abstract：:Positron emission tomography (PET) imaging using 68Ga-labeled bisphosphonates to target bone metastasis could be a valuable tool in cancer diagnosis and monitoring therapeutic treatment. A 68Ga labeled ligand, N,N'-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N'-diacetic acid (HBED-CC) containing one bisphos...

journal_title：Molecular pharmaceutics

authors： Zha Z,Wu Z,Choi SR,Ploessl K,Smith M,Alexoff D,Zhu L,Kung HF

更新日期：2020-05-04 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

abstract：:The acetylcholinesterase inhibitor, acotiamide, improves gastric motility and is clinically used to treat functional dyspepsia. The present study aimed to identify the transporters involved in the distribution of acotiamide in stomach tissue. Acotiamide uptake by the gastric cancer-derived model cell line, Hs746 T, wa...

journal_title：Molecular pharmaceutics

authors： Hirayama M,Hoshino Y,Yoshii K,Toda R,Kawabata Y,Nakanishi T,Tamai I

更新日期：2020-04-06 00:00:00

abstract：:meta-Tetra(hydroxyphenyl)chlorin (mTHPC) is one of the most potent second-generation photosensitizers, clinically used for photodynamic therapy (PDT) of head and neck squamous cell carcinomas. However, improvements are still required concerning its present formulation (i.e., Foscan, a solution of mTHPC in ethanol/prop...

journal_title：Molecular pharmaceutics

authors： Liu Y,Scrivano L,Peterson JD,Fens MHAM,Hernández IB,Mesquita B,Toraño JS,Hennink WE,van Nostrum CF,Oliveira S

更新日期：2020-04-06 00:00:00

abstract：:The 1:1 cocrystal of the antifungal agent ketoconazole with p-aminobenzoic acid was successfully crystallized and systematically characterized by a physical and pharmacological point of view. Crystal structure determination confirmed the cocrystal identity, giving full insight in its crystal packing and degree of diso...

journal_title：Molecular pharmaceutics

authors： Martin F,Pop M,Kacso I,Grosu IG,Miclăuş M,Vodnar D,Lung I,Filip GA,Olteanu ED,Moldovan R,Nagy A,Filip X,Bâldea I

更新日期：2020-03-02 00:00:00

abstract：:Olive pollen is one of the most important causes of respiratory allergy, with Ole e 1 being the most clinically relevant sensitizing allergen. Peptide-based vaccines represent promising therapeutic approaches, but the use of adjuvants is required to strengthen the weak immunogenicity of small peptides. We propose the ...

journal_title：Molecular pharmaceutics

authors： Benedé S,Ramos-Soriano J,Palomares F,Losada J,Mascaraque A,López-Rodríguez JC,Rojo J,Mayorga C,Villalba M,Batanero E

更新日期：2020-03-02 00:00:00

abstract：:The caveolin scaffolding domain peptide (CSP) is being developed for the therapeutic intervention of a lethal lung disease, idiopathic pulmonary fibrosis. While direct respiratory delivery of CSP7 (a 7-mer fragment of CSP) is considered an effective route, proper formulation and processing of the peptide are required....

journal_title：Molecular pharmaceutics

authors： Zhang Y,MacKenzie B,Koleng JJ,Maier E,Warnken ZN,Williams RO 3rd

更新日期：2020-02-03 00:00:00

abstract：:In women with human epidermal growth factor 2 (HER2)-positive breast cancer, the improved control of systemic disease with new therapies has unmasked brain metastases that historically would have remained clinically silent. The efficacy of therapeutic agents against brain metastases is limited by their inability to pe...

journal_title：Molecular pharmaceutics

authors： Wyatt EA,Davis ME

更新日期：2020-02-03 00:00:00

abstract：:Human epidermal growth factor receptor 2 (HER2) is a biomarker in breast cancer, and its overexpression is required to initiate therapies using HER2-targeted antibodies. Although trastuzumab is one of the most effective therapeutic antibodies in HER2-overexpressing breast cancer, a significant number of patients do no...

