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<p>To develop and optimize scutellarin-loaded mesoporous silica nanoparticles (MSNs) incorporated within thermosensitive in-situ nasal gel for enhanced Alzheimer’s disease therapy, addressing poor bioavailability and limited brain penetration of conventional oral formulations. MSNs were synthesized using sol-gel method with CTAB as template, TEOS as silica source, and NH₄OH as catalyst. Formulation optimization employed 3³ Box-Behnken factorial design with response surface methodology, evaluating entrapment efficiency, particle size, and zeta potential. Optimized MSNs were incorporated into Poloxamer-based thermosensitive nasal gels. Comprehensive characterization included FTIR, XRD, SEM analysis, in-vitro release studies, <i>ex vivo</i> permeation using goat nasal mucosa, and <i>in vivo</i> Morris water maze behavioral assessments. The optimal formulation contained 625&#xa0;mg CTAB, 7.5 mL TEOS, and 9.5 mL NH₄OH, achieving 76.4 ± 2.6% entrapment efficiency, 68.3 ± 3.1&#xa0;nm particle size, and − 27.1 ± 1.0 mV zeta potential with excellent model predictability (R² &gt; 0.93). NF2 gel formulation demonstrated optimal gelation temperature (35.4&#xa0;°C), sustained drug release (88.9% at 12&#xa0;h), and enhanced permeation (81.7% in 12&#xa0;h). <i>In vivo</i> studies revealed significant cognitive improvement with 18.4% better spatial learning, reduced acetylcholinesterase activity (25.9% decrease), and enhanced antioxidant enzyme activities compared to pure scutellarin treatment. The developed nano-gel system successfully bypassed blood-brain barrier limitations, providing superior therapeutic efficacy through direct nose-to-brain targeting. This innovative formulation demonstrates promising preclinical therapeutic potential for Alzheimer’s disease management, warranting comprehensive preclinical evaluation and eventual clinical translation studies.</p>

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Development and Fabrication of Mesoporous Silica Nanoparticle Loaded in Situ Nasal Gel of Scutellarin for Alzheimer’s Disease

  • 期刊论文

  • 发表日期：

    2026年2月18日

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  • Someshwar Mankar,
  • Prashika Shinde,
  • Suhas Siddheshwar,
  • Rajashree Ghogare,
  • Rahul Godge

摘要

To develop and optimize scutellarin-loaded mesoporous silica nanoparticles (MSNs) incorporated within thermosensitive in-situ nasal gel for enhanced Alzheimer’s disease therapy, addressing poor bioavailability and limited brain penetration of conventional oral formulations. MSNs were synthesized using sol-gel method with CTAB as template, TEOS as silica source, and NH₄OH as catalyst. Formulation optimization employed 3³ Box-Behnken factorial design with response surface methodology, evaluating entrapment efficiency, particle size, and zeta potential. Optimized MSNs were incorporated into Poloxamer-based thermosensitive nasal gels. Comprehensive characterization included FTIR, XRD, SEM analysis, in-vitro release studies, ex vivo permeation using goat nasal mucosa, and in vivo Morris water maze behavioral assessments. The optimal formulation contained 625 mg CTAB, 7.5 mL TEOS, and 9.5 mL NH₄OH, achieving 76.4 ± 2.6% entrapment efficiency, 68.3 ± 3.1 nm particle size, and − 27.1 ± 1.0 mV zeta potential with excellent model predictability (R² > 0.93). NF2 gel formulation demonstrated optimal gelation temperature (35.4 °C), sustained drug release (88.9% at 12 h), and enhanced permeation (81.7% in 12 h). In vivo studies revealed significant cognitive improvement with 18.4% better spatial learning, reduced acetylcholinesterase activity (25.9% decrease), and enhanced antioxidant enzyme activities compared to pure scutellarin treatment. The developed nano-gel system successfully bypassed blood-brain barrier limitations, providing superior therapeutic efficacy through direct nose-to-brain targeting. This innovative formulation demonstrates promising preclinical therapeutic potential for Alzheimer’s disease management, warranting comprehensive preclinical evaluation and eventual clinical translation studies.