Molecular mechanism of poly(vinyl alcohol) mediated prevention of aggregation and stabilization of insulin in nanoparticles.

abstract：:The drug-induced accumulation of phospholipids in lysosomes of various tissues is predominantly observed in regular repeat dose studies, often after prolonged exposure, and further investigated in mechanistic studies prior to candidate nomination. The finding can cause delays in the discovery process inflicting high c...

journal_title：Molecular pharmaceutics

authors： Fusani L,Brown M,Chen H,Ahlberg E,Noeske T

更新日期：2017-12-04 00:00:00

abstract：:Lipid-based nanoparticles are considered as promising candidates for delivering siRNA into the cytoplasm of targeted cells. However, in vivo efficiency of these nanoparticles is critically dependent on formulation strategies of lipid-siRNA complexes. Adsorption of serum proteins to lipid-siRNA complexes and its charge...

journal_title：Molecular pharmaceutics

authors： Dar GH,Gopal V,Rao NM

更新日期：2015-02-02 00:00:00

abstract：:HEPES has been widely employed as an organic buffer agent in cell culture medium as well as uptake and transport experiments in vitro. However, concentrations of HEPES used in such studies vary from one laboratory to another. In this study, we investigated the effect of HEPES on the uptake and bidirectional transport ...

journal_title：Molecular pharmaceutics

authors： Luo S,Pal D,Shah SJ,Kwatra D,Paturi KD,Mitra AK

更新日期：2010-04-05 00:00:00

abstract：:Poly(ethylcyanoacrylate) (PECA) nanoparticles containing the bioactive d-Lys(6)-GnRH were manufactured by an in situ interfacial polymerization process using a w/o-microemulsion template containing the peptide in the dispersed aqueous pseudophase of the microemulsion. Polymeric nanoparticles were characterized using P...

journal_title：Molecular pharmaceutics

authors： Kafka AP,Kleffmann T,Rades T,McDowell A

更新日期：2009-09-01 00:00:00

abstract：:Microcrystalline vinpocetine, coground with cross-linked polyvinylpyrrolidone, affords hybrids containing nanosized drug nanocrystals, the size and size distributions of which depend on milling times and drug-to-polymer weight ratios. Using an innovative approach to microstructural characterization, we analyzed wide-a...

journal_title：Molecular pharmaceutics

authors： Hasa D,Giacobbe C,Perissutti B,Voinovich D,Grassi M,Cervellino A,Masciocchi N,Guagliardi A

更新日期：2016-09-06 00:00:00

abstract：:Cancer is a leading cause of death within developed nations, and part of this morbidity is due to difficulties associated with its treatment. Currently, anticancer therapy relies heavily upon the administration of small molecule cytotoxic drugs that attack both cancerous and noncancerous cells due to limited selectivi...

journal_title：Molecular pharmaceutics

authors： Kaminskas LM,McLeod VM,Porter CJ,Boyd BJ

更新日期：2012-03-05 00:00:00

abstract：:Novel strategy has been developed for fabricating the biocompatible reduction and pH dual-responsive core cross-linked (CCL) micelles as drug delivery system (DDS) for the controlled anticancer drug delivery, via the atom transfer radical polymerization (ATRP) of tert-butyl acrylate (tBA) with N,N'-bis(acryloyl)cystam...

journal_title：Molecular pharmaceutics

authors： Tian K,Jia X,Zhao X,Liu P

更新日期：2017-03-06 00:00:00

abstract：:Peripheral arterial disease (PAD) consists of a persistent obstruction of lower-extremity arteries further from the aortic bifurcation attributable to atherosclerosis. PAD is correlated with an elevated risk of morbidity and mortality as well as of deterioration of the quality of life with claudication and chronic leg...

journal_title：Molecular pharmaceutics

authors： Ferreira CA,Hernandez R,Yang Y,Valdovinos HF,Engle JW,Cai W

更新日期：2018-08-06 00:00:00

abstract：:The goal of this study was to develop a (66)Ga-based positron emission tomography (PET) tracer for noninvasive imaging of CD105 expression during tumor angiogenesis, a hallmark of cancer. (66)Ga was produced using a cyclotron with (nat)Zn or isotopically enriched (66)Zn targets. TRC105, a chimeric anti-CD105 monoclona...

