chemotherapeutic agents to selectively target tumor cells always causes serious side effects on normal tissues. Recently, nano-sized tumor-targeted drug delivery systems (DDSs) that specifically deliver therapeutic agents to desired tumor sites have achieved satisfying outcome in cancer chemotherapy. [1] Among various kinds of nanocarriers, such as inorganic nanomaterials, micelles and liposomes, core-shell structured nanomicelle made from peptide amphiphile (PA) is a class of important nano-sized DDSs in biomedical applications. [2,3] Due to merits of structural and functional diversity, excellent biocompatibility and biodegradability, PA is able to self-assemble to form diverse stable nanostructures such as nanomicelles, nanovesicles, and nanotubes etc. [3] Moreover, PA-based DDSs have been reported to display great potential in drug encapsulation, cell internalization, and specific drug delivery in tumor cells. For example, TAT PAs comprising of a TAT 48-60 peptide and hydrocarbon tails (octanoic acid molecules) could self-assemble into β-sheet structures and transport paclitaxel (PTX) to target tumor cells. [4] A supramolecular peptide-amphiphile (SPAs) comprising of dendritic poly (l-lysine) segment and poly (l-leucine) segment was constructed for intracellular drug delivery of doxorubicin (DOX). Because of non-covalent interactions between two peptide domains, SPAs exhibited pHresponsive DOX release in tumor cells. [5] On the other hand, the distinctive pathophysiological and biological characteristics of tumor environment have been utilized to accelerate drug delivery and stimulate drug release by stimulus-responsive PAbased DDSs. [6] The lysosomal acid protease Cathepsin B, which is highly expressed in various types of metastatic and aggressive tumor cells, has been proved to be able to specifically recognize and cleave a tetra-peptide linker GFLG. [7,16] Much endeavor has been made to fabricate Cathepsin B-responsive DDSs through introducing GFLG linker. An amphiphilic copolymer-gemcitabine conjugate was reported, in which gemcitabine was attached to the hydrophobic segment via GFLG linkage, for enzyme-sensitive drug release and fluorescent imaging-guided cancer therapy. [8] In addition, a multifunctional Ce6-doped nanocomposite (UCNP@mSiO 2-Ce6) containing