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Journal of Drug Targeting

Selin Çeşmeli, Cigir Biray Avci
Cancer is one of the most common diseases all over the world; many people suffer from diverse types of cancer. However, currently there is no exact cure or therapy developed for cancer. On the other hand, nanoparticles are defined as microscopic particles that have dimensions less than 100 nm and they are known with their usage in health sciences and medicine, however a few harmful effects on different animal cells, Therefore, researchers began to use nanoparticles for cancer therapies and to develop new methods for much more efficient therapies...
September 25, 2018: Journal of Drug Targeting
Kamel S Ahmed, Saied A Hussein, Abdelmoneim H Ali, Sameh A Korma, Qiu Lipeng, Chen Jinghua
In the last decades, pharmaceutical interested researches aimed to develop novel and innovative drug delivery techniques in the medical and pharmaceutical fields. Recently, phospholipid vesicles (Liposomes) are the most known versatile assemblies in the drug delivery systems. The discovery of liposomes arises from self-forming enclosed phospholipid bilayer upon coming in contact with the aqueous solution. Liposomes are uni or multilamellar vesicles consisting of phospholipids produced naturally or synthetically, which are readily non-toxic, biodegradable, and are readily produced on a large scale...
October 15, 2018: Journal of Drug Targeting
Jian Zou, Zhang Zhang, Fang Xu, Shengyang Cui, Chunli Qi, Jingfeng Luo, Zhen Wang, Xiaoyun Lu, Zhengchao Tu, Xiaomei Ren, Liyan Song, Ke Ding
Collective data suggest tropomyosin-related kinase B (TrkB), which is correlated with the growth, migration and poor prognosis of neuroblastoma (NB), is a potential target for NB target therapy. Several Phase I/II pan-Trk inhibitors display impressive clinical outcomes but still no drug has been approved for general use. In this paper, we report a novel structural TrkB inhibitor GZD2202, a structural derivative of our previously identified DDR1 antagonists. GZD2202 demonstrates a moderate selectivity between Trk B/C and TrkA...
October 10, 2018: Journal of Drug Targeting
Shoshy Mizrahy, Anna Gutkin, Paolo Decuzzi, Dan Peer
One of the major challenges in drug development is the delivery of therapeutics to the central nervous system (CNS). The blood-brain barrier (BBB), which modulates the passage of molecules from the CNS, presents a formidable obstacle that limits brain uptake of therapeutics and, therefore, impedes the treatment of multiple neurological pathologies. Targeted nanocarriers present an excellent opportunity for drug delivery into the brain leveraging on endogenous receptors to transport therapeutics across the BBB endothelium...
October 8, 2018: Journal of Drug Targeting
S Pascual-Gil, G Abizanda, E Iglesias, E Garbayo, F Prósper, M J Blanco-Prieto
Neuregulin-1 loaded PLGA microparticles hold great promise for treating acute myocardial infarction, as they have been proved to recover heart function and induce positive heart remodeling in preclinical studies. More recently, the inflammatory response of the heart after acute myocardial infarction (AMI) has been identified as one of the major mechanisms in cardiac tissue remodeling and repair. However, the connection between neuregulin-1 PLGA microparticles and inflammation is still not well characterized...
October 5, 2018: Journal of Drug Targeting
Josu Andrieu, Francesca Re, Laura Russo, Francesco Nicotra
Phage display is a powerful and widely used technique to find novel peptide ligands. A massive amount of peptide sequences have been identified for all kinds of materials, and peptides that may have targeting capabilities towards specific cells and tissues have received especial attention in biomedical sciences. As a result, it is increasingly harder to follow all the work that has been done, which sometimes leads to many promising ligands receiving little attention, together with the publication of false positives that have already been found...
October 3, 2018: Journal of Drug Targeting
Aishwarya Shivashankarappa, Konasur Rajesh Sanjay
The present research work describes the use of Photodynamic Therapy (PDT) ofdrug 5-aminolevulinic acid (5-ALA) conjugated with microbial synthesizedsilver nanoparticles on skin melanoma (B16F10) and epidermoid carcinoma (A431) cell lines. Silver nanoparticles were synthesized using the bacterial strain Bacillus licheniformis.The morphology of the nanoparticles were studied using Scanning Electron Microscopy (SEM) and elemental analysis of nanoparticles were carried out using Energy Dispersive X-Ray spectroscopy (EDX)...
