Abstract:
:Surface architecture of pharmaceutical nanocarriers (using polymeric micelles as an example) and the length of the spacer group through which specific ligand is attached to the carrier surface determine the interaction of ligand-bearing nanocarrier with cells. We have prepared surface-modified polyethyleneglycol-phosphatidylethanolamine (PEG-PE) micelles containing TATp attached to PEG-PE with a PEG block longer or shorter (TATp-PEG(1000)-PE or TATp-PEG(3400)-PE) than the PEG block in the main micelle-forming material (PEG(750)-PE and/or PEG(2000)-PE). The length of the PEG spacer in TATp-PEG-PE should allow for a non-hindered interaction of TATp with the cell surface, but it should not be too long to allow for the conformational "folding in" of TATp moiety inside the PEG globule making it unable to interact with the cells. The "folding in" of the ligand attached to an unnecessary long PEG spacer was further supported by the fluorescence resonance energy transfer (FRET) study between fluorescently labeled lipid 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-(7-nitro-2-1,3-benzoxadiazol-4-yl) (NBD-PE) inserted into the core of PEG(750)-PE micelles and micelle-incorporated rhodamine-labeled TATp-PEG-PE. Micelles containing rhodamine-labeled TATp-PEG-PE with the longest PEG spacer (3400 Da) demonstrated strongly enhanced quenching of NBD-PE fluorescence with rhodamine-TATp confirming the "folding in" of TATp moiety into PEG globule bringing it closer to the micelle core-incorporated NBD.
journal_name
J Drug Targetjournal_title
Journal of drug targetingauthors
Sawant RR,Sawant RM,Kale AA,Torchilin VPdoi
10.1080/10611860802230240subject
Has Abstractpub_date
2008-08-01 00:00:00pages
596-600issue
7eissn
1061-186Xissn
1029-2330pii
901337696journal_volume
16pub_type
杂志文章abstract:BACKGROUND:Multifunctional gold nanospheres (MGNs)-loaded with docetaxel (MGN@DTX) were prepared and evaluated for therapeutic efficacy in nude mice bearing human prostate cancer xenografts. METHODS:MGNs were prepared from PEGylated hollow gold nanospheres (HGNs) coated with folic acid and DTPTT chelate. Then, the eff...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2015.1018910
更新日期:2015-01-01 00:00:00
abstract::Therapeutic peptides are conventionally administered via subcutaneous injection. Chitosan-based nanoparticles are gaining increased attention for their ability to serve as a carrier for oral delivery of peptides and vaccination. They offered superior biocompatibiltiy, controlled drug release profile and facilitated ga...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/1061186X.2017.1400552
更新日期:2018-08-01 00:00:00
abstract::Acyclovir is an antiviral agent and it has been particularly used for the treatment of herpes simplex infections. The treatment of infection in the oral cavity is often difficult, because of insufficient drug concentration in saliva when acyclovir is administered via the oral route in conventional tablet form for syst...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860600566548
更新日期:2006-01-01 00:00:00
abstract::Targeting of anti-tumor drugs to the urinary bladder for the treatment of bladder carcinoma may be useful, since these agents generally have a low degree of urinary excretion and are highly toxic elsewhere in the body. The anti-tumor drug doxorubicin was coupled to the low-molecular weight protein lysozyme via the aci...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860290007568
更新日期:2002-02-01 00:00:00
abstract::Recent studies have shown that drugs that are normally unable to cross the blood-brain barrier (BBB) following intravenous injection can be transported across this barrier by binding to poly(butyl cyanoacrylate) nanoparticles and coating with polysorbate 80. However, the mechanism of this transport so far was not know...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860290031877
更新日期:2002-06-01 00:00:00
abstract::Cytokine inhibiting drugs are much more effective when delivered intracellularly to phagocytic cells in the microencapsulated form. Dexamethasone is a powerful inhibitor of TNF-α cytokine through inhibition of NF-κB which is a gene regulator of multiple pro-inflammatory cytokines. We have determined the effect of micr...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2011.561856
更新日期:2011-11-01 00:00:00
abstract::Increased generation of reactive oxygen species (ROS) has been implicated in the pathogenesis of a variety of diseases such as cardiovascular diseases and cancer. NADPH oxidase (Nox), a multicomponent enzyme, has been identified as one of the key sources of ROS. Nox4, one of the seven members of Nox family (Nox1, Nox2...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/1061186X.2015.1036276
更新日期:2015-12-01 00:00:00
