PurposeCell membrane-camouflaged nanoparticles (NPs) are drawing increasing attention because their surfaces acquire some characteristics of the cell membranes, making them a unique class of biomimetic materials for diverse applications. Modification of cell membrane or combination of different types of membranes can enhance their functionality.MethodsWe prepared platelet and tumor cell membrane camouflaged β-mangostin-loaded NPs, which were synthesized with platelet–C6 hybrid biomimetic coating, poly(lactic-co-glycolic acid), and β-mangostin (β-PCNPs). Then, we evaluated their targeting ability and anticancer activity against glioma in vitro and in vivo.ResultsBiomimetic coating enhanced active drug targeting and immune escape properties of nanocarrier in C6 and THP-1 cells, respectively, which improved their cytotoxicity. β-PCNPs were characterized to study the inherent properties of both source cells. Compared with bare β-NPs, β-PCNPs exhibited high tumor-targeting capability and induced apoptosis of C6 cells in vitro. Similarly, intravenous administration of drug through β-PCNPs resulted in enhanced tumor-targeting and exhibited excellent rate of inhibition of glioma tumor growth in mice. Moreover, the blood circulation time of drug in mice in the β-PCNP group was markedly prolonged and these mice exhibited better outcome than those in the β-NP group.ConclusionThese results provide a new strategy of utilizing PCNPs as carriers for drug delivery, which improves the targeting efficiency and therapeutic efficacy of chemotherapeutic agents for glioma therapy.