Dual targeted polymeric nanoparticles based on tumor endothelium and tumor cells for enhanced antitumor drug delivery.

abstract：:Three different types of atom accessibility descriptors are investigated in relation to site of metabolism predictions. To enable the integration of local accessibility we have constructed 2DSASA, a method for the calculation of the atomic solvent accessible surface area that is independent of 3D coordinates. The meth...

journal_title：Molecular pharmaceutics

authors： Rydberg P,Rostkowski M,Gloriam DE,Olsen L

更新日期：2013-04-01 00:00:00

abstract：:Constitutive activation of signal transducer and activator of transcription 3 (STAT3) in tumor cells and tumor associated dendritic cells (DCs) plays a major role in the progression of cancer. JSI-124 (cucurbitacin I) is a potent inhibitor of STAT3; however, its poor solubility and nonspecificity limit its effectivene...

journal_title：Molecular pharmaceutics

authors： Garg SM,Vakili MR,Molavi O,Lavasanifar A

更新日期：2017-08-07 00:00:00

abstract：:A redox-sensitive prodrug, octreotide(Phe)-polyethene glycol-disulfide bond-paclitaxel [OCT(Phe)-PEG-ss-PTX], was successfully developed for targeted intracellular delivery of PTX. The formulation emphasizes long-circulation-time polymer-drug conjugates, combined targeting based on EPR and OCT-receptor mediated endocy...

journal_title：Molecular pharmaceutics

authors： Yin T,Wu Q,Wang L,Yin L,Zhou J,Huo M

更新日期：2015-08-03 00:00:00

abstract：:Cyclic RGD (cRGD) peptide-conjugated boronated albumin was developed to direct toward integrin αvβ3, which overexpresses on many cancer cells. A stepwise conjugation of c[RGDfK(Mal)] and maleimide-conjugated closo-dodecaborate (MID) to bovine serum albumin (BSA) afforded cRGD-MID-BSA, which was noncytotoxic toward bot...

journal_title：Molecular pharmaceutics

authors： Kawai K,Nishimura K,Okada S,Sato S,Suzuki M,Takata T,Nakamura H

更新日期：2020-10-05 00:00:00

abstract：:Cancer is a leading cause of death within developed nations, and part of this morbidity is due to difficulties associated with its treatment. Currently, anticancer therapy relies heavily upon the administration of small molecule cytotoxic drugs that attack both cancerous and noncancerous cells due to limited selectivi...

journal_title：Molecular pharmaceutics

authors： Kaminskas LM,McLeod VM,Porter CJ,Boyd BJ

更新日期：2012-03-05 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：:This research determined the uptake of individual components of topically applied microemulsions into the stratum corneum (SC) and assessed their molecular effects on skin barrier function. The microemulsions comprised oleic acid, Tween20, Transcutol and water. The effects of selected formulations, and of the individu...

journal_title：Molecular pharmaceutics

authors： Hathout RM,Mansour S,Mortada ND,Geneidi AS,Guy RH

更新日期：2010-08-02 00:00:00

abstract：:Glutamic acid is a commonly used linker to form dimeric peptides with enhanced binding affinity than their corresponding monomeric counterparts. We have previously labeled NOTA-Bn-NCS-PEG3-E[c(RGDyK)]2 (NOTA-PRGD2) [1] with [(18)F]AlF and (68)Ga for imaging tumor angiogenesis. The p-SCN-Bn-NOTA was attached to E[c(RGD...

journal_title：Molecular pharmaceutics

authors： Lang L,Ma Y,Kiesewetter DO,Chen X

更新日期：2014-11-03 00:00:00

abstract：:In this study, a facile strategy for efficient codelivery of gene and drug was developed. Using a coprecipitation method, doxorubicin hydrochloride (DOX), an antitumor drug, and p53 expression plasmid were encapsulated in alginate/CaCO(3)/DNA/DOX nanoparticles with high encapsulation efficiency. The in vitro cell inhi...

