Enhanced effects of curcumin encapsulated in polycaprolactone-grafted oligocarrageenan nanomicelles, a novel nanoparticle drug delivery system
[Display omitted] •κ-Carrageenans from seaweeds were functionalized to form amphiphilic copolymers.•These copolymers formed nanomicelles which efficiently encapsulate hydrophobic drugs.•The micelles are non-cytotoxic on endothelial cells and zebrafish.•Micelles improved cellular uptake and anti-infl...
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Veröffentlicht in: | Carbohydrate polymers 2019-08, Vol.217, p.35-45 |
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Sprache: | eng |
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•κ-Carrageenans from seaweeds were functionalized to form amphiphilic copolymers.•These copolymers formed nanomicelles which efficiently encapsulate hydrophobic drugs.•The micelles are non-cytotoxic on endothelial cells and zebrafish.•Micelles improved cellular uptake and anti-inflammatory effects of curcumin.•Delivery of hydrophobic compounds into different organs in mice was enhanced.
One of the most effective strategies to enhance the bioavailability and the therapeutic effect of hydrophobic drugs is the use of nanocarriers. We have used κ-carrageenan extracted from Kappaphycus alvarezii to produce oligocarrageenan via an enzymatic degradation process. Polycaprolactone (PCL) chains were grafted onto the oligocarrageenans using a protection/deprotection technique yielding polycaprolactone-grafted oligocarrageenan. The resulting amphiphilic copolymers formed spherical nanomicelles with a mean size of 187 ± 21 nm. Hydrophobic drugs such as curcumin were efficiently encapsulated in the micelles and released within 24–72 h in solution. The micelles were non-cytotoxic and facilitated the uptake of curcumin by endothelial EA-hy926 cells. They also increased the anti-inflammatory effect of curcumin in TNF-alpha-induced inflammation experiments. Finally, in vivo experiments supported a lack of toxicity in zebrafish and thus the potential use of polycaprolactone-grafted oligocarrageenan to improve the delivery of hydrophobic compounds to different organs, including liver, lung and brain as shown in mice. |
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ISSN: | 0144-8617 1879-1344 |
DOI: | 10.1016/j.carbpol.2019.04.014 |