Reduced skin photosensitivity with meta-tetra(hydroxyphenyl)chlorin-loaded micelles based on a poly(2-ethyl-2-oxazoline)-b-poly(d,l-lactide) diblock copolymer in vivo.

abstract：:The purpose of this study was to examine and compare the melanoma targeting and imaging properties of (64)Cu-NOTA-GGNle-CycMSH(hex) {(64)Cu-1,4,7-triazacyclononane-1,4,7-triacetic acid-Gly-Gly-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-CONH2} and (64)Cu-DOTA-GGNle-CycMSH(hex) {(64)Cu-1,4,7,10-tetraazacyclononane-1,4,7,10-tetraac...

journal_title：Molecular pharmaceutics

authors： Guo H,Miao Y

更新日期：2012-08-06 00:00:00

abstract：:Fexofenadine is a nonsedative antihistamine that exhibits good oral bioavailability despite its zwitterionic chemical structure and efflux by P-gp. Evidence exists that multiple uptake and efflux transporters play a role in hepatic disposition of fexofenadine. However, the roles of specific transporters and their inte...

journal_title：Molecular pharmaceutics

authors： Ming X,Knight BM,Thakker DR

更新日期：2011-10-03 00:00:00

abstract：:The effect of a lipidated prodrug of mitomycin C (MLP) on the membrane of a pegylated liposome formulation (PL-MLP), also known as Promitil, was characterized through high-sensitivity differential scanning calorimetry (DSC) and cryo-TEM. The thermodynamic analysis demonstrated that MLP led to the formation of heteroge...

journal_title：Molecular pharmaceutics

authors： Wei X,Patil Y,Ohana P,Amitay Y,Shmeeda H,Gabizon A,Barenholz Y

更新日期：2017-12-04 00:00:00

abstract：:Hyaluronan (HA) is a biocompatible and biodegradable linear polysaccharide which is of interest for tumor targeting through cell surface CD44 receptors. HA binds with high affinity to CD44 receptors, which are overexpressed in many tumors and involved in cancer metastasis. In the present study, we investigated the imp...

journal_title：Molecular pharmaceutics

authors： Qhattal HS,Liu X

更新日期：2011-08-01 00:00:00

abstract：:Safe and effective gene delivery is essential to the success of gene therapy. We synthesized and characterized a novel nonviral gene delivery system in which folate (FA) molecules were functioned as blockers on cationic polyrotaxanes (PR) composed of poly(ethylenimine) (PEI)(600)-grafted α-cyclodextrin rings linearize...

journal_title：Molecular pharmaceutics

authors： Zhou Y,Wang H,Wang C,Li Y,Lu W,Chen S,Luo J,Jiang Y,Chen J

更新日期：2012-05-07 00:00:00

abstract：:Microspheres of bovine serum albumin (BSA) and silk fibroin are produced by applying ultrasound in a biphasic system consisting of an aqueous protein solution and an organic solvent. The protein microspheres are dispersed in an aqueous media where the protein remains at the interface covering the organic solvent. This...

journal_title：Molecular pharmaceutics

authors： Silva R,Ferreira H,Azoia NG,Shimanovich U,Freddi G,Gedanken A,Cavaco-Paulo A

更新日期：2012-11-05 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：: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：: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：:Tumor-associated inflammation has been linked to angiogenesis, metastasis and poor prognosis. The 18 kDa translocator protein (TSPO), also known as the peripheral benzodiazepine receptor (PBR), is expressed in activated immune cells such as macrophages, but also in a number of cancer cell lines such as those of breast...

journal_title：Molecular pharmaceutics

authors： Zheng J,Boisgard R,Siquier-Pernet K,Decaudin D,Dollé F,Tavitian B

更新日期：2011-06-06 00:00:00

abstract：:Tumor endothelial marker 8 (TEM8) is a cell surface receptor that is highly expressed in a variety of human tumors and promotes tumor angiogenesis and cell growth. Antibodies targeting TEM8 block tumor angiogenesis in a manner distinct from the VEGF receptor pathway. Development of a TEM8 imaging agent could aid in pa...

journal_title：Molecular pharmaceutics

authors： Kuo F,Histed S,Xu B,Bhadrasetty V,Szajek LP,Williams MR,Wong K,Wu H,Lane K,Coble V,Vasalatiy O,Griffiths GL,Paik CH,Elbuluk O,Szot C,Chaudhary A,St Croix B,Choyke P,Jagoda EM

更新日期：2014-11-03 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：:The particular characteristics of the tumor microenvironment have the potential to strongly promote tumor growth, metastasis and angiogenesis and induce drug resistance. Therefore, the development of effective, systemic therapeutic approaches specifically based on the tumor microenvironment is highly desirable. Hypoxi...

journal_title：Molecular pharmaceutics

authors： Liu XQ,Xiong MH,Shu XT,Tang RZ,Wang J

更新日期：2012-10-01 00:00:00

abstract：:In this work, we have developed covalent and low molecular weight docetaxel delivery systems based on conjugation with N-acetyl-d-galactosamine and studied their properties related to hepatocellular carcinoma cells. The resulting glycoconjugates have an excellent affinity to the asialoglycoprotein receptor (ASGPR) in ...

journal_title：Molecular pharmaceutics

authors： Petrov RA,Mefedova SR,Yamansarov EY,Maklakova SY,Grishin DA,Lopatukhina EV,Burenina OY,Lopukhov AV,Kovalev SV,Timchenko YV,Ondar EE,Ivanenkov YA,Evteev SA,Vaneev AN,Timoshenko RV,Klyachko NL,Erofeev AS,Gorelkin PV,Bel

