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<p>Apocynin (APO), a plant-derived acetophenone, is recognized for its potent antioxidant and anti-inflammatory properties. This positions it as a potential treatment for ulcerative colitis (UC). Despite its therapeutic promise, APO’ s clinical effectiveness is limited by poor aqueous solubility and lack of targeted delivery. This leads to suboptimal bioavailability and systemic side effects. This study aimed to overcome these challenges by formulating APO-loaded nanostructured lipid carriers (NLCs) with a dual polymeric coating of chitosan (CS) and Eudragit S100 (ES-100) for colon-targeted delivery and improved mucosal adhesion. NLCs were prepared using a hot homogenization method and optimized with Design Expert software. The uncoated formulation exhibited a particle size of 71 ± 0.2&#xa0;nm, a zeta potential of –17.8 ± 0.1&#xa0;mV, an entrapment efficiency of 83.4 ± 1.2%, and a drug loading of 4.6 ± 0.5%. Coating with CS and ES-100 increased the particle size to 262.4 ± 1.5&#xa0;nm and shifted the zeta potential to –24.6 ± 0.1&#xa0;mV. Morphological and structural assessments using SEM, FT-IR, and XRD verified spherical shape, drug-polymer compatibility, and a transition to an amorphous state. The coated formulation exhibited strong mucoadhesion and colon specific drug release. In vitro drug release was pH-responsive, with minimal release in stomach and small intestine, and sustained release at colonic pH (89.5 ± 3.1% over 48&#xa0;h). In vivo studies in a murine colitis model showed marked therapeutic improvement and downregulation of pro-inflammatory markers like COX-2, TNF-α, and IL-1β. This confirms the formulation’s mucoadhesive and colon-specific efficacy for UC treatment.</p>

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Novel Dual Coated Apocynin Nanoparticles: Mucoadhesive and pH-Based Targeted Drug Release Approach For Ulcerative Colitis Treatment

  • 期刊论文

  • 发表日期：

    2025年12月17日

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  • Irfa Basharat Rajput,
  • Dildar Khan,
  • Asim.ur. Rehman,
  • Noor Ullah,
  • Rashna Mirza,
  • Salman Khan,
  • Naveed Ahmed,
  • Kifayat Ullah Shah

摘要

Apocynin (APO), a plant-derived acetophenone, is recognized for its potent antioxidant and anti-inflammatory properties. This positions it as a potential treatment for ulcerative colitis (UC). Despite its therapeutic promise, APO’ s clinical effectiveness is limited by poor aqueous solubility and lack of targeted delivery. This leads to suboptimal bioavailability and systemic side effects. This study aimed to overcome these challenges by formulating APO-loaded nanostructured lipid carriers (NLCs) with a dual polymeric coating of chitosan (CS) and Eudragit S100 (ES-100) for colon-targeted delivery and improved mucosal adhesion. NLCs were prepared using a hot homogenization method and optimized with Design Expert software. The uncoated formulation exhibited a particle size of 71 ± 0.2 nm, a zeta potential of –17.8 ± 0.1 mV, an entrapment efficiency of 83.4 ± 1.2%, and a drug loading of 4.6 ± 0.5%. Coating with CS and ES-100 increased the particle size to 262.4 ± 1.5 nm and shifted the zeta potential to –24.6 ± 0.1 mV. Morphological and structural assessments using SEM, FT-IR, and XRD verified spherical shape, drug-polymer compatibility, and a transition to an amorphous state. The coated formulation exhibited strong mucoadhesion and colon specific drug release. In vitro drug release was pH-responsive, with minimal release in stomach and small intestine, and sustained release at colonic pH (89.5 ± 3.1% over 48 h). In vivo studies in a murine colitis model showed marked therapeutic improvement and downregulation of pro-inflammatory markers like COX-2, TNF-α, and IL-1β. This confirms the formulation’s mucoadhesive and colon-specific efficacy for UC treatment.