Vitamin E Succinate-Grafted-Chitosan Oligosaccharide/RGD-Conjugated TPGS Mixed Micelles Loaded with Paclitaxel for U87MG Tumor Therapy.

abstract：:Hydrophilic matrices are an effective option for oral controlled release but can face challenges in terms of bioavailability and efficacy when used in conjunction with poorly soluble, weakly basic drugs. Attenuated total reflectance Fourier transform infrared (ATR-FTIR) imaging provides dynamic information relating to...

journal_title：Molecular pharmaceutics

authors： Zahoor FD,Mader KT,Timmins P,Brown J,Sammon C

更新日期：2020-04-06 00:00:00

abstract：:The transfection activity and the phase behavior of two novel cationic O-alkyl-phosphatidylcholines, 1,2-dioleoyl- sn-glycero-3-hexylphosphocholine (C6-DOPC) and 1,2-dierucoyl- sn-glycero-3-ethylphosphocholine (di22:1-EPC), have been examined with the aim of more completely understanding the mechanism of lipid-mediate...

journal_title：Molecular pharmaceutics

authors： Koynova R,Wang L,Macdonald RC

更新日期：2008-09-01 00:00:00

abstract：:A wide variety of chemotherapy and radiotherapy agents are available for treating cancer, but a critical challenge is to deliver these agents locally to cancer cells and tumors while minimizing side effects from systemic delivery. Nanomedicine uses nanoparticles with diameters in the range of ∼1-100 nm to encapsulate ...

journal_title：Molecular pharmaceutics

authors： Moore T,Chen H,Morrison R,Wang F,Anker JN,Alexis F

更新日期：2014-01-06 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：: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：:p53 is a key tumor suppressor gene involved in key cellular processes and implicated in cancer therapy. However, it is inactivated in more than 50% of all cancers due to mutation or overexpression of its negative regulators. This leads to drug resistance and poor chemotherapeutic outcome as most clinical drugs act via...

journal_title：Molecular pharmaceutics

authors： Chow MJ,Babak MV,Wong DY,Pastorin G,Gaiddon C,Ang WH

更新日期：2016-07-05 00:00:00

abstract：:Formulation of a cocrystal into a solid pharmaceutical dosage form entails numerous processing steps during which there is risk of dissociation. In an effort to reduce the number of unit operations, we have attempted the in situ formation of an indomethacin-saccharin (INDSAC) cocrystal during high-shear wet granulatio...

journal_title：Molecular pharmaceutics

authors： Tanaka R,Duggirala NK,Hattori Y,Otsuka M,Suryanarayanan R

更新日期：2020-01-06 00:00:00

abstract：:Currently, the screening of new drug candidates for intestinal permeation is typically based on in vitro models which give no information regarding regional differences along the gut. When evaluation of intestinal permeability by region is undertaken, two preclinical rat models are commonly used, the Ussing chamber me...

journal_title：Molecular pharmaceutics

authors： Roos C,Dahlgren D,Sjögren E,Tannergren C,Abrahamsson B,Lennernäs H

更新日期：2017-12-04 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：: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：:Solubility limited compounds require enabling formulations such as amorphous solid dispersions (ASDs) to increase the apparent solubility by dissolving to a concentration higher than the equilibrium solubility of the drug. This may lead to subsequent precipitation and thus the loss of the solubility advantage. Althoug...

journal_title：Molecular pharmaceutics

authors： Han YR,Lee PI

更新日期：2017-01-03 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：:Iron oxide nanoparticles have great potential as diagnostic and therapeutic agents in cancer and other diseases; however, biological aggregation severely limits their function in vivo. Aggregates can cause poor biodistribution, reduced heating capability, and can confound their visualization and quantification by magn...

journal_title：Molecular pharmaceutics

authors： Hurley KR,Ring HL,Etheridge M,Zhang J,Gao Z,Shao Q,Klein ND,Szlag VM,Chung C,Reineke TM,Garwood M,Bischof JC,Haynes CL

更新日期：2016-07-05 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：:In this work, we have developed covalent and low molecular weight docetaxel delivery systems based on conjugation with N-acetyl-d-galactosamine and studied their properties related to hepatocellular carcinoma cells. The resulting glycoconjugates have an excellent affinity to the asialoglycoprotein receptor (ASGPR) in ...

journal_title：Molecular pharmaceutics

authors： Petrov RA,Mefedova SR,Yamansarov EY,Maklakova SY,Grishin DA,Lopatukhina EV,Burenina OY,Lopukhov AV,Kovalev SV,Timchenko YV,Ondar EE,Ivanenkov YA,Evteev SA,Vaneev AN,Timoshenko RV,Klyachko NL,Erofeev AS,Gorelkin PV,Bel