journal_title：Molecular pharmaceutics

authors： Zhao D,Liu CJ,Zhuo RX,Cheng SX

更新日期：2012-10-01 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：: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：:The maytansinoid antibody-drug conjugates (ADCs) in clinical development for cancer therapy each contain a derivative of the microtubule-targeting agent, maytansine, covalently attached to the antibody via an engineered linker. A sample of any of these conjugates contains molecules with different numbers of maytansino...

journal_title：Molecular pharmaceutics

authors： Goldmacher VS,Amphlett G,Wang L,Lazar AC

更新日期：2015-06-01 00:00:00

abstract：:Microcrystalline vinpocetine, coground with cross-linked polyvinylpyrrolidone, affords hybrids containing nanosized drug nanocrystals, the size and size distributions of which depend on milling times and drug-to-polymer weight ratios. Using an innovative approach to microstructural characterization, we analyzed wide-a...

journal_title：Molecular pharmaceutics

authors： Hasa D,Giacobbe C,Perissutti B,Voinovich D,Grassi M,Cervellino A,Masciocchi N,Guagliardi A

更新日期：2016-09-06 00:00:00

abstract：:Folate receptor (FR) targeting is an attractive strategy for nuclear imaging of cancer and activated macrophages through application of folic acid radioconjugates. However, significant renal accumulation of folate radioconjugates and hence exceedingly high emission of radiation from the kidneys may mask uptake of radi...

journal_title：Molecular pharmaceutics

authors： Müller C,Reber J,Schlup C,Leamon CP,Schibli R

更新日期：2013-03-04 00:00:00

abstract：:Carbonic anhydrase IX (CAIX) plays an important role in glioma cell proliferation, invasion, metastasis, and resistance to radiotherapy and chemotherapy. An effective and noninvasive PET molecular imaging agent targeting CAIX would help its diagnosis and treatment but is not currently available. Recently, a low-molecu...

journal_title：Molecular pharmaceutics

authors： Yang X,Zhu H,Yang X,Li N,Huang H,Liu T,Guo X,Xu X,Xia L,Deng C,Tian X,Yang Z

更新日期：2019-04-01 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：:The poor therapeutic efficacy of hydrophobic chemotherapeutic drugs is an intrinsic limitation to successful chemotherapy. In the present study, a multitask delivery system based on arginine-glycine-aspartic acid peptide (RGD) decorated vitamin E succinate (VES)-grafted-chitosan oligosaccharide (CSO)/RGD-conjugated d-...

journal_title：Molecular pharmaceutics

authors： Chen Y,Feng S,Liu W,Yuan Z,Yin P,Gao F

更新日期：2017-04-03 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：:Gemcitabine (GEM), a first-line chemotherapy for pancreatic cancer undergoes rapid metabolism and develops chemoresistance after repeated administration. We previously demonstrated that the combination of GEM and miR-205 provides an effective therapeutic strategy to sensitize GEM-resistant pancreatic cancer cells. Sin...

journal_title：Molecular pharmaceutics

authors： Mondal G,Almawash S,Chaudhary AK,Mahato RI

更新日期：2017-09-05 00:00:00

abstract：:Due to overexpression of glycyrrhetinic acid (GA) receptor in liver cancer cells, glycyrrhetinic acid modified recombinant human serum albumin (rHSA) nanoparticles for targeting liver tumor cells may result in increased therapeutic efficacy and decreased adverse effects of cancer therapy. In this study, doxorubicin (D...

journal_title：Molecular pharmaceutics

authors： Qi WW,Yu HY,Guo H,Lou J,Wang ZM,Liu P,Sapin-Minet A,Maincent P,Hong XC,Hu XM,Xiao YL

更新日期：2015-03-02 00:00:00

abstract：:Lipid-based drug delivery systems have been vastly investigated as a pharmaceutical method to enhance oral absorption of lipophilic drugs. However, these vehicles not only affect drug bioavailability but may also have an impact on gastric emptying, drug disposition, lymphatic absorption and be affected by lipid digest...

