期刊
JOURNAL OF DRUG TARGETING
卷 16, 期 4, 页码 311-320出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/10611860801899300
关键词
chloramphenicol; chloramphenicol-loaded PLGA nanoparticles; polysorbate-80-coated; technetium-99m; radiolabeling; biodistribution
Chloramphenicol-loaded (CHL) poly-d,l-lactic-co-glycolic acid (PLGA) nanoparticles (NPs) were prepared by emulsification solvent evaporation technique either by using polyvinyl alcohol (PVA) as emulsion stabilizer or polysorbate-80 (PS-80) as surfactant and characterised by transmission electron microscopy, zeta-potential measurements. The NPs were radiolabeled with technetium-99m Tc-(99m) by stannous reduction method. Labeling conditions were optimised to achieve high-labeling efficiency, in vitro and in vivo (serum) stability. The labeled complexes also showed very low transchelation as determined by DTPA challenge test. Biodistribution studies of Tc-99m-labeled complexes were performed after intravenous administration in mice. The CHL-loaded PLGA NPs coated with PS-80 exhibited relatively high brain uptake with comparatively low accumulation in bone marrow to that of free drug and CHL-loaded PLGA NPs (PVA, used as emulsion stabilizer) at 24h post injection time period. This indicates the usefulness of the above delivery system for prolonged use of the antibiotic.
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