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Journal of Drug Targeting

Uday Krishna Baruah, Kuppusamy Gowthamarajan, Ravisankar Vanka, Veera Venkata Satyanarayana Reddy Karri, Kousalya Selvaraj, Gifty M Jojo
We reside in an era of technological innovation and advancement despite which infectious diseases like malaria remain to be one of the greatest threats to the humans. Mortality rate caused by malaria disease is a huge concern in the 21(st) century. Multiple drug resistance and non-specific drug targeting of the most widely used drugs are the main reasons/drawbacks behind the failure in malarial therapy. Dose related toxicity because of high doses is also a major concern. Therefore, to overcome these problems nano based drug delivery systems are being developed to facilitate site specific or target based drug delivery and hence minimising the development of resistance progress and dose dependent toxicity issues...
February 6, 2017: Journal of Drug Targeting
Jiaojiao Ding, Yujiao Sun, Jinfeng Li, Huimin Wang, Shirui Mao
The blood brain barrier represents an insurmountable obstacle for the therapy of central nervous system related diseases. Polymeric micelles have many desirable properties for brain targeting by oral delivery but the stability and targeting efficiency needs to be improved. In this study, it was demonstrated that binary micelle system can compensate the drawbacks of mono system by preparing mixed micelles in combination with PEG based copolymers. Here we explored a brain targeting drug delivery system via facile approaches using P123 based mixed micelles in combination with a message guider from traditional Chinese medicine, borneol, for oral delivery...
February 2, 2017: Journal of Drug Targeting
Asadullah Madni, Amna Batool, Sobia Noreen, Irsah Maqbool, Faizza Rehman, Prince Muhammad Kashif, Nayab Tahir, Ahmad Raza
Lung cancer is the leading cause of cancer-related deaths in the world. Conventional therapy for lung cancer is associated with lack of specificity and access to the normal cells resulting in cytotoxicity, reduced cellular uptake, drug resistance, and rapid drug clear from the body. The emergence of nanotechnology has revolutionized the treatment of lung cancer. The focus of nanotechnology is to target tumor cells with improved bioavailability and reduced toxicity. In the recent years, nanoparticulate systems have extensively been exploited in order to overcome the obstacles in treatment of lung cancer...
February 2, 2017: Journal of Drug Targeting
Muhammad Kashif, Antonio Moreno-Herrera, Edgar E Lara-Ramirez, Esther Ramírez-Moreno, Virgilio Bocanegra-García, Muhammad Ashfaq, Gildardo Rivera
Chagas is a lethal chronic disease that currently affects 8 to 10 million people worldwide, primarily in South and Central America. Trypanosoma cruzi trans-sialidase is an enzyme that is of vital importance for the survival of the parasite due to its key role in the transfer of sialic acid from the host to the parasite surface and it also helps the parasite combat the host´s immune system. This enzyme has no equivalent human enzyme, thus it has become an interesting target for the development of inhibitors that combat the parasite...
January 31, 2017: Journal of Drug Targeting
Fathia Zaki El Sharkawi, Shaimaa Mohammed Ewais, Rania Hassan Fahmy, Laila Ahmed Rashed
Gene therapy is one of the recent approaches in treatment of hepatocellular carcinoma (HCC). Development of a vector or vehicle that can selectively and efficiently deliver the gene to target cells with minimal toxicity is an urgent demand. In the present study, Phosphatase and Tensin homolog (PTEN) and Tumor Necrosis Factor (TNF)-Related Apoptosis-Inducing Ligand (TRAIL) genes were loaded to Zein nanoparticles (ZNPs). The formulated PTEN and TRAIL-loaded ZNPs were tested for their in-vitro and in-vivo potential antitumor efficacy using liver tumor cells (HepG2) and HCC-induced rats as animal model...
January 31, 2017: Journal of Drug Targeting
Teuta Opačak-Bernardi, Jung Su Ryu, Drazen Raucher
Notch pathway was found to be activated in most glioblastomas (GBM), underlining the importance of Notch in formation and recurrence of GBM. In this study, a Notch inhibitory peptide, dominant negative MAML (dnMAML), was conjugated to Elastin-like polypeptide (ELP) for tumor targeted delivery. ELP is a thermally responsive polypeptide that can be actively and passively targeted to the tumor site by localized application of hyperthermia. This complex was further modified with the addition of a cell penetrating peptide, SynB1, for improved cellular uptake and blood-brain barrier penetration...
January 31, 2017: Journal of Drug Targeting
Li-Yan Zhao, Wan-Ming Zhang
This review focuses on recent investigations that used Pluronic P123 (P123) as pharmaceutical ingredients in vesicle, micelle, mixed micelle, in situ gel, tablet and emulsion, et al. The main results from these studies show that P123 can significantly increase the stability of incorporated hydrophobic drugs with enhanced in vitro cytotoxicity and cellular uptake of anticancer drugs. Moreover, modified forms of P123 with RGD, folate or other targeted marker have shown its therapeutic potentials in various types of tumors and cancers...
