| Development of a novel method for the preparation of thiolated polyacrylic acid nanoparticles. | |
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MedLine Citation:
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PMID: 16952008 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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PURPOSE: To develop a novel method for the preparation of thiolated polyacrylic acid nanoparticles via ionic gelation. MATERIALS AND METHODS: In a first step nanoparticles were generated by ionotropic gelation of polyacrylic acid (PAA) of three different molecular weights (100, 240 and 450 kDa) and various cations including Ca2+, Mg2+, Zn2+, Al3+ and Fe3+. Via in vitro characterization of the particles (particle size, size distribution and zeta potential) the optimal preparation conditions were established. Taking into consideration, that thiolated polyacrylic acid (PAA-Cys) displays higher mucoadhesive and permeation enhancing properties than unmodified PAA, PAA-Cys nanoparticles were produced in the same manner with Ca2+, as the most promising results concerning particle size and stability of particles could be achieved with this ionic crosslinker. The nanoparticles were stabilized via the formation of inter- and intrachain disulfide bonds within these particles due to oxidation with H2O2. Ca2+ was removed proximately by the addition of EDTA and exhaustive dialysis. RESULTS: Using the preparation method described above PAA-Cys nanoparticles of a mean diameter of about 220 nm (PAA(100)-Cys), 250 nm (PAA(240)-Cys) and 295 nm (PAA(450)-Cys) can be generated. In comparison to PAA nanoparticles ionically crosslinked with Ca2+, the removal of the crosslinker Ca2+ from PAA-Cys particles led to a nearly three-fold decrease in the zeta potential, from about -7 up to -20 mV. Apart from this advantage, covalently crosslinked PAA-Cys nanoparticles were more firm as they remained stable when incubated in hydrochloride solution, whereas ionically crosslinked particles dissolved at pH lower than 5. CONCLUSIONS: This novel nanoparticulate delivery system seems to be a promising vehicle for the administration of therapeutic proteins, genes and antigens via mucosal membranes. |
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Authors:
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Melanie Greindl; Andreas Bernkop-Schnürch |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2006-08-09 |
Journal Detail:
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Title: Pharmaceutical research Volume: 23 ISSN: 0724-8741 ISO Abbreviation: Pharm. Res. Publication Date: 2006 Sep |
Date Detail:
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Created Date: 2006-09-04 Completed Date: 2006-10-30 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8406521 Medline TA: Pharm Res Country: United States |
Other Details:
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Languages: eng Pagination: 2183-9 Citation Subset: IM |
Affiliation:
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Department of Pharmaceutical Technology, Institute of Pharmacy, Leopold-Franzens-University Innsbruck, Innrain 52, Josef-Möller-Haus, 6020 Innsbruck, Austria. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Acrylic Resins
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chemistry* Cations / chemistry Cross-Linking Reagents Disulfides / chemistry Electrochemistry Hydrogen Peroxide / chemistry Hydrogen-Ion Concentration Microscopy, Electron, Transmission Molecular Weight Nanostructures / chemistry* Oxidants / chemistry Particle Size Sulfhydryl Compounds / chemistry* |
| Chemical | |
Reg. No./Substance:
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0/Acrylic Resins; 0/Cations; 0/Cross-Linking Reagents; 0/Disulfides; 0/Oxidants; 0/Sulfhydryl Compounds; 7722-84-1/Hydrogen Peroxide; 9003-01-4/carbopol 940 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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