Development of a poly(d,l-lactic-co-glycolic acid) nanoparticle formulation of STAT3 inhibitor JSI-124: implication for cancer immunotherapy.

abstract：:Ritonavir is a well-known CYP3A4 and CYP2D6 enzyme inhibitor, frequently used to assess the drug-drug interaction (DDI) liability of susceptible drugs. It is also used as a pharmacokinetic booster to increase exposure to CYP3A4 substrates. This study aimed to develop a mechanistic absorption and disposition model to d...

journal_title：Molecular pharmaceutics

authors： Arora S,Pansari A,Kilford P,Jamei M,Gardner I,Turner DB

更新日期：2020-07-06 00:00:00

abstract：:The tumor microenvironments are often acidic and overexpress specific enzymes. In this work, we synthesized a poly(AA-b-NIPAAm) copolymer (PAA-b-PNIPAAm) using a reversible addition-fragmentation chain transfer (RAFT) polymerization method. PAA-b-PNIPAAm and a cationic protein (protamine) were self-assembled into nano...

journal_title：Molecular pharmaceutics

authors： Don TM,Lu KY,Lin LJ,Hsu CH,Wu JY,Mi FL

更新日期：2017-12-04 00:00:00

abstract：:Ipratropium bromide, an anticholinergic drug used for the treatment of asthma and chronic obstructive pulmonary disease, has low oral bioavailability, but systemic exposure, superior to oral administration, can be achieved by inhalation. Therefore, we investigated the pulmonary absorption mechanism of ipratropium usin...

journal_title：Molecular pharmaceutics

authors： Nakamura T,Nakanishi T,Haruta T,Shirasaka Y,Keogh JP,Tamai I

更新日期：2010-02-01 00:00:00

abstract：:Simvastatin is one of the most widely used active pharmaceutical ingredients for the treatment of hyperlipidemias. Because the compound is employed as a solid in drug formulations, particular attention should be given to the characterization of different polymorphs, their stability domains, and the nature of the phase...

journal_title：Molecular pharmaceutics

authors： Simões RG,Bernardes CES,Joseph A,M Piedade MF,Kraus W,Emmerling F,Diogo HP,Minas da Piedade ME

更新日期：2018-11-05 00:00:00

abstract：:Paracetamol has been one of the most commonly used and prescribed analgesic drugs for more than a hundred years. Despite being generally well tolerated, it can result in high liver toxicity when administered in specific conditions, such as overdose, or in vulnerable individuals. We have synthesized and characterized a...

journal_title：Molecular pharmaceutics

authors： Sodano F,Lazzarato L,Rolando B,Spyrakis F,De Caro C,Magliocca S,Marabello D,Chegaev K,Gazzano E,Riganti C,Calignano A,Russo R,Rimoli MG

更新日期：2019-10-07 00:00:00

abstract：:Stably transfected MDCK/hPepT1-V5&His clonal cell lines expressing varying levels of epitope-tagged hPepT1 protein were established to quantify the relationship between transgene hPepT1 expression levels and its functional kinetics in facilitating peptide and peptide-like drug uptake and transport in vitro. The hPepT1...

journal_title：Molecular pharmaceutics

authors： Herrera-Ruiz D,Faria TN,Bhardwaj RK,Timoszyk J,Gudmundsson OS,Moench P,Wall DA,Smith RL,Knipp GT

更新日期：2004-03-01 00:00:00

abstract：:Nonviral transfections of six low passage human colon cancer cell lines using the artificial beta-catenin/TCF-dependent promoter CTP4 demonstrated a high promoter activity which was 1000- to 70000-fold higher than in HeLa control cells. Luciferase gene expression levels obtained with CTP4 in epithelial-like tumor cell...

journal_title：Molecular pharmaceutics

authors： Gaedtke L,Pelisek J,Lipinski KS,Wrighton CJ,Wagner E

更新日期：2007-01-01 00:00:00

abstract：:Selective ligands to the peripheral benzodiazepine receptor (PBR) may induce apoptosis and cell cycle arrest. An overexpression of PBR in certain cancers allowed us to consider the use of highly selective ligands to PBR for receptor-mediated drug targeting to tumors. With this in mind, we prepared PBR-targeted nanopar...

journal_title：Molecular pharmaceutics

authors： Musacchio T,Laquintana V,Latrofa A,Trapani G,Torchilin VP

更新日期：2009-03-01 00:00:00

abstract：:Stereoregularity of polymers is known to influence their physicochemical and functional properties in the bulk form. Recent studies have also provided evidence for the effect of polymer stereoregularity on the physicochemical and functional properties of their self-assembled nanostructures. Research in this area has w...

