Novel Integrin αvβ3-Specific Ligand for the Sensitive Diagnosis of Glioblastoma.

abstract：:Dissolution is a crucial process for the oral delivery of drug products. Before being absorbed through epithelial cell membranes to reach the systemic circulation, drugs must first dissolve in the human gastrointestinal (GI) tract. In vivo and in vitro dissolutions are complex because of their dependency upon the drug...

journal_title：Molecular pharmaceutics

authors： Salehi N,Al-Gousous J,Mudie DM,Amidon GL,Ziff RM,Amidon GE

更新日期：2020-10-05 00:00:00

abstract：:Solid lipid nanoparticles (SLNs) are one of the most promising nanocarriers to increase the oral absorption of drugs with poor solubility and low permeability. However, the absorption mechanism of SLNs remains incomplete and thus requires further careful consideration. In this study, positively charged chitosan (CS) m...

journal_title：Molecular pharmaceutics

authors： Shi LL,Xie H,Lu J,Cao Y,Liu JY,Zhang XX,Zhang H,Cui JH,Cao QR

更新日期：2016-08-01 00:00:00

abstract：:Adsorption of antibody therapeutics to air-liquid interfaces can enhance aggregation, particularly when the solution does not contain protective surfactant or when the surfactant is diluted as occurs during preparation of intravenous infusion bags. The ability to predict an antibody's propensity for interfacially medi...

journal_title：Molecular pharmaceutics

authors： Shieh IC,Patel AR

更新日期：2015-09-08 00:00:00

abstract：:Platinum(IV) complexes generally require reduction to reactive Pt(II) species to exert their chemotherapeutic activity. The process of reductive activation of (15)N-labeled (OC-6-43)-bis(acetato)diamminedichloridoplatinum(IV), in the presence of nicotinamide adenine dinucleotide (NADH) and horse heart cytochrome c (cy...

journal_title：Molecular pharmaceutics

authors： Lasorsa A,Stuchlíková O,Brabec V,Natile G,Arnesano F

更新日期：2016-09-06 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：:Herein, we elucidated the mechanisms and key factors for the tumor-targeting ability of nanoparticles that presented high targeting efficiency for liver tumor. We used several different nanoparticles with sizes of 200-300 nm, including liposome nanoparticles (LNPs), polystyrene nanoparticles (PNPs) and glycol chitosan...

journal_title：Molecular pharmaceutics

authors： Na JH,Koo H,Lee S,Han SJ,Lee KE,Kim S,Lee H,Lee S,Choi K,Kwon IC,Kim K

更新日期：2016-11-07 00:00:00

abstract：:Erythropoietin (EPO), a hematopoietic growth factor and a promising therapy for Alzheimer's disease, has low permeability across the blood-brain barrier. The transferrin receptor antibody fused to EPO (TfRMAb-EPO) is a chimeric monoclonal antibody that ferries EPO into the brain via the transvascular route. However, T...

journal_title：Molecular pharmaceutics

authors： Yang J,Sun J,Castellanos DM,Pardridge WM,Sumbria RK

更新日期：2020-08-03 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：:Retinal pigment epithelium, which forms the outer blood-retinal barrier, is a critical barrier for transport of drugs to the retina. The purpose of this study was to develop a pigmented MDCK (P-MDCK) cell line as a rapidly established in vitro model for the outer blood-retinal barrier to assess the influence of melani...

journal_title：Molecular pharmaceutics

authors： Kadam RS,Scheinman RI,Kompella UB

更新日期：2012-11-05 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：:Liposomes are widely used for systemic delivery of chemotherapeutic agents to reduce their nonspecific side effects. Gemcitabine (Gem) makes a great candidate for liposomal encapsulation due to the short half-life and nonspecific side effects; however, it has been difficult to achieve liposomal Gem with high drug load...

journal_title：Molecular pharmaceutics

authors： Tamam H,Park J,Gadalla HH,Masters AR,Abdel-Aleem JA,Abdelrahman SI,Abdelrahman AA,Lyle LT,Yeo Y

更新日期：2019-07-01 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：:Organic anion-transporting polypeptides (OATPs) mediate the uptake of various drugs from blood into the liver in the basolateral membrane of hepatocytes. Positron emission tomography (PET) is a potentially powerful tool to assess the activity of hepatic OATPs in vivo, but its utility critically depends on the availabi...

journal_title：Molecular pharmaceutics

authors： Bauer M,Traxl A,Matsuda A,Karch R,Philippe C,Nics L,Klebermass EM,Wulkersdorfer B,Weber M,Poschner S,Tournier N,Jäger W,Wadsak W,Hacker M,Wanek T,Zeitlinger M,Langer O

更新日期：2018-10-01 00:00:00

abstract：:The present work investigates the influence of electrostatic surface potential distribution of monoclonal antibodies (MAbs) on intermolecular interactions and viscosity. Electrostatic models suggest MAb-1 has a less uniform surface charge distribution than MAb-2. The patches of positive and negative potential on MAb-1...

