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Targeted drug delivery

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https://www.readbyqxmd.com/read/28102776/targeted-delivery-of-cisplatin-to-tumor-xenografts-via-the-nanoparticle-component-of-nano-diamino-tetrac
#1
Thangirala Sudha, Dhruba J Bharali, Murat Yalcin, Noureldien He Darwish, Melis Debreli Coskun, Kelly A Keating, Hung-Yun Lin, Paul J Davis, Shaker A Mousa
AIM: Nano-diamino-tetrac (NDAT) targets a receptor on integrin αvβ3; αvβ3 is generously expressed by cancer cells and dividing endothelial cells and to a small extent by nonmalignant cells. The tetrac (tetraiodothyroacetic acid) of NDAT is covalently bound to a poly(lactic-co-glycolic acid) nanoparticle that encapsulates anticancer drugs. We report NDAT delivery efficiency of cisplatin to agent-susceptible urinary bladder cancer xenografts. MATERIALS & METHODS: Cisplatin-loaded NDAT (NDAT-cisplatin) was administered to xenograft-bearing nude mice...
January 19, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28101766/crossing-the-blood-brain-barrier-recent-advances-in-drug-delivery-to-the-brain
#2
Mayur M Patel, Bhoomika M Patel
CNS disorders are on the rise despite advancements in our understanding of their pathophysiological mechanisms. A major hurdle to the treatment of these disorders is the blood-brain barrier (BBB), which serves as an arduous janitor to protect the brain. Many drugs are being discovered for CNS disorders, which, however fail to enter the market because of their inability to cross the BBB. This is a pronounced challenge for the pharmaceutical fraternity. Hence, in addition to the discovery of novel entities and drug candidates, scientists are also developing new formulations of existing drugs for brain targeting...
January 18, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28101622/-use-of-vasopressors-and-inotropics-in-cardiogenic-shock
#3
H Lemm, S Dietz, M Janusch, M Buerke
Vasoactive drugs and inotropic agents are important for the hemodynamic management of cardiogenic shock. In this article the use of different vasoactive and ionotropic drugs in cardiogenic shock is presented. Hemodynamic management during cardiogenic shock occurs after initial moderate volume delivery by dobutamine to increase inotropism. If adequate perfusion pressures are not achieved norepinephrine is administered. If a sufficient increase in cardiac performance can still not be achieved by the treatment, administration of levosimendan or phosphodiesterase (PDE) inhibitors may be necessary...
January 18, 2017: Herz
https://www.readbyqxmd.com/read/28098453/surface-engineered-multifunctional-eu-gd2o3-nanoplates-for-targeted-and-ph-responsive-drug-delivery-and-imaging-applications
#4
Arindam Saha, Subas Chandra Mohanta, Kashmiri Deka, Pritam Deb, Parukuttyamma Sujatha Devi
In this paper, we report the synthesis of surface-engineered multifunctional Eu:Gd2O3 triangular nanoplates with small size and uniform shape via a high-temperature solvothermal technique. Surface engineering has been performed by a one-step polyacrylate coating, followed by controlled conjugation chemistry. This creates the desired number of surface functional groups that can be used to attach folic acid as a targeting ligand on the nanoparticle surface. To specifically deliver the drug molecules in the nucleus, the folate density on the nanoparticle surface has been kept low...
January 18, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28097871/redox-responsive-self-assembly-micelles-from-poly-n-acryloylmorpholine-block-2-acryloyloxyethyl-ferrocene-carboxylate-amphiphilic-block-copolymers-as-drug-release-carriers
#5
Feng Xu, He Li, Yan-Ling Luo, Wei Tang
Novel well-defined redox-responsive ferrocene-containing amphiphilic block copolymers (PACMO-b-PAEFC) were synthesized by ATRP, with poly(N-acryloylmorpholine) (PACMO) as hydrophilic blocks and poly(2-acryloyloxyethyl ferrocenecarboxylate) (PAEFC) as hydrophobic blocks. The copolymers were characterized by FTIR, 1H NMR, and gel permeation chromatography, and the crystalline behavior was determined by X-ray diffraction and small-angle X-ray scattering. The results showed that the size of the lamellar crystals and crystallinity vary with the systematic compositions while the periodic structure of the lamellar stacks has no obvious change...
