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<p>Coenzyme Q10 (CoQ10) is an essential lipophilic molecule involved in mitochondrial ATP synthesis and antioxidant defense, yet its therapeutic potential in neurodegenerative diseases remains limited due to poor aqueous solubility, low oral bioavailability, and restricted brain penetration. This study aimed to develop and characterize a lipid-based nanosuspension of CoQ10 (NS-CoQ10) to overcome these limitations and enhance oral absorption and brain exposure. The formulation was prepared by inverse nanoprecipitation followed by homogenization using biodegradable polymers and surfactants, then optimized based on particle size, zeta potential, entrapment efficiency, dissolution, and permeability. The optimized NS-CoQ10 exhibited favorable physicochemical characteristics, including a mean particle size of about 80.1 ± 4.40&#xa0;nm, a negative zeta potential (− 34.9 ± 0.07 mV), and high entrapment efficiency (86.8 ± 1.27%). Fourier transform infrared spectroscopy (FTIR) suggested the presence of possible interactions between CoQ10 and the selected excipients within the NS-CoQ10 matrix. These interactions may have contributed to improved drug encapsulation and enhanced apparent solubility. In vitro studies further demonstrated markedly improved dissolution (76.52 ± 3.51% at 120&#xa0;min, <i>p</i> &lt; 0.001) and mucus permeability (9.57 ± 0.35&#xa0;µg/mL, <i>p</i> &lt; 0.0001) compared with crystalline CoQ10. Pharmacokinetic evaluation in rats (100&#xa0;mg-CoQ10/kg, <i>p.o.</i>) showed markedly enhanced systemic exposure, with NS-CoQ10 achieving an 11.4-fold rise in oral bioavailability and prolonged circulation compared to crystalline CoQ10. Moreover, brain tissue analysis revealed a nearly 4.3-fold higher concentration of CoQ10 with NS-CoQ10, resulting in significantly enhanced brain exposure and brain biodistribution compared with crystalline CoQ10. These findings suggest that the developed NS-CoQ10 offers a promising and practical way to enhance both systemic and brain exposure of CoQ10, which could help manage neurodegenerative and oxidative stress-related conditions.</p>

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Biopharmaceutical Characterization of Lipid-Based Nanosuspension of Coenzyme Q10 for Enhanced Delivery to the Brain

  • 期刊论文

  • 发表日期：

    2026年7月7日

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  • Shimul Halder,
  • Najibah Nasrin,
  • Faria Nasrin,
  • Madhabi Lata Shuma,
  • Sania Ashrafi,
  • Manik Chandra Shill,
  • Md. Zakir Sultan,
  • Md. Selim Reza,
  • Syed Shabbir Haider

摘要

Coenzyme Q10 (CoQ10) is an essential lipophilic molecule involved in mitochondrial ATP synthesis and antioxidant defense, yet its therapeutic potential in neurodegenerative diseases remains limited due to poor aqueous solubility, low oral bioavailability, and restricted brain penetration. This study aimed to develop and characterize a lipid-based nanosuspension of CoQ10 (NS-CoQ10) to overcome these limitations and enhance oral absorption and brain exposure. The formulation was prepared by inverse nanoprecipitation followed by homogenization using biodegradable polymers and surfactants, then optimized based on particle size, zeta potential, entrapment efficiency, dissolution, and permeability. The optimized NS-CoQ10 exhibited favorable physicochemical characteristics, including a mean particle size of about 80.1 ± 4.40 nm, a negative zeta potential (− 34.9 ± 0.07 mV), and high entrapment efficiency (86.8 ± 1.27%). Fourier transform infrared spectroscopy (FTIR) suggested the presence of possible interactions between CoQ10 and the selected excipients within the NS-CoQ10 matrix. These interactions may have contributed to improved drug encapsulation and enhanced apparent solubility. In vitro studies further demonstrated markedly improved dissolution (76.52 ± 3.51% at 120 min, p < 0.001) and mucus permeability (9.57 ± 0.35 µg/mL, p < 0.0001) compared with crystalline CoQ10. Pharmacokinetic evaluation in rats (100 mg-CoQ10/kg, p.o.) showed markedly enhanced systemic exposure, with NS-CoQ10 achieving an 11.4-fold rise in oral bioavailability and prolonged circulation compared to crystalline CoQ10. Moreover, brain tissue analysis revealed a nearly 4.3-fold higher concentration of CoQ10 with NS-CoQ10, resulting in significantly enhanced brain exposure and brain biodistribution compared with crystalline CoQ10. These findings suggest that the developed NS-CoQ10 offers a promising and practical way to enhance both systemic and brain exposure of CoQ10, which could help manage neurodegenerative and oxidative stress-related conditions.