MRI-visible micellar nanomedicine for targeted drug delivery to lung cancer cells.

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：:Solid-state hydrogen-deuterium exchange with mass spectrometric analysis (ssHDX) is a promising method for characterizing proteins in amorphous solids. Though analysis of HDX kinetics is informative and well-established in solution, application of these methods to solid samples is complicated by possible heterogeneiti...

journal_title：Molecular pharmaceutics

authors： Sophocleous AM,Topp EM

更新日期：2012-04-02 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：:BCS classification is a vital tool in the development of both generic and innovative drug products. The purpose of this work was to provisionally classify the world's top selling oral drugs according to the BCS, using in silico methods. Three different in silico methods were examined: the well-established group contri...

journal_title：Molecular pharmaceutics

authors： Dahan A,Wolk O,Kim YH,Ramachandran C,Crippen GM,Takagi T,Bermejo M,Amidon GL

更新日期：2013-11-04 00:00:00

abstract：:Following oral administration, dabigatran etexilate (DABE) is rapidly hydrolyzed to its active form, dabigatran. DABE, but not dabigatran, presents as a P-glycoprotein (P-gp) substrate and has increasingly been used as a probe drug. Therefore, although dosed as DABE, a P-gp drug-drug interaction (DDI) is reported as a...

journal_title：Molecular pharmaceutics

authors： Shen H,Yao M,Sinz M,Marathe P,Rodrigues AD,Zhu M

更新日期：2019-09-03 00:00:00

abstract：:Milk has been used as a vehicle for the delivery of antimalarial drugs during clinical trials to test for a food effect and artefenomel (OZ439) showed enhanced oral bioavailability with milk. However, the nature of the interaction between milk and OZ439 in the gastrointestinal tract remains poorly understood. To under...

journal_title：Molecular pharmaceutics

authors： Salim M,Khan J,Ramirez G,Clulow AJ,Hawley A,Ramachandruni H,Boyd BJ

更新日期：2018-08-06 00:00:00

abstract：:The wet form of age-related macular degeneration (AMD) is a leading cause of blindness among elderly Americans and is characterized by abnormal vessel growth, termed choroidal neovascularization (CNV). Integrin α5β1 is a transmembrane receptor that binds matrix macromolecules and proteinases to stimulate angiogenesis....

journal_title：Molecular pharmaceutics

authors： Wang WQ,Wang FH,Qin WX,Liu HY,Lu B,Chung C,Zhu J,Gu Q,Shi W,Wen C,Wu F,Zhang K,Sun XD

更新日期：2016-09-06 00:00:00

abstract：:Deferoxamine mesylate (DFO) is an FDA-approved, hexadentate iron chelator routinely used to alleviate systemic iron burden in thalassemia major and sickle cell patients. Iron accumulation in these disease states results from the repeated blood transfusions required to manage these conditions. Iron accumulation has als...

journal_title：Molecular pharmaceutics

authors： Farr AC,Xiong MP

更新日期：2021-02-01 00:00:00

abstract：:Invasion and metastasis of cancer directly related to human death have been associated with interactions among many different types of cells and three-dimensional (3D) tissue matrices. Precise mechanisms related to cancer invasion and metastasis still remain unknown due to their complexities. Development of tumor micr...

journal_title：Molecular pharmaceutics

authors： Park MH,Song B,Hong S,Kim SH,Lee K

更新日期：2016-07-05 00:00:00

abstract：:Cytochrome c (Cyt c) is a small mitochondrial heme protein involved in the intrinsic apoptotic pathway. Once Cyt c is released into the cytosol, the caspase mediated apoptosis cascade is activated resulting in programmed cell death. Herein, we explore the covalent immobilization of Cyt c into mesoporous silica nanopar...

journal_title：Molecular pharmaceutics

authors： Méndez J,Morales Cruz M,Delgado Y,Figueroa CM,Orellano EA,Morales M,Monteagudo A,Griebenow K

