Systemic delivery of stable siRNA-encapsulating lipid vesicles: optimization, biodistribution, and tumor suppression.

abstract：:Barbital is a hypnotic agent that has been intensely studied for many decades. The aim of this work was to establish a clear and comprehensible picture of its polymorphic system. Four of the six known solid forms of barbital (denoted I(0), III, IV, and V) were characterized by various analytical techniques, and the th...

journal_title：Molecular pharmaceutics

authors： Zencirci N,Griesser UJ,Gelbrich T,Apperley DC,Harris RK

更新日期：2014-01-06 00:00:00

abstract：:We report on tailored lipid-polymer hybrid nanoparticles (NPs) delivering nitric oxide (NO) under the control of visible light as a tool for overcoming doxorubicin (DOX) resistance. The NPs consist of a polymeric core and a coating. They are appropriately designed to entrap DOX in the poly(lactide-co-glycolide) core a...

journal_title：Molecular pharmaceutics

authors： Fraix A,Conte C,Gazzano E,Riganti C,Quaglia F,Sortino S

更新日期：2020-06-01 00:00:00

abstract：:The Biopharmaceutical Classification System (BCS) guidance issued by the FDA allows waivers for in vivo bioavailability and bioequivalence studies for immediate-release (IR) solid oral dosage forms only for BCS class I drugs. However, a number of drugs within BCS class III have been proposed to be eligible for biowaiv...

journal_title：Molecular pharmaceutics

authors： Tsume Y,Amidon GL

更新日期：2010-08-02 00:00:00

abstract：:The killing efficacy of doxorubicin from liposome-based delivery carriers has been shown to correlate strongly with its intracellular trafficking and, in particular, its fast and extensive release from the delivery carrier. However, previously explored pH-triggered mechanisms that were designed to become activated dur...

journal_title：Molecular pharmaceutics

authors： Mamasheva E,O'Donnell C,Bandekar A,Sofou S

更新日期：2011-12-05 00:00:00

abstract：:The synthesis and biodistribution of three triazine dendrimers differing in PEGylation are described. Dendrimers 1, 2, and 3 are derived from a common intermediate, dendrimer 4, and vary in molecular mass from 11 to 73 kDa as a result of PEGylation with multiple (theoretically, 16) PEG groups of 0.6, 2, and 5 kDa, res...

journal_title：Molecular pharmaceutics

authors： Lim J,Guo Y,Rostollan CL,Stanfield J,Hsieh JT,Sun X,Simanek EE

更新日期：2008-07-01 00:00:00

abstract：:Cholestasis is a significant risk factor for immediate hepatic failure due to ischemia reperfusion (I/R) injury in patients undergoing liver surgery or transplantation. We recently demonstrated that inhibition of Hedgehog (Hh) signaling with cyclopamine (CYA) before I/R prevents liver injury. In this study we hypothes...

journal_title：Molecular pharmaceutics

authors： Pratap A,Panakanti R,Yang N,Lakshmi R,Modanlou KA,Eason JD,Mahato RI

更新日期：2011-06-06 00:00:00

abstract：:For aggressive brain glioblastoma, the therapy is significantly impaired by blood-brain barrier (BBB) and blood-tumor barrier (BTB). Choosing more than one target from the pool of tumor-stroma interactions is profoundly beneficial to therapeutic approaches. Thus, a multifunctional liposomal system based on anchoring t...

journal_title：Molecular pharmaceutics

authors： Yang ZZ,Gao W,Liu YJ,Pang N,Qi XR

更新日期：2017-04-03 00:00:00

abstract：:The use of adult stem cells for therapeutic purposes has met with great success in recent years. Among several types of adult stem cells, mesenchymal stem cells (MSCs) derived from bone marrow (BM) and other sources have gained popularity for basic research and clinical applications because of their therapeutic potent...

journal_title：Molecular pharmaceutics

authors： Wu H,Ye Z,Mahato RI

更新日期：2011-10-03 00:00:00

abstract：:One hallmark of neuroinflammation is the activation of microglia, which triggers the production and release of reactive oxygen species (ROS), nitrate, nitrite, and cytokines. N-Acetyl cysteine (NAC) is a free radical scavenger that is involved in the intracellular and extracellular detoxification of reactive oxygen sp...