October 3, 2018: Journal of Drug Targeting
Qing You, Talea Hopf, Werner Hintz, Stefan Rannabauer, Nadine Voigt, B van Wachem, Petra Henrich-Noack, Bernhard A Sabel
Because the blood-brain barrier (BBB) is an obstacle for drug-delivery, carrier systems such as polybutylcyanoacrylate (PBCA) nanoparticles (NPs) have been studied. Yet, little is known of how physiochemical features such as size, surfactants and surface charge influence BBB passage in vivo. We now used a rat model of in vivo imaging of the retina - which is brain tissue and can reflect the situation at the BBB - to study how size and surface charge determine NPs' ability to cross the blood-retina barrier (BRB)...
October 3, 2018: Journal of Drug Targeting
Amirhosein Kefayat, Fatemeh Ghahremani, Hasan Motaghi, Soodabeh Rostami, Masoud A Mehrgardi
In the present study, alive attenuated Salmonella typhi Ty21a was introduced as a vehicle for smart delivery of gold nanoparticles to the tumours' hypoxic regions. At the first step, the uptakes of gold nanoparticles with seven different decorations by S. typhi Ty21a was investigated using flow cytometry and inductively coupled plasma optical emission spectroscopy. The analyses demonstrated that folic acid functionalised gold nanoparticles (FA-GNPs) are the best candidates for producing the Golden Bacteria (GB)...
October 3, 2018: Journal of Drug Targeting
Cong-Hui Zhang, Jun-Xia Wang, Mei-Lian Cai, Rongguang Shao, Hong Liu, Wu-Li Zhao
Ras-GTPase-activating protein SH3 domain-binding protein 1 (G3BP1) is a SH3 domain-binding protein that is overexpressed in a variety of tumour tissues and cancers, such as head and neck cancer, lung cancer, prostate cancer, colon cancer and breast cancer. G3BP1 promotes tumour cell proliferation and metastasis and inhibits apoptosis by regulating the Ras, TGF-β/Smad, Src/FAK and p53 signalling pathways. At present, polypeptides targeting G3BP1 have shown anti-tumour activity and G3BP1 also involved in anti-cancer effects of some polyphenolic compounds (resveratrol and EGCG)...
October 3, 2018: Journal of Drug Targeting
Fabiana de Sousa Cunha, Laise Nayra Dos Santos Pereira, Thâmara Pryscilla de Costa E Silva, Roberto Alves de Sousa Luz, Anderson Nogueira Mendes
The use of nanoparticulate systems with action in breast and ovarian cancer has been highlighted in recent years as an alternative to increasing the therapeutic index of conventional anticancer drugs. Thus, nanoparticles have advantageous characteristics in the treatment of cancer. Several nanocarriers of drugs and nanoparticles are described in the literature. The pharmacokinetics of the drugs can be modified by the use of nanocarriers, which in turn facilitate the specific delivery of the drug to the tumour cell...
October 3, 2018: Journal of Drug Targeting
Xuefei Zhou, Zimo Liu, Huifang Wang, Xin Liu, Zhuxian Zhou, Jianbin Tang, Xiangrui Liu, Min Zheng, Youqing Shen
Non-viral gene delivery is an attractive approach for the treatment of many diseases including cancer, benefiting from its safety and large-scale production concerns. However, the relatively low transfection efficacy compared with viral vectors restricts the clinical applications of non-viral gene vectors. Reactive oxygen species (ROS) triggered charge reversal polymers (named B-PDEAEA) presented improved transfection efficacy, because of fast release of plasmid DNA responding to enhanced oxidative stress in cancer cells...
September 25, 2018: Journal of Drug Targeting
Feng Yu, Sajid Asghar, Mei Zhang, Jingwei Zhang, Qineng Ping, Yanyu Xiao
Glioma is one of the most common type of malignant tumours with high morbidity and mortality rates. Due to the particular features of the brain, such as blood-brain barrier or blood-tumour barrier, therapeutic agents are ineffective by systemic administration. The tumour inevitably recurs and devitalises patients. Herein, an overview of the localised gliomas treatment strategies is provided, including direct intratumoural/intracerebral injection, convection-enhanced delivery, and the implant of biodegradable polymer systems...
September 19, 2018: Journal of Drug Targeting
Snigdha Tiash, Ezharul Hoque Chowdhury
Chemotherapy, the commonly favored approach to treat cancer is frequently associated with treatment failure and recurrence of disease as a result of development of multidrug resistance (MDR) with concomitant over-expression of drug efflux proteins on cancer cells. One of the most widely used drugs, doxorubicin (Dox) is a substrate of three different ATP-binding cassette (ABC) transporters, namely, ABCB1, ABCG2 and ABCC1, predominantly contributing to MDR phenotype in cancer. To silence these transporter-coding genes and thus enhance the therapeutic efficacy of Dox, pH-sensitive carbonate apatite (CA) nanoparticles (NPs) were employed as a carrier system to co-deliver siRNAs against these genes and Dox in breast cancer cells and in a syngeneic breast cancer mouse model...
