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Graphical abstract Figure. No caption available. ABSTRACT A polymer‐lipid hybrid nanocarrier was developed to encapsulate psoralen (PSO) to improve its water solubility and bioavailability. The effects of PSO‐loaded polymer‐lipid hybrid nanoparticles (PSO‐PLNs) on breast cancer MCF‐7 cells were investigated. PSO‐PLNs were prepared through a nanoprecipitation method and were optimized by a central composite design‐response surface methodology using particle size and entrapment efficiency as indices. Dynamic light scattering and transmission electron microscopy analysis confirmed the physicochemical characterizations of PSO‐PLNs, which had an average size of 93.44 ± 2.39 nm and a zeta potential of −27.63 ± 0.31 mV. In vitro drug release of PSO‐PLNs was evaluated using dialysis and showed a delayed release compared with free PSO. The in vivo anticancer efficiency of PSO‐PLNs was appreciated using a MCF‐7 breast tumor model. Administration of PSO‐PLNs showed similar antitumor efficacy but lower toxicity compared with doxorubicin. Our designed nanocarriers successfully optimized the pharmacokinetics of PSO via improved systemic delivery.