Abstract:
:Toxoplasmic encephalitis (TE) is the most common clinical manifestation of reactivated infection with Toxoplasma gondii in immunocompromised patients that is lethal if untreated. The combination of pyrimethamine plus sulfadiazine or clindamycin is the standard therapy for the treatment of TE, but these combinations are associated with hematologic toxicity and/or life-threatening allergic reactions. Therefore, alternative treatment options are needed. Atovaquone is safe and highly effective against T. gondii in vitro, but the oral micronized solution shows poor bioavailability. We synthesized atovaquone nanosuspensions (ANSs) coated with poloxamer 188 (P188) and sodium dodecyl sulfate (SDS) to improve oral bioavailability and passage through the blood-brain barrier (BBB). Coating of ANSs with SDS resulted in enhanced oral bioavailability and enhanced brain uptake of atovaquone compared to Wellvone(®) in murine models of acute and reactivated toxoplasmosis as measured by high performance liquid chromatography (HPLC). Parasite loads and inflammatory changes in brains of mice treated with SDS-coated ANS were significantly reduced compared to untreated controls and to Wellvone(®)-treated mice. In conclusion, nanosuspensions coated with SDS may ultimately lead to improvements in the treatment of TE and other cerebral diseases.
journal_name
J Drug Targetjournal_title
Journal of drug targetingauthors
Shubar HM,Lachenmaier S,Heimesaat MM,Lohman U,Mauludin R,Mueller RH,Fitzner R,Borner K,Liesenfeld Odoi
10.3109/10611861003733995subject
Has Abstractpub_date
2011-02-01 00:00:00pages
114-24issue
2eissn
1061-186Xissn
1029-2330journal_volume
19pub_type
杂志文章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::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:UNLABELLED:Polyethyleneimine (PEI) can be used as a DNA delivery mechanism in cell culture and in vivo. Cells can be transfected by using surface-bound PEI, as well as by PEI/DNA microparticles. In the present experiments we extended these observations by preparing microspheres with covalently attached PEI. Blends of p...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611860108995629
更新日期:2001-01-01 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
pub_type: 杂志文章
doi:10.1080/1061186X.2020.1722137
更新日期:2020-06-01 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::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::Gene transfer offers a potential way to correct local and systemic protein deficiency disorders by using genes as drugs, so called gene therapeutics. Salivary glands present an interesting target site for gene therapeutic applications. Herein, we review proofs of concept achieved for salivary glands with in vivo anima...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/10611860108998782
更新日期:2001-01-01 00:00:00
abstract::As a percutaneous sustained-release preparation, insulin micropiles (MPs) were prepared with biodegradable polymers poly(lactic acid) (PLA), poly(ϵ-caprolactone) (PCL) and poly(lactic-co-glycolic acid) (PLGA) as the base. The obtained PLA, PCL, and PLGA MPs of which the insulin:polymer ratio was 1:2 were administered ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2010.492521
更新日期:2011-04-01 00:00:00
abstract:BACKGROUND:High expression of glucagon-like peptide-1 receptor (GLP-1R) in insulinoma supplies a potential drug target for tumor imaging. Exendin-4 can specifically bind to GLP-1R as an agonist and its analogs are extensively used in receptor imaging studies. PURPOSE:A new GLP-1R imaging agent, [(18)F]AlF-NOTA-MAL-Cys...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2015.1020808
更新日期:2015-01-01 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::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::Highly lipophilic antitumor agent, palmitoyl rhizoxin (RS-1541), was incorporated into stable lipid emulsions about 100-1000nm in mean diameter consisting of triglyceride ODO and surfactant HCO-60. The pharmacokinetics of RS-1541 were studied after i.v. injection in mice, rats, rabbits, and dogs. Dog showed characteri...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869808997875
更新日期:1998-01-01 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 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::A nuclear localization signal (NLS) is a short amino acid sequence derived from eukaryotic nuclear proteins and viral proteins. Many NLS peptides can efficiently mediate the intranucleus transport of cargo molecules, so they have been widely used for non-viral gene transfer and shown potential ability to improve nucle...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/1061186X.2016.1184273
更新日期:2016-12-01 00:00:00
abstract::To design a novel cytospecific photosensitizer for photodynamic antitumor therapy, a fullerene (C(60)) was chemically modified with pullulan which is a water-soluble polysaccharide with a high affinity for asialoglycoprotein receptors. Ethylene diamine was introduced to the terminal aldehyde groups of pullulan by the ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611861003599479
更新日期:2010-09-01 00:00:00
abstract::Tissue plasminogen activator (tPA) is the only FDA approved medical treatment for the ischaemic stroke. However, it associates with some inevitable limitations, including: short therapeutic window, extremely short half-life and low penetration in large clots. Systemic administration may lead to complications such as h...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/1061186X.2017.1365874
更新日期:2018-02-01 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 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:INTRODUCTION:Peptide antibiotics as new therapeutic agents are becoming a popular option to investigate due to their broad bacterial target selectivity and limited resistance problems. Although attractive, these new drug candidates have several limitations including low potency and delivery issues which face all peptid...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860600907767
更新日期:2006-11-01 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::Nanoparticles have shown great promise in the treatment of cancer, with a demonstrated potential in targeted drug delivery. Among a myriad of nanocarriers that have been recently developed, dendrimers have attracted a great deal of scientific interests due to their unique chemical and structural properties that allow ...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/1061186X.2015.1052077
更新日期:2015-01-01 00:00:00
abstract::Submicron sized hydrophobic and hydrophilic albumin microspheres (MS) were prepared using a chemical crosslinking technique. Spermine was linked to the surface of the hydrophilic MS. The degree of hydrophobicity for these three types of MS was investigated using a novel technique of sedimentation volume. The surface t...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869509015933
更新日期:1995-01-01 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::Tissue factor (TF) is aberrantly expressed on tumor vascular endothelial cells (VECs) and on cancer cells in many malignant tumors, but not on normal VECs, making it a promising target for cancer therapy. As a transmembrane receptor for coagulation factor VIIa (fVIIa), TF forms a high-affinity complex with its cognate...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860801890093
更新日期:2008-04-01 00:00:00
abstract::DNA nanoparticles (DNA NPs), which self-assemble from DNA plasmids and poly-L-lysine (pLL)-polyethylene glycol (PEG) block copolymers, transfect several cell types in vitro and in vivo with minimal toxicity and immune response. To further enhance the gene transfer efficiency of DNA NP and control its tropism, we estab...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2012.712128
更新日期:2012-09-01 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::Germ-free (GF) animals lack a colonic microflora like that seen in conventional (CV) animals. Bacterial presence plays a role in the development of glycoproteins in the gastrointestinal (GI) tract; the absence of a microbiota has been seen to suppress the production of certain glycoproteins and glycolipids. Binding pa...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611860108997920
更新日期:2001-04-01 00:00:00
abstract::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 effec...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2016.1200588
更新日期:2017-01-01 00:00:00
abstract::A promising strategy to carry genetic material to brain cells either in vitro or in vivo is using the LDL receptor (LDLr) on blood-brain barrier. LDLr naturally help to low density lipoproteins (LDL(S)) transporting across the BBB by endocytosis. Here we present the idea of using the LDLr-mediated pathway for transpor...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860601148908
更新日期:2007-04-01 00:00:00