abstract：:A wide variety of chemotherapy and radiotherapy agents are available for treating cancer, but a critical challenge is to deliver these agents locally to cancer cells and tumors while minimizing side effects from systemic delivery. Nanomedicine uses nanoparticles with diameters in the range of ∼1-100 nm to encapsulate ...

journal_title：Molecular pharmaceutics

authors： Moore T,Chen H,Morrison R,Wang F,Anker JN,Alexis F

更新日期：2014-01-06 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：:We investigated the effects of the hot-melt extrusion (HME) process on the properties of itraconazole (ITZ) amorphous solid dispersions made by thin film freezing (TFF) technology. The ITZ-HPMCAS L (1:2) TFF composition exhibited limited drug release in acidic media. HME of the ITZ-HPMCAS TFF composition with hydrophi...

journal_title：Molecular pharmaceutics

authors： Lang B,McGinity JW,Williams RO 3rd

更新日期：2014-01-06 00:00:00

abstract：:Barbital is a hypnotic agent that has been intensely studied for many decades. The aim of this work was to establish a clear and comprehensible picture of its polymorphic system. Four of the six known solid forms of barbital (denoted I(0), III, IV, and V) were characterized by various analytical techniques, and the th...

journal_title：Molecular pharmaceutics

authors： Zencirci N,Griesser UJ,Gelbrich T,Apperley DC,Harris RK

更新日期：2014-01-06 00:00:00

abstract：:Solid-state NMR (SSNMR) (1)H T1 and T1ρ relaxation times were used to evaluate the miscibility of amorphous solid dispersions of nifedipine (NIF) and polyvinylpyrrolidone (PVP) prepared by three different methods: melt quenching in the typical lab setting, spray drying and melt quenching in the NMR rotor while spinnin...

journal_title：Molecular pharmaceutics

authors： Yuan X,Sperger D,Munson EJ

更新日期：2014-01-06 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：:Dendrimers are being explored in many preclinical studies as drug, gene, and imaging agent delivery systems. Understanding their detailed organ, tissue, cellular uptake, and retention can provide valuable insights into their effectiveness as delivery vehicles and the associated toxicity. This work explores a fluoresce...

journal_title：Molecular pharmaceutics

authors： Lesniak WG,Mishra MK,Jyoti A,Balakrishnan B,Zhang F,Nance E,Romero R,Kannan S,Kannan RM

更新日期：2013-12-02 00:00:00

abstract：:In this paper the preparation of magnetic nanocarriers (MNCs), containing superparamagnetic domains, is reported, useful as potential magnetically targeted drug delivery systems. The preparation of MNCs was performed by using the PHEA-IB-p(BMA) graft copolymer as coating material through the homogenization-solvent eva...

journal_title：Molecular pharmaceutics

authors： Licciardi M,Scialabba C,Fiorica C,Cavallaro G,Cassata G,Giammona G

更新日期：2013-12-02 00:00:00

abstract：:Plant or microbial lectins are known to exhibit potent antiviral activities against viruses with glycosylated surface proteins, yet the mechanism(s) by which these carbohydrate-binding proteins exert their antiviral activities is not fully understood. Hepatitis C virus (HCV) is known to possess glycosylated envelope p...

journal_title：Molecular pharmaceutics

authors： Kachko A,Loesgen S,Shahzad-Ul-Hussan S,Tan W,Zubkova I,Takeda K,Wells F,Rubin S,Bewley CA,Major ME

更新日期：2013-12-02 00:00:00

abstract：:Harmane and norharmane are representative members of the large group of natural β-carboline alkaloids featured with diverse pharmacological activities. In blood, these agents are transported by human serum albumin (HSA) which has a profound impact on the pharmacokinetic and pharmacodynamic properties of many therapeut...

journal_title：Molecular pharmaceutics

authors： Domonkos C,Fitos I,Visy J,Zsila F

更新日期：2013-12-02 00:00:00

abstract：:Polycationic polymers like poly(ethylene imine)s (PEIs) are extensively explored for the nonviral transfer of DNA or small RNAs (siRNAs). To enhance biocompatibility and alter pharmacokinetic properties, hyperbranched PEI was recently grafted with the nonligand oligosaccharides maltose or maltotriose at various degree...

journal_title：Molecular pharmaceutics

authors： Gutsch D,Appelhans D,Höbel S,Voit B,Aigner A

更新日期：2013-12-02 00:00:00

abstract：:Block copolymer micelles (BCMs) have been employed as effective drug delivery systems to solid tumors by virtue of their capacity to transport large therapeutic payloads and passively target tumor sites. Active targeting of nanoparticles (NPs) has been exploited as a means to increase the therapeutic efficacy of NP-ba...

journal_title：Molecular pharmaceutics

authors： Hoang B,Ekdawi SN,Reilly RM,Allen C

更新日期：2013-11-04 00:00:00

abstract：:Understanding in vivo drug release kinetics is critical for the development of nanoparticle-based delivery systems. In this study, we developed a fluorescence resonance energy transfer (FRET) imaging approach to noninvasively monitor in vitro and in vivo cargo release from polymeric nanoparticles. The FRET donor dye (...

