<p>Quercetin (QRT), a bioactive flavonoid, exhibits significant antioxidant and antibacterial properties, but its therapeutic potential is limited by poor solubility and bioavailability. To address these limitations, this study developed self-nanoemulsifying drug delivery systems (SNEDDS) incorporating QRT and Humic acid (HA) as a surface modifier. The developed SNEDDS formulations were characterized by employing an atomic force microscope, FTIR, and a zetasizer. They were then examined for thermodynamic stability and dilution. The average droplet size and zeta potential (ZP) of QRT-loaded SNEDDS were 126.44 ± 21.23&#xa0;nm and − 22.3 ± 2.82, respectively, whereas those of HA-incorporated QRT-SNEDDS were 147.72 ± 16.42&#xa0;nm and − 26.1 ± 3.20 mV. The prepared SNEDDS were highly stable and demonstrated no chemical variation in the drug. The antioxidant activity of all the prepared SNEDDS formulations was evaluated using the DPPH assay, where HA-modified QRT-loaded SNEDDS demonstrated the highest radical scavenging property with an IC<sub>50</sub> value of 2.10 ± 3.21&#xa0;µg/mL, compared to 75.14 ± 2.16&#xa0;µg/mL for QRT. Similarly, antibacterial activity was assessed against <i>S. aureus</i>; HA-modified QRT-loaded SNEDDS exhibited a MIC value of 25&#xa0;µg/mL, outperforming QRT (62.5&#xa0;µg/mL). The observed results were further confirmed through morphological analysis using a scanning electron microscope, showing the severe structural damage to bacterial cells treated with HA-modified QRT-loaded SNEDDS. These findings highlight the potential of HA-modified SNEDDS as a novel platform for enhancing the therapeutic performance of poorly soluble bioactives like QRT, with applications in addressing oxidative stress-related disorders and bacterial infections.</p> Graphical Abstract <p></p>

错误:搜索内容不能为空,请输入英文关键词
错误:关键词超出字数限制,请精简
高级检索

A Humic Acid-Modified Self-Nanoemulsifying Drug Delivery System for Improved Anti-Bacterial Activity of Quercetin Against S. Aureus

  • Saba Zafar,
  • Muhammad Hasnain,
  • Rukesh Maharjan,
  • Aziz Balouch,
  • Wajeeha Muzafar,
  • Tasmina Kanwal,
  • Khadija Rehman,
  • Jawaid Akram,
  • Iqbal Azhar,
  • Muhammad Raza Shah

摘要

Quercetin (QRT), a bioactive flavonoid, exhibits significant antioxidant and antibacterial properties, but its therapeutic potential is limited by poor solubility and bioavailability. To address these limitations, this study developed self-nanoemulsifying drug delivery systems (SNEDDS) incorporating QRT and Humic acid (HA) as a surface modifier. The developed SNEDDS formulations were characterized by employing an atomic force microscope, FTIR, and a zetasizer. They were then examined for thermodynamic stability and dilution. The average droplet size and zeta potential (ZP) of QRT-loaded SNEDDS were 126.44 ± 21.23 nm and − 22.3 ± 2.82, respectively, whereas those of HA-incorporated QRT-SNEDDS were 147.72 ± 16.42 nm and − 26.1 ± 3.20 mV. The prepared SNEDDS were highly stable and demonstrated no chemical variation in the drug. The antioxidant activity of all the prepared SNEDDS formulations was evaluated using the DPPH assay, where HA-modified QRT-loaded SNEDDS demonstrated the highest radical scavenging property with an IC50 value of 2.10 ± 3.21 µg/mL, compared to 75.14 ± 2.16 µg/mL for QRT. Similarly, antibacterial activity was assessed against S. aureus; HA-modified QRT-loaded SNEDDS exhibited a MIC value of 25 µg/mL, outperforming QRT (62.5 µg/mL). The observed results were further confirmed through morphological analysis using a scanning electron microscope, showing the severe structural damage to bacterial cells treated with HA-modified QRT-loaded SNEDDS. These findings highlight the potential of HA-modified SNEDDS as a novel platform for enhancing the therapeutic performance of poorly soluble bioactives like QRT, with applications in addressing oxidative stress-related disorders and bacterial infections.

Graphical Abstract