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  • 1
    ISSN: 1520-6882
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1573-904X
    Keywords: nanoparticles ; ampicillin ; peritoneal macrophage ; Salmonella typhimurium ; intracellular infection
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Intracellular targeting of ampicillin by means of polyisohexylcyanoacrylate (PIHCA) nanoparticles was studied in murine peritoneal macrophages infected with Salmonella typhimurium. The intracellular distribution of actively endocytosed nanoparticles was visualized by transmission electron microscopy and confocal microscopy. Nanoparticles were either isolated or closely associated with bacteria within phagosomes or phagolysosomes. Thus the potential of ampicillin-loaded nanoparticles .in targeting of intracellular bacteria is demonstrated. Consequently, ampicillin, which usually penetrates into cells at a low level, is directly carried in, when loaded on nanoparticles, and brought into contact with intracellular bacteria.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 12 (1995), S. 998-1002 
    ISSN: 1573-904X
    Keywords: iontophoresis ; iontohydrokinesis ; angiotensin 2 ; transdermal delivery ; direct current ; pulsed current
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The feasibility of using iontophoresis to enhance the permeation rate of a model peptide was investigated in vitro using hairless mouse skin. Methods. Angiotensin 2 (AT 2) was employed as a permeant probe, using optimum iontophoresis conditions. A number of physicochemical parameters (donor ionic strength; valence of competitive ions; pH of donor solution) were studied with the aim of exploring the mechanisms involved in the iontophoretic transport through the skin: electrokinetic transport or convective transport. For this purpose, the magnitude of the convective solvent flow was also evaluated by the permeation of (3H) H2O. The interest of pulsed currents for peptide delivery was also investigated and the effect of current density and frequency was studied. Results. AT 2 transport was found to be enhanced 20-fold in comparison to passive permeation and was found to be proportional to the current density with direct currents as with pulsed currents. Conclusions. Although the flux enhancement of ions during iontophoresis is due principally to the electrical potential gradient, secondary effects such as convective solvent flow contribute also to flux enhancement of peptide delivery. This effect is dependent of physicochemical conditions of formulation.
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  • 4
    ISSN: 1573-904X
    Keywords: mucoadhesion ; bioadhesion ; latex ; infrared spectroscopy ; adsorption ; nanoparticle
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A Fourier transform infrared spectroscopy/attenuated total reflection technique for direct quantification of adsorbed poly(styrene) latexes on rat intestinal mucosa was developed for deposited latex amounts up to 1.5 g/m2. The method agreed well with another dosage assay of adsorbed particles by turbidimetry after denaturation of the mucus. Adsorption kinetics were made under static conditions at latex concentrations of 4 g/L in physiological saline. Ninety percent of equilibrium was reached after 10 min for a particle size of 230 nm, 20 min for a size of 320 nm, and 30 min for a size of 670 nm. The plateaus were between 0.6 and 0.9 g/m2 (adsorbed mass per apparent surface of mucosa). The first phase of the kinetics was theoretically approached by a diffusion model in the suspension medium. Mucosa from rat jejunum and ileum could be considered as a homogeneous biological model for latex adsorption.
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  • 5
    ISSN: 1573-904X
    Keywords: peptides ; oral delivery ; glycerolipidic prodrugs ; gastric juice ; intestinal juice ; α-chymotrypsin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A diglyceride derivative of a pentapeptide renin inhibitor, the 1,3-dipalmitoyl-[Iva-Phe-Nle-Sta-Ala-Sta-acetyl]-glycerol was synthesized and tested in vitro as a potential prodrug for oral administration. The ability of the diglyceride analog to inhibit the renin activity was equivalent to that of the parent peptide after predigestion with pancreatic lipase. Furthermore, the presence of the palmitoyl groups was found to induce, in vitro, an efficient protection of the peptide from gastric and intestinal hydrolysis. During incubation with intestinal and gastric fluids, and with α-chymotrypsin and pancreatic lipase, the glycerolipidic derivative was more stable than the peptide alone. These results support the use of glycerolipidic prodrug for oral administration of peptides.
