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Issue 12, 2018
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Superior proapoptotic activity of curcumin-loaded mixed block copolymer micelles with mitochondrial targeting properties

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Abstract

Targeting tumor cell mitochondria is a prospective strategy for highly effective anticancer therapy. Consequently, the development of potent systems for the targeted delivery of mitochondria-acting therapeutics to mitochondria has the potential to boost this sector of nanomedicine. In this study, a functional mixed micellar system based on two co-assembled triblock copolymers, poly(2-(dimethylamino)ethyl methacrylate)-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate) bearing triphenylphosphonium ligands (PDMAEMA(TPP+)20-b-PCL70-b-PDMAEMA(TPP+)20) and poly(ethylene oxide)-b-poly(ε-caprolactone)-b-poly(ethylene oxide) (PEO113-b-PCL70-b-PEO113), was assessed for the mitochondria targeted delivery of curcumin. The high proapoptotic activity of the system and the sub-cellular mechanisms of cytotoxicity were demonstrated using a chemosensitive HL-60 cell line and its resistant alternative HL-60/DOX. Next, the successful localization of nanocarriers in mitochondria was proved by fluorescence microscopy with the aid of DAPI (4′,6-diamidino-2-phenylindole) as a cellular localization tracker. The in vitro experiments revealed the great potential of the functional system developed for the targeted delivery of curcumin to mitochondria, causing programmed tumor cell death.

Graphical abstract: Superior proapoptotic activity of curcumin-loaded mixed block copolymer micelles with mitochondrial targeting properties

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Supplementary files

Article information


Submitted
11 Jun 2018
Accepted
05 Oct 2018
First published
08 Oct 2018

Biomater. Sci., 2018,6, 3309-3317
Article type
Paper

Superior proapoptotic activity of curcumin-loaded mixed block copolymer micelles with mitochondrial targeting properties

D. Momekova, I. Ugrinova, M. Slavkova, G. Momekov, G. Grancharov, V. Gancheva and P. D. Petrov, Biomater. Sci., 2018, 6, 3309
DOI: 10.1039/C8BM00644J

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