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<p>Quercetin (QU), a polyphenolic antioxidant, has anti-inflammatory, anti-apoptotic, and anti-ageing potential. Poor aqueous solubility of QU (13&#xa0;µg/mL) limits its oral bioavailability (10%). To improve its dissolution, antioxidant potential, and cell viability, self-nanoemulsifying systems (SNEs) were developed, investigating the effect of long-chain triglycerides (LCTs) vs. mono-terpene (MT). MT vs. LCTs were screened as dispersed phase components to exhibit fully dilutable potential in SNEs from the selected ternary components. Followed by solubility assessment, MT/LCTs were further explored for one-phase region (OPR) in a ternary phase constructed in Tween 80/ethanol mixture (S<sub>mix</sub>) in the ratio 1:1 using olive oil (OL) and coconut oil (CO) as LCTs; meanwhile, cardamom oil (CA) was used at MT Six SNEs of QU were formulated using LCTs and MT on the basis of OPR availability in the respective phase diagram. SNEs had a droplet size ranging from 126 to 160&#xa0;nm with a zeta potential of 2.3–4.8 (–mV). As evidenced by partition coefficient measurement, QU was preferentially positioned in the dispersed phase formed from LCTs SNEs, demonstrating a sustained release pattern of QU in HCl buffer at pH 1.2 and pH 6.8. However, CA-based SNEs produced a much rapid release of QU.F5 and F6 systems (MT) possessed antioxidant potential as measured by DPPH scavenging action at 25&#xa0;µg/mL compared to their control. Placebo SNEs exhibited DPPH activity in comparison to OL and CO systems. MTT assay of F5 and F6 in fibroblast culture (L929) showed that cells were viable at the required dilution (100X) and no significant differences (<i>p</i> &lt; 0.01) between MT/LCTs. QU-loaded SNEs made from CA (LCT) as the former of dispersed phase had improved QU dissolution rate, antioxidant, and cell viability in the L929 cell line.</p>

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Quercetin-Loaded Self-Nanoemulsifying Systems: Lipid Carrier Effects on Phase Behaviour, Release, and Cellular Impacts

  • 期刊论文

  • 发表日期：

    2025年8月1日

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  • Shivanshu Sharma,
  • Anoop Kumar,
  • Ratneshwar Kumar Ratnesh,
  • Jay Singh,
  • Abhinav Garg,
  • Amulya Jindal

摘要

Quercetin (QU), a polyphenolic antioxidant, has anti-inflammatory, anti-apoptotic, and anti-ageing potential. Poor aqueous solubility of QU (13 µg/mL) limits its oral bioavailability (10%). To improve its dissolution, antioxidant potential, and cell viability, self-nanoemulsifying systems (SNEs) were developed, investigating the effect of long-chain triglycerides (LCTs) vs. mono-terpene (MT). MT vs. LCTs were screened as dispersed phase components to exhibit fully dilutable potential in SNEs from the selected ternary components. Followed by solubility assessment, MT/LCTs were further explored for one-phase region (OPR) in a ternary phase constructed in Tween 80/ethanol mixture (Smix) in the ratio 1:1 using olive oil (OL) and coconut oil (CO) as LCTs; meanwhile, cardamom oil (CA) was used at MT Six SNEs of QU were formulated using LCTs and MT on the basis of OPR availability in the respective phase diagram. SNEs had a droplet size ranging from 126 to 160 nm with a zeta potential of 2.3–4.8 (–mV). As evidenced by partition coefficient measurement, QU was preferentially positioned in the dispersed phase formed from LCTs SNEs, demonstrating a sustained release pattern of QU in HCl buffer at pH 1.2 and pH 6.8. However, CA-based SNEs produced a much rapid release of QU.F5 and F6 systems (MT) possessed antioxidant potential as measured by DPPH scavenging action at 25 µg/mL compared to their control. Placebo SNEs exhibited DPPH activity in comparison to OL and CO systems. MTT assay of F5 and F6 in fibroblast culture (L929) showed that cells were viable at the required dilution (100X) and no significant differences (p < 0.01) between MT/LCTs. QU-loaded SNEs made from CA (LCT) as the former of dispersed phase had improved QU dissolution rate, antioxidant, and cell viability in the L929 cell line.