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Journal of Drug Targeting

Yukako Ito, Shinji Kobuchi, Genta Inoue, Eisaku Kakumu, Miki Aoki, Toshiyuki Sakaeda, Kanji Takada
Capsaicin-loaded dissolving microneedles (DMNs) were prepared to investigate the analgesic effect of capsaicin on the skin. The dimensions of each microneedle were as follows: diameter of the basement, 17 mm; length, 500 μm; and width, 300 μm. The average capsaicin content in the DMNs loaded with a low and high dose of capsaicin was 8.8 ± 0.5 mg and 12.5 ± 0.4 mg. Almost all of the capsaicin, 99.3 ± 4.1% and 99.7 ± 2.2% for low-dose and high-dose DMNs were released within 20 min. High amounts of capsaicin were recovered with 102...
December 5, 2016: Journal of Drug Targeting
Nzungize Lambert, Abualgasim Elgaili Abdalla, Xiangke Duan, Jianping Xie
Mycobacterium tuberculosis (M. tuberculosis), the causative agent of tuberculosis, uses various tactics to resist on antibiotics and evade host immunity. To control tuberculosis, antibiotics with novel mechanisms of action are urgently needed. Emerging new antibiotics and underlying novel drug targets are summarized in this paper.
December 2, 2016: Journal of Drug Targeting
Yuan Xie, Anqiang Wang, Jianzhen Lin, Liangcai Wu, Haohai Zhang, Xiaobo Yang, Xueshuai Wan, Ruoyu Miao, Xinting Sang, Haitao Zhao
Monopolar spindle1 (Mps1, also known as TTK) is the core component of the spindle assembly checkpoint, which functions to ensure proper distribution of chromosomes to daughter cells. Mps1 is hardly detectable in normal organs except the testis and placenta. However, high levels of Mps1 are found in many types of human malignancies, including glioblastoma, thyroid carcinoma, breast cancer, and other cancers. Several Mps1 inhibitors can inhibit the proliferation of cancer cells and exhibit demonstrable survival benefits...
December 1, 2016: Journal of Drug Targeting
Yu-Jie Liu, Xiao-Qian Dou, Fang Wang, Jing Zhang, Xiao-Lin Wang, Gui-Li Xu, Shen-Si Xiang, Xin Gao, Jie Fu, Hai-Feng Song
Tumour immunosuppressive microenvironments inhibit antigen-specific cellular responses and interfere with CpG-mediated immunotherapy. Overcoming tumour microenvironment (TME) immunosuppression is an important strategy for effective therapy. This study investigated the ability of a tumour-targeting IL-4Rα aptamer-liposome-CpG ODN delivery system to introduce CpG into tumours and overcome the immunosuppressive TME. The IL-4Rα-liposome-CpG delivery system was prepared. FAM-CpG visualisation was used to demonstrate tumour targeting in vitro and in vivo...
December 1, 2016: Journal of Drug Targeting
Zhu Xiali, Yingjie Zhang, Heqing Huang, Huijuan Zhang, Lin Hou, Zhenzhong Zhang
Recent studies have identified that CuS nanocrystal (CuS NCs) could be used as a new class of promising photo-thermal agents due to their excellent plasmonic absorption abilities in a wide near-infrared (NIR) region. However, most of nanocarriers lack target capacity for combining chemotherapy and photothermal therapy effects. Herein, we reported chitosan (CS)-encapsulated and folic acid (FA)-modified nanoparticles (NPs) simultaneously loading with functionalized CuS NCs and docetaxel (DTX) (FA-DTX-PVP/CuS-NPs)...
November 30, 2016: Journal of Drug Targeting
Mohammad Arabpour, Robbert Cool, Klaas Nico Faber, Wim J Quax, Hidde J Haisma
Activated Hepatic Stellate Cells (HSCs) are known to play a central role in liver fibrosis and their elimination is a crucial step towards the resolution and reversion of liver fibrosis. Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is a molecule that may contribute to the apoptotic removal of activated HSC through binding to its dedicated receptors. In the present study, we investigated the potential application of recombinant receptor-specific TRAIL proteins in the efficient elimination of activated HSCs...
November 25, 2016: Journal of Drug Targeting
Leila Rahbarnia, Safar Farajnia, Hossein Babaei, Jafar Majidi, Kamal Veisi, Vahideh Ahmadzadeh, Bahman Akbari
Phage display technology as a selection-based system is an attractive method for evolution of new biological drugs. Unique ability of phage libraries for displaying proteins on bacteriophage surfaces enable them to make a major contribution in diverse fields of researches related to the diagnosis and therapy of diseases. One of the great challenges facing researchers is the modification of phage display technology and the development of new applications. This article reviews the molecular basis of phage display library, and summarizes the novel and specific applications of this technique in the field of biological drugs development including therapeutic antibodies, peptides, vaccines, and catalytic antibodies...