abstract::An aqueous dispersion of self-organized phospholipid tubules has been utilized as the template for silica-deposited nanotubules (approximately 0.5 microm thick and >10 microm long) by a sol-gel method. The formation of the hybrid tubules was mechanistically investigated by controlled sol-gel reaction. The incorporatio...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860802295581
更新日期:2008-11-01 00:00:00
abstract::Human epidermal growth factor receptor 2 (HER2) expression has been shown to be increased in several types of human tumours. In this study, for the imaging of HER2-related tumours, a modified RNA aptamer with HER2-specific targeting was labelled with (99m)Tc, by using hydrazino nicotinamide (HYNIC) as the chelator in ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2013.839688
更新日期:2014-02-01 00:00:00
abstract::Diabetes is a condition that is not completely treatable but life of a diabetic patient can be smoothed by preventing or delaying the associate conditions like diabetic retinopathy, nephropathy, impaired wound healing process, etc. Apart from conventional methods to regulate diabetic condition, new techniques using si...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/1061186X.2018.1476518
更新日期:2019-02-01 00:00:00
abstract::beta-Glucuronidase (GUSB) is a lysosomal enzyme that could be developed as a brain therapy for Type VII Mucopolysaccharidosis. However, GUSB does not cross the blood-brain barrier (BBB). To enable BBB transport of the enzyme, human GUSB was re-engineered as a fusion protein with the chimeric monoclonal antibody (MAb) ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611860903353362
更新日期:2010-04-01 00:00:00
abstract::An in vivo study has been performed in order to determine the influence of amphotericin B (AMB) molecular organization on the toxicity and activity of this drug in the treatment of experimental visceral leishmaniasis. Three formulations with similar composition but different drug molecular self-association in aqueous ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860400006596
更新日期:2004-01-01 00:00:00
abstract::There are much said about Pieter Cullis in this special volume honoring him. He was the pioneer to study the role of hexagonal HII phase in membrane fusion and the one who applied this concept for the design of lipid nanoparticles. He was also the first to utilize remote loading techniques for the delivery of amphipat...
journal_title:Journal of drug targeting
pub_type: 传,历史文章,杂志文章
doi:10.3109/1061186X.2016.1172590
更新日期:2016-11-01 00:00:00
abstract::The present work describes the potential for using lectin-conjugated gliadin nanoparticles as a means of locating and anchoring a drug delivery system on the carbohydrate receptors of Helicobacter pylori (H. pylori). Gliadin nanoparticles (GNP) bearing acetohydroxamic acid (AHA) were prepared by a desolvation method. ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860310001647771
更新日期:2003-08-01 00:00:00
abstract::In this review, we emphasize the efforts on the development of radiolabeled nanoparticles (NPs) for cancer treatment, i.e. theranostic tools based on nanotechnology and nuclear medicine. Currently, radionuclide therapy remains to be an important treatment option. The ionizing radiation from radionuclides (not provided...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/1061186X.2014.988216
更新日期:2015-04-01 00:00:00
abstract::A polymeric gene carrier was developed to deliver vascular endothelial growth factor (VEGF) small interfering RNA (siRNA) for prostate cancer cells in a target-specific manner. Prostate cancer-binding peptide (PCP) was conjugated with polyethylenimine (PEI) via a poly(ethylene glycol) (PEG) linker (PEI-PEG-PCP). The P...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860902767232
更新日期:2009-05-01 00:00:00
abstract::We hypothesized that immunoliposomes (ILs) constructed using Fab' from the humanized anti-EGFR monoclonal antibody, EMD72000, can provide efficient intracellular drug delivery in EGFR-overexpressing colorectal tumor cells.ILs were constructed modularly with various MAb fragments, including Fab' from EMD72000 (matuzuma...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860600691049
更新日期:2006-05-01 00:00:00
abstract::Insulin and dexamethasone were encapsulated in poly(lactic-co-glycolic acid) (PLGA) microspheres to induce adipogenesis for potential applications in soft tissue reconstruction. Release kinetics and bioactivity of the drugs were examined. Surface morphology and diameter of the PLGA microspheres was evaluated using sca...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860802669231
更新日期:2009-04-01 00:00:00
abstract::Necrosis avid agents (NAAs) can be used for diagnose of necrosis-related diseases, evaluation of therapeutic responses and targeted therapeutics of tumor. In order to probe into the effects of molecular skeleton structure on necrosis targeting and clearance properties of radioiodinated dianthrones, four dianthrone com...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2015.1113541
