regulator of multidrug resistance 1 (MDR1) gene transcription. This study aimed t...

journal_title：Molecular pharmaceutics

authors： Choi HK,Cho KB,Phuong NT,Han CY,Han HK,Hien TT,Choi HS,Kang KW

更新日期：2013-07-01 00:00:00

abstract：:Lipid nanoemulsions are being investigated for the parenteral administration of poorly soluble drugs. A narrow particle size distribution in these formulations is a prerequisite for meaningful research and safe administration to patients. Autoclaving a poloxamer-stabilized trimyristin nanoemulsion resulted in moderate...

journal_title：Molecular pharmaceutics

authors： Göke K,Roese E,Bunjes H

更新日期：2018-08-06 00:00:00

abstract：:Targeted therapies are emerging as a preferred strategy for treatment of cancer and other diseases. To evaluate the effect of high affinity receptors on the rate and extent of tumor penetration of receptor-targeted drugs, we have characterized the kinetics of folate-rhodamine uptake by folate receptor (FR)-expressing ...

journal_title：Molecular pharmaceutics

authors： Vlashi E,Sturgis JE,Thomas M,Low PS

更新日期：2009-11-01 00:00:00