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<p>α-Tocopherol (AT) exhibits poor aqueous dispersibility owing to its lipophilic nature and has constraint of low bioavailability. Phospholipid-α-tocopherol complexes (PL-ATs) were developed to improve its nanodispersibility, stability in lipolytic milieu, and proapoptotic potential. PL-ATs were prepared using phospholipid (PL) and AT in the 1.25:1, 1:1, and 1:1.25 weight ratios using solvent evaporation method. 1H-NMR (p-nuclear magnetic resonance), FTIR (Fourier transform infra-red), DSC (differential scanning calorimetry), and conductometric characterization showed that PL-ATs complexation resulted from hydrophobic interaction between their carbons chains, as well weak interaction between polar moieties of PL and AT. Ternary plots were constructed using Tween 20/ethanol taken as surfactant/co-surfactant mix (<i>S</i><sub>mix</sub>) at 1:1, 2:1, and 3:1 weight ratios taking PL-AT complex (1:1) as oil phase. PL-ATs exhibit marked variations in the ternary phase behavior over non-complexed AT. Fully dilutable pattern could be ascribed to formation of one phase region among ternary components (PL-AT, <i>S</i><sub>mix</sub>, and water) producing self-nanoemulsification of PL-AT. However, its non-complexed counterpart had two-phase region in ternary plots with no distinct dilution lines, eventually become coarse dispersion. Optimized formulation (F2) had <i>S</i><sub>mix</sub> 1:1 (65% w/w), containing PL-AT 13.0% (w/w) produced self-nanoemulsification of PL-AT (1:1) upon aqueous phase dilution with droplet size of 12 ± 1.5&#xa0;nm. F2 showed an extended release over a non-complexed AT (F7) in the phosphate buffer at pH 6.8 and in HCl buffer at pH 1.2. PL-AT (1:1) formulations were stable in pancreatic lipase milieu and remained nanoemulsified up to 2&#xa0;h longer than non-complexed AT, without releasing free fatty acids (FFA) in the digest medium. MTT assays showed that the optimized nanoemulsion formulation (F2) had proapoptotic activity in MDA-MB-231 (breast cancer) cell lines. PL-AT interaction confers physical and lipolysis stability to AT through phospholipid complexation and facilitated development of nanoemulsion systems. PL-AT complexation–based self nanoemulsifying systems could be exploited as SNEDDS to improve aqueous solubilization of AT and their stabilization.</p> Graphical Abstract <p></p>

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Phospholipid-α-Tocopherol Complexation Based Self-Nanoemulsifying System: Assessment of Phase Behaviour, Lipolysis Stability & Apoptotic Activity

  • 期刊论文

  • 发表日期：

    2025年2月26日

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  • Anoop Kumar,
  • Lakshya Veer Singh,
  • Sobhna Singh

摘要

α-Tocopherol (AT) exhibits poor aqueous dispersibility owing to its lipophilic nature and has constraint of low bioavailability. Phospholipid-α-tocopherol complexes (PL-ATs) were developed to improve its nanodispersibility, stability in lipolytic milieu, and proapoptotic potential. PL-ATs were prepared using phospholipid (PL) and AT in the 1.25:1, 1:1, and 1:1.25 weight ratios using solvent evaporation method. 1H-NMR (p-nuclear magnetic resonance), FTIR (Fourier transform infra-red), DSC (differential scanning calorimetry), and conductometric characterization showed that PL-ATs complexation resulted from hydrophobic interaction between their carbons chains, as well weak interaction between polar moieties of PL and AT. Ternary plots were constructed using Tween 20/ethanol taken as surfactant/co-surfactant mix (Smix) at 1:1, 2:1, and 3:1 weight ratios taking PL-AT complex (1:1) as oil phase. PL-ATs exhibit marked variations in the ternary phase behavior over non-complexed AT. Fully dilutable pattern could be ascribed to formation of one phase region among ternary components (PL-AT, Smix, and water) producing self-nanoemulsification of PL-AT. However, its non-complexed counterpart had two-phase region in ternary plots with no distinct dilution lines, eventually become coarse dispersion. Optimized formulation (F2) had Smix 1:1 (65% w/w), containing PL-AT 13.0% (w/w) produced self-nanoemulsification of PL-AT (1:1) upon aqueous phase dilution with droplet size of 12 ± 1.5 nm. F2 showed an extended release over a non-complexed AT (F7) in the phosphate buffer at pH 6.8 and in HCl buffer at pH 1.2. PL-AT (1:1) formulations were stable in pancreatic lipase milieu and remained nanoemulsified up to 2 h longer than non-complexed AT, without releasing free fatty acids (FFA) in the digest medium. MTT assays showed that the optimized nanoemulsion formulation (F2) had proapoptotic activity in MDA-MB-231 (breast cancer) cell lines. PL-AT interaction confers physical and lipolysis stability to AT through phospholipid complexation and facilitated development of nanoemulsion systems. PL-AT complexation–based self nanoemulsifying systems could be exploited as SNEDDS to improve aqueous solubilization of AT and their stabilization.

Graphical Abstract