journal_title：Molecular pharmaceutics

authors： Soleymani Abyaneh H,Vakili MR,Shafaati A,Lavasanifar A

更新日期：2017-08-07 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：:The formation mechanism of drug nanoparticles was investigated using solid-state nuclear magnetic resonance (NMR) techniques for the efficient discovery of an optimized nanoparticle formulation. The cogrinding of nifedipine (NIF) with polymers, including hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (P...

journal_title：Molecular pharmaceutics

authors： Ueda K,Higashi K,Moribe K

更新日期：2016-03-07 00:00:00

abstract：:The melanocortin 1 receptor (MC1R) is overexpressed in most melanoma metastases, making it a promising target for imaging of melanomas. In this study, the expression of MC1R in a large fraction of patients with melanoma was confirmed using mRNA and tissue microarray. Here, we have characterized the in vivo tumor and t...

journal_title：Molecular pharmaceutics

authors： Tafreshi NK,Silva A,Estrella VC,McCardle TW,Chen T,Jeune-Smith Y,Lloyd MC,Enkemann SA,Smalley KS,Sondak VK,Vagner J,Morse DL

更新日期：2013-08-05 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 combination of microbubbles (MBs) and ultrasound (US) is an emerging method for noninvasive and targeted enhancement of anti-cancer drug uptake. This method showed an increase local drug extravasation in tumor tissue while reducing the systemic adverse effects in various tumor models. The present study aims to evalu...

journal_title：Molecular pharmaceutics

authors： Bressand D,Novell A,Girault A,Raoul W,Fromont-Hankard G,Escoffre JM,Lecomte T,Bouakaz A

更新日期：2019-09-03 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：:Structural features of lysine-conjugated antibody-drug conjugate (ADC) from humanized IgG1 were studied by small-angle X-ray scattering (SAXS). As the physicochemical properties of the cytotoxic drug (payload) and linker may impact the conformational and colloidal stabilities of the conjugated monoclonal antibody (mAb...

journal_title：Molecular pharmaceutics

authors： Law-Hine D,Rudiuk S,Bonestebe A,Ienco R,Huille S,Tribet C

更新日期：2019-12-02 00:00:00

abstract：:DEK protein is critical to the formation of neutrophil extracellular traps (NETs) in rheumatoid arthritis (RA). Blocking DEK using the aptamer DTA via articular injection has been shown to have robust anti-inflammatory efficacy in a previous study. However, DTA is prone to nuclease degradation and renal clearance in v...

journal_title：Molecular pharmaceutics

authors： Cao J,Su J,An M,Yang Y,Zhang Y,Zuo J,Zhang N,Zhao Y

更新日期：2021-01-04 00:00:00

abstract：:Polymeric micelles are emerging as a highly integrated nanoplatform for cancer targeting, drug delivery and tumor imaging applications. In this study, we describe a multifunctional micelle (MFM) system that is encoded with a lung cancer-targeting peptide (LCP), and encapsulated with superparamagnetic iron oxide (SPIO)...

journal_title：Molecular pharmaceutics

authors： Guthi JS,Yang SG,Huang G,Li S,Khemtong C,Kessinger CW,Peyton M,Minna JD,Brown KC,Gao J

更新日期：2010-02-01 00:00:00

abstract：:Process-induced phase transformations (PIPTs) of active pharmaceutical ingredients (APIs) can alter APIs' physicochemical properties and impact performance of pharmaceutical drug products. In this study, we investigated compression-induced amorphization of crystalline posaconazole (POSA), where the impact of mechanica...

journal_title：Molecular pharmaceutics

authors： Huang C,Klinzing G,Procopio A,Yang F,Ren J,Burlage R,Zhu L,Su Y

更新日期：2019-02-04 00:00:00

abstract：:Achieving effective gene therapy for glioma depends on gene delivery systems. The gene delivery system should be able to cross the blood-brain barrier (BBB) and further target glioma at its early stage. Active brain tumor targeted delivery can be achieved using the "Trojan horse" technology, which involves either endo...

journal_title：Molecular pharmaceutics

authors： Liu Y,He X,Kuang Y,An S,Wang C,Guo Y,Ma H,Lou J,Jiang C

更新日期：2014-10-06 00:00:00

abstract：:A promising strategy to enable patient stratification for targeted therapies is to monitor the target expression in a tumor by radionuclide molecular imaging. Affibody molecules (7 kDa) are nonimmunoglobulin scaffold proteins with a 25-fold smaller size than intact antibodies. They have shown an apparent potential as ...