September 17, 2018: Journal of Drug Targeting
Yuandi Zhao, Bo Wang, Jinzhi Liu, Pei Sun, Hongmin Liu
Immune escape plays an important hallmark of cancer. The tryptophan-catabolizing enzyme indoleamine 2, 3-dioxygenase 1 (IDO1) is involved in the immune escape mechanism of human tumors, the expression of which is associated with a poor prognosis in cancer and correlated with tumor progression clinically. Therefore, finding the inhibitors targeting IDO1 may be an impellent approach that can reverse the complicated processes in tumor immune escape and induce an antitumor response as well. Here, we summarized and compared some methods of determining the activity of IDO1 and they can be used to screen IDO1 inhibitors as well, including HPLC, fluorescence detection, cell-based assay, NFK GreenScreenTM and absorbance assay...
September 14, 2018: Journal of Drug Targeting
Fajun Qu, Jianqing Ye, Xiuwu Pan, Junkai Wang, Sishun Gan, Chuanmin Chu, Jian Chu, Xiangmin Zhang, Mei Liu, Hua He, Xingang Cui
Recent advances in immunotherapy are raising hope to treat clear cell renal cell carcinoma (ccRCC) with PD-L1 inhibitors, but only a small portion of patients are PD-L1 positive. The heterogeneous expression pattern of PD-L1 in patient population suggests that PD-L1 expression is under the control of diverse regulatory mechanisms. Although recent studies have identified numerous novel PD-L1 regulators, reports on microRNAs which modulate PD-L1 expression are much scarce. In this study, we confirmed that PD-L1 expression was up-regulated in ccRCC compared to paired normal tissues...
September 11, 2018: Journal of Drug Targeting
Taehoon Park, Kyoung Ah Min, Heesun Cheong, Cheol Moon, Meong Cheol Shin
Despite substantial advances in its treatment, brain cancer remains a life-threatening disease with a poor survival rate. The main challenges for the conventional chemotherapy include an insufficient efficacy of drugs and toxicity caused by their nonselective mode of action. Recently, great attention has been paid to highly potent macromolecules such as gelonin, a type 1 ribosome-inactivating protein that inhibits protein translation. However, gelonin is poorly internalised into tumour cells and cannot distinguish between cancer and normal cells...
September 11, 2018: Journal of Drug Targeting
Lian Li, Jiyuan Yang, Jiawei Wang, Jindřich Kopeček
Drug-free macromolecular therapeutics (DFMT) have been recently developed to treat non-Hodgkin lymphoma (NHL). It is a consecutive delivery of two nanoconjugates: (1) bispecific engager that pretargets surface CD20, and (2) multivalent effector polymer that hybridizes with CD20-bound engagers. Without the need of low molecular weight drug, the hybridization of morpholino oligonucleotide containing DFMT at NHL cell surface triggers CD20 crosslinking and subsequent apoptosis. We have previously determined various factors that affect the efficacy of DMFT regarding the synthetic structures...
September 10, 2018: Journal of Drug Targeting
Yoshiyuki Hattori, Mari Nakamura, Nozomi Takeuchi, Kyoko Tamaki, Satono Shimizu, Yuki Yoshiike, Masamitsu Taguchi, Hiroaki Ohno, Kei-Ichi Ozaki, Hiraku Onishi
Cationic liposomes composed of dialkyl cationic lipid such as 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) can efficiently deliver siRNA to the lungs following the intravenous injection of cationic liposome/siRNA complexes (lipoplexes). In this study, we examined the effect of cationic lipid of cationic liposomes on siRNA delivery to the lungs after intravenous injection. We used six kinds of cationic cholesterol derivatives and 11 kinds of dialkyl or trialkyl cationic lipids as cationic lipids, and prepared 17 kinds of cationic liposomes composed of a cationic lipid and 1,2-dioleoyl-L-α-glycero-3-phosphatidylethanolamine (DOPE) for evaluation of siRNA biodistribution and in vivo gene silencing effects...
September 7, 2018: Journal of Drug Targeting
Daniel Cristian Ferreira Soares, Caroline Mari Ramos Oda, Liziane Oliveira Fonseca Monteiro, Andre Luis Branco de Barros, Marli Luiza Tebaldi
Protein-polymer conjugates have achieved tremendous attention in the last few years, since their importance in diverse fields including drug delivery, biotechnology and nanotechnology. Over the past few years, numerous chemical strategies have been developed to conjugate different synthetic polymers onto proteins and great progress has been made. Currently, there are a handful of therapeutic polymer conjugates that have been approved by the FDA, while many hundreds of products are under extensive clinical trials and preclinical development phases...
September 7, 2018: Journal of Drug Targeting
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