November 21, 2016: Journal of Drug Targeting
Shalmali Bivalkar-Mehla, Rajeev Mehla, Ashok Chauhan
Persistent human immunodeficiency virus 1 (HIV-1) infection provokes immune activation and depletes CD4(+ )lymphocytes, leading to acquired immunodeficiency syndrome. Uninterrupted administration of combination antiretroviral therapy (cART) in HIV-infected patients suppresses viral replication to below the detectable level and partially restores the immune system. However, cART-unresponsive residual HIV-1 infection and elusive transcriptionally silent but reactivatable viral reservoirs maintain a permanent viral DNA blue print...
November 14, 2016: Journal of Drug Targeting
Min Jun Kim, Yong Hwa Hwang, Yong Hee Kim, Dong Yun Lee
Pancreatic islet transplantation is a promising treatment for treatment of type 1 diabetes; however, transplantation outcomes have been disappointing due to early graft loss that is mediated by many immune responses. Immune cells not only directly damaged islet but also produced reactive oxygen species (ROS), which is highly toxic to islet cells. Metallothionein (MT) can provide protection against oxidative stress by scavenging various range of ROS including superoxide, hydroxyl radical, hydrogen peroxide, and nitric oxide...
November 10, 2016: Journal of Drug Targeting
Maliheh Ghadiri, Paul M Young, Wolfgang Jarolimek, Georges E R Grau, Brian Oliver, Daniela Traini
The epithelial barrier in the respiratory system is a major obstacle for drug delivery to the systemic circulation both locally and systemically in the lung. Epithelial barrier hinders the transport of large macromolecules or polar drugs. Essential components of this epithelial fence are physical intercellular structures termed tight junctions. Therefore, modulating tight junctions can enhance paracellular transport across epithelial barrier. In this study, the effect of some of non-specific tight junction modulators (TJMs); (Sodium (Na) decanoate, oleic acid and ethyleneglycol-bis-(β-aminoethyl ether)-N, N'-tetraacetic acid (EGTA)) with established effect on intestinal tight junctions was evaluated for its effects on bronchial epithelial cells (Calu-3 cells)...
November 8, 2016: Journal of Drug Targeting
Irfan Ullah, Kunho Chung, Jagadish Beloor, Jongkil Kim, Minyoung Cho, Nahyun Kim, Kuen Yong Lee, Priti Kumar, Sang-Kyung Lee
siRNA entrapment within endosomes is a significant problem encountered with siRNA delivery platforms that co-opt receptor mediated entry pathways. Attachment of a cell penetrating peptide (CPP), such as nona-arginine (9R) to a cell receptor-binding ligand like the Rabies virus glycoprotein, RVG, allows effective siRNA delivery to the cytoplasm by non-endocytic pathways, but a significant amount of siRNA complexes also enters the cell by ligand-induced receptor endocytosis and remain localized in endosomes. Here, we report that the incorporation of trileucine (3 Leu) residues as an endo-osmolytic moiety in the peptide improves endosomal escape and intracellular delivery of siRNA...
November 8, 2016: Journal of Drug Targeting
Anup Jose, Suman Labala, Venkata Vamsi Krishna Venuganti
Skin cancer is one of the most widely prevalent cancer types with over expression of multiple oncogenic signaling molecules including STAT3. Curcumin is a natural compound with effective anti-cancer properties. The objective of this work was to investigate the liposomal co-delivery of curcumin and STAT3 siRNA by non-invasive topical iontophoretic application to treat skin cancer. Curcumin was encapsulated in cationic liposomes and then complexed with STAT3 siRNA. The liposomal nanocomplex was characterized for particle size, zeta-potential, drug release and stability...
November 7, 2016: Journal of Drug Targeting
Theresa M Allen
No abstract text is available yet for this article.
October 31, 2016: Journal of Drug Targeting
Keren Turjeman, Yechezkel Barenholz
BACKGROUND: Steroids are the most efficacious anti-inflammatory agents. However, their toxicities and side-effects compromise their clinical application. Various strategies and major efforts were dedicated for formulating viable liposomal glucocorticosteroids (GCs), so far none of these were approved. OBJECTIVES: To evaluate these approaches for formulating GC-delivery systems, especially liposomes, and with focus on the Barenholz Lab experience. METHODS: We developed PEGylated nano-liposomes (NSSL) remotely loaded with water-soluble amphipathic weak acid GC-prodrugs...