journal_title：Molecular pharmaceutics

authors： Markoutsa E,Xu P

更新日期：2017-05-01 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：:Breast cancer is the second most common cause of cancer-related deaths in women. Chemotherapy is an important treatment modality, and paclitaxel (PTX) is often the first-line therapy for its metastatic form. The two most notable limitations related to PTX-based treatment are the poor hydrophilicity of the drug and the...

journal_title：Molecular pharmaceutics

authors： Satsangi A,Roy SS,Satsangi RK,Vadlamudi RK,Ong JL

更新日期：2014-06-02 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：: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：:The aim of the research work was to develop and characterize a concanavalin-A (Con-A) conjugated gastroretentive multiparticulate delivery system of clarithromycin (CM) for the effective treatment of colonization of Helicobacter pylori (H. pylori). Ethylcellulose (EC) microspheres containing CM were prepared using emu...

journal_title：Molecular pharmaceutics

authors： Jain SK,Jangdey MS

更新日期：2009-01-01 00:00:00

abstract：:Lung-delivered polymer nanoparticles provoked dysfunction of the essential lung surfactant system. A steric shielding of the nanoparticle surface with poloxamers could minimize the unwanted interference of polymer nanoparticles with the biophysical function of lung surfactant. The extent of poly(styrene) and poly(lact...

journal_title：Molecular pharmaceutics

authors： Beck-Broichsitter M,Bohr A,Ruge CA

更新日期：2017-10-02 00:00:00

abstract：:A big hurdle for the use of protein-based drugs is that they are easily degraded by proteases in the human body. In an attempt to solve this problem, we show the possibility to functionalize TM encapsulin nanoparticles with an mEETI-II knottin miniprotein from the cysteine-stabilized knot class. The resulting particle...

journal_title：Molecular pharmaceutics

authors： Klem R,de Ruiter MV,Cornelissen JJLM

更新日期：2018-08-06 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：:Dual-targeted imaging agents have shown improved targeting efficiencies in comparison to single-targeted entities. The purpose of this study was to quantitatively assess the tumor accumulation of a dual-labeled heterobifunctional imaging agent, targeting two overexpressed biomarkers in pancreatic cancer, using positro...

journal_title：Molecular pharmaceutics

authors： Luo H,England CG,Goel S,Graves SA,Ai F,Liu B,Theuer CP,Wong HC,Nickles RJ,Cai W

更新日期：2017-05-01 00:00:00

abstract：:In our previous studies, ethylene glycol-linked amino acid diester prodrugs of oleanolic acid (OA), a Biopharmaceutics Classification System (BCS) class IV drug, designed to target peptide transporter 1 (PepT1) have been synthesized and evaluated. Unlike ethylene glycol, propylene glycol is of very low toxicity in viv...

journal_title：Molecular pharmaceutics

authors： Cao F,Gao Y,Wang M,Fang L,Ping Q

更新日期：2013-04-01 00:00:00

abstract：:Targeted delivery of anticancer drugs to brain tumors, especially glioblastoma multiforme, which is the most frequent and aggressive type, is one of the important objectives in nanomedicine. Vascular endothelial growth factor (VEGF) and its receptor type II (VEGFR2) are promising targets because they are overexpressed...

journal_title：Molecular pharmaceutics

authors： Shein SA,Kuznetsov II,Abakumova TO,Chelushkin PS,Melnikov PA,Korchagina AA,Bychkov DA,Seregina IF,Bolshov MA,Kabanov AV,Chekhonin VP,Nukolova NV

更新日期：2016-11-07 00:00:00

abstract：:Currently, the most prominent barrier to the success of orally delivered paclitaxel (PTX) is the extremely limited bioavailability of delivered therapeutic. In light of this issue, an amphiphilic sulfhydrylated N-deoxycholic acid-N,O-hydroxyethyl chitosan (TGA-DHC) was synthesized to improve the oral bioavailability o...