journal_title：Molecular pharmaceutics

authors： Zou P,Chen H,Paholak HJ,Sun D

更新日期：2013-11-04 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：: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：:5P12-RANTES is a recently developed chemokine analogue that has shown high level protection from SHIV infection in macaques. However, the feasibility of using 5P12-RANTES as a long-term HIV prevention agent has not been explored partially due to the lack of available delivery devices that can easily be modified for lo...

journal_title：Molecular pharmaceutics

authors： Wang NX,Sieg SF,Lederman MM,Offord RE,Hartley O,von Recum HA

更新日期：2013-10-07 00:00:00

abstract：:2-Methoxyestradiol (2ME), a natural metabolite of estradiol, has antiproliferative and antiangiogenic activity. However, its clinical success is limited due to poor water solubility and poor pharmacokinetic parameters suggesting the need for a delivery vehicle. In this study we evaluated cathepsin B degradable star-sh...

journal_title：Molecular pharmaceutics

authors： Shankar R,Samykutty A,Riggin C,Kannan S,Wenzel U,Kolhatkar R

更新日期：2013-10-07 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：:This work demonstrates the way to achieve efficient and target specific delivery of a graphene quantum dot (GQD) using hyaluronic acid (HA) (GQD-HA) as a targeting agent. HA has been anchored to a GQD that accepts the fascinating adhesive properties of the catechol moiety, dopamine hydrochloride, conjugated to HA, whi...

journal_title：Molecular pharmaceutics

authors： Abdullah-Al-Nahain,Lee JE,In I,Lee H,Lee KD,Jeong JH,Park SY

更新日期：2013-10-07 00:00:00

abstract：:We have identified and characterized a new solid form of trehalose, the δ form (Tδ) using (13)C solid-state NMR spectroscopy (SSNMR). Tδ is formed from dehydrations of trehalose dihydrate (T(h)) performed at or below 100 °C, and it is generated concurrently with the α form of trehalose (Tα) and amorphous trehalose (T(...

journal_title：Molecular pharmaceutics

authors： Pyszczynski SJ,Munson EJ

更新日期：2013-09-03 00:00:00

abstract：:Although nanocarriers hold promise for cancer chemotherapy, their intracellular drug delivery pathways are not fully understood. In particular, the influence of nanocarrier stability on cellular uptake is still uncertain. By physically loading hydrophobic FRET probes, we revealed different intracellular drug delivery ...

journal_title：Molecular pharmaceutics

authors： Lee SY,Tyler JY,Kim S,Park K,Cheng JX

更新日期：2013-09-03 00:00:00

abstract：:The purpose of this study was to examine the melanoma targeting and imaging properties of two new (99m)Tc-labeled Arg-X-Asp-conjugated α-melanocyte stimulating hormone (α-MSH) peptides. RTD-Lys-(Arg(11))CCMSH {c[Asp-Arg-Thr-Asp-DTyr]-Lys-Cys-Cys-Glu-His-DPhe-Arg-Trp-Cys-Arg-Pro-Val-NH2} and RVD-Lys-(Arg(11))CCMSH pept...

journal_title：Molecular pharmaceutics

authors： Flook AM,Yang J,Miao Y

更新日期：2013-09-03 00:00:00

abstract：:Despite significant potential of oligonucleotides (ONs) for therapeutic and diagnostic applications, rapid and widespread intracellular delivery of ONs in cells situated in tissues such as skin, head and neck cavity, and eye has not been achieved. This study was aimed at evaluating the synergistic combination of micro...

journal_title：Molecular pharmaceutics

authors： Luo Z,Ye T,Ma Y,Gill HS,Nitin N

更新日期：2013-08-05 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：:The most abundant polyphenol in green tea, epigallocatechin-3-gallate (EGCg), has recently received considerable attention due to the discovery of numerous health-promoting bioactivities. Despite reports of its poor oral bioavailability, EGCg has been included in many dietary supplement formulations. Conventional pref...

journal_title：Molecular pharmaceutics

authors： Smith AJ,Kavuru P,Arora KK,Kesani S,Tan J,Zaworotko MJ,Shytle RD

更新日期：2013-08-05 00:00:00

abstract：:Hyperbilirubinemia may arise due to inadequate clearance of bilirubin from the body. Bilirubin elimination is a multifaceted process consisting of uptake of bilirubin into the hepatocytes facilitated by OATP1B1 and OATP1B3. Once in the hepatocytes, it is extensively glucuronidated by UGT1A1. Eventually, the glucuronid...

