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<p>Currently available brain disorder therapies mainly offer symptomatic relief and face challenges in crossing the blood–brain barrier. Auranofin, a gold-based compound with strong antioxidative and anti-inflammatory effects, shows promise for neurological conditions but suffers from low oral bioavailability, with only 20–25% absorption. Nanoformulation strategies are being developed to enhance its BBB penetration and improve targeted drug delivery, thereby increasing its therapeutic potential in brain-related disorders. In this study, Auranofin-loaded poly (lactide-co-glycolic acid) (PLGA) nanoparticles (AF NPs) were prepared using the double-emulsion solvent evaporation method and optimized through a central composite design of response surface methodology. The optimization focused on critical formulation variables, including PLGA concentration (mg), polyvinyl alcohol concentration (% w/v), and homogenization speed (rpm), with quality responses assessed in terms of entrapment efficiency and particle size. Characterization studies confirmed the compatibility between AF and PLGA. The optimized AF NPs demonstrated high entrapment efficiency (98%) and drug loading (76%), with a mean particle size of 101.5 ± 10.3&#xa0;nm, surface charge of 27.5 ± 5.10 mV, and a polydispersity index of 0.438 ± 0.12. These attributes suggest that AF NPs exhibit improved stability and enhanced capability to traverse the BBB compared to free AF. Collectively, the developed nanoformulation holds promise for therapeutic application in a range of neurodegenerative disorders, including Alzheimer’s disease, Parkinson’s disease, and epilepsy. Moreover, such nanocarriers are expected to improve the pharmacokinetic profile, enhance bioavailability, and expand the pharmaceutical spectrum of AF, thereby potentiating its already established pharmacological benefits.</p>

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Formulation by Design-based Development and Characterization of Auranofin-loaded Nanoparticles for Brain Targeting

  • 期刊论文

  • 发表日期：

    2026年1月16日

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  • Shiv Kumar Kushawaha,
  • Mahendra Singh Ashawat,
  • Ashish Baldi

摘要

Currently available brain disorder therapies mainly offer symptomatic relief and face challenges in crossing the blood–brain barrier. Auranofin, a gold-based compound with strong antioxidative and anti-inflammatory effects, shows promise for neurological conditions but suffers from low oral bioavailability, with only 20–25% absorption. Nanoformulation strategies are being developed to enhance its BBB penetration and improve targeted drug delivery, thereby increasing its therapeutic potential in brain-related disorders. In this study, Auranofin-loaded poly (lactide-co-glycolic acid) (PLGA) nanoparticles (AF NPs) were prepared using the double-emulsion solvent evaporation method and optimized through a central composite design of response surface methodology. The optimization focused on critical formulation variables, including PLGA concentration (mg), polyvinyl alcohol concentration (% w/v), and homogenization speed (rpm), with quality responses assessed in terms of entrapment efficiency and particle size. Characterization studies confirmed the compatibility between AF and PLGA. The optimized AF NPs demonstrated high entrapment efficiency (98%) and drug loading (76%), with a mean particle size of 101.5 ± 10.3 nm, surface charge of 27.5 ± 5.10 mV, and a polydispersity index of 0.438 ± 0.12. These attributes suggest that AF NPs exhibit improved stability and enhanced capability to traverse the BBB compared to free AF. Collectively, the developed nanoformulation holds promise for therapeutic application in a range of neurodegenerative disorders, including Alzheimer’s disease, Parkinson’s disease, and epilepsy. Moreover, such nanocarriers are expected to improve the pharmacokinetic profile, enhance bioavailability, and expand the pharmaceutical spectrum of AF, thereby potentiating its already established pharmacological benefits.