journal_title：Molecular pharmaceutics

authors： Westerlund K,Honarvar H,Norrström E,Strand J,Mitran B,Orlova A,Eriksson Karlström A,Tolmachev V

更新日期：2016-05-02 00:00:00

abstract：:Heart transplantation (HT) is an effective treatment for end-stage heart disease. However, acute rejection (AR) is still the main cause of death within one year after HT. AR is an acute immune response mediated by T lymphocytes, mainly CD4+ T lymphocytes. This study innovatively develops a radiolabeled probe 99mTc-HYN...

journal_title：Molecular pharmaceutics

authors： Li H,Chen Y,Jin Q,Wu Y,Deng C,Gai Y,Sun Z,Li Y,Wang J,Yang Y,Lv Q,Zhang Y,An R,Lan X,Zhang L,Xie M

更新日期：2021-01-28 00:00:00

abstract：:Folate receptor (FR) targeting is an attractive strategy for nuclear imaging of cancer and activated macrophages through application of folic acid radioconjugates. However, significant renal accumulation of folate radioconjugates and hence exceedingly high emission of radiation from the kidneys may mask uptake of radi...

journal_title：Molecular pharmaceutics

authors： Müller C,Reber J,Schlup C,Leamon CP,Schibli R

更新日期：2013-03-04 00:00:00

abstract：:Understanding protein stability is central to combatting protein aggregation diseases and developing new protein therapeutics. At the high concentrations often present in biological systems, purified proteins can exhibit undesirable high solution viscosities and poor solubilities mediated by short-range electrostatic ...

journal_title：Molecular pharmaceutics

authors： Laber JR,Dear BJ,Martins ML,Jackson DE,DiVenere A,Gollihar JD,Ellington AD,Truskett TM,Johnston KP,Maynard JA

更新日期：2017-10-02 00:00:00

abstract：:Rho-GTPases are small GTP-binding proteins that contribute to the epithelial-to-mesenchymal transition by regulating several cellular processes including organization of the actin cytoskeleton, cell motility, transcription, and cell proliferation. Overexpression of RhoC-GTPases (RhoC) in breast cancer has been implica...

journal_title：Molecular pharmaceutics

authors： Kaushal N,Durmaz YY,Bao L,Merajver SD,ElSayed ME

更新日期：2015-07-06 00:00:00

abstract：:Prediction of the rate and extent of drug absorption upon oral dosing needs models that capture the complexities of both the drug molecule and intestinal physiology. We report here the development of a continuous intestinal absorption model based on the convection-diffusion equation. The model includes explicit entero...

journal_title：Molecular pharmaceutics

authors： Nagar S,Korzekwa RC,Korzekwa K

更新日期：2017-09-05 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDAC) is highly chemo-resistant and has an extremely poor patient prognosis, with a survival rate at five years of <8%. There remains an urgent need for innovative treatments. Targeting polyamine biosynthesis through inhibition of ornithine decarboxylase with difluoromethylornithine (...

journal_title：Molecular pharmaceutics

authors： Gitto SB,Pandey V,Oyer JL,Copik AJ,Hogan FC,Phanstiel O 4th,Altomare DA

更新日期：2018-02-05 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：:Encapsulation and release behavior of a water-insoluble drug, magnolol, using a core-shell polysaccharide-based nanoparticle, manipulating the cellular internalization and controlled cytotoxic effect of magnolol-loaded nanoparticles over the A10 vascular smooth muscle cells (VSMCs) was reported. A magnolol-polyvinylpy...

journal_title：Molecular pharmaceutics

authors： Wang YJ,Chien YC,Wu CH,Liu DM

更新日期：2011-12-05 00:00:00

abstract：:Antibody-based near-infrared photoimmunotherapy (NIR-PIT) is an attractive strategy for cancer treatment. Tumor cells can be selectively and efficiently killed by the targeted delivery of an antibody-photoabsorber complex followed by exposure to NIR light. Glycoprotein A33 antigen (GPA33) is highly expressed in most h...

journal_title：Molecular pharmaceutics

authors： Wei D,Tao Z,Shi Q,Wang L,Liu L,She T,Yi Q,Wen X,Liu L,Li S,Yang H,Jiang X

更新日期：2020-07-06 00:00:00