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Purpose <p>Alzheimer’s disease (AD) is prevalent among older adults due to reduced acetylcholine levels and increased oxidative stress. Oral treatments cause severe side effects, promoting topical patches as alternatives. This study evaluated turmeric extracts for anti-acetylcholinesterase (AChE) and antioxidative activities, and developed a topical delivery system.</p> Methods <p>Crude ethanolic (EF), curcuminoids-rich (CRF), and alkaloid-rich fractions (ARF) were extracted from turmeric and evaluated for <i>in vitro</i> AChE inhibitory and <i>in vitro</i> antioxidant activities. Molecular docking explored curcuminoid-AChE interactions. CRF was formulated into emulsions and topical polysaccharide gel patches, then evaluated for physicochemical properties and <i>in vitro</i> release.</p> Results <p>CRF demonstrated highest <i>in vitro</i> AChE inhibitory effects (IC<sub>50</sub>: 18.49 ± 1.36&#xa0;µg/mL), comparable to galantamine (IC<sub>50</sub>: 13.62 ± 9.22&#xa0;µg/mL), and significant <i>in vitro</i> antioxidant activity (DPPH IC<sub>50</sub>: 45.6 ± 2.61&#xa0;µg/mL). Molecular docking showed strong binding affinities for curcumin, bis-desmethoxy curcumin, and desmethoxy curcumin with binding energies of − 9.91 to − 10.51&#xa0;kcal/mol. Optimal CRF solubility occurred in olive oil: PEG: water (1:19:30 v/v). CRF emulsion-loaded patches achieved 41.63% AChE inhibition versus 16.65% for non-emulsified patches.</p> Conclusions <p>CRF-containing topical patches demonstrate promising therapeutic potential for AD treatment, offering a cost-effective, biocompatible alternative with enhanced bioavailability through emulsion formulation.</p>

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In Vitro and In Silico Evaluation of Turmeric Extracts for Anticholinesterase Effects and their Topical Formulation for Future Application in Alzheimer’s Disease

  • 期刊论文

  • 发表日期：

    2025年10月18日

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  • Sirirat Srirat,
  • Tussavee Jongnui,
  • Than Bunmanee,
  • Panita Kongsune,
  • Pimpun Chanakeat,
  • Netnapa Chana

摘要

Purpose

Alzheimer’s disease (AD) is prevalent among older adults due to reduced acetylcholine levels and increased oxidative stress. Oral treatments cause severe side effects, promoting topical patches as alternatives. This study evaluated turmeric extracts for anti-acetylcholinesterase (AChE) and antioxidative activities, and developed a topical delivery system.

Methods

Crude ethanolic (EF), curcuminoids-rich (CRF), and alkaloid-rich fractions (ARF) were extracted from turmeric and evaluated for in vitro AChE inhibitory and in vitro antioxidant activities. Molecular docking explored curcuminoid-AChE interactions. CRF was formulated into emulsions and topical polysaccharide gel patches, then evaluated for physicochemical properties and in vitro release.

Results

CRF demonstrated highest in vitro AChE inhibitory effects (IC50: 18.49 ± 1.36 µg/mL), comparable to galantamine (IC50: 13.62 ± 9.22 µg/mL), and significant in vitro antioxidant activity (DPPH IC50: 45.6 ± 2.61 µg/mL). Molecular docking showed strong binding affinities for curcumin, bis-desmethoxy curcumin, and desmethoxy curcumin with binding energies of − 9.91 to − 10.51 kcal/mol. Optimal CRF solubility occurred in olive oil: PEG: water (1:19:30 v/v). CRF emulsion-loaded patches achieved 41.63% AChE inhibition versus 16.65% for non-emulsified patches.

Conclusions

CRF-containing topical patches demonstrate promising therapeutic potential for AD treatment, offering a cost-effective, biocompatible alternative with enhanced bioavailability through emulsion formulation.