更新日期：2021-01-04 00:00:00

abstract：:Here, we report the antiproliferative/cytotoxic properties of 8-hydroxyquinoline (8-HQ) derivatives on HeLa cells in the presence of transition metal ions (Cu(2+), Fe(3+), Co(2+), Ni(2+)). Two series of ligands were tested, the arylvinylquinolinic L1-L8 and the arylethylenequinolinic L9-L16, which can all interact wit...

journal_title：Molecular pharmaceutics

authors： Barilli A,Atzeri C,Bassanetti I,Ingoglia F,Dall'Asta V,Bussolati O,Maffini M,Mucchino C,Marchiò L

更新日期：2014-04-07 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：:Multidrug resistance (MDR), a major obstacle to successful cancer chemotherapy, may be induced by amplification of the MDR1 gene and overexpression of the P-glycoprotein (P-gp), which acts as drug efflux pump decreasing intracellular drug accumulation. In this study, an antisense oligodeoxynucleotide--doxorubicin conj...

journal_title：Molecular pharmaceutics

authors： Ren Y,Wang Y,Zhang Y,Wei D

更新日期：2008-07-01 00:00:00

abstract：:The bladder is an important tissue in which to evaluate xenobiotic drug interactions and toxicities due to the concentration of parent drug and hepatic/enteric-derived metabolites in the urine as a result of renal excretion. Breaching of the barrier provided by the bladder epithelial lining (the urothelium) can expose...

journal_title：Molecular pharmaceutics

authors： Baker SC,Shabir S,Southgate J

更新日期：2014-07-07 00:00:00

abstract：:Nerve damage during surgery is a common morbidity experienced by patients that leaves them with chronic pain and/or loss of function. Currently, no clinically approved imaging technique exists to enhance nerve visualization in the operating room. Fluorescence image-guided surgery has gained in popularity and clinical ...

journal_title：Molecular pharmaceutics

authors： Hackman KM,Doddapaneni BS,Barth CW,Wierzbicki IH,Alani AW,Gibbs SL

更新日期：2015-12-07 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：:Hydrophilic peptides constitute most of the active peptides. They mostly permeate via tight junctions (paracellular pathway) in the intestine. This permeability mechanism restricts the magnitude of their oral absorption and bioavailability. We hypothesized that concealing the hydrophilic residues of the peptide using ...

journal_title：Molecular pharmaceutics

authors： Schumacher-Klinger A,Fanous J,Merzbach S,Weinmüller M,Reichart F,Räder AFB,Gitlin-Domagalska A,Gilon C,Kessler H,Hoffman A

更新日期：2018-08-06 00:00:00

abstract：:Photostability conditions as prescribed by ICH guidelines induced highly reduction-resistant scrambled disulfides that contribute to the population of apparent nonreducible aggregates in an IgG1 mAb. Photoinduced cross-linked species were isolated under reducing conditions using an organic phase size exclusion chromat...

journal_title：Molecular pharmaceutics

authors： Wecksler AT,Yin J,Lee Tao P,Kabakoff B,Sreedhara A,Deperalta G

更新日期：2018-04-02 00:00:00

abstract：:Milk has been used as a vehicle for the delivery of antimalarial drugs during clinical trials to test for a food effect and artefenomel (OZ439) showed enhanced oral bioavailability with milk. However, the nature of the interaction between milk and OZ439 in the gastrointestinal tract remains poorly understood. To under...

journal_title：Molecular pharmaceutics

authors： Salim M,Khan J,Ramirez G,Clulow AJ,Hawley A,Ramachandruni H,Boyd BJ

更新日期：2018-08-06 00:00:00

abstract：:The ultrasmall nanoparticle AGuIX is a versatile platform that tolerates a range of chemical diversity for theranostic applications. Our previous work showed that AGuIX clears rapidly from normal tissues, while durably accumulating within the tumor microenvironment. On this basis, AGuIX was used to detect tumor tissue...

journal_title：Molecular pharmaceutics

authors： Truillet C,Thomas E,Lux F,Huynh LT,Tillement O,Evans MJ

更新日期：2016-07-05 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：:The objective of this study was to enhance oral mucosal permeation of fenretinide by coincorporation of propylene glycol (PG) and menthol in fenretinide/Eudragit RL PO mucoadhesive patches. Fenretinide is an extremely hydrophobic chemopreventive compound with poor tissue permeability. Coincorporation of 5-10 wt % PG (...

journal_title：Molecular pharmaceutics

authors： Wu X,Desai KG,Mallery SR,Holpuch AS,Phelps MP,Schwendeman SP

更新日期：2012-04-02 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 objective of this work was to investigate the feasibility of using a novel granulation technique, namely, fluidized hot melt granulation (FHMG), to prepare gastroretentive extended-release floating granules. In this study we have utilized FHMG, a solvent free process in which granulation is achieved with the aid o...

journal_title：Molecular pharmaceutics

authors： Zhai H,Jones DS,McCoy CP,Madi AM,Tian Y,Andrews GP

更新日期：2014-10-06 00:00:00

abstract：:Process-induced phase transformations (PIPTs) of active pharmaceutical ingredients (APIs) can alter APIs' physicochemical properties and impact performance of pharmaceutical drug products. In this study, we investigated compression-induced amorphization of crystalline posaconazole (POSA), where the impact of mechanica...

journal_title：Molecular pharmaceutics

authors： Huang C,Klinzing G,Procopio A,Yang F,Ren J,Burlage R,Zhu L,Su Y

更新日期：2019-02-04 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