January 30, 2017: Journal of Drug Targeting
Kousalya Selvaraj, Kuppusamy Gowthamarajan, Veera Venkata Satyanarayana Reddy Karri, Uday K Barauah, Vanka Ravisankar, Gifty M Jojo
Diabetic retinopathy (DR) is a leading cause of blindness in all working age groups which contribute to patient's quality of life. Considering the anatomy and physiology of barriers in the eye, the treatment and management of pathologic ocular neovascularization in the posterior segment of the eye in DR is a challenging task. The current and emerging treatment strategies are discussed in this review for better understanding and treatment of the DR. Challenges in conventional therapy and recent developments in nanocarrier based approaches (polymeric, lipid nanoparticles, liposomes and dendrimers) and their advantages in targeting ocular tissues were also discussed in this review...
January 25, 2017: Journal of Drug Targeting
Suhui Ni, Yuwen Xie, Yue Tang, Yun Liu, Jing Chen, Siyan Zhu
This study developed a pH-sensitive anionic system composed of guanidinylated O-carboxymethyl chitosan (GOCMCS) and N-2-hydroxypropyltimehyl ammonium chloride chitosan (N-2-HACC) for efficient siRNA delivery to the lung following nebulization. About 16.8% of guanidine groups were incorporated into O-carboxymethyl chitosan (OCMCS) with the aid of O-methylisourea. Gel electrophoresis images demonstrated that siRNA was successfully encapsulated in nanoparticles ranging from 150 nm to 180 nm with zeta potential of about -17 mV...
January 23, 2017: Journal of Drug Targeting
Abdel-Azim Zaghloul, Ahmad Lila, Fathy Abd-Allah, Aly Nada
BACKGROUND: Metformin hydrochloride (MtHCL) is an oral antidiabetic drug and has many other therapeutic benefits. It has poor bioavailability, narrow absorption window and extensive liver metabolism. Moreover, children and elders face difficulty to swallow the commercial oral tablets. OBJECTIVES: Preparation, in vitro/in vivo evaluation of MtHCL suppositories for rectal administration to solve some of these problems. METHODS: Suppository fatty bases (Witepsol®, Suppocire® and Massa®; different grades) and PEG bases 1000, 4000 and 6000 (different ratios), were used to prepare rectal suppository formulations each containing 500 mg drug...
January 16, 2017: Journal of Drug Targeting
Marie Iwanaga, Yukinobu Kodama, Takahiro Muro, Hiroo Nakagawa, Tomoaki Kurosaki, Kayoko Sato, Tadahiro Nakamura, Takashi Kitahara, Hitoshi Sasaki
The purpose of this study was to develop a ternary complex of plasmid DNA (pDNA) electrostatically assembled with dendrigraft poly-L-lysine (DGL) and biodegradable glycosaminoglycan for effective and secure gene delivery. High gene expression of pDNA/DGL complex was confirmed with slight cytotoxicity and erythrocyte agglutination. Anionic ternary complexes of 55.4-223.8 nm were formed by the addition of a glycosaminoglycan such as chondroitin sulfate A (CS-A), chondroitin sulfate B (CS-B), chondroitin sulfate C (CS-C), or hyaluronic acid (HA)...
January 3, 2017: Journal of Drug Targeting
Xiali Zhu, 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)...
December 28, 2016: Journal of Drug Targeting
Mohammad Arabpour, Robbert H 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 toward 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...
December 28, 2016: 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 (MN) 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 the capsaicin, 99.3 ± 4.1% and 99.7 ± 2.2% for low-dose and high-dose DMNs were released within 20 min...
December 14, 2016: Journal of Drug Targeting
Prashant Bhattarai, Dylan Vance, Arash Hatefi, Ban An Khaw
Drug resistance is a common phenomenon that occurs in cancer chemotherapy. Delivery of chemotherapeutic agents as polymer pro-drug conjugates (PPDCs) pretargeted with bispecific antibodies could circumvent drug resistance in cancer cells. To demonstrate this approach to overcome drug resistance, Paclitaxel (Ptxl) resistant SKOV3 TR human ovarian- and doxorubicin (Dox) resistant MCF7 ADR human mammary-carcinoma cell lines were used. Pre-targeting over-expressed biotin or HER2/neu receptors on cancer cells was conducted by biotinylated anti-DTPA or Anti-HER2/neu affibody - anti-DTPA Fab bispecific antibody complexes...
December 12, 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
Chuanjin Wang, Wei Li, Bingcheng Hu
In this study, folate receptor (FR) targeted liposome microbubbles loaded with oridonin (ORI) (F-LMB-ORI), liposome loaded with ORI (L-ORI) and liposome microbubbles loaded with ORI (LMB-ORI) were prepared. In vitro release properties, cellular uptake and cytotoxicity in HepG-2 cells as well as in vivo antitumor effects in HepG-2 cells tumor-bearing mice of F-LMB-ORI, L-ORI and LMB-ORI were evaluated upon ultrasound exposure. Results showed cytotoxicity assay on F-LMB-ORI gave IC50 of 0.508 ± 0.018 µmol/mL on HepG-2 cells and LMB-ORI; L-ORI gave IC50 of 2...
January 2017: Journal of Drug Targeting
Hye-Rin Jeong, Han-Sol Lee, In-Jeong Choi, Jung-Hwan Park
Transdermal delivery using microneedles is gaining increasing attention from pharmaceutical and cosmetic companies as one of the promising drug delivery methods. Microneedle products have recently become available on the market, and some of them are under evaluation for efficacy and safety. To be available in the market for cosmetic and therapeutic use, several factors should be considered, including pain, anxiety, convenience and safety. These factors are summarized and reviewed in this article according to type of microneedle...
January 2017: Journal of Drug Targeting
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