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Updated: Mar 13, 2026

PLGA Nanoparticles Formed by Single- or Double-emulsion with Vitamin E-TPGS
Published on: December 27, 2013
Development of EL/PLGA nanoparticles for oral delivery of methotrexate with enhanced bioavailability and reduced
Xianwei Wu1, Qianyu Zhang1, Xiaolin Zeng1
1Pharmaceutical Preparations and Nanomedicine Technology Research Center, College of Pharmacy, Medical School Road, Chongqing Medical University, Yuzhong District, Chongqing, 400042, People's Republic of China.
Abstract:
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.
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