journal_title：Molecular pharmaceutics

authors： Yu Y,Huo M,Fu Y,Xu W,Cai H,Yao L,Chen Q,Mu Y,Zhou J,Yin T

更新日期：2017-12-04 00:00:00

abstract：:Modifying nanoparticles with targeting peptides which can specifically bind to intestinal epithelium was recently suggested as a strategy to further enhance their ability for the oral delivery of macromolecular drugs. However, few studies were focused on comprehensive understanding of the uptake and transport processe...

journal_title：Molecular pharmaceutics

authors： Zhang J,Zhu X,Jin Y,Shan W,Huang Y

更新日期：2014-05-05 00:00:00

abstract：:Herein, we report on the role of endocytosis in the selective chemotherpeutic toxicity of rhodamine 6G (R6G) based nanomaterials, i.e., nanoGUMBOS, that are derived from a group of uniform materials based on organic salts (GUMBOS). Evaluation of cellular uptake in the presence and absence of endocytosis inhibitors sug...

journal_title：Molecular pharmaceutics

authors： Bhattarai N,Mathis JM,Chen M,Pérez RL,Siraj N,Magut PKS,McDonough K,Sahasrabudhe G,Warner IM

更新日期：2018-09-04 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：:Delivery of plasmid DNA for protein production in mammalian cells is not an efficient process. In this study, the theory that cellular localization of plasmid DNA increases transfection efficiency is examined with an emphasis on the understanding of the cellular association of the components of a ternary transfection ...

journal_title：Molecular pharmaceutics

authors： Guo C,Gemeinhart RA

更新日期：2004-07-01 00:00:00

abstract：:Metallacarborane moieties have been identified as promising pharmacophores. The pharmaceutical use of such compounds is, however, complicated by their low solubility and tendency to self-assemble in aqueous solution. In this work, we estimated the solubilities of a vast series of metallacarboranes [cobalt bis(dicarbol...

journal_title：Molecular pharmaceutics

authors： Rak J,Dejlová B,Lampová H,Kaplánek R,Matějíček P,Cígler P,Král V

更新日期：2013-05-06 00:00:00

abstract：:Recently we characterized an unusual switch in the internalization mechanism of the monomeric and dimeric forms of the cell-penetrating peptide RDLWEMMMVSLACQY. Here, we observed both energy-dependent and energy-independent modes of peptide uptake by the target B-lymphocytes WI-L2-729HF2, suggesting that higher-order ...

journal_title：Molecular pharmaceutics

authors： Kim Y,Lillo A,Moss JA,Janda KD

更新日期：2005-11-01 00:00:00

abstract：:While highly efficacious in treating rheumatoid arthritis (RA), the approved Janus kinase (JAK) inhibitor, Tofacitinib (Tofa, CP-690 550), has dose-dependent toxicities that limit its clinical application. In this study, we have examined whether a prodrug design that targets arthritic joints would enhance Tofa's thera...

journal_title：Molecular pharmaceutics

authors： Wei X,Wu J,Zhao G,Galdamez J,Lele SM,Wang X,Liu Y,Soni DM,Purdue PE,Mikuls TR,Goldring SR,Wang D

更新日期：2018-08-06 00:00:00

abstract：:Antibody-based near-infrared photoimmunotherapy (NIR-PIT) is an attractive strategy for cancer treatment. Tumor cells can be selectively and efficiently killed by the targeted delivery of an antibody-photoabsorber complex followed by exposure to NIR light. Glycoprotein A33 antigen (GPA33) is highly expressed in most h...

journal_title：Molecular pharmaceutics

authors： Wei D,Tao Z,Shi Q,Wang L,Liu L,She T,Yi Q,Wen X,Liu L,Li S,Yang H,Jiang X

更新日期：2020-07-06 00:00:00

abstract：:This study describes the interactions between two amphiphilic molecules with antileishmanial activity, amphotericin B (AmB) and miltefosine [hexadecylphosphocholine (HePC)], the latter being effective by the oral route. The effect of HePC on the aggregation state of AmB in aqueous solution and the interactions between...

journal_title：Molecular pharmaceutics

authors： Ménez C,Legrand P,Rosilio V,Lesieur S,Barratt G

更新日期：2007-03-01 00:00:00