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Background <p>Alzheimer’s disease (AD) is a progressive neurodegenerative disorder marked by amyloid-beta (Aβ) plaque deposition, neurofibrillary tangles, oxidative stress, and acetylcholine deficiency, culminating in cognitive deterioration. Cromolyn Sodium (CS), a known anti-Aβ aggregation agent, exhibits limited oral bioavailability (BA) due to its high solubility and low permeability. Niosomal encapsulation provides a potential approach to enhance CS permeability, stability, and therapeutic efficacy.</p> Objective <p>This study aimed to develop and optimize CS-loaded niosomes using a Box–Behnken Design (BBD) for improved oral delivery and to evaluate their physicochemical attributes, antioxidant potential, and acetylcholinesterase (AChE) inhibitory activities.</p> Methods <p>Niosomes were formulated via the thin-film hydration method. The formulations were characterized for drug content, entrapment efficiency (EE), particle size, and zeta potential, along with FTIR, TEM, DSC, AFM, and accelerated stability studies. In vitro release kinetics were assessed using dialysis bag diffusion method, antioxidant activity by DPPH radical scavenging assay, and AChE inhibition by Ellman’s colorimetric method.</p> Results <p>The optimized formulation demonstrated high drug content (87.61%), EE (83.97%), and a particle size of 175.83&#xa0;nm with a zeta potential of − 35.64 mV, confirming stability. Tween 80 and cholesterol positively influenced EE and drug loading. The formulation showed potent antioxidant activity (94.86% inhibition; IC₅₀ = 19.7&#xa0;µg/mL) and significant AChE inhibition (88.33% at 200&#xa0;µg/mL; IC₅₀ = 28.9&#xa0;µg/mL) with sustained drug release compared to pure CS.</p> Conclusion <p>Optimized CS-loaded niosomes exhibited improved apparent bioavailability surrogates, antioxidant activity, and AChE inhibition in vitro, indicating their potential as an oral nanocarrier for further preclinical evaluation in AD.</p>

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Design Development and Optimization Using Box-Behnken Design (BBD) and in Vitro Evaluation of Cromolyn-Loaded Niosomes for Management of Alzheimer’s Disease

  • 期刊论文

  • 发表日期：

    2026年3月23日

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  • Anmol Kanda,
  • Anjna Rani

摘要

Background

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder marked by amyloid-beta (Aβ) plaque deposition, neurofibrillary tangles, oxidative stress, and acetylcholine deficiency, culminating in cognitive deterioration. Cromolyn Sodium (CS), a known anti-Aβ aggregation agent, exhibits limited oral bioavailability (BA) due to its high solubility and low permeability. Niosomal encapsulation provides a potential approach to enhance CS permeability, stability, and therapeutic efficacy.

Objective

This study aimed to develop and optimize CS-loaded niosomes using a Box–Behnken Design (BBD) for improved oral delivery and to evaluate their physicochemical attributes, antioxidant potential, and acetylcholinesterase (AChE) inhibitory activities.

Methods

Niosomes were formulated via the thin-film hydration method. The formulations were characterized for drug content, entrapment efficiency (EE), particle size, and zeta potential, along with FTIR, TEM, DSC, AFM, and accelerated stability studies. In vitro release kinetics were assessed using dialysis bag diffusion method, antioxidant activity by DPPH radical scavenging assay, and AChE inhibition by Ellman’s colorimetric method.

Results

The optimized formulation demonstrated high drug content (87.61%), EE (83.97%), and a particle size of 175.83 nm with a zeta potential of − 35.64 mV, confirming stability. Tween 80 and cholesterol positively influenced EE and drug loading. The formulation showed potent antioxidant activity (94.86% inhibition; IC₅₀ = 19.7 µg/mL) and significant AChE inhibition (88.33% at 200 µg/mL; IC₅₀ = 28.9 µg/mL) with sustained drug release compared to pure CS.

Conclusion

Optimized CS-loaded niosomes exhibited improved apparent bioavailability surrogates, antioxidant activity, and AChE inhibition in vitro, indicating their potential as an oral nanocarrier for further preclinical evaluation in AD.