January 18, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28097007/safety-assessment-in-rats-and-dogs-of-acoustic-cluster-therapy-a-novel-concept-for-ultrasound-mediated-targeted-drug-delivery
#6
Oddvar Myhre, Marie Bjørgan, Derek Grant, Svein-Olaf Hustvedt, Per C Sontum, Hubert Dirven
Acoustic Cluster Therapy (ACT) represents a novel concept for targeted drug delivery. Ultrasound is applied to activate intravenously administered free-flowing clusters of microbubbles and microdroplets within the target pathology, depositing 20-30 μm large bubbles in the microvasculature for 5-10 min. Further application of ultrasound induces biomechanical effects which increase vascular permeability and enhance localized extravasation of coadministered drugs. Herein we report investigations done to assess the preclinical safety of ACT, using doses up to 1 mL/kg (3 μL perfluoromethyl-cyclopentane/kg)...
December 2016: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28096670/lung-targeting-drug-delivery-system-of-baicalin-loaded-nanoliposomes-development-biodistribution-in-rabbits-and-pharmacodynamics-in-nude-mice-bearing-orthotopic-human-lung-cancer
#7
Yumeng Wei, Jing Liang, Xiaoli Zheng, Chao Pi, Hao Liu, Hongru Yang, Yonggen Zou, Yun Ye, Ling Zhao
The present study aims to develop a kind of novel nanoliposomes for the lung-targeting delivery system of baicalin as a Chinese medicine monomer. Baicalin-loaded nanoliposomes were prepared by the effervescent dispersion and lyophilized techniques. Baicalin-loaded nanoliposomes had an average particle size of 131.7±11.7 nm with 0.19±0.02 polydispersity index, 82.8%±1.24% entrapment efficiency and 90.47%±0.93% of yield and sustaining drug release effect over 24 h and were stable for 12 months at least. In vitro no hemolytic activity was observed for the experimental drug concentration...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28096156/bacterial-derived-cell-penetrating-peptides-deliver-gentamicin-to-kill-intracellular-pathogens
#8
Marta Gomarasca, Thaynan F C Martins, Lilo Greune, Philip R Hardwidge, M Alexander Schmidt, Christian Rüter
Commonly used antimicrobials show poor cellular uptake and often have limited access to intracellular targets, resulting in low antimicrobial activity against intracellular pathogens. An efficient delivery system to transport these drugs to the intracellular site of action is needed. Cell-penetrating peptides (CPPs) mediate the internalization of biologically active molecules into the cytoplasm. Here we characterized two CPPs, α1H and α2H, derived from the Y. enterocolitica YopM effector protein. These CPPs, as well as Tat(Trans-activator of transcription) from HIV-1 virus, were used to deliver the antibiotic gentamicin to target intracellular bacteria...
January 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28095918/anti-staphylococcal-activity-resulting-from-epithelial-lining-fluid-elf-concentrations-of-amikacin-inhale-administered-via-the-pulmonary-drug-delivery-system
#9
Islam M Ghazi, Mordechai Grupper, David P Nicolau
BACKGROUND: Amikacin inhale (BAY41-6551), a unique drug-device combination of a specially formulated drug solution and a pulmonary drug delivery system device (AMK-I) is currently under phase III study as an adjunctive therapy to IV antibiotics for the treatment of Gram-negative pneumonia in mechanically ventilated patients. While the epidemiology of nosocomial pneumonia is predominated by Gram-negative pathogens such as Pseudomonas aeruginosa and the Enterobacteriaceae, Staphylococcus aureus is increasingly recognized as a pathogen of concern for these pulmonary based infections...
January 17, 2017: Annals of Clinical Microbiology and Antimicrobials
https://www.readbyqxmd.com/read/28095907/the-targeted-smac-mimetic-sw-iv-134-is-a-strong-enhancer-of-standard-chemotherapy-in-pancreatic-cancer
#10
Yassar M Hashim, Suwanna Vangveravong, Narendra V Sankpal, Pratibha S Binder, Jingxia Liu, S Peter Goedegebuure, Robert H Mach, Dirk Spitzer, William G Hawkins
BACKGROUND: Pancreatic cancer is a lethal malignancy that frequently acquires resistance to conventional chemotherapies often associated with overexpression of inhibitors of apoptosis proteins (IAPs). We have recently described a novel means to deliver second mitochondria-derived activator of caspases (SMAC) mimetics selectively to cancer cells employing the sigma-2 ligand/receptor interaction. The intrinsic death pathway agonist SMAC offers an excellent opportunity to counteract the anti-apoptotic activity of IAPs...