journal_title：Molecular pharmaceutics

authors： Pereira PMR,Ragupathi A,Shmuel S,Mandleywala K,Viola NT,Lewis JS

更新日期：2020-01-06 00:00:00

abstract：:Boron neutron capture therapy (BNCT) has received extensive attention as noninvasive cell-level oncotherapy for treating solid cancer tumors. However, boron-containing drugs such as l-boronophenylalanine (BPA) and sodium borocaptate have low boron content and/or poor tumor-targeting ability, limiting their application...

journal_title：Molecular pharmaceutics

authors： Li R,Zhang J,Guo J,Xu Y,Duan K,Zheng J,Wan H,Yuan Z,Chen H

更新日期：2020-01-06 00:00:00

abstract：:The controversy surrounding the use of diphtheria toxin (DT) as a therapeutic agent against tumor cells arises mainly from its unexpected harmfulness to healthy tissues. We encoded the cytotoxic fragment A of DT (DTA) as an objective gene in the Light-On gene-expression system to construct plasmids pGAVPO (pG) and pU5...

journal_title：Molecular pharmaceutics

authors： Xu J,He M,Hou X,Wang Y,Shou C,Cai X,Yuan Z,Yin Y,Lan M,Lou K,Zhao Y,Yang Y,Chen X,Gao F

更新日期：2020-01-06 00:00:00

abstract：:Formulation of a cocrystal into a solid pharmaceutical dosage form entails numerous processing steps during which there is risk of dissociation. In an effort to reduce the number of unit operations, we have attempted the in situ formation of an indomethacin-saccharin (INDSAC) cocrystal during high-shear wet granulatio...

journal_title：Molecular pharmaceutics

authors： Tanaka R,Duggirala NK,Hattori Y,Otsuka M,Suryanarayanan R

更新日期：2020-01-06 00:00:00

abstract：:We report the development of novel tumor-targeted conjugated polymer nanoparticles (CPNPs) carrying iron for chemodynamic therapy (CDT). Tumor cell killing proceeds through ferroptosis, a reactive oxygen species (ROS) mechanism that is not dependent on external activation by, for example, light, as is the case in phot...

journal_title：Molecular pharmaceutics

authors： Jasim KA,Gesquiere AJ

更新日期：2019-12-02 00:00:00

abstract：:Structural features of lysine-conjugated antibody-drug conjugate (ADC) from humanized IgG1 were studied by small-angle X-ray scattering (SAXS). As the physicochemical properties of the cytotoxic drug (payload) and linker may impact the conformational and colloidal stabilities of the conjugated monoclonal antibody (mAb...

journal_title：Molecular pharmaceutics

authors： Law-Hine D,Rudiuk S,Bonestebe A,Ienco R,Huille S,Tribet C

更新日期：2019-12-02 00:00:00

abstract：:Similar to glycolysis, glutaminolysis acts as a vital energy source in tumor cells, providing building blocks for the metabolic needs of tumor cells. To capture glutaminolysis in tumors, 18F-(2S,4R)4-fluoroglutamine ([18F]FGln) and 18F-fluoroboronoglutamine ([18F]FBQ) have been successfully developed for positron emis...

journal_title：Molecular pharmaceutics

authors： Chen J,Li C,Hong H,Liu H,Wang C,Xu M,Han Y,Liu Z

更新日期：2019-12-02 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：:A deep convolutional generative adversarial network (dcGAN) model was developed in this study to screen and design target-specific novel compounds for cannabinoid receptors. In the adversarial process of training, two models, the discriminator D and the generator G, are iteratively trained. D is trained to discover th...

journal_title：Molecular pharmaceutics

authors： Bian Y,Wang J,Jun JJ,Xie XQ

更新日期：2019-11-04 00:00:00

abstract：:Despite holding promise for cancer immunotherapy, the strong pro-inflammatory properties of lipopolysaccharide (LPS) also account for severe localized and systemic side effects, restricting its administrable dosage and the possibility of chronic dosing. Herein, we exploited the surface-active properties of LPS molecul...

journal_title：Molecular pharmaceutics

authors： Shetab Boushehri MA,Yazeji T,Stein V,Lamprecht A

更新日期：2019-11-04 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：:Paracetamol has been one of the most commonly used and prescribed analgesic drugs for more than a hundred years. Despite being generally well tolerated, it can result in high liver toxicity when administered in specific conditions, such as overdose, or in vulnerable individuals. We have synthesized and characterized a...

