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 media were prepared. Acute toxicity was evaluated by injecting them in healthy hamsters. Sub-acute toxicity and efficacy were studied administering them to animals previously infected with Leishmania infantum. The preparation with drug molecules completely dissolved into monomers (formulation "C") and produced the highest acute toxicity. The formulation whose AMB molecules were disposed as non-water-soluble multi-aggregates (formulation "B") proved to provide the lowest acute toxicity. This formula also showed an improved activity, mainly in the liver, if compared with the third tested formulation containing AMB molecules disposed as smaller dimerical "water-soluble" aggregates (formulation "A"). As a conclusion, molecular aggregation in biological media should be an important factor to consider when researching or optimizing medicines containing AMB. The liberation of molecules as large dispersed non-water-soluble multi-aggregates seems to improve the narrow therapeutic margin attached to the use of this drug.
journal_name
J Drug Targetjournal_title
Journal of drug targetingauthors
Sánchez-Brunete JA,Dea MA,Rama S,Bolás F,Alunda JM,Torrado-Santiago S,Torrado JJdoi
10.1080/10611860400006596keywords:
subject
Has Abstractpub_date
2004-01-01 00:00:00pages
453-60issue
7eissn
1061-186Xissn
1029-2330pii
NKCNC4UXLNC1T4GLjournal_volume
12pub_type
杂志文章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
doi:10.1080/1061186X.2020.1797754
更新日期:2020-08-01 00:00:00
abstract::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 twenty-first century. Multiple drug resistance and nonspecific drug targeting of the m...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/1061186X.2017.1291645
更新日期:2017-08-01 00:00:00
abstract::Radiolabeled cytochrome c (Cyt c), either as a free protein or as cell penetrating peptide (CPP)-conjugates, was tested for cellular uptake and nuclear transport in Human embryonic kidney 293 (HEK293) cells and HeLa cells. Conjugation of Cyt c with either the amphipathic peptide model amphipathic peptide (MAP) or the ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2011.649481
更新日期:2012-05-01 00:00:00
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
pub_type: 杂志文章
doi:10.1080/10611860600648494
更新日期:2006-04-01 00:00:00
abstract::Resveratrol is a promising neuroprotective agent against neurodegenerative disorders such as Alzheimer's disease. Resveratrol-loaded transferosomes and nanoemulsions were developed and labelled with gold nanoparticles (GNPs). The water maze test was utilised to identify the effect on spatial memory recovery. The treat...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2019.1608553
更新日期:2019-12-01 00:00:00
abstract::Poly(D,L-lactic-co-glycolic) acid (PLGA) microspheres containing plasmid DNA encoding the firefly luciferase gene were prepared using the water-in-oil-in-water (w/o/w) double emulsion and solvent evaporation method. In this study, we investigated the effects of three process parameters on DNA microencapsulation: (1) e...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869909085514
更新日期:1999-12-01 00:00:00
abstract:BACKGROUND:The polycationic nanopeptide RKKRRQRRR is a fragment of HIV-Tat protein known to be a transfection enhancer. Such factors control the transfection efficiency of plasmid DNA complexed with tat peptide. However, their actions are poorly understood. METHODS AND RESULTS:Several cell lines and primary cells were...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/106118604200041403
更新日期:2004-01-01 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::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::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 ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2018.1502775
更新日期:2019-02-01 00:00:00
abstract::The aim of the present study was to develop a polymeric delivery system for water-insoluble drug oridonin. Amphiphilic block copolymers, poly(epsilon-caprolactone)-poly(ethylene glycol)-poly (epsilon-caprolactone) (PCL-PEO-PCL), were synthesized by ring-opening polymerization of caprolactone initiated by the hydroxyl ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860802200938
更新日期:2008-07-01 00:00:00
abstract::Gene delivery systems face the problem not only of the route toward the cell and tissues in question, but also of the molecularly crowded environment of both the cytoplasm and the nucleus itself. One of the physical barriers in the cytoplasm for diffusing nanoparticles is an actin network. Here, we describe the findin...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2010.521159
更新日期:2010-12-01 00:00:00
abstract::Doxorubicin (DXR) was encapsulated in long-circulating liposomes, composed of ganglioside GM1 (GM1)/distearoylphosphatidylcholine (DSPC)/cholesterol (CH) (0.13:1:1 in molar ratio) and sized to approximately 100 nm in mean diameter, with 98% entrapping efficiency by the transmembrane pH gradient method. Free DXR, DXR-D...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869308996086
更新日期:1993-01-01 00:00:00
