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  • 1
    ISSN: 1573-904X
    Keywords: polymeric micelles ; AFM ; DLS ; pyrene
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To directly visualize and evaluate the aqueous block copolymeric micelles, poly(ethylene oxide)-poly(β-benzyl L-aspartate) (PEO-PBLA) chemically conjugated with pyrene fluorescence molecule, by nanotechnology of atomic force microscopy (AFM). Methods. The block copolymers' PEO-PBLA-Pyrene was first synthesized by reacting with pyrene sulfonyl chloride and PEO-PBLA in tetrahydrofuran (THF) solution and were identified by GPC reflect index, UV and fluorescence detectors. The characterization of physical and chemical properties of PEO-PBLA-Pyrene polymeric micellar solution were examined by the dynamic light scattering (DLS) and critical micelles concentrations (CMC). In addition, the nanotechnology of AFM was used to directly visualize the size and shape of nanopolymeric micelles. Results. The pyrene fluorescence molecule were successfully conjugated at the amino group of the end of PBLA chain by GPC with three different detectors. The size of the aqueous PEO-PBLA-Pyrene polymeric micelles was detected around 57 nm with unimodal distribution by DLS measurement. As a result of this finding, the CMC test was also found out that the fluorescence intensity was increasing around 0.01 ∼ 0.05 mg/ml. Using AFM evaluation of polymeric micellar solution, the morphology of aqueous PEO-PBLA-Pyrene polymeric micelles was observed on round shape and with the narrow dispersity of size range 50 ∼ 80 nm. Conclusions. The presence of PEO-PBLA copolymers with pyrene in an aqueous system formed in a spherical and nano range of polymeric micelles.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1573-904X
    Keywords: polymeric micelles ; FITC ; endothelial ; endocytosis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To determine aortic endothelial cells permeation ability and mechanisms of the aqueous block copolymeric micelles, poly(ethylene oxide)-poly ((β-benzyl L-aspartate) (PEO-PBLA) chemically conjugated with fluroescein isothiocyanate (FITC) by transport study and confocal laser scanning microscopy. Methods. The block copolymers' PEO-PBLA-FITC was first synthesized and characterized by gel permeation chromatography (GPC) reflect index, UV, fluorescence detectors, and critical micelles concentrations (CMC), and atomic force microscopy (AFM). Permeation ability and mechanisms of polymeric micelles in aortic endothelial cells were evaluated by incubating with NaF, NaN3, wortmannin, cytochalasin B inhibitors, at 20°C, and under reverse conditions. FITC and latex particles (40 nm) were also used for comparison of transport ability. The extent of localization of uptake polymeric micelles was established by confocal laser scanning microscopy. Results. The size of the aqueous PEO-PBLA-FITC polymeric micelles was detected at around 56 nm with unimodal distribution by AFM. The CMC test revealed the fluorescence intensity increased to around 0.01 ∼ 0.05 mg/ml. NaF, NaN3, wortmannin, cytochalasin B, 20°C, and reverse experiments inhibited the absorption of polymeric micelles through aortic endothelial cells with apparent permeability coefficients (P) of 18.07 ± 1.03 to 12.98 ± 0.93, 11.31 ± 0.77, 12.44 ±1.23, 6.40 ± 0.23, 11.11 ± 0.46, and 10.22 ± 1.09 X 10−7 cm/sec, respectively. Also, the permeation of FITC and latex on aortic endothelial cells was 70.02 ±4.71, and 2.05± 0.41 X 10−7 cm/sec, respectively. Confocal laser microscopy showed that fluorescent compounds were distributed in the intracellular cytoplasm and nucleus. Conclusions. PEO-PBLA-FITC copolymeric micelles in an aqueous system were transported by energy-dependent endocytosis with 18.07 X 10−7 cm/sec penetrated range and were localized on intracellular and nucleus endothelial cells.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 10 (1993), S. 970-974 
    ISSN: 1573-904X
    Keywords: polymeric micelles ; drug delivery systems ; cancer therapy ; Adriamycin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Polymeric micelles have potential utility as drug carriers. To this end, polymeric micelles based on AB block copolymers of polyethylene oxide (PEG) and poly(aspartic acid) [p(Asp)] with covalently bound Adriamycin (ADR) were prepared. The micelle forming polymer–drug conjugates [PEO-p(Asp(ADR)] were radiolabeled and their biodistribution was investigated after intravenous injection in mice. Long circulation times in blood for some compositions of PEO-p[Asp(ADR)] conjugates were evident, which are usually atypical of colloidal drug carriers. This was attributed to the low interaction of the PEO corona region of the micelles with biocomponents (e.g., proteins, cells). Low uptake of the PEO-p(Asp(ADR)] conjugates in the liver and spleen was determined. The biodistribution of the PEO-p[Asp(ADR)] conjugates was apparently dependent on micelle stability; stable micelles could maintain circulation in blood, while unstable micelles readily formed free polymer chains which rapidly underwent renal excretion. Long circulation times in blood of PEO-p(Asp(ADR)] conjugates are thought to be prerequisite for enhanced uptake at target sites (e.g., tumors).
