Herein,　an　amphiphilic　block　copolymer　CD44-targeting　peptide-conjugated　polyethylene　glycol-block-hydroxyethyl　starch-block-poly　(L-lactic　acid)　(CD44p-conjugated　PEG-b-HES-b-PLA)　are　synthesized,　which　could　self-assemble　into　the　pH-responsive　and　CD44-targeting　polymer　micelles　against　breast　cancer　cells　MDA-MB-231.　Emodin　(Emo)　is　a　natural　anthraquino　with　pharmacological　activities　in　anti-tumor　effects.　However,　Emo　suffers　from　poor　water　solubility,　low　biocompatibility,　rapid　systemic　elimination,　and　off-target　side　effects,　resulting　in　unsatisfactory　treatment　outcomes.　Nanotechnology-based　drug　delivery　systems　have　proven　great　potential　for　cancer　chemotherapy.　The　constructed　polymeric　micelles　Emo@CD44p-PM　have　exhibited　an　average　size　of　154.5　±　0.9　nm　characterized　by　DLS　and　TEM.　Further,　the　Emo@CD44p-PM　have　effective　Emo-loading　capacity,　good　thermal　stability,　and　pH　responsiveness.　Intracellular　uptake　study　shows　the　enhanced　cellular　internalization　of　Emo@CD44p-PM　due　to　the　increased　exposure　of　CD44p　enhances　the　cellular　internalization　of　Emo@CD44p-PM　effectively.　Furthermore,　the　in　vitro　results　showed　Emo@CD44p-PM　has　been　observed　good　biocompatibility　and　anti-tumor　effects.　Therefore,　the　polymeric　micelles　Emo@CD44p-PM　provide　a　promising　delivery　strategy　of　targeted　therapy　for　breast　cancer.　©　2022　The　Author(s).　Published　by　IOP　Publishing　Ltd.