Pharmacokinetics, Pharmacodynamics, and Efficacy of a Novel Long-Acting Human Growth Hormone: Fc Fusion Protein.

abstract：:The success of targeted cancer therapy largely relies upon the selection of target and the development of efficient therapeutic agents that specifically bind to the target. In the current study, we chose a cannabinoid CB2 receptor (CB2R) as a new target and used a CB2R-targeted photosensitizer, IR700DX-mbc94, for phot...

journal_title：Molecular pharmaceutics

authors： Jia N,Zhang S,Shao P,Bagia C,Janjic JM,Ding Y,Bai M

更新日期：2014-06-02 00:00:00

abstract：:The purpose of this study was to determine the effect of PEGylation on the interaction of poly(amidoamine) (PAMAM) dendrimer nanocarriers (DNCs) with in vitro and in vivo models of the pulmonary epithelium. Generation-3 PAMAM dendrimers with varying surface densities of PEG 1000 Da were synthesized and characterized. ...

journal_title：Molecular pharmaceutics

authors： Bharatwaj B,Mohammad AK,Dimovski R,Cassio FL,Bazito RC,Conti D,Fu Q,Reineke J,da Rocha SR

更新日期：2015-03-02 00:00:00

abstract：:Most anticancer drugs are poorly soluble and nonspecific, which restricts their clinical application. Drug conjugates, as a prodrug strategy, provide the possibility to overcome these shortcomings, especially combined with nanotechnology. Drug conjugate nanoparticles possess the advantages of high drug loading capacit...

journal_title：Molecular pharmaceutics

authors： Song Q,Wang X,Wang Y,Liang Y,Zhou Y,Song X,He B,Zhang H,Dai W,Wang X,Zhang Q

更新日期：2016-01-04 00:00:00

abstract：:Novel strategy has been developed for fabricating the biocompatible reduction and pH dual-responsive core cross-linked (CCL) micelles as drug delivery system (DDS) for the controlled anticancer drug delivery, via the atom transfer radical polymerization (ATRP) of tert-butyl acrylate (tBA) with N,N'-bis(acryloyl)cystam...

journal_title：Molecular pharmaceutics

authors： Tian K,Jia X,Zhao X,Liu P

更新日期：2017-03-06 00:00:00

abstract：:The barrier epithelia of the cornea and retina control drug and nutrient access to various compartments of the human eye. While ocular transporters are likely to play a critical role in homeostasis and drug delivery, little is known about their expression, localization and function. In this study, the mRNA expression ...

journal_title：Molecular pharmaceutics

authors： Dahlin A,Geier E,Stocker SL,Cropp CD,Grigorenko E,Bloomer M,Siegenthaler J,Xu L,Basile AS,Tang-Liu DD,Giacomini KM

更新日期：2013-02-04 00:00:00

abstract：:Two coamorphous drug-amino acid systems, indomethacin-tryptophan (Ind-Trp) and furosemide-tryptophan (Fur-Trp), were analyzed toward their ease of amorphization and mechanism of coamorphization during ball milling. The two mixtures were compared to the corresponding amorphization of the pure drug without amino acid. P...

journal_title：Molecular pharmaceutics

authors： Jensen KT,Larsen FH,Cornett C,Löbmann K,Grohganz H,Rades T

更新日期：2015-07-06 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：:Cold crystallization of amorphous pharmaceuticals is an important aspect in the search to stabilize amorphous or glassy compounds used as amorphous pharmaceutical ingredients (APIs). In the present work, we report results for the isothermal crystallization of the compound GDC-0276 based on differential scanning calori...

journal_title：Molecular pharmaceutics

authors： Cheng S,Chakravarty P,Nagapudi K,McKenna GB

更新日期：2021-01-04 00:00:00

abstract：:Amino acids derivative are well established molecular probes for diagnosis of a variety of cancer using positron emission tomography (PET). Recently, boramino acid (BAAs) was found as a prospective molecular platform for developing PET tracer. The objective of this study was to develop a 18F-labeled alanine derivative...

journal_title：Molecular pharmaceutics

authors： Liu H,Han Y,Li J,Qin M,Fu Q,Wang C,Liu Z

更新日期：2018-03-05 00:00:00

abstract：:Photodynamic therapy (PDT) has been shown to kill cancer cells and improve survival and quality of life in cancer patients, and numerous new approaches have been considered for maximizing the efficacy of PDT. In this study, a new multifunctional nanophotosensitizer Ce6/GE11-(pH)micelle was developed to target epiderma...

journal_title：Molecular pharmaceutics

authors： Chu WY,Tsai MH,Peng CL,Shih YH,Luo TY,Yang SJ,Shieh MJ

更新日期：2018-04-02 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：:Targeted delivery system would be an interesting platform to enhance the therapeutic effect and to reduce the side effects of anticancer drugs. In this study, we have developed lactobionic acid (LA)-modified chitosan-stearic acid (CS-SA) (CSS-LA) to deliver doxorubicin (DOX) to hepatic cancer cells. The average partic...

journal_title：Molecular pharmaceutics

authors： Yang Y,Yuan SX,Zhao LH,Wang C,Ni JS,Wang ZG,Lin C,Wu MC,Zhou WP

更新日期：2015-02-02 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDAC) is highly chemo-resistant and has an extremely poor patient prognosis, with a survival rate at five years of <8%. There remains an urgent need for innovative treatments. Targeting polyamine biosynthesis through inhibition of ornithine decarboxylase with difluoromethylornithine (...

