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Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Triggered doxorubicin release using redox-sensitive hyaluronic acid-g-stearic acid micelles for targeted cancer
Gyeong-Won Jeong1, Young-Il Jeong2, Jae-Woon Nah1
1Department of Polymer Science and Engineering, Sunchon National University, 255 Jungang-ro, Suncheon, Jeonnam 57922, Republic of Korea.
Abstract:
To develop a carrier for targeted drug delivery and triggered drug release in a reducing-tumor environment, reduction-sensitive hyaluronic acid-g-stearic acid (HCS) micelles were synthesized using a coupling agent. The HCS 40% was shown to have a more compact particle size than HCS 20% and the particle size of doxorubicin (DOX)-loaded HCS (HCSD) was increased relative to that of HCS micelles. The behavior of DOX release from HCSD showed that DOX was rapidly released in GSH (10 mM) solution. The site-specific targeting effect of HCSD nanoparticles was investigated by cellular uptake and competition assay at HCT116 and CT26 cell lines. An in vivo study of HCSD revealed that tumor suppression and site-specific targeted delivery of HCSD nanoparticles in HCT116-xenografted tumors were more superb than in the CT26-xenografted tumor. These results suggest that HCSD nanoparticles can be expected to have high therapeutic efficacy because they enable targeted drug delivery and rapid drug release.
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