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  • Elsevier (CrossRef)  (127)
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  • 1
    Article
    Article
    Language: English
    In: International Journal of Pharmaceutics, 02/22/2007, Vol.331(1), pp.1-10
    Description: To link to full-text access for this article, visit this link: http://dx.doi.org/10.1016/j.ijpharm.2006.10.021 Byline: Jorg Kreuter Keywords: Nanoparticles; Historical development Abstract: The historical development of nanoparticles starting with Paul Ehrlich and then first attempts by Ursula Scheffel and colleagues and the extensive work by the group of Professor Peter Speiser at the ETH Zurich in the late 1960s and early 1970s are described from a personal point of view. Special attention is given to the years between 1970 and the early 1980s. Further developments resulting from this work are also followed, and focus is placed on especially interesting improvements such as nanoparticles for the delivery of drugs across the blood-brain barrier (BBB) and PEGylated nanoparticles with a prolonged blood circulation time. Author Affiliation: Institut fur Pharmazeutische Technologie, Biozentrum, J.W. Goethe-Universitat, D-60439 Frankfurt, Germany Article History: Received 4 October 2006; Accepted 10 October 2006
    Keywords: Nanotechnology ; Nanoparticles;
    ISSN: 03785173
    E-ISSN: 18733476
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  • 2
    Language: English
    In: International Journal of Pharmaceutics, 2007, Vol.341(1), pp.207-214
    Description: Human serum albumin (HSA) nanoparticles represent promising drug carrier systems. Binding of cytostatics to HSA nanoparticles may diminish their toxicity, optimise their body distribution and/or may overcome multidrug resistance. In the present study, doxorubicin-loaded HSA nanoparticle preparations were prepared. Doxorubicin was loaded to the HSA nanoparticles either by adsorption to the nanoparticles’ surfaces or by incorporation into the particle matrix. Both loading strategies resulted in HSA nanoparticles of a size range between 150 nm and 500 nm with a loading efficiency of 70–95%. The influence on cell viability of the resulting nanoparticles was investigated in two different neuroblastoma cell lines. The anti-cancer effects of the drug-loaded nanoparticles were increased in comparison to doxorubicin solution. Based on these result a standard protocol for the preparation of doxorubicin-loaded HSA nanoparticles for further antitumoural studies was established.
    Keywords: Nanoparticles ; Doxorubicin ; Human Serum Albumin (HSA) ; Physicochemical Characterisation ; Cell Viability ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0378-5173
    E-ISSN: 1873-3476
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  • 3
    Language: English
    In: Journal of Controlled Release, 28 September 2015, Vol.214, pp.76-84
    Description: Highly aggressive cancer types such as pancreatic cancer possess a mortality rate of up to 80% within the first 6 months after diagnosis. To reduce this high mortality rate, more sensitive diagnostic tools allowing an early stage medical imaging of even very small tumours are needed. For this purpose, magnetic, biodegradable nanoparticles prepared using recombinant human serum albumin (rHSA) and incorporated iron oxide (maghemite, -Fe O ) nanoparticles were developed. Galectin-1 has been chosen as target receptor as this protein is upregulated in pancreatic cancer and its precursor lesions but not in healthy pancreatic tissue nor in pancreatitis. Tissue plasminogen activator derived peptides (t-PA-ligands), that have a high affinity to galectin-1 have been chosen as target moieties and were covalently attached onto the nanoparticle surface. Improved targeting and imaging properties were shown in mice using single photon emission computed tomography–computer tomography (SPECT–CT), a handheld gamma camera, and magnetic resonance imaging (MRI).
    Keywords: Rhsa Nanoparticles ; Maghemite ; T-PA-Ligands to Galectins ; T-Papeptide1lac ; Single Photon Emission Computed Tomography–Computer Tomography (Spect–CT) ; Handheld Gamma Camera ; Magnetic Resonance Imaging (Mri) ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0168-3659
    E-ISSN: 1873-4995
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  • 4
    Language: English
    In: International Journal of Pharmaceutics, 1983, Vol.16(1), pp.105-113
    Description: Polybutylcyanoacrylate nanoparticles have been used for the intravenous and intramuscular administration of a steroidal material ([ 75 Se]norcholestenol) to the rabbit. Whole body profiles of 75 Se, obtained using a gamma camera over a period of 30 days, show that the [ 75 Se]norcholestenol is retained for a longer period of time with the nanoparticle system than for the control system where the drug was dissolved in a micellar system. In vitro dialysis experiments indicate that the thermodynamic activity of the drug can be increased by its incorporation within nanoparticles. This increased activity may affect the distribution of the drug into body tissues.
