New Biotechnological Microencapsulating Methodology Utilizing Individualized Gradient-Screened Jet Laminar Flow Techniques for Pancreatic β-Cell Delivery: Bile Acids Support Cell Energy-Generating Mechanisms.

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：: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：:Combinatorial chemistry has enabled the production of very potent drugs that might otherwise suffer from poor solubility and low oral bioavailability. One approach to increase solubility is to make the drug amorphous, which leads to problems associated with drug stability. To improve stability, one option is to molecu...

journal_title：Molecular pharmaceutics

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

更新日期：2014-07-07 00:00:00

abstract：:The most promising F508del-CFTR corrector, VX-809, has been unsuccessful as an effective, stand-alone treatment for CF patients, but the rescue effect in combination with other drugs may confer an acceptable level of therapeutic benefit. Targeting cellular factors that modify trafficking may act to enhance the cell su...

journal_title：Molecular pharmaceutics

authors： Perkins LA,Fisher GW,Naganbabu M,Schmidt BF,Mun F,Bruchez MP

更新日期：2018-03-05 00:00:00

abstract：:Therapeutic monoclonal antibodies are currently delivered mainly via the intravenous route, since large volumes are often required to deliver a therapeutic dose. Administration via the subcutaneous route would have several therapeutic advantages; the absorption mechanisms for antibodies dosed subcutaneously are poorly...

journal_title：Molecular pharmaceutics

authors： Dahlberg AM,Kaminskas LM,Smith A,Nicolazzo JA,Porter CJ,Bulitta JB,McIntosh MP

更新日期：2014-02-03 00:00:00

abstract：:Bisphosphonates (BPs) are a class of bone resorptive drug with a high affinity for the hydroxyapatite structure of bone matrices that are used for the treatment of osteoporosis. However, clinical application is limited by a common toxicity, BP-related osteonecrosis of the jaw. There is emerging evidence that BPs posse...

journal_title：Molecular pharmaceutics

authors： Massey AS,Pentlavalli S,Cunningham R,McCrudden CM,McErlean EM,Redpath P,Ali AA,Annett S,McBride JW,McCaffrey J,Robson T,Migaud ME,McCarthy HO

更新日期：2016-04-04 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：:The bicarbonate buffer capacity is usually considered in a phase-homogeneous system, at equilibrium, with no CO2 transfer between the liquid buffer phase and another phase. However, typically, an in vitro bicarbonate buffer-based system is a phase-heterogeneous system, as it entails continuously sparging (bubbling) th...

journal_title：Molecular pharmaceutics

authors： Al-Gousous J,Sun KX,McNamara DP,Hens B,Salehi N,Langguth P,Bermejo M,Amidon GE,Amidon GL

更新日期：2018-11-05 00:00:00

abstract：:The impact of OATP drug uptake transporters in drug-drug interactions (DDIs) is increasingly recognized. OATP1B1 and OATP1B3 are human hepatic uptake transporters that can mediate liver uptake of a wide variety of drugs. Recently, we generated transgenic mice with liver-specific expression of human OATP1B1 or OATP1B3 ...

journal_title：Molecular pharmaceutics

authors： Durmus S,Lozano-Mena G,van Esch A,Wagenaar E,van Tellingen O,Schinkel AH

更新日期：2015-12-07 00:00:00

abstract：:The objective was to determine the disposition of polymer nanoparticles and an associated, lipophilic, model "active" component on and within the skin following topical application. Polystyrene and poly(methyl methacrylate) nanoparticles containing covalently bound fluorescein methacrylate and dispersed Nile Red were ...

journal_title：Molecular pharmaceutics

authors： Wu X,Price GJ,Guy RH

更新日期：2009-09-01 00:00:00

abstract：:The objectives of this study were as follows: (i) To develop an in silico technique, based on molecular dynamics (MD) simulations, to predict glass transition temperatures (Tg) of amorphous pharmaceuticals. (ii) To computationally study the effect of plasticizer on Tg. (iii) To investigate the intermolecular interacti...