journal_title：Molecular pharmaceutics

authors： Engle JW,Hong H,Zhang Y,Valdovinos HF,Myklejord DV,Barnhart TE,Theuer CP,Nickles RJ,Cai W

更新日期：2012-05-07 00:00:00

abstract：:To overcome the P-glycoprotein (P-gp)-induced multidrug resistance (MDR) of cancer cells, a novel copolymer, chitosan-graft-D-α-tocopheryl polyethylene glycol 1000 (TPGS) (CT) was synthesized for doxorubicin (DOX) delivery by the P-gp inhibiting virtue of TPGS. DOX-loaded CT nanoparticles (NPs) were fabricated by a mo...

journal_title：Molecular pharmaceutics

authors： Guo Y,Chu M,Tan S,Zhao S,Liu H,Otieno BO,Yang X,Xu C,Zhang Z

更新日期：2014-01-06 00:00:00

abstract：:2-Methoxyestradiol (2MeO-E2) is an endogenous metabolite of estrogen which was initially considered to be inactive. During the last few decades it has been shown that 2MeO-E2 is a promising anticancer drug. In vitro experiments have demonstrated that it has several anticancer activities, and potential to alleviate hyp...

journal_title：Molecular pharmaceutics

authors： Verenich S,Gerk PM

更新日期：2010-12-06 00:00:00

abstract：:The successful applicability of gene therapy approaches will heavily rely on the development of efficient and safe nonviral gene delivery vectors, for example, cell-penetrating peptides (CPPs). CPPs can condense oligonucleotides and plasmid DNA (pDNA) into nanoparticles, thus allowing the transfection of genetic mater...

journal_title：Molecular pharmaceutics

authors： Veiman KL,Mäger I,Ezzat K,Margus H,Lehto T,Langel K,Kurrikoff K,Arukuusk P,Suhorutšenko J,Padari K,Pooga M,Lehto T,Langel Ü

更新日期：2013-01-07 00:00:00

abstract：:Ultrasound-targeted microbubble destruction (UTMD) is a promising technique to facilitate the delivery of chemotherapy in cancer treatment. However, the process typically uses nonspecific microbubbles, leading to low tumor-to-normal tissue uptake ratio and adverse side effects. In this study, we synthesized the LHRH r...

journal_title：Molecular pharmaceutics

authors： Pu C,Chang S,Sun J,Zhu S,Liu H,Zhu Y,Wang Z,Xu RX

更新日期：2014-01-06 00:00:00

abstract：:The human organic anion-transporting polypeptides OATP1B1 (SLCO1B1) and OATP1B3 (SLCO1B3) are liver-enriched membrane transporters of major importance to hepatic uptake of numerous endogenous compounds, including bile acids, steroid conjugates, hormones, and drugs, including the 3-hydroxy-3-methylglutaryl Co-A reducta...

journal_title：Molecular pharmaceutics

authors： DeGorter MK,Ho RH,Leake BF,Tirona RG,Kim RB

更新日期：2012-04-02 00:00:00

abstract：:The pharmacological exploitation of resveratrol is hindered by rapid phase-II conjugative metabolism in enterocytes and hepatocytes. One approach to the solution of this problem relies on prodrugs. We report the synthesis and characterization as well as the assessment of in vivo absorption and metabolism of a set of p...

journal_title：Molecular pharmaceutics

authors： Mattarei A,Azzolini M,Carraro M,Sassi N,Zoratti M,Paradisi C,Biasutto L

更新日期：2013-07-01 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：:TGX-221 is a highly potent phosphoinositide 3-kinase β (PI3Kβ) inhibitor that holds great promise as a novel chemotherapeutic agent to treat prostate cancer. However, poor solubility and lack of targetability limit its therapeutic applications. The objective of this present study is to develop a peptide-drug conjugate...

journal_title：Molecular pharmaceutics

authors： Tai W,Shukla RS,Qin B,Li B,Cheng K

更新日期：2011-06-06 00:00:00

abstract：:RNA oligonucleotides capable of inducing controlled immunostimulation combined with specific oncogene silencing via an RNA interference (RNAi) mechanism provide synergistic inhibition of cancer cell growth. With this concept, we previously designed a potent immunostimulatory long double stranded RNA, referred to as li...