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1573-904X
    Keywords: Adriamycin ; polymeric micelles ; AB block copolymer ; drug delivery systems
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The entrapment of Adriamycin (ADR) in micelles composed of AB block copolymers (poly(ethylene oxide-co-β-benzyl L-aspartate) (PEO-PBLA)) was investigated. The loading process involved transfer of ADR and PEO-PBLA into an aqueous milieu from dimethyl-formamide (DMF) through a dialysis procedure. Evidence for the physical entrapment of ADR in the polymeric micelles was derived from fluorescence spectroscopy and gel permeation chromatography (GPC). The total fluorescence intensity of ADR was low, suggesting that the drug was self-associated in the micelles. In addition, quenching experiments, using a water-soluble quencher (iodide (I–)), showed that the fluorescence of ADR present in micellar solutions was largely unaffected by I–, whereas the fluorescence of free ADR was readily quenched. From Stern-Volmer plots, quenching constants (KSV) of 2.2 and 17 M−l were determined for ADR in micellar solutions and free ADR, respectively. As a result of the entrapment of ADR in the micelles, ADR binds only slightly serum albumin as evidenced by GPC. In contrast, ADR readily binds serum albumin in aqueous solutions. The findings suggest that ADR is stably entrapped in PEO-PBLA micelles. ADR entrapment in polymeric micelles is expected to affect markedly the pharmacokinetics of ADR.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Bognor Regis [u.a.] : Wiley-Blackwell
    Journal of Polymer Science Part A: Polymer Chemistry 29 (1991), S. 1725-1737 
    ISSN: 0887-624X
    Keywords: (heparin-PEO) grafted segmented polyurethaneurea ; surface modification ; nonthrombogenic surface ; Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: A new synthetic approach for the preparation of segmented polyurethaneurea (SPUU)-PEO-Heparin graft copolymers (B-PEO-Hep) has been developed. The procedure involved the coupling of hexamethylene diisocyanate (HMDI) to soluble Biomer® (B) through an allophanate/biuret reaction. The free isocyanate (NCO) groups attached to Biomer® were then coupled to PEO terminal hydroxyl groups to form PEO grafted Biomer® (B-PEO). B-PEO free hydroxy groups were modified with HMDI to introduce terminal isocyanate groups. The NCO functionalized B-PEO was then coupled to heparin (Hep) functional groups (—OH, —NH2) producing B-PEO-Hep graft copolymer. Synthetic intermediates were confirmed by FTIR, NCO group determination, and toluidine blue heparin assay. Physical characterization techniques, such as contact angle measurements, water swelling, light scattering measurements, and DSC thermal analysis, detailed properties of the graft copolymer containing covalently bound heparin. This new heparinized copolymer can be applied as a coating on other existing blood contacting surfaces without changing bulk properties. The heparin bioactivity observed attests to the usefulness of this new procedure as a coating to improve the blood compatibility of blood-contacting surfaces.
    Additional Material: 13 Ill.