journal_title：Molecular pharmaceutics

authors： Chang JH,Plise E,Cheong J,Ho Q,Lin M

更新日期：2013-08-05 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：:Our previous studies have shown that multidrug resistance protein 2 (MRP2) is overexpressed in tamoxifen-resistant MCF-7 breast cancer cells (TAMR-MCF-7 cells) and forkhead box-containing protein, O subfamily1 (FoxO1), functions as a key regulator of multidrug resistance 1 (MDR1) gene transcription. This study aimed t...

journal_title：Molecular pharmaceutics

authors： Choi HK,Cho KB,Phuong NT,Han CY,Han HK,Hien TT,Choi HS,Kang KW

更新日期：2013-07-01 00:00:00

abstract：:An important aspect to ensure progress in biomedicine is the fundamental understanding of the interaction of cells and tissue with (bio)materials. The consideration of shear stress in drug delivery and/or tissue engineering remains largely unexplored. To illustrate the fundamental relevance, we employ a microfluidic s...

journal_title：Molecular pharmaceutics

authors： Hosta-Rigau L,Städler B

更新日期：2013-07-01 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

abstract：:5-Fluorocytosine (FC), an antifungal drug and a cytosine derivative, has a complex solid-state landscape that challenges its development into a drug product. A total of eight new FC salts, both cytosinium and hemicytosinium, with four strong acids were prepared by controlling acid concentration in the crystallization ...

journal_title：Molecular pharmaceutics

authors： Perumalla SR,Pedireddi VR,Sun CC

更新日期：2013-06-03 00:00:00

abstract：:Intracellular unbound drug concentrations determine affinity to targets in the cell interior. However, due to difficulties in measuring them, they are often overlooked in pharmacology. Here we present a simple experimental technique for the determination of unbound intracellular drug concentrations in cultured cells t...

journal_title：Molecular pharmaceutics

authors： Mateus A,Matsson P,Artursson P

更新日期：2013-06-03 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：:Much interest has been expressed in this work on the role of water diffusivity in the release media as a new parameter for predicting drug release. NMR was used to measure water diffusivity in different media varying in their osmolality and viscosity. Water self-diffusion coefficients in sucrose, sodium chloride, and ...

journal_title：Molecular pharmaceutics

authors： Radwan A,Ebert S,Amar A,Münnemann K,Wagner M,Amidon GL,Langguth P

更新日期：2013-06-03 00:00:00

abstract：:Diagnostic imaging of the liver by ultrasound, computed tomography (CT) and magnetic resonance tomography (MRT) is generally limited to the visualization of the morphology. In order to exploit the intriguing liver tropism of the human hepatitis B virus (HBV) for molecular imaging of the liver, peptidic tracers derived...

journal_title：Molecular pharmaceutics

authors： Müller T,Mehrle S,Schieck A,Haberkorn U,Urban S,Mier W

更新日期：2013-06-03 00:00:00

abstract：:Metallacarborane moieties have been identified as promising pharmacophores. The pharmaceutical use of such compounds is, however, complicated by their low solubility and tendency to self-assemble in aqueous solution. In this work, we estimated the solubilities of a vast series of metallacarboranes [cobalt bis(dicarbol...

journal_title：Molecular pharmaceutics

authors： Rak J,Dejlová B,Lampová H,Kaplánek R,Matějíček P,Cígler P,Král V

更新日期：2013-05-06 00:00:00

abstract：:The Biopharmaceutical Classification System (BCS), which is a scientific approach to categorize active drug ingredient based on its solubility and intestinal permeability into one of the four classes, has been used to set the pharmaceutical quality standards for drug products in western society. However, it has receiv...

journal_title：Molecular pharmaceutics

authors： Fong SY,Liu M,Wei H,Löbenberg R,Kanfer I,Lee VH,Amidon GL,Zuo Z

更新日期：2013-05-06 00:00:00

abstract：:Cell penetrating peptides (CPPs) have been extensively studied in polyelectrolyte complexes as a means to enhance the transfection efficiency of plasmid DNA (pDNA). Increasing the molecular weight of CPPs often enhances gene expression but poses a risk of increased cytotoxicity and immunogenicity compared to low molec...

journal_title：Molecular pharmaceutics

authors： Alhakamy NA,Berkland CJ

更新日期：2013-05-06 00:00:00

abstract：:Cancer stem cells (CSCs) are a subpopulation of cancer cells that have stem cell-like properties and are thought to be responsible for tumor drug resistance and relapse. Therapies that can effectively eliminate CSCs will, therefore, likely inhibit tumor recurrence. The objective of our study was to determine the susce...

journal_title：Molecular pharmaceutics

authors： Sadhukha T,Niu L,Wiedmann TS,Panyam J

更新日期：2013-04-01 00:00:00

abstract：:Heparin is a highly sulfated polysaccharide that serves biologically relevant roles as an anticoagulant and anticancer agent. While it is well-known that modification of heparin's sulfation pattern can drastically influence its ability to bind growth factors and other extracellular molecules, very little is known abou...

journal_title：Molecular pharmaceutics

authors： Raman K,Mencio C,Desai UR,Kuberan B

更新日期：2013-04-01 00:00:00