journal_title：Molecular pharmaceutics

authors： Sodano F,Lazzarato L,Rolando B,Spyrakis F,De Caro C,Magliocca S,Marabello D,Chegaev K,Gazzano E,Riganti C,Calignano A,Russo R,Rimoli MG

更新日期：2019-10-07 00:00:00

abstract：:In this study, the polymer-free electrospinning was performed in order to produce cyclodextrin/ibuprofen inclusion complex nanofibers, which could have potential as the fast dissolving oral drug delivery system. Ibuprofen is a poorly water-soluble nonsteroidal anti-inflammatory drug; however, the water solubility of i...

journal_title：Molecular pharmaceutics

authors： Celebioglu A,Uyar T

更新日期：2019-10-07 00:00:00

abstract：:A combination of microbubbles (MBs) and ultrasound (US) is an emerging method for noninvasive and targeted enhancement of anti-cancer drug uptake. This method showed an increase local drug extravasation in tumor tissue while reducing the systemic adverse effects in various tumor models. The present study aims to evalu...

journal_title：Molecular pharmaceutics

authors： Bressand D,Novell A,Girault A,Raoul W,Fromont-Hankard G,Escoffre JM,Lecomte T,Bouakaz A

更新日期：2019-09-03 00:00:00

abstract：:To predict the outcome of intestinal drug transporter induction on pharmacokinetics, signaling of the DNA message along with messenger RNA (mRNA) transcription and protein translation leading to transporter function must be understood. We quantified the gene expression of PXR and CAR, gene expression and protein abund...

journal_title：Molecular pharmaceutics

authors： Brueck S,Bruckmueller H,Wegner D,Busch D,Martin P,Oswald S,Cascorbi I,Siegmund W

更新日期：2019-09-03 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：:Drug self-delivery systems consisting of small-molecule active drugs with nanoscale features for intracellular delivery without the need for additional polymeric carriers have drawn much attention recently. In this work, we proposed a highly efficient strategy to fabricate protonized and reduction-responsive self-asse...

journal_title：Molecular pharmaceutics

authors： Dong S,He J,Sun Y,Li D,Li L,Zhang M,Ni P

更新日期：2019-09-03 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：:P-glycoprotein (Pgp) is highly expressed on blood-brain barrier (BBB) and glioblastoma (GB) cells, particularly on cancer stem cells (SC). Pgp recognizes a broad spectrum of substrates, limiting the therapeutic efficacy of several chemotherapeutic drugs in eradicating GB SC. Finding effective and safe inhibitors of Pg...

journal_title：Molecular pharmaceutics

authors： Salaroglio IC,Abate C,Rolando B,Battaglia L,Gazzano E,Colombino E,Costamagna C,Annovazzi L,Mellai M,Berardi F,Capucchio MT,Schiffer D,Riganti C

更新日期：2019-08-05 00:00:00

abstract：:Alkylphosphocholine (APC) analogs are a novel class of broad-spectrum tumor-targeting agents that can be used for both diagnosis and treatment of cancer. The potential for clinical translation for APC analogs will strongly depend on their pharmacokinetic (PK) profiles. The aim of this work was to understand how the ch...

journal_title：Molecular pharmaceutics

authors： Zhang RR,Grudzinksi JJ,Mehta TI,Burnette RR,Hernandez R,Clark PA,Lubin JA,Pinchuk AN,Jeffrey J,Longino M,Kuo JS,Weichert JP

更新日期：2019-08-05 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：:Preferential interactions of formulation excipients govern their overall interactions with protein molecules, and molecular dynamics simulations allow for the examination of the interactions at the molecular level. We used molecular dynamics simulations to examine the interactions of sorbitol, sucrose, and trehalose w...

journal_title：Molecular pharmaceutics

authors： Cloutier T,Sudrik C,Mody N,Sathish HA,Trout BL

更新日期：2019-08-05 00:00:00

abstract：:Engineered superparamagnetic iron oxide nanoparticles (SPIONs) have been studied extensively for their localized homogeneous heat generation in breast cancer therapy. However, challenges such as aggregation and inability to produce sub-10 nm SPIONs limit their potential in magnetothermal ablation. We report a facile, ...

