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<p>γ-Tocotrienol (TE), a free radical scavenger confers antioxidant activity via per-oxidative pathways during cell/tissue damage. TE ameliorates the risk of hyperlipidemic, hypercholesterolemia, hyperglycemia, and anti-apoptosis. To improve aqueous dispersibility of TE, a self-nanoemulsifying system (SNE) was developed to assess lipolytic stability, anti-neuroblastoma in human cell lines (SHSY-5Y), and anti-hyperlipidemia. The&#xa0;phase behavior of TE containing Tween80/PEG600/phospholipid (PL) as a system forming ternary components with PL (either 5% or 10% w/w), was assessed at Smix ratios of 1:0, 1:1, 2:1, and 1:2. Phase dynamics revealed that PL complemented Smix activity and facilitated the self-nanoemulsification of TE as quantified from one-phase region (OPR). PL conferred interfacial action up to 10%w/w on OPR, and linearly followed OPR vs. Smix 1:0 &gt; 2:1 &gt; 1:1 &gt; 1:2. Six pre-concentrate SNEs were formulated at different Smix ratios, and PL loading had droplet size range (32–180&#xa0;nm) and zeta potential (− 3.7 to − 5.1&#xa0;mV), yielded nanoemulsification of TE. Upon aqueous dilution, pre-concentrate SNEs exhibit phase transformations, as evident from conductivity and refractive index. In vitro TE release was assessed in HCl at pH 1.2 and in phosphate buffer at pH 6.8, showing that SNE (F5 &amp; F6) had a significant difference from coarse emulsion (<i>p</i> &lt; 0.01). In vitro lipolysis of SNEs in the pancreatic milieu demonstrated that liberation of free fatty acid (less than 15%) from SNEs was significantly different (<i>p</i> &lt; 0.01) from the coarse TE (without PL). Preclinical assessment of SNE (F5) in the dexamethasone induced rat model produced anti-hyperlipidemic activity when compared to standard (atorvastatin). Further, lipid profile markers, viz., total cholesterol (TC), triglyceride (TG), and low density lipoprotein (LDL), from SNE (F5) produced a significant difference from the coarse emulsion of TE and the standard (atorvastatin treated). TE nanoemulsion inhibited human neuroblastoma cell line growth from 100 to 1000 × fold dilutions compared to the coarse emulsion (<i>p</i> &lt; 0.01). Optimized SNE of TE containing Tween80/PEG600 Smix components, along with PL, had sustained release of TE with lipolysis stability, anti-hyperlipidemic, and anti-neuroblastoma potential in human cells.</p> Graphical Abstract <p></p>

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Self-Nanoemulsifying Pre-concentrate of γ-Tocotrienol Embedding Phospholipid: Phase Dynamics, Anti-hyperlipidemic and Anti-neuroblastoma Potential

  • 期刊论文

  • 发表日期：

    2025年5月20日

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  • Anoop Kumar,
  • Arshad Saifi,
  • Anshika Sharma,
  • Divya Chaudhary

摘要

γ-Tocotrienol (TE), a free radical scavenger confers antioxidant activity via per-oxidative pathways during cell/tissue damage. TE ameliorates the risk of hyperlipidemic, hypercholesterolemia, hyperglycemia, and anti-apoptosis. To improve aqueous dispersibility of TE, a self-nanoemulsifying system (SNE) was developed to assess lipolytic stability, anti-neuroblastoma in human cell lines (SHSY-5Y), and anti-hyperlipidemia. The phase behavior of TE containing Tween80/PEG600/phospholipid (PL) as a system forming ternary components with PL (either 5% or 10% w/w), was assessed at Smix ratios of 1:0, 1:1, 2:1, and 1:2. Phase dynamics revealed that PL complemented Smix activity and facilitated the self-nanoemulsification of TE as quantified from one-phase region (OPR). PL conferred interfacial action up to 10%w/w on OPR, and linearly followed OPR vs. Smix 1:0 > 2:1 > 1:1 > 1:2. Six pre-concentrate SNEs were formulated at different Smix ratios, and PL loading had droplet size range (32–180 nm) and zeta potential (− 3.7 to − 5.1 mV), yielded nanoemulsification of TE. Upon aqueous dilution, pre-concentrate SNEs exhibit phase transformations, as evident from conductivity and refractive index. In vitro TE release was assessed in HCl at pH 1.2 and in phosphate buffer at pH 6.8, showing that SNE (F5 & F6) had a significant difference from coarse emulsion (p < 0.01). In vitro lipolysis of SNEs in the pancreatic milieu demonstrated that liberation of free fatty acid (less than 15%) from SNEs was significantly different (p < 0.01) from the coarse TE (without PL). Preclinical assessment of SNE (F5) in the dexamethasone induced rat model produced anti-hyperlipidemic activity when compared to standard (atorvastatin). Further, lipid profile markers, viz., total cholesterol (TC), triglyceride (TG), and low density lipoprotein (LDL), from SNE (F5) produced a significant difference from the coarse emulsion of TE and the standard (atorvastatin treated). TE nanoemulsion inhibited human neuroblastoma cell line growth from 100 to 1000 × fold dilutions compared to the coarse emulsion (p < 0.01). Optimized SNE of TE containing Tween80/PEG600 Smix components, along with PL, had sustained release of TE with lipolysis stability, anti-hyperlipidemic, and anti-neuroblastoma potential in human cells.

Graphical Abstract