    Keywords: Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0378-5173
    E-ISSN: 1873-3476
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  • 5
    Language: English
    In: International Journal of Pharmaceutics, 1996, Vol.137(1), pp.67-74
    Description: Methylmethacrylate (MMA) sulfopropylmethacrylate (SPM) copolymer nanoparticles were prepared by free radical polymerization. The conditions of preparation were varied with regard to the concentration of initiator and monomer, and copolymer composition. Nanoparticles with a yield greater than 80% were produced. The particles were characterized in terms of particle size, size distribution, particle charge (zetapotential) and molecular weight. The data were compared to pure polymethylmethacrylate (PMMA) nanoparticles. The copolymer composition was shown to influence particle size and particle charge. The influence of the total monomer amount in the polymerization medium on the particle size was characteristic up to a concentration of 2% depending on the solubility of MMA in water at the temperature of reaction. An increasing amount of total monomer led to particle sizes of 60–130 nm for low monomer concentrations (0.5%), depending on the proportion of SPM (0–10%), to 120–280 nm for higher total monomer concentrations (greater than 2%). Surface charge as well as particle size were influenced mainly by the proportion of the comonomer SPM in the copolymer. The negative surface charge increased from - 52 mV for pure PMMA nanoparticles to − 80mV for the copolymer particles with an SPM content of 10%. In the same range of 0–10%), SPM of the total monomer, the particle sizes decreased from 187 to 100 run. The concentration of the initiator up to a concentration of 0.3% showed no effect on the particle size of the resulting nanoparticle suspension. Higher concentrations led to intolerably large variability in the polymerization process.
    Keywords: Nanoparticles ; Copolymer ; Methylmethacrylate (Mma) ; Sulfopropylmethacrylate (Spm) ; Physicochemical Characterization ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0378-5173
    E-ISSN: 1873-3476
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  • 6
    Language: English
    In: International Journal of Pharmaceutics, 1992, Vol.85(1), pp.7-17
    Description: The influence of various penetration enhancers including propylene glycol, oleic acid, Azone ® , isopropyl myristate, valine, and nanoparticles on the permeation coefficient for the permeation of amino acids through hairless mouse skin as well as a dialysis membrane was assessed in vitro. The two different types of membranes were employed in order to distinguish between effects due to thermodynamic parameters and those due to barrier resistance. Furthermore, the influence of these penetration enhancers on the amount of amino acids remaining within the skin was determined. Oleic acid was found to be the most efficient enhancer for amino acids (enhancement factor (EF) of 176 for histidine) followed by Azone ® (EF of 45 for phenylalanine). All other penetration enhancers failed to exert any significant effect on the skin permeation of amino acids. The fact that the enhancement effects of oleic acid and Azone ® are not reversible and that the enhancers exhibited no influence with dialysis membranes clearly indicate that both penetration enhancers induce their effects on the basis of changes in skin morphology. Choosing arginine, histidine and phenylalanine as test permeants enabled a correlation between the enhancement effects and the degree of ionization of the test permeant. Histidine is the only amino acid which is unionized at pH 7.4 due to its isoelectric point. This might be the reason why the permeation enhancement induced by valine was only detectable with histidine, and not with the other two amino acids. Neither penetration enhancer resulted in any significant effect on the amount of the amino acid accumulated in the skin.
