Mechanistic studies of a peptidic GRP78 ligand for cancer cell-specific drug delivery.

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：: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：:Supersaturable active pharmaceutical ingredients (sAPI), such as salts, cocrystals, and amorphous solids, can form supersaturated solutions after dissolving in the gastrointestinal fluids. However, there are cases in which supersaturation is not observed in an in vitro nonsink dissolution test. The purpose of the pres...

journal_title：Molecular pharmaceutics

authors： Oki J,Watanabe D,Uekusa T,Sugano K

更新日期：2019-04-01 00:00:00

abstract：:Bioadhesive nanoparticles based on poly(vinyl methyl ether/maleic anhydride) (PVMMA) and poly(ethylene glycol) methyl ether-b-poly(d,l-lactic acid) (mPEG-b-PLA) were produced by the emulsification solvent evaporation method. Paclitaxel was utilized as the model drug, with an encapsulation efficiency of up to 90.2 ± 4....

journal_title：Molecular pharmaceutics

authors： Wang Q,Li C,Ren T,Chen S,Ye X,Guo H,He H,Zhang Y,Yin T,Liang XJ,Tang X

更新日期：2017-10-02 00:00:00

abstract：:Cold crystallization of amorphous pharmaceuticals is an important aspect in the search to stabilize amorphous or glassy compounds used as amorphous pharmaceutical ingredients (APIs). In the present work, we report results for the isothermal crystallization of the compound GDC-0276 based on differential scanning calori...

journal_title：Molecular pharmaceutics

authors： Cheng S,Chakravarty P,Nagapudi K,McKenna GB

更新日期：2021-01-04 00:00:00

abstract：:The present work reports a thorough conformational analysis of iodinated contrast media: iomeprol, iopamidol (the world's most utilized contrast agent), and iopromide. Its main aim is the understanding of the complex structural features of these atropisomeric molecules, characterized by the presence of many conformers...

journal_title：Molecular pharmaceutics

authors： Fontanive L,D'Amelio N,Cesàro A,Gamini A,Tavagnacco L,Paolantoni M,Brady JW,Maiocchi A,Uggeri F

更新日期：2015-06-01 00:00:00

abstract：:Aerosol glucocorticoid medications have become more and more important in treating BA (bronchial asthma). Although these agents are dosed to directly target airway inflammation, adrenocortical suppression and other systematic effects are still seen. To tackle this problem in a novel way, two L-carnitine ester derivati...

journal_title：Molecular pharmaceutics

authors： Mo JX,Shi SJ,Zhang Q,Gong T,Sun X,Zhang ZR

更新日期：2011-10-03 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：: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：:Amorphous solid dispersions (ASD) of a poorly soluble water-soluble VR1 antagonist (AMG 517) were explored for improving physical stability and in vivo exposure. AMG 517 was incorporated at 15 or 50 wt % into polymeric microparticles of hydroxypropyl methylcellulose acetate succinate (HPMCAS) and hydroxypropyl methylc...

journal_title：Molecular pharmaceutics

authors： Kennedy M,Hu J,Gao P,Li L,Ali-Reynolds A,Chal B,Gupta V,Ma C,Mahajan N,Akrami A,Surapaneni S

更新日期：2008-11-01 00:00:00

abstract：:Nucleic acid biopharmaceuticals are being investigated as potential therapeutics. They need to be incorporated into a biocompatible carrier so as to overcome several biological barriers. Rational development of suitable nanocarriers requires high-quality characterization techniques. While size, concentration, and stab...

journal_title：Molecular pharmaceutics

authors： Zagato E,Vermeulen L,Dewitte H,Van Imschoot G,Vandenbroucke RE,Demeester J,De Smedt SC,Neyts K,Remaut K,Braeckmans K