abstract::Tumour microenvironment provides the 'soil' for tumour growth. Besides tumour cells, there are also numbers of stromal cells, extracellular matrix and other components in the tumour microenvironment. In the past years, kinds of ligands and markers specifically high-expressed on the surface of the tumour stromal cells ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2020.1744157
更新日期:2020-08-01 00:00:00
abstract::Mitochondria are one type of the major organelles in the cell, participating in a variety of important physiological and biochemical processes, such as tricarboxylic acid cycle, fatty acid metabolism and oxidative phosphorylation. Meanwhile, it also happens to be the key regulator of apoptosis by triggering the comple...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/1061186X.2015.1108325
更新日期:2016-01-01 00:00:00
abstract::Gelatin microspheres (ms) and gelatin/BSA (bovine serum albumin) or gelatin/alginate ms were prepared by encapsulating fluorescein isothiocyanate (FITC) labeled dextran or interferon alpha (IFN-alpha). Ms were obtained by an emulsion-solvent-extraction method. Gelatin and gelatin/BSA ms were obtained by treating water...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869908996851
更新日期:1999-01-01 00:00:00
abstract::Intracellular compartmentalisation is a significant barrier to the successful nucleocytosolic delivery of biologics. The endocytic system has been shown to be responsible for compartmentalisation, providing an entry point, and trigger(s) for the activation of drug delivery systems. Consequently, many of the technologi...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2017.1358725
更新日期:2017-01-01 00:00:00
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
doi:10.1080/10611860600809112
更新日期:2006-06-01 00:00:00
abstract::Glioma is one of the most commonly occurring malignant brain tumours which need proper treatment strategy. The current therapies for treating glioma like surgical resection, radiotherapy, and chemotherapy have failed in achieving satisfactory results and this forms a rationale for the development of novel drug deliver...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/1061186X.2014.916712
更新日期:2014-07-01 00:00:00
abstract::The aim of the present study was to evaluate the transfer of N-acetyl-p-aminobenzoic acid (AcPABA) across the rat term placenta and the rat small intestine and to compare it with that of its parent drug p-aminobenzoic acid (PABA). Umbilical perfusion of the rat term placenta was used to determine the materno-fetal tra...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869808995875
更新日期:1998-01-01 00:00:00
abstract::The adsorption behaviour of a tetrafunctional copolymer of poly (ethylene oxide)-poly (propylene oxide) ethylene diamine (commercially available as Poloxamine 908) and a diblock copolymer of poly (lactic acid)-poly (ethylene oxide) (PLA/PEG 2:5) onto a model colloidal drug carrier (156 nm sized polystyrene latex) is d...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860500246175
更新日期:2005-09-01 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 aspargine-glycine-arginine (NGR) peptide modified single-walled carbon nanotubes (SWCNTs) system, developed by a simple non-covalent approach, could be loaded with the anticancer drug doxorubicin (DOX) and magnetic resonance imaging (MRI) contrast agent gadolinium-diethylenetriamine pentaacetic acid (Gd-DTPA). This...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2016.1221958
更新日期:2017-02-01 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
doi:10.3109/10611869808997880
更新日期:1998-01-01 00:00:00
abstract::N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers containing doxorubicin and galactosamine have been developed to target the hepatocyte galactose receptor with the aim of organ-specific chemotherapy of primary and metastatic liver disease. Previous biodistribution studies in rats and mice have used tyrosinamide inco...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869308996068
更新日期:1993-01-01 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::Local treatment of middle ear (ME) disease currently requires surgical penetration of the tympanic membrane (TM). We previously discovered 12-mer peptides that are actively transported across the intact TM, a process that could be used for non-invasive drug delivery into the ME. To optimise transport and provide furth...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2017.1347791
更新日期:2018-02-01 00:00:00
abstract::In vitro transfection efficiency of a plasmid DNA for rat gastric mucosal (RGM)-1 cells was enhanced by ultrasound (US) irradiation. Ethylenediamine was introduced to the carboxyl groups of gelatin to prepare a cationized gelatin as the vector of plasmid DNA encoding luciferase. An electrophoresis experiment revealed ...
journal_title:Journal of drug targeting
pub_type: 杂志文章,收录出版
doi:10.1080/10611860290022624
更新日期:2002-05-01 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::Intravenous targeting of anticancer agents should improve both efficacy and therapeutic index. However, rational design of targeting constructs requires detailed definition of receptor targets and must take account of polarised tissue architecture that may restrict access to chosen receptors from the bloodstream. Bact...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860701195510
更新日期:2007-05-01 00:00:00