Convergent synthesis and characterization of fatty acid-conjugated poly(ethylene glycol)-block-poly(epsilon-caprolactone) nanoparticles for improved drug delivery to the brain
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AbstractHerein, for the first time, we report the synthesis, preparation, and characterization of fatty acid-conjugated poly(ethylene glycol)-block-poly(epsilon-caprolactone) nanoparticles (FA-NPs), with the ultimate goal of improving drug delivery to the brain. These nanoparticles had a nano-size (<100 nm) with a fairly narrow size distribution (PDI = 0.2–0.3). They were non-hemolytic and non-cytotoxic. By employing curcumin, a poorly soluble herbal molecule, as a model, FA-NPs enhanced the drug solubility by >5.4 × 105x. They showed moderate stability in serum and exhibited zero-order drug release. As a proof-of-concept, the brain uptake of oleic acid-NPs (OA-NPs) was examined in rats after intravenous injections. Relative to 1% DMSO and PEG-NPs formulations, the OA-NPs enhanced the brain accumulation of the loaded cargo by 4.28 and 1.94x, respectively. Apparently, these nanoparticles hold considerable promise in drug delivery to the brain and their potential applications for disorders of the central nervous system should be explored.
All Author(s) ListHo Yin Li, Bowen Zhang, Pui Shan Chan, Jingwen Weng, Chi Kwan Tsang, Wai Yip Thomas Lee
Journal nameEuropean Polymer Journal
Year2018
Month1
Volume Number98
Pages394 - 401
ISSN0014-3057
eISSN1873-1945
LanguagesEnglish-United Kingdom

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