journal_title：Molecular pharmaceutics

authors： Yadav S,Laue TM,Kalonia DS,Singh SN,Shire SJ

更新日期：2012-04-02 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：:The ultrasmall nanoparticle AGuIX is a versatile platform that tolerates a range of chemical diversity for theranostic applications. Our previous work showed that AGuIX clears rapidly from normal tissues, while durably accumulating within the tumor microenvironment. On this basis, AGuIX was used to detect tumor tissue...

journal_title：Molecular pharmaceutics

authors： Truillet C,Thomas E,Lux F,Huynh LT,Tillement O,Evans MJ

更新日期：2016-07-05 00:00:00

abstract：:There is evidence that encapsulating glucocorticoids into nucleic acid-containing nanoparticles reduces the inflammatory toxicities of the nanoparticles. Herein, using betamethasone acetate (BA), a glucocorticoid, and a solid lipid nanoparticle formulation of siRNA, we confirmed that coencapsulating BA into the siRNA ...

journal_title：Molecular pharmaceutics

authors： O'Mary HL,Hanafy MS,Aldayel AM,Valdes SA,Alzhrani RF,Hufnagel S,Koleng JJ,Cui Z

更新日期：2019-11-04 00:00:00

abstract：:The particular characteristics of the tumor microenvironment have the potential to strongly promote tumor growth, metastasis and angiogenesis and induce drug resistance. Therefore, the development of effective, systemic therapeutic approaches specifically based on the tumor microenvironment is highly desirable. Hypoxi...

journal_title：Molecular pharmaceutics

authors： Liu XQ,Xiong MH,Shu XT,Tang RZ,Wang J

更新日期：2012-10-01 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：:Ritonavir is a protease inhibitor utilized primarily as a pharmaco-enhancer with concomitantly administered antiviral drugs including other protease inhibitors. However, poor tolerance, serious side effects, and toxicities associated with drug-drug interactions are common during exposure to ritonavir. The aim of this ...

journal_title：Molecular pharmaceutics

authors： Martin P,Giardiello M,McDonald TO,Smith D,Siccardi M,Rannard SP,Owen A

更新日期：2015-10-05 00:00:00

abstract：:Novel multivalent copper(II)-conjugated phosphorus dendrimers and their corresponding mononuclear copper(II) complexes were synthesized, characterized, and screened for antiproliferative activity against human cancer cell lines. Selected copper ligands were grafted on the surface of phosphorus dendrimers of generation...

journal_title：Molecular pharmaceutics

authors： El Brahmi N,El Kazzouli S,Mignani SM,Essassi el M,Aubert G,Laurent R,Caminade AM,Bousmina MM,Cresteil T,Majoral JP

更新日期：2013-04-01 00:00:00

abstract：:The applicability of the computational docking approach was investigated to create a novel method for quick additive screening to inhibit the crystallization taking place in amorphous drugs. Surface energy and attachment energy were utilized to recognize the morphologically most important crystal faces. The surfaces (...

journal_title：Molecular pharmaceutics

authors： Pajula K,Lehto VP,Ketolainen J,Korhonen O

更新日期：2012-10-01 00:00:00

abstract：:Photodynamic therapy, a procedure that uses a photosensitizer to enable light therapy selectively at diseased sites, remains underutilized in oncological clinic. To further improve its cancer selectivity, we developed a polymeric nanosystem by conjugating a photosensitizer IRDye 700DX (IR700) and cancer targeting RGD ...

journal_title：Molecular pharmaceutics

authors： Zhao Y,Li F,Mao C,Ming X

更新日期：2018-07-02 00:00:00

abstract：:One hypothesis for persisting HIV-associated neurocognitive disorders (HAND) in effectively treated individuals is the limited permeation of antiretroviral agents (ARV) across the blood-brain barrier (BBB). However, the physicochemical factors limiting the brain entry of a given ARV and the mutual interactions of comb...

journal_title：Molecular pharmaceutics

authors： Marzolini C,Mueller R,Li-Blatter X,Battegay M,Seelig A

更新日期：2013-06-03 00:00:00

abstract：:Lipophilic cations such as phosphonium salts can accumulate in mitochondria of heart in response to the negative inner-transmembrane potentials. Two phosphonium salts [(18)F]FMBTP and [(18)F]mFMBTP were prepared and evaluated as potential myocardial perfusion imaging (MPI) agents in this study. The cations were radiol...

journal_title：Molecular pharmaceutics

authors： Zhao Z,Yu Q,Mou T,Liu C,Yang W,Fang W,Peng C,Lu J,Liu Y,Zhang X

更新日期：2014-11-03 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：: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

abstract：:Most vaccines contain aluminum adjuvants; however, their exact mechanism of action remains unclear. A novel mechanism by Shi and colleagues proposes aluminum adjuvants may enhance immune activation by binding and reorganizing lipids that are key components of lipid rafts. To better understand the specificity of intera...

journal_title：Molecular pharmaceutics

authors： Antúnez LR,Livingston A,Berkland C,Dhar P

更新日期：2016-05-02 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：: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