Authors:
Cheng-Liang Peng
1
;
Yuan-I Chen
2
;
Ying-Hsia Shih
1
;
Tsai-Yueh Luo
1
and
Ming-Jium Shieh
2
Affiliations:
1
Institute of Nuclear Energy Research, Taiwan
;
2
National Taiwan University, Taiwan
Keyword(s):
Thermosensitive, Photothermal Therapy, Chemotherapy, Micelle, Control Release, Synergistic Effect.
Related
Ontology
Subjects/Areas/Topics:
Bioimaging
;
Biomedical Engineering
;
Medical Imaging and Diagnosis
Abstract:
Multifunctional theranostics have recently been intensively explored to optimize the efficacy and safety. Herein, we report multifunctional micelle that constructed from graft copolymer PEGMA-co-PDPA and diblock copolymer mPEG-b-PCL as the carrier of hydrophobic photosensitizer, chlorin e6 (Ce6) for simultaneous fluorescence imaging and photodynamic therapy. The functional inner core of PEGMA-co-PDPA exhibited pH stimulate to accelerate drug release under slightly acidic microenvironments of tumors and the outer shell of micelles with epidermal growth factor receptor (EGFR)-targeting GE11 peptides for active targeting of EGFR-overexpressing cancer cells. The results demonstrate that GE11-conjugated chlorin e6-loaded micelles (GE11-Ce6-micelles) with particle size around 100 nm and the micelles had well defined core shell structure which was evaluated by TEM. In the in vitro cellular uptake studies, GE11-Ce6-micelles exhibited a higher amount of intracellular uptake of chlorin e6 in H
CT116 cancer cells (EGFR high expression) via receptor-mediated endocytosis, in contrast with the time-dependent passive uptake of the non-targeted Ce6-micelles, thereby providing a effective photocytotoxic effect on the HCT116 cancer cells. In vivo study revealed that GE11-Ce6-micelles exhibited tumor targeting for photodynamic detection and excellent inhibition on tumor growth after irradiation, indicating that GE11-Ce6-micelles could be successfully applied to the effective fluorescence imaging and photodynamic therapy of cancer.
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