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<p>For rheumatoid arthritis (RA), low-dose methotrexate (MTX) is first-line therapy but limited by gastrointestinal irritation, low bioavailability, and systemic toxicity. Herein, EL/PLGA nanoparticles loaded with MTX (MTX@EL/PLGA NPs) were prepared via double emulsion solvent evaporation method and evaluated in vitro and in vivo. Optimized NPs had uniform morphology with particle size of (140.3 ± 2.01) nm and zeta potential of (-30.53 ± 1.79) mV. Compared with free MTX, MTX@EL/PLGA NPs exhibited pH-responsive release in vitro, which minimized drug leakage in simulated gastric fluid and achieved efficient release in simulated intestinal fluid. In vivo, these NPs increased relative bioavailability by 195.07% with sustained plasma concentrations, accompanied with mitigated MTX-induced gastrointestinal damage and hematotoxicity without liver/kidney impairment. This study demonstrated that MTX@EL/PLGA NPs improved oral bioavailability and safety of MTX, a promising oral nano-delivery system for rheumatoid arthritis therapy.</p>

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Development of EL/PLGA nanoparticles for oral delivery of methotrexate with enhanced bioavailability and reduced toxicity

  • 期刊论文

  • 发表日期：

    2026年3月11日

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  • Xianwei Wu,
  • Qianyu Zhang,
  • Xiaolin Zeng,
  • Peng Qian,
  • Xianchun Gao,
  • Dongjun Jiang,
  • Huali Chen

摘要

For rheumatoid arthritis (RA), low-dose methotrexate (MTX) is first-line therapy but limited by gastrointestinal irritation, low bioavailability, and systemic toxicity. Herein, EL/PLGA nanoparticles loaded with MTX (MTX@EL/PLGA NPs) were prepared via double emulsion solvent evaporation method and evaluated in vitro and in vivo. Optimized NPs had uniform morphology with particle size of (140.3 ± 2.01) nm and zeta potential of (-30.53 ± 1.79) mV. Compared with free MTX, MTX@EL/PLGA NPs exhibited pH-responsive release in vitro, which minimized drug leakage in simulated gastric fluid and achieved efficient release in simulated intestinal fluid. In vivo, these NPs increased relative bioavailability by 195.07% with sustained plasma concentrations, accompanied with mitigated MTX-induced gastrointestinal damage and hematotoxicity without liver/kidney impairment. This study demonstrated that MTX@EL/PLGA NPs improved oral bioavailability and safety of MTX, a promising oral nano-delivery system for rheumatoid arthritis therapy.