journal_title：Molecular pharmaceutics

authors： Gitto SB,Pandey V,Oyer JL,Copik AJ,Hogan FC,Phanstiel O 4th,Altomare DA

更新日期：2018-02-05 00:00:00

abstract：:It is a challenge to formulate polymer based nanoparticles of therapeutic proteins as excipients and process conditions affect stability and structural integrity of the protein. Hence, understanding the protein stability and complex aggregation phenomena is an important area of research in therapeutic protein delivery...

journal_title：Molecular pharmaceutics

authors： Rawat S,Gupta P,Kumar A,Garg P,Suri CR,Sahoo DK

更新日期：2015-04-06 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：: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：:Major obstacles in the development of new therapeutic anticancer drugs are the low bioavailability of hydrophilic substances and the nonspecific toxicity toward healthy tissues. As such, cell-targeting oligopeptides have emerged as attractive drug delivery vehicles for a variety of different types of cargo. The recent...

journal_title：Molecular pharmaceutics

authors： Liu Y,Steiniger SC,Kim Y,Kaufmann GF,Felding-Habermann B,Janda KD

更新日期：2007-05-01 00:00:00

abstract：:For the purpose of improving the tumor delivery of doxorubicin (DOX), a kind of peptide-DOXO conjugate was designed and prepared, in which the peptide composed of an albumin-binding domain (ABD) and a tumor-specific internalizing sequence (RGDK or RPARPAR) was conjugated to a (6-maleimidocaproyl) hydrazone derivative ...

journal_title：Molecular pharmaceutics

authors： Liu L,Zhang C,Li Z,Wang C,Bi J,Yin S,Wang Q,Yu R,Liu Y,Su Z

更新日期：2017-11-06 00:00:00

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：: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：:Although tumor-targeting nanovehicles for hepatocellular carcinoma (HCC) chemotherapy have attracted great research and clinic interest, the poor cancer penetration, inefficient cellular uptake, and slow intracellular drug release greatly compromise their therapeutic outcomes. In this work, a multifunctional mixed mic...

journal_title：Molecular pharmaceutics

authors： Zhang J,Zheng Y,Xie X,Wang L,Su Z,Wang Y,Leong KW,Chen M

更新日期：2017-11-06 00:00:00

abstract：:Cationic poly-L-lysine 3H-dendrimers with either 16 or 32 surface amine groups (BHALys [Lys]4 [3H-Lys]8 [NH2]16 and BHALys [Lys]8 [3H-Lys]16 [NH2]32, generation 3 and 4, respectively) have been synthesized and their pharmacokinetics and biodistribution investigated after intravenous administration to rats. The species...

journal_title：Molecular pharmaceutics

authors： Boyd BJ,Kaminskas LM,Karellas P,Krippner G,Lessene R,Porter CJ

更新日期：2006-09-01 00:00:00

abstract：:We have developed a macromolecular prodrug platform based on poly(l-lysine succinylated) (PLS) that targets scavenger receptor A1 (SR-A1), a receptor expressed by myeloid and endothelial cells. We demonstrate the selective uptake of PLS by murine macrophage, RAW 264.7 cells, which was eliminated upon cotreatment with ...

journal_title：Molecular pharmaceutics

authors： Stevens DM,Adiseshaiah P,Dasa SSK,Potter TM,Skoczen SL,Snapp KS,Cedrone E,Patel N,Busman-Sahay K,Rosen EP,Sykes C,Cottrell M,Dobrovolskaia MA,Estes JD,Kashuba ADM,Stern ST

更新日期：2020-10-05 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：:Targeted therapies are emerging as a preferred strategy for treatment of cancer and other diseases. To evaluate the effect of high affinity receptors on the rate and extent of tumor penetration of receptor-targeted drugs, we have characterized the kinetics of folate-rhodamine uptake by folate receptor (FR)-expressing ...

journal_title：Molecular pharmaceutics

authors： Vlashi E,Sturgis JE,Thomas M,Low PS

更新日期：2009-11-01 00:00:00

abstract：:Metastasis is the primary cause resulting in the high mortality of breast cancer. The inherent antimetastasis bioactivity of Pluronic copolymers with a wide range of hydrophilic-lipophilic balance (HLB) including Pluronic L61, P85, P123, F127, F68, and F108 was first explored on metastatic 4T1 breast cancer cells. The...

journal_title：Molecular pharmaceutics

authors： Sun H,Meng Q,Tang S,Su J,Yin Q,Chen L,Gu W,Yu H,Zhang Z,Wang S,Li Y

更新日期：2015-09-08 00:00:00

abstract：:Currently, the screening of new drug candidates for intestinal permeation is typically based on in vitro models which give no information regarding regional differences along the gut. When evaluation of intestinal permeability by region is undertaken, two preclinical rat models are commonly used, the Ussing chamber me...

journal_title：Molecular pharmaceutics

authors： Roos C,Dahlgren D,Sjögren E,Tannergren C,Abrahamsson B,Lennernäs H

更新日期：2017-12-04 00:00:00

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：:Our primary objective is to characterize the self-association of rafoxanide in alkaline media. The second objective is to illustrate the feasibility of using rafoxanide micellar solution as the feed solution to prepare amorphous solid dispersion via spray drying. Rafoxanide is a poorly water-soluble drug. It is a weak...

journal_title：Molecular pharmaceutics

authors： Meng F,Liu T,Schneider E,Alzobaidi S,Gil M,Zhang F

更新日期：2017-05-01 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