journal_title：Molecular pharmaceutics

authors： Sajeesh S,Lee TY,Hong SW,Dua P,Choe JY,Kang A,Yun WS,Song C,Park SH,Kim S,Li C,Lee DK

更新日期：2014-03-03 00:00:00

abstract：:P-glycoprotein (Pgp) is highly expressed on blood-brain barrier (BBB) and glioblastoma (GB) cells, particularly on cancer stem cells (SC). Pgp recognizes a broad spectrum of substrates, limiting the therapeutic efficacy of several chemotherapeutic drugs in eradicating GB SC. Finding effective and safe inhibitors of Pg...

journal_title：Molecular pharmaceutics

authors： Salaroglio IC,Abate C,Rolando B,Battaglia L,Gazzano E,Colombino E,Costamagna C,Annovazzi L,Mellai M,Berardi F,Capucchio MT,Schiffer D,Riganti C

更新日期：2019-08-05 00:00:00

abstract：:The controversy surrounding the use of diphtheria toxin (DT) as a therapeutic agent against tumor cells arises mainly from its unexpected harmfulness to healthy tissues. We encoded the cytotoxic fragment A of DT (DTA) as an objective gene in the Light-On gene-expression system to construct plasmids pGAVPO (pG) and pU5...

journal_title：Molecular pharmaceutics

authors： Xu J,He M,Hou X,Wang Y,Shou C,Cai X,Yuan Z,Yin Y,Lan M,Lou K,Zhao Y,Yang Y,Chen X,Gao F

更新日期：2020-01-06 00:00:00

abstract：:Recent developments in pharmaceutical technology have facilitated the design and production of modified release formulas for drugs whose physical, chemical or biological properties impede release and thus might compromise their efficacy or safety. One such drug is morphine, whose short half-life requires repeated dose...

journal_title：Molecular pharmaceutics

authors： Morales ME,López G,Gallardo V,Ruiz MA

更新日期：2011-04-04 00:00:00

abstract：:The adenovirus (Ad) is widely used as a vaccine because of its ability to induce a cellular and humoral immune response. In addition, human clinical trials have validated the safety and efficacy of Ad as a vaccine vector. The traditional approach for employing the adenovirus as vaccine is to configure the antigen gene...

journal_title：Molecular pharmaceutics

authors： van Winkel CAJ,Moreno A,Curiel DT

更新日期：2018-12-03 00:00:00

abstract：:The primary cause of mortality for glioblastoma (GBM) is local tumor recurrence following standard-of-care therapies, including surgical resection. With most tumors recurring near the site of surgical resection, local delivery of chemotherapy at the time of surgery is a promising strategy. Herein drug-loaded polymer s...

journal_title：Molecular pharmaceutics

authors： Graham-Gurysh E,Moore KM,Satterlee AB,Sheets KT,Lin FC,Bachelder EM,Miller CR,Hingtgen SD,Ainslie KM

更新日期：2018-03-05 00:00:00

abstract：:Indocyanine green (ICG) is a conventional dye that can be used in clinical near-infrared (NIR) imaging, and it is also an effective light absorber for laser-mediated photothermal therapy. However, applications of ICG were limited due to its fast degradation in aqueous media and quick clearance from the body. Herein, a...

journal_title：Molecular pharmaceutics

authors： Zheng X,Zhou F,Wu B,Chen WR,Xing D

更新日期：2012-03-05 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：: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：: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：:Herein, we report on the role of endocytosis in the selective chemotherpeutic toxicity of rhodamine 6G (R6G) based nanomaterials, i.e., nanoGUMBOS, that are derived from a group of uniform materials based on organic salts (GUMBOS). Evaluation of cellular uptake in the presence and absence of endocytosis inhibitors sug...

journal_title：Molecular pharmaceutics

authors： Bhattarai N,Mathis JM,Chen M,Pérez RL,Siraj N,Magut PKS,McDonough K,Sahasrabudhe G,Warner IM

更新日期：2018-09-04 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：:In the present age of pharmaceutical research and development, focused delivery of decision making data is more imperative than ever before. Resulting from several years' success, failure and consequential learning, this article also proffers advice and guidance on which in vitro and in vivo experiments to perform to ...

journal_title：Molecular pharmaceutics

authors： Grime KH,Barton P,McGinnity DF

更新日期：2013-04-01 00:00:00