journal_title：Molecular pharmaceutics

authors： Alhasan AH,Fardous RS,Alsudir SA,Majrashi MA,Alghamdi WM,Alsharaeh EH,Almalik AM

更新日期：2019-08-05 00:00:00

abstract：:The encapsulation of glucocorticoids, such as dexamethasone, in nanoparticles (NPs) faces two main issues: a low drug loading and the destabilization of the nanoparticle suspension due to drug crystallization. Here, we successfully formulated a prodrug of dexamethasone, dexamethasone palmitate (DXP), into nanoparticle...

journal_title：Molecular pharmaceutics

authors： Lorscheider M,Tsapis N,Simón-Vázquez R,Guiblin N,Ghermani N,Reynaud F,Canioni R,Abreu S,Chaminade P,Fattal E

更新日期：2019-07-01 00:00:00

abstract：:The lack of specificity of traditional cytostatics and increasing resistance of cancer cells represent important challenges in cancer therapy. One of the characteristics of cancer cells is their intrinsic oxidative stress caused by higher metabolic activity, mitochondrial malfunction, and oncogene stimulation. This fe...

journal_title：Molecular pharmaceutics

authors： Majerská M,Jakubec M,Klimša V,Rimpelová S,Král V,Štěpánek F

更新日期：2019-07-01 00:00:00

abstract：:As microRNAs (miRNAs) have been reported to be a type of novel high-value small molecule (SM) drug targets for disease treatments, many researchers are engaged in the field of exploring new SM-miRNA associations. Nevertheless, because of the high cost, adopting traditional biological experiments constrains the efficie...

journal_title：Molecular pharmaceutics

authors： Yin J,Chen X,Wang CC,Zhao Y,Sun YZ

更新日期：2019-07-01 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：:In this study, dinitrosyl iron complexes (DNICs) are shown to deliver nitric oxide (NO) into the cytosol of vascular smooth muscle cells (SMCs), which play a major role in vascular relaxation and contraction. Malfunction of SMCs can lead to hypertension, asthma, and erectile dysfunction, among other disorders. For com...

journal_title：Molecular pharmaceutics

authors： Pectol DC,Khan S,Chupik RB,Elsabahy M,Wooley KL,Darensbourg MY,Lim SM

更新日期：2019-07-01 00:00:00

abstract：:The controlled release of anticancer drugs at the tumor site is a central challenge in treating cancer. To achieve this goal, our strategy was based on tumor-specific targeting and ultrasound-triggered release of an anticancer agent from liposomal nanocarriers. To enhance the ultrasound-triggered drug release, we inco...

journal_title：Molecular pharmaceutics

authors： Zhou C,Xie X,Yang H,Zhang S,Li Y,Kuang C,Fu S,Cui L,Liang M,Gao C,Yang Y,Gao C,Yang C

更新日期：2019-07-01 00:00:00

abstract：:Peritoneal fibrosis (PF) is a common complication of long-term peritoneal dialysis (PD). It is considered as the main reason for dialysis inadequacy and PD withdrawal. Transforming growth factor beta (TGF-β) regulates the expression of stromal cell-derived factor 1 (SDF-1α) and its receptor C-X-C chemokine receptor ty...

journal_title：Molecular pharmaceutics

authors： Asifullah K,Zhou Z,He W,Gao K,Khan MW,Faisal R,Muhammad H,Sun M

更新日期：2019-06-03 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：:In the current study, nanoparticles containing the antimetabolite drug methotrexate (MTX) and the novel tubulin-binding drug pretubulysin (PT) were developed for combination chemotherapy. Polyelectrolyte complexes were formed based on ∼20 nm cationic nanomicelles of lipo-oligomer 454 with the anionic MTX at the molar ...

journal_title：Molecular pharmaceutics

authors： Truebenbach I,Kern S,Loy DM,Höhn M,Gorges J,Kazmaier U,Wagner E

更新日期：2019-06-03 00:00:00