更新日期：2021-01-04 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

abstract：:Metastatic breast cancer is incurable. The goal of this study was to develop a positron emission tomography (PET)/near-infrared fluorescent (NIRF) probe for imaging CD105 expression in breast cancer experimental lung metastasis. TRC105, a chimeric anti-CD105 antibody, was dual-labeled with a NIRF dye (IRDye 800CW) and...

journal_title：Molecular pharmaceutics

authors： Hong H,Zhang Y,Severin GW,Yang Y,Engle JW,Niu G,Nickles RJ,Chen X,Leigh BR,Barnhart TE,Cai W

更新日期：2012-08-06 00:00:00

abstract：:It is a challenge to formulate polymer based nanoparticles of therapeutic proteins as excipients and process conditions affect stability and structural integrity of the protein. Hence, understanding the protein stability and complex aggregation phenomena is an important area of research in therapeutic protein delivery...

journal_title：Molecular pharmaceutics

authors： Rawat S,Gupta P,Kumar A,Garg P,Suri CR,Sahoo DK

更新日期：2015-04-06 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：:Here, we report the antiproliferative/cytotoxic properties of 8-hydroxyquinoline (8-HQ) derivatives on HeLa cells in the presence of transition metal ions (Cu(2+), Fe(3+), Co(2+), Ni(2+)). Two series of ligands were tested, the arylvinylquinolinic L1-L8 and the arylethylenequinolinic L9-L16, which can all interact wit...

journal_title：Molecular pharmaceutics

authors： Barilli A,Atzeri C,Bassanetti I,Ingoglia F,Dall'Asta V,Bussolati O,Maffini M,Mucchino C,Marchiò L

更新日期：2014-04-07 00:00:00

abstract：:Amphotericin B (AmB) is a lifesaving polyene antibiotic used widely to treat deep-seated mycoses. Both the pharmaceutical effectiveness as well as toxic side effects depend on molecular organization of the drug. In the present study, we analyzed steady-state fluorescence, fluorescence anisotropy spectra, fluorescence ...

journal_title：Molecular pharmaceutics

authors： Wasko P,Luchowski R,Tutaj K,Grudzinski W,Adamkiewicz P,Gruszecki WI

更新日期：2012-05-07 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：: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：: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：:Lipid-based drug delivery systems have been vastly investigated as a pharmaceutical method to enhance oral absorption of lipophilic drugs. However, these vehicles not only affect drug bioavailability but may also have an impact on gastric emptying, drug disposition, lymphatic absorption and be affected by lipid digest...

journal_title：Molecular pharmaceutics

authors： Izgelov D,Regev A,Domb AJ,Hoffman A

更新日期：2020-06-01 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：:Human epidermal growth factor receptor 2 (HER2) is a biomarker in breast cancer, and its overexpression is required to initiate therapies using HER2-targeted antibodies. Although trastuzumab is one of the most effective therapeutic antibodies in HER2-overexpressing breast cancer, a significant number of patients do no...

journal_title：Molecular pharmaceutics

authors： Pereira PMR,Ragupathi A,Shmuel S,Mandleywala K,Viola NT,Lewis JS

更新日期：2020-01-06 00:00:00

abstract：:Curcumin (CUR) is a unique natural compound with promising anticancer and anti-inflammatory activities. However, the therapeutic efficacy of curcumin was challenged in clinical trials, mostly due to its low bioavailability, rapid metabolism, and elimination. We designed a nanodrug form of curcumin, which makes it stab...

journal_title：Molecular pharmaceutics

authors： Wei X,Senanayake TH,Bohling A,Vinogradov SV

更新日期：2014-09-02 00:00:00

abstract：:The synthesis and biodistribution of three triazine dendrimers differing in PEGylation are described. Dendrimers 1, 2, and 3 are derived from a common intermediate, dendrimer 4, and vary in molecular mass from 11 to 73 kDa as a result of PEGylation with multiple (theoretically, 16) PEG groups of 0.6, 2, and 5 kDa, res...

journal_title：Molecular pharmaceutics

authors： Lim J,Guo Y,Rostollan CL,Stanfield J,Hsieh JT,Sun X,Simanek EE

更新日期：2008-07-01 00:00:00

abstract：:In this work, we demonstrated that the simple substitution of the 1,2,4-triazole moiety in 5-( 4H-1,2,4-triazol-4-yl)isophthalic acid (5-TIA) by the 1 H-1,2,3-triazol-5-yl unit enables the preparation of a hydrogelator (click-TIA). In sharp contrast to 5-TIA, its isostere click-TIA undergoes self-assembly in water upo...

journal_title：Molecular pharmaceutics

authors： Häring M,Rodríguez-López J,Grijalvo S,Tautz M,Eritja R,Martín VS,Díaz Díaz D

更新日期：2018-08-06 00:00:00