更新日期：2018-03-05 00:00:00

abstract：:Understanding in vivo drug release kinetics is critical for the development of nanoparticle-based delivery systems. In this study, we developed a fluorescence resonance energy transfer (FRET) imaging approach to noninvasively monitor in vitro and in vivo cargo release from polymeric nanoparticles. The FRET donor dye (...

journal_title：Molecular pharmaceutics

authors： Zou P,Chen H,Paholak HJ,Sun D

更新日期：2013-11-04 00:00:00

abstract：:It is highly demanded and still a big challenge to develop an effective formulation for immunochemotherapy against advanced tumors. We have previously reported a PEG-NLG-based immunostimulatory nanocarrier (PEG2k-Fmoc-NLG919) for co-delivery of an IDO1 inhibitor (NLG919) and a chemotherapeutic agent (paclitaxel, PTX)....

journal_title：Molecular pharmaceutics

authors： Chen Y,Sun J,Huang Y,Lu B,Li S

更新日期：2018-11-05 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：:A number of folate-based radioconjugates have been synthesized and evaluated for nuclear imaging purposes of folate receptor (FR)-positive tumors and potential therapeutic application. A common shortcoming of radiofolates is, however, a significant accumulation of radioactivity in the kidneys. This situation has been ...

journal_title：Molecular pharmaceutics

authors： Farkas R,Siwowska K,Ametamey SM,Schibli R,van der Meulen NP,Müller C

更新日期：2016-06-06 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：:Constitutive activation of signal transducer and activator of transcription 3 (STAT3) in tumor cells and tumor associated dendritic cells (DCs) plays a major role in the progression of cancer. JSI-124 (cucurbitacin I) is a potent inhibitor of STAT3; however, its poor solubility and nonspecificity limit its effectivene...

journal_title：Molecular pharmaceutics

authors： Garg SM,Vakili MR,Molavi O,Lavasanifar A

更新日期：2017-08-07 00:00:00

abstract：:We report herein on the preparation of thermoresponsive hydrogels by taking advantage of the interaction of cyclodextrins (CDs) and a hydrophobically modified polymer. A hydrophobically modified hydroxypropyl methylcellulose (HM-HPMC) gel formed thermoresponsive hydrogels when small amounts of α-CD were added to the s...

journal_title：Molecular pharmaceutics

authors： Iohara D,Okubo M,Anraku M,Uramatsu S,Shimamoto T,Uekama K,Hirayama F

更新日期：2017-08-07 00:00:00

abstract：:Amorphous solids and crystalline salts are both of interest as a means of improving the dissolution characteristics and apparent solubility of poorly water soluble active pharmaceutical ingredients which have low bioavailability in humans. The theory and selection of both crystalline drug substance salt forms and amor...

journal_title：Molecular pharmaceutics

authors： Towler CS,Li T,Wikström H,Remick DM,Sanchez-Felix MV,Taylor LS

更新日期：2008-11-01 00:00:00

abstract：:The 1:1 cocrystal of the antifungal agent ketoconazole with p-aminobenzoic acid was successfully crystallized and systematically characterized by a physical and pharmacological point of view. Crystal structure determination confirmed the cocrystal identity, giving full insight in its crystal packing and degree of diso...

journal_title：Molecular pharmaceutics

authors： Martin F,Pop M,Kacso I,Grosu IG,Miclăuş M,Vodnar D,Lung I,Filip GA,Olteanu ED,Moldovan R,Nagy A,Filip X,Bâldea I

更新日期：2020-03-02 00:00:00

abstract：:Porous silicon microparticles presenting pathogen-associated molecular patterns mimic pathogens, enhancing internalization of the microparticles and activation of antigen presenting dendritic cells. We demonstrate abundant uptake of microparticles bound by the TLR-4 ligands LPS and MPL by murine bone marrow-derived de...

