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) into MDR cells. The uptake of Dox into the leukemia cell line K562 and its P-gp overexpressing subline KD30 increased in the presence of DBM-Tat peptide. Confocal microscopy indicated that DBM-Tat associated Dox was directed to a perinuclear area of KD30 cells, while this was not observed in parent K562 cells. When KD30 cells were pretreated with the endosomotropic agent chloroquine (CLQ), peptide associated Dox redistributed into the cytosol, indicating that endocytosis was the predominant uptake route. Altered drug uptake kinetics observed by cellular accumulation assay also supported an endocytic uptake. In the presence of CLQ, DBM-Tat was able to enhance the cytotoxicity of Dox by 68.4% at 5 microM peptide concentration in KD30 cells but there were only minor effects on Dox cytotoxicity in K562 cells even in the presence of CLQ. Thus, combining Dox with DBM-Tat reduces P-gp mediated drug efflux, without a requirement for drug modification or inhibiting P-gp function.
journal_name
J Drug Targetjournal_title
Journal of drug targetingauthors
Zheng Z,Aojula H,Clarke Ddoi
10.3109/10611860903548347subject
Has Abstractpub_date
2010-07-01 00:00:00pages
477-87issue
6eissn
1061-186Xissn
1029-2330journal_volume
18pub_type
杂志文章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
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abstract::The aim of this study was to evaluate the pharmacokinetics (PK), tissue distribution, and the specific drug targeting of cefpiramide sodium-loaded liposomes (CPMS-Lips) compared with cefpiramide sodium solution (CPMS-Sol) in mice. CPMS-Lips were prepared by reverse phase evaporation method. In the PK and biodistributi...
journal_title:Journal of drug targeting
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abstract::Lopinavir (LPV), an efficient drug for HIV infection treatment, was incorporated into biodegradable PLGA nanocapsules (NCs) embedded in microparticles (MCPs) using the spray-drying technique in an attempt to bypass the P-gp efflux and protect the drug from CYP3A pre-systemic metabolism without ritonavir (RTV). SEM obs...
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journal_title:Journal of drug targeting
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doi:10.3109/10611861003801842
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abstract::The objective of this study was to estimate the colon-specific delivery of [Asu1,7]-eel calcitonin (ECT) using chitosan capsules in rats. The intestinal absorption of ECT was evaluated by measuring the plasma calcium levels after oral administration of the chitosan capsules containing ECT and different combinations of...
journal_title:Journal of drug targeting
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doi:10.1080/10611860600648494
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abstract::Local tissue toxicity, systemic toxicity and platinum pharmacokinetics were evaluated in 6 normal healthy beagle dogs injected subcutaneously with two formulations of a polylactide biodegradable polymer (Atrigel) system containing cisplatin. Dogs were injected 4 times at 30 day intervals at platinum dosages of 70, 105...
journal_title:Journal of drug targeting
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abstract::Notch pathway was found to be activated in most glioblastomas (GBMs), 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 resp...
journal_title:Journal of drug targeting
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doi:10.1080/1061186X.2017.1289537
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abstract::Background: Sonodynamic therapy (SDT) has emerged as an alternative to the traditional treatments of cancer. However, the oxygen consumption induced by SDT and glucose oxidase (GOx) mediated starvation therapy would worsen the hypoxic tumor environment, which further impeded therapeutic efficacy. Purpose: To develop a...
journal_title:Journal of drug targeting
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doi:10.1080/1061186X.2019.1641507
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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-phosp...
journal_title:Journal of drug targeting
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doi:10.1080/10611860802230240
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abstract::Despite the advantages of drug delivery through skin, transdermal drug delivery is only used with a small subset of drugs because most compounds cannot cross the skin at therapeutically useful rates. Recently, a new concept known as microneedle was introduced and could be used to pierce effectively to deliver drugs us...
journal_title:Journal of drug targeting
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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
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abstract::Cyclodextrins (CDs) are macrocyclic oligosaccharides composed of α(1,4)-linked glucopyranose subunits. These molecules possess a cage-like supramolecular structure, comparable with the structures of crown ethers, cryptands, spherands, cyclophanes, or calixarenes. However, it took 50 years to establish the molecular st...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/10611861003622552
更新日期:2010-11-01 00:00:00
abstract::Micro-needle arrays increase skin permeability by forming channels through the outer physical barrier, without stimulating pain receptors populating the underlying dermis. It was postulated that micro-needle arrays could facilitate transfer of DNA to human skin epidermis for cutaneous gene therapy applications. Platin...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860500383705
更新日期:2005-08-01 00:00:00
abstract::To identify an agent with specific activity against B-lineage leukaemia stem cells (B-LSCs), we generated norcantharidin (NCTD)-encapsulated liposomes modified with a novel humanised anti-human CD19 monoclonal antibody, Hm2E8b (Hm2E8b-NCTD-liposomes). These liposomes were specially designed to recognise and kill B-LSC...
journal_title:Journal of drug targeting
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doi:10.1080/1061186X.2017.1339193
更新日期:2018-01-01 00:00:00
abstract::Aim was to develop and optimize multiunit gastro-retentive floating beads (FBs) intended for localized and prolonged release of ginger for treating gastric ulcers. Protective effect of ginger extract (GE) against ulcer is well documented, but therapeutic use is compromised due to poor bioavailability and physicochemic...