journal_title：Molecular pharmaceutics

authors： Gupta J,Nunes C,Jonnalagadda S

更新日期：2013-11-04 00:00:00

abstract：:Solubility limited compounds require enabling formulations such as amorphous solid dispersions (ASDs) to increase the apparent solubility by dissolving to a concentration higher than the equilibrium solubility of the drug. This may lead to subsequent precipitation and thus the loss of the solubility advantage. Althoug...

journal_title：Molecular pharmaceutics

authors： Han YR,Lee PI

更新日期：2017-01-03 00:00:00

abstract：:Reversible aqueous lipidization (REAL) at the interdisulfide bond has been shown to improve the deliverability of some peptide drugs. Recently, we developed a nonreversible aqueous lipidization method targeted at the interdisulfide bond of salmon calcitonin (sCT). The resultant derivative had comparable hypocalcemic a...

journal_title：Molecular pharmaceutics

authors： Cheng W,Lim LY

更新日期：2008-07-01 00:00:00

abstract：:Polymer therapeutics has emerged as a new clinical option for the treatment of human diseases. However, little is known about pharmacogenetic responses to drugs formulated with polymers. In this study, we demonstrate that a formulation containing the block copolymer Pluronic P85 and antineoplastic drug doxorubicin (Do...

journal_title：Molecular pharmaceutics

authors： Batrakova EV,Kelly DL,Li S,Li Y,Yang Z,Xiao L,Alakhova DY,Sherman S,Alakhov VY,Kabanov AV

更新日期：2006-03-01 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：:Itraconazole is a drug of choice for the treatment of severe fungal infections and parasitic diseases, but its use is limited by its low water solubility and varying bioavailability. New self-emulsifying drug delivery systems (SEDDS) based on PEGylated bile acids (BA-PEGs) were designed and prepared, where the number ...

journal_title：Molecular pharmaceutics

authors： Le Dévédec F,Strandman S,Hildgen P,Leclair G,Zhu XX

更新日期：2013-08-05 00:00:00

abstract：:Gold nanoparticles (AuNPs) have a number of physical properties that make them appealing for medical applications. For example, the attenuation of X-rays by gold nanoparticles has led to their use in computed tomography imaging and as adjuvants for radiotherapy. AuNPs have numerous other applications in imaging, thera...

journal_title：Molecular pharmaceutics

authors： Mieszawska AJ,Mulder WJ,Fayad ZA,Cormode DP

更新日期：2013-03-04 00:00:00

abstract：:Although tumor-targeting nanovehicles for hepatocellular carcinoma (HCC) chemotherapy have attracted great research and clinic interest, the poor cancer penetration, inefficient cellular uptake, and slow intracellular drug release greatly compromise their therapeutic outcomes. In this work, a multifunctional mixed mic...

journal_title：Molecular pharmaceutics

authors： Zhang J,Zheng Y,Xie X,Wang L,Su Z,Wang Y,Leong KW,Chen M

更新日期：2017-11-06 00:00:00

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：:Metastatic breast cancer is incurable. The goal of this study was to develop a positron emission tomography (PET)/near-infrared fluorescent (NIRF) probe for imaging CD105 expression in breast cancer experimental lung metastasis. TRC105, a chimeric anti-CD105 antibody, was dual-labeled with a NIRF dye (IRDye 800CW) and...

journal_title：Molecular pharmaceutics

authors： Hong H,Zhang Y,Severin GW,Yang Y,Engle JW,Niu G,Nickles RJ,Chen X,Leigh BR,Barnhart TE,Cai W

更新日期：2012-08-06 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：:Our previous studies have demonstrated that a generation 5 dendrimer (G5) conjugated with both folic acid (FA) and methotrexate (MTX) has a higher chemotherapeutic index than MTX alone. Despite this, batch-to-batch inconsistencies in the number of FA and MTX molecules linked to each dendrimer led to conjugate batches ...