January 17, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28095746/targeting-of-herbal-bioactives-through-folate-receptors-a-novel-concept-to-enhance-intracellular-drug-delivery-in-cancer-therapy
#11
Anshita Gupta, Chanchal Deep Kaur, Shailendra Saraf, Swarnlata Saraf
Targeted drug delivery through folate receptor (FR) has emerged as a most biocompatible, target oriented, and non-immunogenic cargoes for the delivery of anticancer drugs. FRs are highly overexpressed in many tumor cells (like ovarian, lung, breast, kidney, brain, endometrial, and colon cancer), and targeting them through conjugates bearing specific ligand with encapsulated nanodrug moiety is undoubtedly, a promising approach toward tumor targeting. Folate, being an endogenous ligand, can be exploited well to affect various cellular events occurring during the progress of tumor, in a more natural and definite way...
January 17, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/28095689/folate-binding-protein-self-aggregation-drives-agglomeration-of-folic-acid-targeted-iron-oxide-nanoparticles
#12
Junjie Chen, Sarah Klem, Alexis K Jones, Bradford Orr, Mark M Banaszak Holl
Folate-conjugated nanomaterials have been widely investigated for drug and imaging-agent delivery. In this work, two folic acid (FA) conjugated iron oxide particles (IOP), a ∼40 nm diameter FA-IOP and a ∼450 nm diameter FA-IOP(FA-SeraMag), were synthesized. Both particles aggregated in the presence of serum folate-binding protein (FBP) at physiological concentration and buffer conditions. Mixing 0.01% w/w FA-conjugated iron oxide particles with FBP-induced agglomeration generated an average hydrodynamic particle diameter of 3800 ± 1100 nm for ∼40 nm FA-IOP and 4030 ± 1100 nm for FA-SeraMag as measured by dynamic light scattering (DLS)...
January 18, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28095578/a-clinical-evaluation-of-a-next-generation-non-invasive-selective-radiofrequency-hands-free-body-shaping-device
#13
Nicole Hayre, Melanie Palm, Peter Jenkin
OBJECTIVE: The aim of this study was to compare clinical outcomes of a noninvasive selective radiofrequency (RF) eld device (BTL Vanquish METM, BTL Industries Inc., Boston MA) with its predecessor (VanquishTM, BTL Industries Inc., Boston MA). The BTL Vanquish METM system has been thoroughly redesigned for more efficient, predictable and homogenous energy delivery to the targeted tissue. MATERIALS AND METHODS: In this multi-center study, 36 subjects with BMIs under 30 were randomly assigned to be treated in Group A (BTL Vanquish METM) or Group B (VanquishTM) in order to obtain a side by side comparison of the devices' ef cacies...
December 1, 2016: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/28095317/formulation-of-liposomes-functionalized-with-lotus-lectin-and-effective-in-targeting-highly-proliferative-cells
#14
Cinzia Della Giovampaola, Antonietta Capone, Leonardo Ermini, Pietro Lupetti, Elisa Vannuccini, Federica Finetti, Sandra Donnini, Marina Ziche, Agnese Magnani, Gemma Leone, Claudio Rossi, Floriana Rosati, Claudia Bonechi
BACKGROUND: Liposomes, used to improve the therapeutic index of new and established drugs, have advanced with the insertion of active targeting. The lectin from Lotus tetragonolobus (LTL), which binds glycans containing alpha-1,2-linked fucose, reveals surface regionalized glycoepitopes in highly proliferative cells not detectable in normally growing cells. In contrast, other lectins localize the corresponding glycoepitopes all over the cell surface. LTL also proved able to penetrate the cells by an unconventional uptake mechanism...
January 14, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28093969/traumatic-brain-injury-preclinical-imaging-diagnostic-s-and-therapeutic-approaches
#15
Eric L Kaijzel, Ermond R van Beek, Marieke A Stammes, Ivo Que, Alan B Chan, Clemens W G M Löwik, Luis J Cruz
BACKGROUND: Traumatic brain injury (TBI) is a result of an external physical force to the head that traumatically injures the brain. It is a major public health problem worldwide and mainly results from falls, vehicle accidents and violence. Clinical problem: The management of TBI, causing a wide spectrum of possible health outcomes, has barely changed over the years as encouraging outcomes from many pre-clinical therapeutic and pharmacological studies have only rarely been translated to the clinical situation...