更新日期：2014-01-06 00:00:00

abstract：:Effective penetration of drug-carrying nanoparticles into solid tumors is a major challenge in cancer therapy. Exploration of the physicochemical properties of nanoparticles that affect penetration efficiency is required to achieve maximum therapeutic effects. Here, we used confocal laser scanning microscopy to evalua...

journal_title：Molecular pharmaceutics

authors： Takechi-Haraya Y,Goda Y,Sakai-Kato K

更新日期：2017-06-05 00:00:00

abstract：:We investigated the feasibility and efficacy of a drug delivery strategy to vascularized cancer that combines targeting selectivity with high uptake by targeted cells and high bioexposure of cells to delivered chemotherapeutics. Targeted lipid vesicles composed of pH responsive membranes were designed to reversibly fo...

journal_title：Molecular pharmaceutics

authors： Bandekar A,Zhu C,Gomez A,Menzenski MZ,Sempkowski M,Sofou S

更新日期：2013-01-07 00:00:00

abstract：:OATP1B3 is a member of the OATP (organic anion transporting polypeptides) superfamily, responsible for mediating the transport of numerous endogenous and xenobiotic substances. Although initially reported to be exclusively expressed in the liver, several studies reported that OATP1B3 is frequently expressed in multipl...

journal_title：Molecular pharmaceutics

authors： Thakkar N,Kim K,Jang ER,Han S,Kim K,Kim D,Merchant N,Lockhart AC,Lee W

更新日期：2013-01-07 00:00:00

abstract：:Cationic poly-L-lysine 3H-dendrimers with either 16 or 32 surface amine groups (BHALys [Lys]4 [3H-Lys]8 [NH2]16 and BHALys [Lys]8 [3H-Lys]16 [NH2]32, generation 3 and 4, respectively) have been synthesized and their pharmacokinetics and biodistribution investigated after intravenous administration to rats. The species...

journal_title：Molecular pharmaceutics

authors： Boyd BJ,Kaminskas LM,Karellas P,Krippner G,Lessene R,Porter CJ

更新日期：2006-09-01 00:00:00

abstract：:We examined the inhibitory effect of hydroxypropyl methylcellulose acetate succinate (HPMC-AS) on drug recrystallization from a supersaturated solution using carbamazepine (CBZ) and phenytoin (PHT) as model drugs. HPMC-AS HF grade (HF) inhibited the recrystallization of CBZ more strongly than that by HPMC-AS LF grade ...

journal_title：Molecular pharmaceutics

authors： Ueda K,Higashi K,Yamamoto K,Moribe K

更新日期：2013-10-07 00:00:00

abstract：BACKGROUND:For the development of novel buccoadhesive formulations, their physicochemical properties, strength of the interfacial joint, and residence time on the buccal mucosa are considered as a measure for their in vivo mucoadhesive properties. Focusing on these parameters, the predictive power of established in vit...

journal_title：Molecular pharmaceutics

authors： Baus RA,Haug MF,Leichner C,Jelkmann M,Bernkop-Schnürch A

更新日期：2019-06-03 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：:The Biopharmaceutical Classification System (BCS) guidance issued by the FDA allows waivers for in vivo bioavailability and bioequivalence studies for immediate-release (IR) solid oral dosage forms only for BCS class I drugs. However, a number of drugs within BCS class III have been proposed to be eligible for biowaiv...

journal_title：Molecular pharmaceutics

authors： Tsume Y,Amidon GL

更新日期：2010-08-02 00:00:00

abstract：:The bladder is an important tissue in which to evaluate xenobiotic drug interactions and toxicities due to the concentration of parent drug and hepatic/enteric-derived metabolites in the urine as a result of renal excretion. Breaching of the barrier provided by the bladder epithelial lining (the urothelium) can expose...

journal_title：Molecular pharmaceutics

authors： Baker SC,Shabir S,Southgate J

更新日期：2014-07-07 00:00:00

abstract：:Integrin αvβ3 is a cell adhesion molecule involved in the progression and invasion of glioblastoma, making it an attractive target for the diagnosis of glioblastoma. Although some integrin αvβ3 specific ligands, such as RGD and its mimetic peptides (Cilengitide), have been devoted in detecting glioblastoma, their clin...