journal_title：Molecular pharmaceutics

authors： Izgelov D,Regev A,Domb AJ,Hoffman A

更新日期：2020-06-01 00:00:00

abstract：:Current chemotherapy strategies for second-line treatment of relapsed ovarian cancer are unable to effectively treat residual disease post-cytoreduction. The findings presented herein suggest that tissue penetration of drug is not only an issue for large, unresectable tumors, but also for invisible, microscopic lesion...

journal_title：Molecular pharmaceutics

authors： Eetezadi S,De Souza R,Vythilingam M,Lessa Cataldi R,Allen C

更新日期：2015-11-02 00:00:00

abstract：:How genotypic variation results in phenotypic differences is still a challenge for biology. In the field of drug metabolism, the means by which specific cytochrome P4502D6 (CYP2D6) genotypes yield different phenotypes at various levels (molecular, cellular, and organismal) is an important question, as differences in C...

journal_title：Molecular pharmaceutics

authors： Gao J,Tian X,Zhou J,Cui MZ,Zhang HF,Gao N,Wen Q,Qiao HL

更新日期：2017-03-06 00:00:00

abstract：:Achieving effective gene therapy for glioma depends on gene delivery systems. The gene delivery system should be able to cross the blood-brain barrier (BBB) and further target glioma at its early stage. Active brain tumor targeted delivery can be achieved using the "Trojan horse" technology, which involves either endo...

journal_title：Molecular pharmaceutics

authors： Liu Y,He X,Kuang Y,An S,Wang C,Guo Y,Ma H,Lou J,Jiang C

更新日期：2014-10-06 00:00:00

abstract：:Our work has focused on defining the utility of fluorine (19F)-labeled bile acid analogues and magnetic resonance imaging (MRI) to identify altered bile acid transport in vivo. In the current study, we explored the ability of this approach to differentiate fibroblast growth factor-15 (FGF15)-deficient from wild-type (...

journal_title：Molecular pharmaceutics

authors： Metry M,Felton J,Cheng K,Xu S,Ai Y,Xue F,Raufman JP,Polli JE

更新日期：2018-11-05 00:00:00

abstract：:The objective of this study is to synthesize and evaluate acute toxicity of the bacterial cellulose (BC)/acrylamide (Am) hydrogels as noncytotoxic and biocompatible oral drug delivery vehicles. A novel series of solubilized BC/Am hydrogels were synthesized using a microwave irradiation method. The hydrogels were chara...

journal_title：Molecular pharmaceutics

authors： Pandey M,Mohamad N,Amin MC

更新日期：2014-10-06 00:00:00

abstract：:Dissolution is a crucial process for the oral delivery of drug products. Before being absorbed through epithelial cell membranes to reach the systemic circulation, drugs must first dissolve in the human gastrointestinal (GI) tract. In vivo and in vitro dissolutions are complex because of their dependency upon the drug...

journal_title：Molecular pharmaceutics

authors： Salehi N,Al-Gousous J,Mudie DM,Amidon GL,Ziff RM,Amidon GE

更新日期：2020-10-05 00:00:00

abstract：:Therapeutic efficacy of nanocarriers can be amplified by active targeting and overcoming the extracellular matrix associated barriers of tumors. The aim of the present study was to investigate the effect of oral antifibrotic agent (telmisartan) on tumor uptake and anticancer efficacy of EphA2 receptor targeted liposom...

journal_title：Molecular pharmaceutics

authors： Patel K,Doddapaneni R,Sekar V,Chowdhury N,Singh M

更新日期：2016-06-06 00:00:00

abstract：:Low molecular weight nucleoside gelators hold great promise in drug delivery and particularly for the delivery of biologics because of their excellent biocompatibility. However, the influence of these gelators on protein aggregation inhibition has not yet been studied. Protein aggregation is the most significant cause...

journal_title：Molecular pharmaceutics

authors： Johnson L,Faidra Angelerou MG,Surikutchi BT,Allen S,Zelzer M,Marlow M

更新日期：2019-01-07 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