Journal
ACS APPLIED MATERIALS & INTERFACES
Volume 6, Issue 24, Pages 22709-22718Publisher
AMER CHEMICAL SOC
DOI: 10.1021/am5068723
Keywords
polyphosphoester; hydrophobicity; micellar core; cancer therapy; drug delivery
Funding
- Ministry of Science and Technology of the People's Republic of China [2014AA020708]
- National Natural Science Foundation of China [51473043, 51203145, 21304028, 51390482]
- Fundamental Research Funds for the Central Universities [2014HGCH0014]
- Key Project of Anhui Provincial Educational Department [JZ2014AJZR0113]
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Recently, micelles, which are self-assembled by amphiphilic copolymers, have attracted tremendous attention as promising drug delivery systems for cancer treatment. Thus, the hydrophobic core of the micelles, which could efficiently encapsulate small molecular drug, will play a significant role for the anticancer efficiency. Unfortunately, the effect of hydrophobicity of micellar core on its anticancer efficiency was rarely reported. Herein, the amphiphilic diblock polymers of poly(ethylene glycol) and polyphosphoester with different side groups (butyl, hexyl, octyl) were synthesized to tune the hydrophobicity of the micellar core. We found that the in vitro cytotoxicity of the DOX-loaded micelles decreased with the increasing hydrophobicity of micellar core due to the drug release rate. However, following systemic delivery, the DOX-loaded micelles with the most hydrophobic core exhibited the most significant inhibition of tumor growth in a MDA-MB-231 tumor model, indicating the importance of hydrophobicity of core on the antitumor efficacy of drug delivery systems.
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