Acta Pharmaceutica Sinica B (Oct 2020)

Lactoferrin-mediated macrophage targeting delivery and patchouli alcohol-based therapeutic strategy for inflammatory bowel diseases

  • Yuge Zhao,
  • Yuting Yang,
  • Jiaxin Zhang,
  • Rong Wang,
  • Biyun Cheng,
  • Dipika Kalambhe,
  • Yingshu Wang,
  • Zeyun Gu,
  • Dongying Chen,
  • Bing Wang,
  • Yongzhuo Huang

Journal volume & issue
Vol. 10, no. 10
pp. 1966 – 1976

Abstract

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Inflammatory bowel diseases (IBD) are the incurable chronic recurrent gastrointestinal disorders and currently lack in safe and effective drugs. In this study, patchouli alcohol, a main active compound of traditional Chinese herb patchouli, was developed into biomimetic liposomes for macrophage-targeting delivery for IBD treatment. The developed lactoferrin-modified liposomes (LF-lipo) can specifically bind to LRP-1 expressed on the activated colonic macrophages and achieve cell-targeting anti-inflammatory therapy. LF-lipo reduced the levels of inflammatory cytokines and ROS and suppressed the MAPK/NF-κB pathway. LF-lipo also suppressed the formation of NLRP3 inflammasome and the consequent IL-1β activation. LF-lipo showed improved therapeutic efficacy in a DSS-induced colitis murine model, evidenced by the reduced disease activity index, the improved colon functions, and the downregulated inflammatory cytokines in the colon. LF-lipo provided an effective and safe macrophage-targeting delivery and therapeutic strategy for addressing the unmet medical need in IBD management.

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