journal_title：Molecular pharmaceutics

authors： Zhang L,Shan X,Meng X,Gu T,Guo L,An X,Jiang Q,Ge H,Ning X

更新日期：2019-09-03 00:00:00

abstract：:Lipid-core nanocapsules (LCNs) have been proposed as drug carriers to improve brain delivery by modulating drug pharmacokinetics (PK). However, it is not clear whether the LCNs carry the drug through the blood-brain barrier or increase free drug penetration due to changes in the barrier permeability. Quetiapine (QTP) ...

journal_title：Molecular pharmaceutics

authors： Carreño F,Paese K,Silva CM,Guterres SS,Dalla Costa T

更新日期：2016-04-04 00:00:00

abstract：:The impact of the chain length or dispersity of polymers in controlling the crystallization of amorphous active pharmaceutical ingredients (APIs) has been discussed for a long time. However, because of the weak control of these parameters in the majority of macromolecules used in pharmaceutical formulations, the above...

journal_title：Molecular pharmaceutics

authors： Minecka A,Tarnacka M,Jurkiewicz K,Hachuła B,Wrzalik R,Kamiński K,Paluch M,Kamińska E

更新日期：2021-01-04 00:00:00

abstract：:Bacterial capsular polysaccharides are components of many modern vaccines, but they are weakly immunogenic. Herein, we describe the delivery of pneumococcal capsular polysaccharide serotype-1 (PCP-1) in polylactide polymeric particles to enhance its immunogenicity. Immunization with PCP-1-entrapped particles elicited ...

journal_title：Molecular pharmaceutics

authors： Anish C,Khan N,Upadhyay AK,Sehgal D,Panda AK

更新日期：2014-03-03 00:00:00

abstract：:Conventional drug solubilization strategies limit the understanding of the full potential of poorly water-soluble drugs during drug screening. Here, we propose a screening approach in which poorly water-soluble drugs are entrapped in poly(2-(methacryloyloxyethyl phosphorylcholine)-poly(2-(diisopropylaminoethyl methacr...

journal_title：Molecular pharmaceutics

authors： Sola-Barrado B,M Leite D,Scarpa E,Duro-Castano A,Battaglia G

更新日期：2020-12-07 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 N-glycosylation pattern of Asn-297 may have impacts on monoclonal antibody (mAb) drug plasma clearance, antibody-dependent cell mediated cytotoxicity (ADCC), and complement-dependent cytotoxicity (CDC). Notably, the changes in the relative abundance of certain minor glycans, like the afucosylation, high-mannose, o...

journal_title：Molecular pharmaceutics

authors： Zhuo Y,Keire DA,Chen K

更新日期：2021-01-04 00:00:00

abstract：:This study describes a novel nonlinear variant of the well-known Yalkowsky general solubility equation (GSE). The modified equation can be trained with small molecules, mostly from the Lipinski Rule of 5 (Ro5) chemical space, to predict the intrinsic aqueous solubility, S0, of large molecules (MW > 800 Da) from beyond...

journal_title：Molecular pharmaceutics

authors： Avdeef A,Kansy M

更新日期：2020-10-05 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：:Deep generative adversarial networks (GANs) are the emerging technology in drug discovery and biomarker development. In our recent work, we demonstrated a proof-of-concept of implementing deep generative adversarial autoencoder (AAE) to identify new molecular fingerprints with predefined anticancer properties. Another...

journal_title：Molecular pharmaceutics

authors： Kadurin A,Nikolenko S,Khrabrov K,Aliper A,Zhavoronkov A

更新日期：2017-09-05 00:00:00

abstract：:Today, about 50% of men and 15-30% of women suffer from hair loss as well as the associated psychological impact. Drug therapy, especially through topical administration, is the main treatment strategy for stimulating hair regrowth. However, challenges exist due to the skin barrier that hinders drug penetration. To th...

journal_title：Molecular pharmaceutics

authors： Yang G,Chen G,Gu Z

更新日期：2021-02-01 00:00:00