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Objective <p>This study aimed to develop polyethylene glycol (PEG)-modified liposomes (PG-1-Ls) to overcome the poor oral bioavailability and burst release of phenolic glycoside 1 (PG-1), an anti-aging compound isolated from <i>Moringa oleifera</i> seeds.</p> Methods <p>PG-1-Ls were preparedby thin-film dispersion and optimized via a Box-Behnken design. The formulation wascharacterized for particle size, encapsulation efficiency (EE%), drug loading (DL%), andmorphology. Stability, in vitro release in four media, and safety in zebrafish were evaluated. Pharmacokinetics were studied in rats, and anti-aging efficacy was assessed in a D-galactose-induced zebrafish model by measuring β-galactosidase activity.</p> Results <p>The optimized PG-1-Lswere spherical and uniform (154.6 ± 3.8 nm), with high EE% (88.29%) and good stability. They successfully eliminated the initial burst release of PG-1, demonstrating sustained release profiles. In rats, PG-1-Ls increased the oral bioavailability (AUC) by 6.25-fold and the peak concentration(C~max~) by 3.9-fold compared to free PG-1. The formulation also showed improved safety in zebrafish. In the aging model, both PG-1 and PG-1-Ls significantly reduced β-galactosidaseactivity, with PG-1-Ls exhibiting superior efficacy comparable to the positive control.</p> Conclusion <p>PEGylated liposomes significantly enhance the sustained release, oral bioavailability, safety, and in vivo anti-aging activity of PG-1, representing a promising delivery system for its application.</p> Graphical abstract <p></p>

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Development of Polyethylene Glycol-Modified Liposomes of Phenolic Glycoside 1 for Enhanced Anti-Aging Effect

  • 期刊论文

  • 发表日期：

    2026年2月5日

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  • Qilong Wang,
  • Mingjie Gong,
  • Jiaying Li,
  • Tingyuan Li,
  • Xia Jiang,
  • Xiaowen Wang,
  • Qinyang Hua,
  • Elmurat Toreniyazov,
  • Feng Shi,
  • Jiangnan Yu,
  • Xia Cao,
  • Ximing Xu,
  • Michael Adu-Frimpong

摘要

Objective

This study aimed to develop polyethylene glycol (PEG)-modified liposomes (PG-1-Ls) to overcome the poor oral bioavailability and burst release of phenolic glycoside 1 (PG-1), an anti-aging compound isolated from Moringa oleifera seeds.

Methods

PG-1-Ls were preparedby thin-film dispersion and optimized via a Box-Behnken design. The formulation wascharacterized for particle size, encapsulation efficiency (EE%), drug loading (DL%), andmorphology. Stability, in vitro release in four media, and safety in zebrafish were evaluated. Pharmacokinetics were studied in rats, and anti-aging efficacy was assessed in a D-galactose-induced zebrafish model by measuring β-galactosidase activity.

Results

The optimized PG-1-Lswere spherical and uniform (154.6 ± 3.8 nm), with high EE% (88.29%) and good stability. They successfully eliminated the initial burst release of PG-1, demonstrating sustained release profiles. In rats, PG-1-Ls increased the oral bioavailability (AUC) by 6.25-fold and the peak concentration(C~max~) by 3.9-fold compared to free PG-1. The formulation also showed improved safety in zebrafish. In the aging model, both PG-1 and PG-1-Ls significantly reduced β-galactosidaseactivity, with PG-1-Ls exhibiting superior efficacy comparable to the positive control.

Conclusion

PEGylated liposomes significantly enhance the sustained release, oral bioavailability, safety, and in vivo anti-aging activity of PG-1, representing a promising delivery system for its application.

Graphical abstract