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Development, Characterization, and Investigation of In Vivo Targeted Delivery Efficacy of Luteolin-Loaded, Eudragit S100-Coated mPEG-PLGA Nanoparticles

  • Research Article
  • Theme: Advancements in Modified-release Oral Drug Delivery - Delivery throughout the Gastro-intestinal Tract
  • Published:
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Abstract

Luteolin (Lu) is a kind of flavonoid that has been proved to treat non-alcoholic fatty liver disease by alleviating intestinal microbiota disorder. In this study, luteolin was coated with methoxy poly(ethylene glycol)–poly(dl-lactide-co-glycolic acid) (mPEG-PLGA) using an emulsion solvent evaporation method, and the optimum preparation process was determined by a single-factor experiment combined with response surface methodology (RSM). Methacrylic acid-methyl methacrylate (1:2) copolymer (Eudragit S100) was then used to coat the surface of Lu/mPEG-PLGA nanoparticles. The physical parameters of Eudragit S100-coated Lu/mPEG-PLGA nanoparticles (Lu-NPs), such as appearance, particle size, potential, particle size distribution and drug release, and stability in vitro, were evaluated. In addition, its cytotoxicity in vitro, pharmacokinetics, tissue distribution, and toxicity in vivo were also studied. The results showed that the prepared Lu-NPs had uniform particle size distribution, high encapsulation efficiency, and good stability. Normal colonic epithelial cells showed good tolerance to Lu-NPs. After oral administration, the blood concentration of luteolin peaked at 8 h, and the main tissue distribution was within the colon, confirming its colon-targeted profile. Safety assessments also indicated that no significant changes were observed in main organs after administration of Lu-NPs. The use of Eudragit S100-coated Lu/mPEG-PLGA nanoparticles is a new strategy for colon-targeted delivery of luteolin that encourages luteolin to fulfill its role in the colon.

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Funding

This research was supported by the National Innovation and Entrepreneurship Training Program for College Students (Project No: S202010426025).

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Author notes

  1. Xia Liu and Mengying Zhang contributed equally to this work.

Authors and Affiliations

  1. Department of Pharmacy, College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao, Shandong, China

    Xia Liu, Mengying Zhang, Yuxin Tian, Ruijia Liu & Yanling Gong

  2. Shandong Xinhua Pharmaceutical Company Limited, Zibo, Shandong, China

    Yunfei Wang

  3. Department of Physiology and Pathophysiology, School of Basic Medicine, QingdaoUniversity, Qingdao, China

    Feifei Guo

  4. Qingdao Women and Children’s Hospital, Qingdao, Shandong, China

    Meixing Yan

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  1. Xia Liu
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Contributions

Xia Liu, Mengying Zhang, Yuxin Tian, and Ruijia Liu took part in data collection; Yanling Gong and Meixing Yan involved in design of the study; Feifei Guo and Yunfei Wang took part in statistical analysis; Xia Liu and Mengying Zhang involved in analysis and interpretation of the data; Xia Liu involved in drafting the manuscript; Yanling Gong took part in critical revision of the manuscript.

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Correspondence to Yanling Gong or Meixing Yan.

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Theme: Advancements in Modified-release Oral Drug Delivery - Delivery throughout the Gastro-intestinal Tract

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Liu, X., Zhang, M., Tian, Y. et al. Development, Characterization, and Investigation of In Vivo Targeted Delivery Efficacy of Luteolin-Loaded, Eudragit S100-Coated mPEG-PLGA Nanoparticles. AAPS PharmSciTech 23, 100 (2022). https://doi.org/10.1208/s12249-022-02255-3

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  • DOI: https://doi.org/10.1208/s12249-022-02255-3

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