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1042-7147
    Keywords: Polymer complex ; diabetes ; phenylboronic acid ; stimuli-responsive polymer drug delivery system ; Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics
    Notes: A novel polymer complex system sensitive to glucose was studied as a candidate material for formulating a chemically regulated insulin release system. A ternary copolymer of N-vinyl-2-pyrrolidone (NVP), 3-acrylamidophenylboronic acid (AAm-PBA) and N,N-dimethylaminopropylacrylamide (DMAPAA) (poly(NVP-co-PBA-co-DMAPAA)) was synthesized by radical copolymerization. The phenylboronic acid group in this copolymer serves as a glucose sensor moiety. Poly(NVP-co-PBA-co-DMAPAA) was soluble in water in the pH range of 3-12, in sharp contrast to a binary copolymer of NVP and AAm-PBA (poly(NVP-co-PBA)) which showed solubility only under alkaline aqueous conditions, where the boronic acid group is in a tetrahedral ionized form. The protonated amino group in poly(NVP-co-PBA-DMAPAA) contributed to increase the solubility of the polymer under physiological and acidic aqueous conditions. Furthermore, poly(NVP-co-PBA-co-DMAPAA) formed a stable polymer complex gel with poly(vinyl alcohol) (PVA) in pH 7.4 phosphate buffered solution due to the formation of a covalent linkage between the boronic acid groups in ternary copolymer and diol units in PVA. The release of myoglobin as model protein from the complex gel was increased immediately after the addition of glucose, due to the transition of gel into sol state, indicating the feasibility of this complex gel as a candidate material for a glucose-responsive delivery system for insulin.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Journal of Applied Polymer Science 54 (1994), S. 1863-1872 
    ISSN: 0021-8995
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: ABCBA-type amphiphilic block copolymers comprising polydimethylsiloxane (PDMS), poly(ethylene oxide) (PEO), and heparin segments were synthesized by coupling reactions between end-functionalized oligomers. These multiblock copolymers were characterized to examine bulk properties using 1H-NMR, FTIR, end-group analysis, and sulfur elemental analysis. Block copolymers were further characterized in bulk using differential scanning calorimetry and X-ray diffraction measurements. The PDMS glass transition remains unchanged with increasing PEO content, indicating coexistence of pure PDMS with mixed phases. Furthermore, endothermic melting of the block copolymers shifts to higher temperatures and becomes more intense with increasing PEO molecular weight. Additionally, the crystallinity of the PEO segment in the block copolymers increases with increasing PEO molecular weight. The PEO melting endotherm peak shifts from near 318 to 323 K with annealing. In the cooling thermogram, the block copolymers exhibit two crystallization exotherms, one near 303 K and the other near 193 K, attributed to PEO and PDMS recrystallization and nucleation, respectively. © 1994 John Wiley & Sons, Inc.
    Additional Material: 11 Ill.
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Journal of Applied Polymer Science 22 (1978), S. 369-377 
    ISSN: 0021-8995
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Cooligomers and ABA-type block copolymers composed of a hydrophilic monomer, 2-hydroxyethyl methacrylate (HEMA), and a hydrophobic monomer, styrene, were synthesized to study the relation between their microstructure and hydrophilic and hydrophobic functions. Films of cooligomers and ABA-type block copolymers were cast from DMF solutions at 40°C. The wettability, which was determined from the contact angle with water, increased considerably when HEMA mole fraction reached around 0.8 in the cooligomer system and around 0.9 in the ABA-type block copolymer system. The microstructures of the copolymer films were observed by electron microscopy using the osmium tetroxide fixation technique. The morphologic change in the domain structure was observed at an HEMA mole fraction of about 0.8 in the cooligomer system and about 0.9 in the ABA-type block copolymer system. It is suggested that hydrophilic and hydrophobic functions are largely influenced by the state of aggregation of each segment, that is, the size and geometry of the hydrophilic and hydrophobic domains.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Journal of Applied Polymer Science 26 (1981), S. 4207-4216 
    ISSN: 0021-8995
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Various polyamides and polyesters having different numbers of methylene groups in their repeating units have been synthesized and their blood compatibilities have been evaluated in terms of the adhesion behavior of blood platelets on the surface of these condensation polymers by a micro-sphere-column method. The number of methylene groups in the repeating units of polyamides and polyesters influenced the adhesion behavior of platelets and there was an optimum number of methylene groups each in polyamides and polyesters. Poly(hexamethylene terephthalamide) and poly(pentamethylene terephthalate) adsorbed platelets in the smallest number in the polyamide and polyester series, respectively. Blood platelets were adsorbed on polyamides in smaller numbers than on corresponding polyesters. It was found that the platelet adhesion on the surface of polyamides and polyesters was closely related to their crystallinities and the number of the adsorbed platelets decreased linearly with increasing their relative crystallinity.
    Additional Material: 7 Ill.
    Type of Medium: Electronic Resource
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  • 10
    ISSN: 0021-8995
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Various polyamides having a different density of hydrogen bonding, of hydrophilic character, and containing ionic groups have been synthesized and their blood compatibilities were evaluated in terms of the adhesion behavior of blood platelets on polyamide by the microsphere column method. Polyamides containing anionically charged groups such as carboxylate or sulfonate groups adsorbed fewer blood platelets than those with undissociated carboxylate groups. Polyamides having thioether groups adsorbed fewer platelets than those having ether groups. Introduction of a rigid piperazine unit caused an increase in platelet adhesion.
    Additional Material: 9 Ill.
    Type of Medium: Electronic Resource
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