October 28, 2016: Journal of Drug Targeting
Min Ren, Ying Wang, Xiaodong Wu, Suxia Ge, Benzhong Wang
OBJECTIVE: The study aimed to investigate the effects of combination treatment of curcumin and β-interferon (IFN-β)/retinoic acid (RA) on breast cancer cells, including cell viability, apoptosis and migration, and to determine the mechanisms related to GRIM-19 through STAT3-dependent and STAT3-independent pathways. METHODS: The following groups were used for the in vitro experiment: control siRNA, GRIM-19 siRNA, IFN-β/RA and IFN-β/RA + curcumin. Cell viability is by the MTT method, cell apoptosis by flow cytometry and cell migration by wound healing experiment; GRIM-19, STAT3, survivin, Bcl-2, GADD153 and COX-2 expression was measured by Western blot...
October 16, 2016: Journal of Drug Targeting
David Needham, Amina Arslanagic, Kasper Glud, Pablo Hervella, Leena Karimi, Poul-Flemming Høeilund-Carlsen, Koji Kinoshita, Jan Mollenhauer, Elisa Parra, Anders Utoft, Prasad Walke
The story starts in Basel at CLINAM in 2013, when I asked Pieter about making nanoparticles and he advised me to "try this solvent-exchange method we have developed for making limit sized particles". We are particularly interested in what are "limit size materials" because we want to test the feasibility of an idea: could we design, make, develop, and test the concept for treating metastatic cancer by, "Putting the Drug in the Cancer's Food? "Limit size" is the size of the cancer's food, ? the common Low Density Lipoprotein, (LDL) ~20 nm diameter...
October 16, 2016: Journal of Drug Targeting
Weipeng Zhang, Xiaowei Zheng, Ti Meng, Haisheng You, Yalin Dong, Jianfeng Xing, Chen Siying
Patient SE translation (SET) is a carcinogen in facilitating cellular growth and proliferation, and promoting tumorigenesis and metastasis. The present study was to investigate the resistance mechanisms associated with SET in paclitaxel-induced human breast cancer cells. The different expressions of SET, ATP-binding cassette (ABC) transporters and PI3K/Akt pathway between paclitaxel sensitive MCF-7/S and paclitaxel resistant MCF-7/PTX cells were identified using Western blotting. We adopted plasmid transfection to upregulate SET in MCF-7/S cells and a novel SET antagonist COG112 to decrease SET in MCF-7/PTX cells...
October 10, 2016: Journal of Drug Targeting
Nazanin Rahmanian, Morteza Eskandani, Jaleh Barar, Yadollah Omidi
Rapid progresses in nanotechnology fields have led us to use a number of advanced nanomaterials (NMs) for engineering smart multifunctional nanoparticles (NPs)/nanosystems (NSs) for targeted diagnosis and therapy of various diseases including different types of malignancies. For the effective therapy of any type of solid tumor, the treatment modality should ideally solely target the aberrant cancerous cells/tissue with no/trivial impacts on the healthy cells. One approach to achieve such unprecedented impacts can be fulfilled through the use of seamless multimodal NPs/NSs with photoacoustic properties that can be achieved using advanced NMs such as graphene oxide (GO)...
October 6, 2016: Journal of Drug Targeting
Chang Liu, Sen Yao, Xuqian Li, Feng Wang, Yanyan Jiang
iRGD (internalizing RGD) with high affinity to αν integrins was reported to enhance tumor penetrability by binding to neuropilin-1 (NRP-1). Based on our previous study, chitosan surface-modified poly (lactide-co-glycolides) nanoparticles (PLGA/CS NPs), loaded with carmustine (BCNU) and its sensitizer (O(6)-benzylguanine, BG) showed stronger anti-tumor effect than free drugs. In present study, PLGA/CS NPs (NPs) with core-shell structure were prepared and modified with iRGD or mPEG. F98, C6 or U87 cell lines with different receptors levels were selected for in vitro and in vivo studies...
October 6, 2016: Journal of Drug Targeting
Victor Fattori, Karla G G Serafim, Ana C Zarpelon, Sergio M Borghi, Felipe A Pinho-Ribeiro, José C Alves-Filho, Thiago M Cunha, Fernando Q Cunha, Rúbia Casagrande, Waldiceu A Verri
The present study investigated whether endothelin-1 acts via ETA or ETB receptors to mediate superoxide anion-induced pain and inflammation. Mice were treated with clazosentan (ETA receptor antagonist) or BQ-788 (ETB receptor antagonist) prior to stimulation with the superoxide anion donor, KO2. Intraplantar treatment with 30 nmol of clazosentan or BQ-788 reduced mechanical hyperalgesia (47% and 42%), thermal hyperalgesia (68% and 76%), oedema (50% and 30%); myeloperoxidase activity (64% and 32%), and overt-pain like behaviours, such as paw flinching (42% and 42%) and paw licking (38% and 62%), respectively...
October 5, 2016: Journal of Drug Targeting
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