更新日期:2016-01-01 00:00:00
abstract::The purpose of this research is to develop ligand-targeted plasmid based gene delivery systems for gene transfer to tumor endothelium. Cell adhesion assays were used to test the peptide inhibition of human endothelial cell adsorption to vitronectin-treated tissue culture plates. A series of RGD containing peptides wer...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860410001724468
更新日期:2004-05-01 00:00:00
abstract::Gene augmentation has been the paradigm in the majority of gene therapy protocols but in recent years the potential of repairing the mutated gene in situ by targeted gene correction has become a reality. In fact, targeted gene repair has many advantages over conventional replacement strategies, notably the possibility...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/10611860290016739
更新日期:2002-03-01 00:00:00
abstract::The aim of this work was to formulate minoxidil loaded liposome and niosome formulations to improve skin drug delivery. Multilamellar liposomes were prepared using soy phosphatidylcholine at different purity degrees (Phospholipon 90, 90% purity, soy lecithin (SL), 75% purity) and cholesterol (Chol), whereas niosomes w...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860600991993
更新日期:2007-02-01 00:00:00
abstract::Drug efflux by the membrane transporter P-glycoprotein (P-gp) plays a key role in multidrug resistance (MDR). In order to bypass P-gp, thus overcoming MDR, a hybrid peptide comprising a cell penetrating peptide (Tat) and a drug binding motif (DBM) has been developed to noncovalently bind and deliver doxorubicin (Dox) ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611860903548347
更新日期:2010-07-01 00:00:00
abstract::Dendrimers, spherical or quasi-spherical synthetic polymers in the nano-size range, have found useful applications as prospective carriers in drug and gene delivery. The investigation of dendrimer uptake by cells has been previously achieved by the incorporation of a fluorescent dye to the dendrimer either by chemical...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860600834441
更新日期:2006-07-01 00:00:00
abstract::The ability of a polymer therapeutic to access the appropriate subcellular location is crucial to its efficacy and is defined to a large part by the many and complex cellular biological and biochemical barriers such that a construct must traverse. It is shown here that model dextrin conjugates are able to pass through...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2017.1378660
更新日期:2017-01-01 00:00:00
abstract::We have previously reported that the transfection efficiency of laminin-derived AG73-peptide labeled polyethyleneglycol-modified liposomes (AG73-PEG liposomes) was enhanced by echo-contrast gas entrapping PEG liposomes (Bubble liposomes, BLs) and ultrasound (US) exposure by improving endosomal escape. However, it has ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2012.660162
更新日期:2012-05-01 00:00:00
abstract::The high-molecular-weight soluble aggregates of Fab fragments of murine antibodies against cardiac myosin were prepared as a potential long-circulating and low immunogenic pharmaceutical carriers by conjugation of thiolated Fab and Fab modified with succinimidyl 3-(2-pyridyldithio)propionate. The clearance time and bi...
journal_title:Journal of drug targeting
pub_type: 杂志文章
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更新日期:1998-01-01 00:00:00
abstract::It is well established that overproduction and accumulation of the β-amyloid (Aβ) peptide 1-42 (Aβ(1-42)) is a trigger of the pathological cascade in Alzheimer's disease (AD) that manifests as cognitive impairment. Ginsenoside Rg3 is an important constituent of ginseng, plays an essential role in memory and improved c...
journal_title:Journal of drug targeting
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doi:10.1080/1061186X.2017.1354002
更新日期:2018-02-01 00:00:00
abstract::Liposomal encapsulation of doxorubicin (DXR) improves tumor accumulation and reduces adverse effects. One possible strategy for further optimization of this delivery technology would be to design the liposome carrier to release its content within the tumor tissue in response to specific stimuli such as ultrasound (US)...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2010.551401
更新日期:2011-09-01 00:00:00
abstract::Finding adequate carriers for proteins/peptides and anticancer drugs delivery has become an urgent need, owing to the growing number of therapeutic macromolecules and the increasing amount of cancer incidence. Polysaccharide-based nanogels have attracted interest as carriers for proteins/peptides and anticancer drugs ...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/1061186X.2017.1326123
更新日期:2017-09-01 00:00:00