Generation and characterization of a new solid form of trehalose.

abstract：:Delta-like ligand 4 (Dll4) expressed in tumor cells plays a key role to promote tumor growth of numerous cancer types. Based on a novel antihuman Dll4 monoclonal antibody (61B), we developed a (64)Cu-labeled probe for positron emission tomography (PET) imaging of tumor Dll4 expression. In this study, 61B was conjugate...

journal_title：Molecular pharmaceutics

authors： Zhou B,Wang H,Liu R,Wang M,Deng H,Giglio BC,Gill PS,Shan H,Li Z

更新日期：2015-10-05 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：:The ATP-binding cassette (ABC) drug transporter ABCG2 can actively efflux a wide variety of chemotherapeutic agents out of cancer cells and subsequently reduce the intracellular accumulation of these drugs. Therefore, the overexpression of ABCG2 often contributes to the development of multidrug resistance (MDR) in can...

journal_title：Molecular pharmaceutics

authors： Wu CP,Hsiao SH,Murakami M,Lu YJ,Li YQ,Huang YH,Hung TH,Ambudkar SV,Wu YS

更新日期：2017-08-07 00:00:00

abstract：:Dysbiosis (alteration of intestinal flora) is associated with various host physiologies, including diseases. The purpose of this study was to clarify the effect of dysbiosis on protein expression levels in mouse liver and kidney by quantitative proteomic analysis, focusing in particular on drug-metabolizing enzymes an...

journal_title：Molecular pharmaceutics

authors： Kuno T,Hirayama-Kurogi M,Ito S,Ohtsuki S

更新日期：2016-08-01 00:00:00

abstract：:Supersaturable active pharmaceutical ingredients (sAPI), such as salts, cocrystals, and amorphous solids, can form supersaturated solutions after dissolving in the gastrointestinal fluids. However, there are cases in which supersaturation is not observed in an in vitro nonsink dissolution test. The purpose of the pres...

journal_title：Molecular pharmaceutics

authors： Oki J,Watanabe D,Uekusa T,Sugano K

更新日期：2019-04-01 00:00:00

abstract：:Terpenoids represent a diverse class of molecules that provide a wealth of opportunities to address many human health and societal issues. The expansive array of structures and functionalities that have been evolved in nature provide an excellent pool of molecules for use in human therapeutics. While this class of mol...

journal_title：Molecular pharmaceutics

authors： Ajikumar PK,Tyo K,Carlsen S,Mucha O,Phon TH,Stephanopoulos G

更新日期：2008-03-01 00:00:00

abstract：:Despite advances in cancer therapies, glioblastoma multiforme treatment remains inefficient due to the brain-blood barrier (BBB) inhibitory activity and to the low temozolomide (TMZ) chemotherapeutic selectivity. To improve therapeutic outcomes, in this work we propose two strategies, (i) photodynamic therapy (PDT) as...

journal_title：Molecular pharmaceutics

authors： Pellosi DS,Paula LB,de Melo MT,Tedesco AC

更新日期：2019-03-04 00:00:00

abstract：:Bioadhesive nanoparticles based on poly(vinyl methyl ether/maleic anhydride) (PVMMA) and poly(ethylene glycol) methyl ether-b-poly(d,l-lactic acid) (mPEG-b-PLA) were produced by the emulsification solvent evaporation method. Paclitaxel was utilized as the model drug, with an encapsulation efficiency of up to 90.2 ± 4....

journal_title：Molecular pharmaceutics

authors： Wang Q,Li C,Ren T,Chen S,Ye X,Guo H,He H,Zhang Y,Yin T,Liang XJ,Tang X

更新日期：2017-10-02 00:00:00

abstract：:The aims of this work were to study pharmacokinetics of randomly selected drugs in plasma and saliva samples in healthy human volunteers, and to introduce a Salivary Excretion Classification System. Saliva and plasma samples were collected for 3-5 half-life values of sitagliptin, cinacalcet, metformin, montelukast, to...

journal_title：Molecular pharmaceutics

authors： Idkaidek N,Arafat T

更新日期：2012-08-06 00:00:00

abstract：:Photodynamic therapy (PDT) is promising for clinical cancer therapy; however, the efficacy was limited as an individual treatment regimen. Here, an approach synergistically combining PDT and nitric oxide (NO) gas therapy along with destruction of the tumor extracellular matrix (ECM) was presented to eliminate cancer. ...

journal_title：Molecular pharmaceutics

authors： Sun Z,Wang X,Liu J,Wang Z,Wang W,Kong D,Leng X

更新日期：2021-01-11 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 small molecule fluorescein is commonly used to guide the repair of cerebral spinal fluid leaks (CSFLs) in the clinic. We modified fluorescein so that it is also visible by positron emission tomography (PET). This probe was used to quantitatively track the fast distribution of small molecules in the CSF of rats. We...

journal_title：Molecular pharmaceutics

authors： Guo H,Kommidi H,Maachani UB,Voronina JC,Zhang W,Magge RS,Ivanidze J,Wu AP,Souweidane MM,Aras O,Ting R

