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Beta-Sitosterol-Conjugated Sinapic Acid-Engineered Nanoliposome: Biomucoadhesive and Enzyme-Responsive Targeted Oral

Kanika1, Ajay Kumar1, Anas Ahmad2

  • 1Chemical Biology Unit, Institute of Nano Science and Technology, Sector 81, Knowledge City, Sahibzada Ajit Singh Nagar, Mohali 140306, Punjab, India.

ACS Applied Materials & Interfaces
|April 29, 2025
PubMed

Insights

Chitosan-armored nanoliposomes (C@MN@DMBe-S) offer a novel oral treatment for ulcerative colitis (UC). This system protects the drug in the stomach, targets the colon, and reduces inflammation for enhanced healing.

Area of Science:

  • Nanomedicine
  • Gastroenterology
  • Drug Delivery Systems

Background:

  • Ulcerative colitis (UC) treatment faces challenges with oral drug delivery, including degradation and poor targeting.
  • Existing therapies require improved efficacy and safety through advanced delivery systems.

Purpose of the Study:

  • To develop an enzyme- and pH-responsive, mucoadhesive oral nanoliposome system for UC treatment.
  • To encapsulate a NLRP3 inhibitor (MNS) and beta-sitosterol-sinapic acid conjugate (Be-S) for synergistic therapeutic effects.

Main Methods:

  • Chitosan-armored 1,2-dimyristoyl-sn-glycero-3-phosphoglycerol (DMPG) nanoliposomes (C@MN@DMBe-S) were formulated using thin-film hydration and extrusion.
  • The nanoliposomes were characterized for stability, mucoadhesion, and drug release kinetics.
  • In vivo studies assessed therapeutic efficacy, anti-inflammatory effects, and impact on gut microbiota.

Main Results:

  • C@MN@DMBe-S demonstrated structural stability, mucoadhesion, and protection from gastric degradation.
  • The formulation showed sustained release of MNS and sinapic acid in the inflamed colon.
  • Therapeutic efficacy was superior to free MNS, with significant downregulation of inflammatory markers (NF-κB, NLRP3, Caspase-1, IL-1β) and upregulation of MUC5AC.
  • Reduced neutrophil infiltration and regulated immune cell expression were observed.

Conclusions:

  • The developed chitosan-armored nanoliposomes (C@MN@DMBe-S) represent a promising oral delivery strategy for ulcerative colitis.
  • This system effectively targets the colon, provides sustained drug release, and exhibits significant anti-inflammatory and mucosal healing properties.
  • The armor- and enzyme-responsive strategy offers a novel approach for oral nanomedicine in mitigating UC.
Keywords:
3,4-methylenedioxy-β-nitrostyreneNLRP3 inhibitorbeta-sitosterol–sinapic conjugatebiomucoadhesive nanoliposomemucosal healingulcerative colitis

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