    Keywords: Amino Acid ; Hairless Mouse Skin ; Permeability ; Penetration Enhancer ; Propylene Glycol ; Azone ® ; Oleic Acid ; Isopropyl Myristate ; Valine ; Nanoparticles ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0378-5173
    E-ISSN: 1873-3476
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  • 7
    Language: English
    In: International Journal of Pharmaceutics, 1991, Vol.72(2), pp.149-155
    Description: The permeation coefficients of protein amino acids through full-thickness hairless mouse skin were determined by means of an infinite dose technique. The permeability coefficients were found to be very low and ranged between 1 and 50 × 10 −5 (cm/h). No significant difference between ionized and unionized transdennal transport was observed. Higher permeation coefficients were clearly attributed to membrane damage caused by alkaline solutions. A significant difference between the permeation of positively and negatively charged molecules was not obvious. The permeability also did not depend on molecular weight or on the hydrophobicity of the amino acids. Hairless mouse skin did not form a reservoir for amino acids.
    Keywords: Amino Acid ; Hairless Mouse Skin ; Permeability ; Skin Reservoir ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0378-5173
    E-ISSN: 1873-3476
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  • 8
    Language: English
    In: Journal of Controlled Release, 2007, Vol.117(1), pp.51-58
    Description: Poly(butyl cyanoacrylate) nanoparticles coated with poloxamer 188 (Pluronic® F68) and also, as shown previously, polysorbate 80 (Tween® 80) considerably enhance the anti-tumour effect of doxorubicin against an intracranial glioblastoma in rats. The investigation of plasma protein adsorption on the surface of the drug-loaded nanoparticles by two-dimensional electrophoresis (2-D PAGE) revealed that both surfactants, besides other plasma components, induced a considerable adsorption of apolipoprotein A-I (ApoA-I). It is hypothesized that delivery of doxorubicin to the brain by means of nanoparticles may be augmented by the interaction of apolipoprotein A-I that is anchored on the surface of the nanoparticles with the scavenger receptor class B type I (SR-BI) located at the blood–brain barrier. This is the first study that shows a correlation between the adsorption of apolipoprotein A-I on the nanoparticle surface and the delivery of the drug across the blood–brain barrier.
    Keywords: Apolipoprotein A-I ; Chemotherapy ; Glioblastoma ; Nanoparticles ; Poly(Butyl Cyanoacrylate) ; Poloxamer 188 ; Polysorbate 80 ; Rats ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0168-3659
    E-ISSN: 1873-4995
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  • 9
    Language: English
    In: International journal of pharmaceutics, 20 July 1999, Vol.184(2), pp.199-206
    Description: Isothermal heat conduction microcalorimetry was used to evaluate chemical stability of a solid drug in tablets. A variety of mixtures were compressed to flat faced tablets of 300 mg weight and 10 mm diameter. The content of drug amounted to 10%. Besides drug containing tablets, also placebo tablets as well as the non compressed mixtures were examined by microcalorimetry at 80 degrees C. The excipient Emcompress exhibited a substantially high exothermic heat flow that was due to a change in crystallinity. For Emcompress containing tablets this interfering signal resulted in such a way that the calorimetric data did not reflect the drug decomposition with sufficient accuracy. In the case of the other preparations the heat flow of the excipients were low, and the calorimetric data did reflect the drug decomposition. The stability increased with increasing content of CaHPO4, respectively, with decreasing content of water.
    Keywords: Drug Stability ; Tablets -- Chemistry
    ISSN: 0378-5173
    E-ISSN: 18733476
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  • 10
    Language: English
    In: International Journal of Pharmaceutics, 1999, Vol.178(1), pp.23-32
    Description: The transport of nanoparticle associated drugs, [ 75 Se]norcholestenol, captopril, methylene blue, hydrocortisone, doxorubicin, and dalargin was determined by permeability measurements in two chamber side by side diffusion cells using cellulose acetate, silicone rubber, pig small intestine, or hairless mice skin as membranes. Solutions of free drugs served as controls. The permeabilities depended on the physico chemical properties of the drugs which governed both, drug interaction with the nanoparticles as well as with the membranes. Consequently, the influence of dilution of the nanoparticle or free drug preparations on permeabilities was complex. With the exception of [ 75 Se]norcholestenol the permeabilities were higher with free drugs than after binding to nanoparticles. The permeabilities of the membranes decreased in the order cellulose acetate, pig small intestine, silicone rubber, and hairless mouse skin.
    Keywords: Nanoparticles ; [75se]Norcholestenol ; Captopril ; Methylene Blue ; Hydrocortisone ; Doxorubicin ; Dalargin ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0378-5173
    E-ISSN: 1873-3476
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