更新日期：2019-08-05 00:00:00

abstract：:2-Methoxyestradiol (2MeO-E2) is an endogenous metabolite of estrogen which was initially considered to be inactive. During the last few decades it has been shown that 2MeO-E2 is a promising anticancer drug. In vitro experiments have demonstrated that it has several anticancer activities, and potential to alleviate hyp...

journal_title：Molecular pharmaceutics

authors： Verenich S,Gerk PM

更新日期：2010-12-06 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：:The primary cause of mortality for glioblastoma (GBM) is local tumor recurrence following standard-of-care therapies, including surgical resection. With most tumors recurring near the site of surgical resection, local delivery of chemotherapy at the time of surgery is a promising strategy. Herein drug-loaded polymer s...

journal_title：Molecular pharmaceutics

authors： Graham-Gurysh E,Moore KM,Satterlee AB,Sheets KT,Lin FC,Bachelder EM,Miller CR,Hingtgen SD,Ainslie KM

更新日期：2018-03-05 00:00:00

abstract：:Diabetic wounds are a worldwide health problem causing extremely heavy public health burden and require effective treatment. Optimal strategies for treating nonhealing diabetic wounds include stem-cell-based therapy and delivery of novel drug substances, such as functional microRNAs (miRNAs); however, miRNA easily deg...

journal_title：Molecular pharmaceutics

authors： Lv Q,Deng J,Chen Y,Wang Y,Liu B,Liu J

更新日期：2020-05-04 00:00:00

abstract：:The development of cancer and fibrotic diseases has been shown to be highly dependent on disregulation of cap-dependent translation. Binding protein eIF4E to N(7)-methylated guanosine capped mRNA has been found to be the rate-limiting step governing translation initiation, and therefore represents an attractive target...

journal_title：Molecular pharmaceutics

authors： Li S,Jia Y,Jacobson B,McCauley J,Kratzke R,Bitterman PB,Wagner CR

更新日期：2013-02-04 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：: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：:Due to the aging of the population, the incidence of neurodegenerative diseases, such as Parkinson's and Alzheimer's, is expected to grow and, hence, the demand for adequate treatment modalities. However, the delivery of medicines into the brain for the treatment of brain-related diseases is hampered by the presence o...

journal_title：Molecular pharmaceutics

authors： Stojanov K,Georgieva JV,Brinkhuis RP,van Hest JC,Rutjes FP,Dierckx RA,de Vries EF,Zuhorn IS

更新日期：2012-06-04 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：: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：: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：:Organic anion transporting polypeptides 1B1 and 1B3 are transporters selectively expressed on the basolateral membrane of the hepatocyte. Several studies reveal that they are involved in drug-drug interactions, cancer, and hyperbilirubinemia. In this study, we developed a set of classification models for OATP1B1 and 1...

journal_title：Molecular pharmaceutics

authors： Kotsampasakou E,Brenner S,Jäger W,Ecker GF

更新日期：2015-12-07 00:00:00

abstract：:The rapid absorptive clearance of drugs delivered to the airways of the lungs means that many inhaled medicines have a short duration of action. The aim of this study was to investigate whether forming polar ion-pairs can modify drug absorption to slow down clearance from the airways. Salbutamol was used as a model dr...

journal_title：Molecular pharmaceutics

authors： Dutton B,Woods A,Sadler R,Prime D,Barlow DJ,Forbes B,Jones SA

更新日期：2020-05-04 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 report the development of sponge Haliclona sp. spicules, referred to as SHS, and its topical application in skin delivery of hydrophilic biomacromolecules, a series of fluorescein isothiocyanate-dextrans (FDs). SHS are silicious oxeas which are sharp-edged and rod-shaped (∼120 μm in length and ∼7 μm in diameter). S...

journal_title：Molecular pharmaceutics

authors： Zhang S,Ou H,Liu C,Zhang Y,Mitragotri S,Wang D,Chen M

更新日期：2017-09-05 00:00:00

abstract：:Nucleic acid biopharmaceuticals are being investigated as potential therapeutics. They need to be incorporated into a biocompatible carrier so as to overcome several biological barriers. Rational development of suitable nanocarriers requires high-quality characterization techniques. While size, concentration, and stab...

journal_title：Molecular pharmaceutics

authors： Zagato E,Vermeulen L,Dewitte H,Van Imschoot G,Vandenbroucke RE,Demeester J,De Smedt SC,Neyts K,Remaut K,Braeckmans K

更新日期：2018-03-05 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：:Amphotericin B is a lifesaving polyene antibiotic used in the treatment of systemic mycoses. Unfortunately, the pharmacological applicability of this drug is limited because of its severe toxic side effects. At the same time, the lack of a well-defined mechanism of selectivity hampers the efforts to rationally design ...

journal_title：Molecular pharmaceutics

authors： Grela E,Wieczór M,Luchowski R,Zielinska J,Barzycka A,Grudzinski W,Nowak K,Tarkowski P,Czub J,Gruszecki WI

更新日期：2018-09-04 00:00:00