Block Copolymer Crosslinked Nanoassemblies Co-Entrapping Acridine Yellow and Doxorubicin for Cancer Theranostics.
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Date
2013-10
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Abstract
Aims: To develop block copolymer crosslinked nanoassemblies (CNAs) that co-entrap an
imaging dye (Acridine Yellow: AY) and therapeutic agent (doxorubicin: DOX) as novel
nanoparticle drug carriers for a combined application of drug delivery-based therapy and
diagnostic imaging technologies (theranostics).
Study Design: Physicochemical properties of AY-CNAs, such as molecular weight,
particle size, surface charge, drug entrapment yield, and drug release profiles, were
characterized prior to determining intracellular uptake profile, in vitro cytotoxicity, and in
vivo tissue distribution patterns of the particles.
Place and Duration of Study: Department of Pharmaceutical Sciences (University of
Kentucky), between June 2012 and January 2013.
Methodology: The AY-crosslinked CNAs (CNAs) were synthesized from biocompatible
poly(ethylene glycol)-poly(aspartate) block copolymers by using AY as a crosslinker while
DOX was physically entrapped in the particle through an ionic interaction. AY-CNAs and
AY-CNAs with DOX were characterized to determine their particle properties (molecular
weight, size, and optical properties), intracellular uptake and cytotoxicity in an in vitro cell
culture system using human colon HT29 and lung A549 cancer cell lines, and tissue
accumulation and tumor-preferential drug delivery efficiency ex vivo with a xenograft mouse tumor model.
Results: AY-CNAs maintained nanoscale particle sizes (< 20 nm), fluorescence optical
properties, and negative surface charge before and after drug entrapment. AY-CNAs with
DOX were confirmed to kill cancer cells as effectively as free drug formulations, and to
enhance intracellular uptake in vitro and tumor accumulation ex vivo.
Conclusion: These results demonstrate that block copolymer nanoassemblies
crosslinked with an imaging dye are promising platforms for the development of
theranostic nanoparticle drug carriers.
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Keywords
Nanoparticles, nanoassemblies, drug carriers, drug delivery, imaging, theranostics
Citation
Cao Pengxiao, Ponta Andrei, Kim JiAe, Bae Younsoo. Block Copolymer Crosslinked Nanoassemblies Co-Entrapping Acridine Yellow and Doxorubicin for Cancer Theranostics. British Journal of Pharmaceutical Research. 2013 Oct; 3(4): 523-535.