journal_title：Molecular pharmaceutics

authors： Meraz IM,Melendez B,Gu J,Wong ST,Liu X,Andersson HA,Serda RE

更新日期：2012-07-02 00:00:00

abstract：:Molecular imaging of programmed cell death (apoptosis) in vivo is an innovative strategy for early assessment of treatment response and treatment efficacy in cancer patients. Externalization of phosphatidylserine (PS) to the cell membrane surface of dying cells makes this phospholipid an attractive molecular target fo...

journal_title：Molecular pharmaceutics

authors： Perreault A,Richter S,Bergman C,Wuest M,Wuest F

更新日期：2016-10-03 00:00:00

abstract：:Amphotericin B (AmB) loaded polymer lipid hybrid nanoparticles (AmB-PLNs) comprised of lecithin (anionic lipid) and gelatin (Type A, cationic below its isoelectric point 7.0-9.0) were prepared by a two-step desolvation method to improve the oral bioavailability of AmB. The optimized AmB-PLNs were found to have particl...

journal_title：Molecular pharmaceutics

authors： Jain S,Valvi PU,Swarnakar NK,Thanki K

更新日期：2012-09-04 00:00:00

abstract：:Targeted gene delivery using nonviral vectors is a highly touted scheme to reduce the potential for toxic or immunological side effects by reducing dose. In previous reports, TAT polyplexes with DNA have shown relatively poor gene delivery. The transfection efficiency has been enhanced by condensing TAT/DNA complexes ...

journal_title：Molecular pharmaceutics

authors： Khondee S,Baoum A,Siahaan TJ,Berkland C

更新日期：2011-06-06 00:00:00

abstract：:Drug repositioning is an important drug development strategy as it saves the time and efforts exerted in drug discovery. Since reepithelization of the cornea is a critical problem, we envisioned that the anticonvulsant phenytoin sodium can promote reepithelization of corneal ulcers as it was repurposed for skin wound ...

journal_title：Molecular pharmaceutics

authors： Mahmoud DB,Afifi SA,El Sayed NS

更新日期：2020-10-05 00:00:00

abstract：:In developing targeted probes for positron emission tomography (PET) based on (64)Cu, stable complexation of the radiometal is key, and a flexible handle for bioconjugation is highly advantageous. Here, we present the synthesis and characterization of the chelator pycup and four derivatives. Pycup is a cross-bridged c...

journal_title：Molecular pharmaceutics

authors： Boros E,Rybak-Akimova E,Holland JP,Rietz T,Rotile N,Blasi F,Day H,Latifi R,Caravan P

更新日期：2014-02-03 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：:Hyperbilirubinemia may arise due to inadequate clearance of bilirubin from the body. Bilirubin elimination is a multifaceted process consisting of uptake of bilirubin into the hepatocytes facilitated by OATP1B1 and OATP1B3. Once in the hepatocytes, it is extensively glucuronidated by UGT1A1. Eventually, the glucuronid...

journal_title：Molecular pharmaceutics

authors： Chang JH,Plise E,Cheong J,Ho Q,Lin M

更新日期：2013-08-05 00:00:00

abstract：:Dry powders from aqueous dispersions, formed by antisolvent precipitation, dissolved to form solutions with supersaturation values up to 12 in 10 min at pH 6.8 with sodium dodecyl sulfate micelles. Itraconazole/hydroxypropylmethylcellulose (HPMC) aqueous particle dispersions were salt flocculated and filtered to produ...

journal_title：Molecular pharmaceutics

authors： Matteucci ME,Paguio JC,Miller MA,Williams RO 3rd,Johnston KP

更新日期：2009-03-01 00:00:00

abstract：:In vivo peptide inhibition of tumor suppressor p53 binding to the protein MDM2 is hampered by inefficient delivery of the peptide. Our approach to couple a hydrophobic lipid-like tail on the inhibitory peptide p53(14-29) allowed its intracellular delivery in vitro, in a panel of different cell lines. The constructed c...

journal_title：Molecular pharmaceutics

authors： Missirlis D,Krogstad DV,Tirrell M

更新日期：2010-12-06 00:00:00