January 16, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28093284/pancreatic-cancer-stroma-and-its-current-and-emerging-targeted-therapies
#16
Janaiah Kota, Julie Hancock, Jason Kwon, Murray Korc
Pancreatic Ductal Adenocarcinoma (PDAC) is one of the most lethal human malignancies with a 5-year survival rate of 8%. Dense, fibrotic stroma associated with pancreatic tumors is a major obstacle for drug delivery to the tumor bed and plays a crucial role in pancreatic cancer progression. Targeting stroma is considered as a potential therapeutic strategy to improve anti-cancer drug efficacy and patient survival. Although numerous stromal depletion therapies have reached the clinic, they add little to overall survival and are often associated with toxicity...
January 13, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28093036/combining-nanoscale-magnetic-nimodipine-liposomes-with-magnetic-resonance-image-for-parkinson-s-disease-targeting-therapy
#17
Bingshuo Ji, Meili Wang, Dawei Gao, Shanshan Xing, Lei Li, Lanxiang Liu, Min Zhao, Ximing Qi, Kun Dai
AIM: To enhance drug targeting and blood-brain barrier penetration for Parkinson's disease (PD), a novel nanoscale magnetic nimodipine (NMD) delivery system was designed and prepared. MATERIALS & METHODS: The PD rats were established and treated with free NMD or Fe3O4-modified NMD liposomes (Fe3O4-NMD-lips). Then, factional anisotropy values were measured by MRI to evaluate therapy efficacy. RESULTS: Fe3O4-NMD-lips showed the best neuroprotective effect, and the NMD concentration of lesions was 2...
January 17, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28090647/the-multifaceted-role-of-extracellular-vesicles-in-metastasis-priming-the-soil-for-seeding
#18
REVIEW
Brunna Dos Anjos Pultz, Felipe Andrés Cordero da Luz, Sara Socorro Faria, Leandro Peixoto Ferreira de Souza, Paula Cristina Brígido Tavares, Vivian Alonso Goulart, Wagner Fontes, Luiz Ricardo Goulart, Marcelo José Barbosa Silva
Extracellular vesicles (EVs), including exosomes, play a key role in inter and intracellular communication, promoting the proliferation and invasion of recipient cells to support tumor growth and metastasis. Metastasis comprises multiple steps that first include the detachment of tumor cells through epithelial to mesenchymal transition (EMT), allowing the physical dissemination to distant organs. Thereafter, cancer-derived exosomes are still critical components for preparing the tumor microenvironment by (i) enabling tumor cells to escape from the immunological surveillance and (ii) arranging the pre-metastatic site for the engraftment of detached cancer cells...
January 16, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28089915/dendrimers-as-nanocarriers-for-nucleoside-analogues
#19
REVIEW
Michał Gorzkiewicz, Barbara Klajnert-Maculewicz
Dendrimers constitute a class of hyperbranched macromolecules with several potential applications due to their unique properties such as a well-defined structure, multivalency and biocompatibility. These polymers became one of the most promising drug nanocarriers, providing improved solubility of therapeutics, high loading capacity and controllable biodistribution pattern. In addition, the use of dendrimers as drug delivery devices in cancer therapies may help to overcome the resistance mechanisms by transporting activated drug molecules directly to cancer cells...
January 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28089660/characterization-pharmacokinetics-and-tissue-distribution-of-chlorogenic-acid-loaded-self-microemulsifying-drug-delivery-system
#20
Li Chen, Chang-Shun Liu, Qing-Zhen Chen, Sen Wang, Yong-Ai Xiong, Jing Jing, Jia-Jia Lv
The purpose of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to improve the oral bioavailability of Chlorogenic acid (CA), an important bioactive compound from Lonicerae Japonicae Flos with poor permeability. SMEDDS was prepared and characterized by self-emulsifying rate, morphological observation, droplet size determination, stability, in vitro release, in vivo bioavailability and tissue distribution experiments. Results shown that the SMEDDS of CA has a high self-emulsifying rate (>98%) in the dissolution media, and its microemulsion exhibits small droplet size (16...
January 12, 2017: European Journal of Pharmaceutical Sciences
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