journal_title:Journal of drug targeting
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doi:10.3109/1061186X.2011.561855
更新日期:2011-11-01 00:00:00
abstract::The myriad of complications associated with diabetes is closely linked with the generation of reactive species or free radicals leading to oxidative and nitrosative stress. Increased oxidative stress is an important cause and result of diabetes and it is thought to underlie the cellular changes that lead to diabetic c...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/1061186X.2017.1419478
更新日期:2018-11-01 00:00:00
abstract::The COVID-19 pandemic is caused by the severe acute-respiratory-syndrome-coronavirus-2 that uses ACE2 as its receptor. Drugs that raise serum/tissue ACE2 levels include ACE inhibitors (ACEIs) and angiotensin-II receptor blockers (ARBs) that are commonly used in patients with hypertension, cardiovascular disease and/or...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
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更新日期:2020-08-01 00:00:00
abstract::Sulpiride (SUL), anti-dopaminergic drug, has a specific site for absorption located in the upper portion of the gastrointestinal tract hence, its oral delivery represents a challenge regarding SUL absorption and bioavailability. So, a gastro-retentive oral platform of SUL was developed to increase its gastric residenc...
journal_title:Journal of drug targeting
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doi:10.1080/1061186X.2019.1663526
更新日期:2020-04-01 00:00:00
abstract::Liposomes have been prepared from dipalmitoylphosphatidylcholine (DPPC), cholesterol (Chol) and dimethyldioctadecylammonium bromide (DDAB). The cationic vesicles adsorb to biofilms of the skin-associated bacteria Staphylococcus epidermidis, which have a negative charge. Encapsulation of the antibacterial drug vancomyc...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869609015975
更新日期:1996-01-01 00:00:00
abstract::This study was aimed to generate a new agent, norcantharidin (NCTD) encapsulated liposomes modified with a novel murine anti-human CD19 monoclonal antibody 2E8 (2E8–NCTD–liposomes), to specifically target the B-lineage leukemia stem cells (B-LSCs) and their progeny in vitro. Our results have shown that the positive pe...
journal_title:Journal of drug targeting
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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
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doi:10.1080/10611860310001647771
更新日期:2003-08-01 00:00:00
abstract::The biodistribution of orally and intravenously administered archaeosomes in mice was compared to that of archaeosomes containing either coenzyme Q10 (archaeosome-CoQ10), polyethylene glycol (archaeosome-PEG), or PEG plus CoQ10 (archaeosome-PEG-CoQ10). The archaeosome formulations were prepared by a reverse-phase evap...
journal_title:Journal of drug targeting
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abstract::Solid tumors such as breast cancer have historically provided many challenges to anti-cancer therapy. Therapeutic hurdles to drug penetration in solid tumors include heterogeneous vascular supply and high interstitial pressures within tumor tissue, particularly in necrotic zones, lower pH and presence of leaky vascula...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
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更新日期:2006-06-01 00:00:00
abstract::Nanoparticles form the fundamental building blocks for many exciting applications in various scientific disciplines due to its unique features such as large surface to mass ratio, targeting potential, ability to adsorbed and carry other compound which makes them suitable for biomedical applications. However, the probl...
journal_title:Journal of drug targeting
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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
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doi:10.1080/10611860290031877
更新日期:2002-06-01 00:00:00
abstract::Anionic, cationic, and neutral liposomes were constructed to contain IL-2 in order to evaluate their affinity to a cervical cancer cell line (INBL) and to determine whether they can present IL-2 on their external surface. When these liposomes were co-cultured with INBL, the anionic liposomes were the only ones found t...
journal_title:Journal of drug targeting
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doi:10.1080/10611860903012810
更新日期:2009-08-01 00:00:00
abstract::A simple method for the separation of polyalkylcyanoacrylate nanoparticles was developed using polyisohexylcyanoacrylate (PIHCA) as a model. Fluorescein isothiocyanate dextran 70 was used to label the nanoparticles. Ultracentrifugation onto a performed sucrose gradient allowed the easy elimination of the dextran and o...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869509059216
更新日期:1995-01-01 00:00:00
abstract::Based on the organotropic characteristics of bile acids towards the liver and the intestine, two novel compounds of the Bamet family, containing at least one bile acid moiety bound to platinum(II), have been synthesized and their cytostatic effect compared to their ability to become accumulated in tumor cells of hepat...
journal_title:Journal of drug targeting
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doi:10.1080/1061186021000001841
更新日期:2002-08-01 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
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doi:10.1080/10611860290007568
更新日期:2002-02-01 00:00:00
abstract:PURPOSE:An octreotide-conjugated polyamidoamine (PAMAM) dendrimer was synthesized and employed as nanocarriers of methotrexate (MTX), for targeting to the somatostatin receptors over-expressed tumor cells. METHODS:PAMAM-PEG-octreotide (PPO) and PAMAM-PEG (PPG) were synthesized and characterized. The cellular uptake of...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2013.879386
更新日期:2014-06-01 00:00:00