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  • 6
    ISSN: 1573-904X
    Keywords: nanoparticles ; poly(isobutylcyanoacrylate) ; cyclodextrins ; hydroxypropyl-β-cyclodextrin ; progesterone ; drug loading
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The aim of this study was to prepare and characterize nanoparticulate systems constituted of poly(isobutylcyanoacrylate) and cyclodextrins and intended for increasing the loading of the particles with lipophilic substances. Progesterone was used as a model substance. Methods. Nanoparticles were prepared by polymerization of isobutyl-cyanoacrylate in presence of cyclodextrins or progesterone/ hydroxy-propyl-β-cyclodextrin complex. Particle size, zeta potential, cyclodextrin and progesterone loading of the particles were determined. Results. Nanoparticles could be easily prepared in presence of cyclodextrins. An increase in hydroxypropyl-β-cyclodextrin concentration resulted in small nanoparticles (less than 50 nm). It was found that large amounts of cyclodextrins remained associated to the particles, resulting in a 50 fold increase in progesterone loading compared to nanoparticles prepared in absence of cyclodextrins. Conclusions. The poly(isobutylcyanoacrylate)—cyclodextrin nanoparticles were characterized by the presence of many lipophilic sites belonging to the cyclodextrins which were firmly anchored to the structure of the particles. Therefore, this new type of nanoparticles offers probably an opportunity for increasing the loading of nanoparticles with various lipophilic drugs.
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  • 7
    ISSN: 1573-904X
    Keywords: Oligonucleotides ; nanoparticles ; polyalkylcyanoacrylate ; ion pairs ; oligonucleotide hydrolysis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Adsorption of oligothymidylates on polyisobutyl- or polyisohexylcyanoacrylate nanoparticles was achieved in the presence of hydrophobic cations such as tetraphenylphosphonium chloride or quaternary ammonium salts. Results suggested that oligonucleotide adsorption on the nanoparticles was mediated by the formation of ion pairs between the negatively charged phosphate groups of the nucleic acid chain and the hydrophobic cations. The adsorption efficiency of oligonucleotide–cation complexes on nanoparticles was found to be highly dependent upon several parameters: oligonucleotide chain length, nature of the cyanoacrylic monomer, hydrophobicity of cations used as ion-pairing agents, and ionic concentration of the medium. Carrier capacity of polyisohexylcyanoacrylate nanoparticles for oligothymidylates (16 nucleotides) complexed with cetyltrimetylammonium bromide in the presence of 0.15 M NaCl was determined to be 5 µmol/g polymer. The in vitro protection of oligothymidylates adsorbed to nanoparticles against degradation by a 3′-exonuclease (snake venom phosphodiesterase) was also demonstrated. These results showed that nanoparticles can be considered as convenient carriers for the protection and delivery of Oligonucleotides to cells in culture and for future applications in vivo.
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  • 8
    ISSN: 1573-904X
    Keywords: oligodeoxynucleotides ; nanoparticles ; polyalkylcy-anoacrylate ; cellular uptake ; oligonucleotide hydrolysis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Oligonucleotides can be adsorbed on polyisohexylcyanoacrylate nanoparticles in the presence of hydrophobic quartenary ammonium salts. Oligonucleotides bound to nanoparticles are protected from nuclease attack both in buffer and in cell culture media. Cellular uptake of Oligonucleotides is increased when they are adsorbed onto nanoparticles as a result of the capture of nanoparticles by an endocytic/phagocytic pathway. Intracellular stability towards nucleolytic degradation is increased in the presence of nanoparticles. These results show that nanoparticles can be considered as convenient carriers for the protection and delivery of oligonucleotides to cells.
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  • 9
    ISSN: 1573-904X
    Keywords: diclofenac ; indomethacin ; nanocapsules ; poly(D,L-Lactide) ; gastrointestinal tolerance ; intravenous ; oral
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 10
    ISSN: 1573-904X
    Keywords: mucoadhesion ; bioadhesion ; latex ; isotherm ; adsorption ; nanoparticle
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Adsorption isotherms of poly(styrene) latexes on rat intestinal mucosa were studied under static conditions and analyzed according to different isotherm classifications. Isotherms of latexes with a particle size up to 670 nm had the characteristic shape of a disperse adsorbate on a porous adsorbent. Plateaus were reached at latex concentrations of about 2.5 g/L. The results indicated an increase in adsorption with the size and the hydrophilicity of the latexes. Typically, a surfactant-free carboxylate latex of 230 nm had a plateau of 0.66 g/m2, and a latex of 320 nm with added sodium dodecyl sulfate had a plateau of 0.881 g/m2. Surfactant-free carboxylate latex of 2 µm had a Langmuirian isotherm with a plateau level of 2.616 g/m2, which corresponded to a monolayer of adsorbed particles on the surface of mucosa. Desorption studies showed that the adsorption was irreversible. Adhesion to the mucous gel layer would therefore be limited by the mucus turnover.
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