journal_title：Molecular pharmaceutics

authors： Thomas TP,Huang B,Choi SK,Silpe JE,Kotlyar A,Desai AM,Zong H,Gam J,Joice M,Baker JR Jr

更新日期：2012-09-04 00:00:00

abstract：:Compared with peripheral tumors, glioma is very difficult to treat, not only because it has general features of tumor but also because the therapy has been restricted by the brain-blood barrier (BBB). The two main features of tumor growth are angiogenesis and proliferation of tumor cells. RNA interference (RNAi) can d...

journal_title：Molecular pharmaceutics

authors： Kuang Y,Jiang X,Zhang Y,Lu Y,Ma H,Guo Y,Zhang Y,An S,Li J,Liu L,Wu Y,Liang J,Jiang C

更新日期：2016-05-02 00:00:00

abstract：:The current regimen of factor IX (FIX) injection is of an episodic format, which leads to limited efficacy. A sustained release dosage form is beneficial in terms of reducing the injection frequency and improving the therapeutic effectiveness. The aim of this study was to formulate a new microsphere form of a FIX-cont...

journal_title：Molecular pharmaceutics

authors： Chang LC,Yang CY,Chua AC,Lin YJ,Lai SM

更新日期：2011-10-03 00:00:00

abstract：:Interest in the use of 225Ac for targeted alpha therapies has increased dramatically over the past few years, resulting in a multitude of new isotope production and translational research efforts. However, 225Ac radioimmunoconjugate (RIC) research is still in its infancy, with most prior experience in hematologic mali...

journal_title：Molecular pharmaceutics

authors： Lakes AL,An DD,Gauny SS,Ansoborlo C,Liang BH,Rees JA,McKnight KD,Karsunky H,Abergel RJ

更新日期：2020-11-02 00:00:00

abstract：:Targeted therapies are emerging as a preferred strategy for treatment of cancer and other diseases. To evaluate the effect of high affinity receptors on the rate and extent of tumor penetration of receptor-targeted drugs, we have characterized the kinetics of folate-rhodamine uptake by folate receptor (FR)-expressing ...

journal_title：Molecular pharmaceutics

authors： Vlashi E,Sturgis JE,Thomas M,Low PS

更新日期：2009-11-01 00:00:00

abstract：:We investigated the effect of polymer composition on nifedipine (NIF) dissolution through molecular-level characterization of NIF/hypromellose (HPMC)/Eudragit S (EUD-S) ternary solid dispersions. The dissolution rates and molecular states of NIF and polymers were evaluated in NIF/HPMC/EUD-S spray-dried samples (SPDs) ...

journal_title：Molecular pharmaceutics

authors： Ueda K,Yamazoe C,Yasuda Y,Higashi K,Kawakami K,Moribe K

更新日期：2018-09-04 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：:Current cancer chemotherapies commonly suffer from nonspecificity, drug resistance, poor bioavailability, and narrow therapeutic indices. To achieve the optimum drug efficacy, we designed a polymeric drug delivery system for targeted intracellular delivery of a clinically approved, water-soluble anticancer drug, gemci...

journal_title：Molecular pharmaceutics

authors： Kulhari H,Pooja D,Kota R,Reddy TS,Tabor RF,Shukla R,Adams DJ,Sistla R,Bansal V

更新日期：2016-05-02 00:00:00

abstract：:Hydrophilic matrices are an effective option for oral controlled release but can face challenges in terms of bioavailability and efficacy when used in conjunction with poorly soluble, weakly basic drugs. Attenuated total reflectance Fourier transform infrared (ATR-FTIR) imaging provides dynamic information relating to...

journal_title：Molecular pharmaceutics

authors： Zahoor FD,Mader KT,Timmins P,Brown J,Sammon C

更新日期：2020-04-06 00:00:00