EGFR-targeting peptide conjugated ph-sensitive micelles as a potential drug carrier for photodynamic detection and therapy of cancer

Peng C.-L.Chen Y.-I.Shih Y.-H.Luo T.-Y.MING-JIUM SHIEH2020-02-272020-02-272016https://www.scopus.com/inward/record.uri?eid=2-s2.0-84969776740&partnerID=40&md5=d8c3fbafb75ad018587bca23a8a4c344https://scholars.lib.ntu.edu.tw/handle/123456789/465739Multifunctional 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 HCT116 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. ? 2016 by SCITEPRESS - Science and Technology Publications, Lda. All rights reserved.Chemotherapy; Control release; Micelle; Photothermal therapy; Synergistic effect; Thermosensitive[SDGs]SDG3Biomedical engineering; Cells; Chemotherapy; Diseases; Fluorescence; Micelles; Molecular biology; Motion Picture Experts Group standards; Particle size; Peptides; Photosensitizers; Tumors; Control release; Core shell structure; Epidermal growth factor receptors; Intracellular uptake; Photothermal therapy; Receptor-mediated endocytosis; Synergistic effect; Thermo sensitive; Photodynamic therapyEGFR-targeting peptide conjugated ph-sensitive micelles as a potential drug carrier for photodynamic detection and therapy of cancerconference paper2-s2.0-84969776740