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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 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.

EGFR-targeting Peptide Conjugated pH-sensitive Micelles as a Potential Drug Carrier for Photodynamic Detection and Therapy of Cancer