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Purpose <p>The study aimed to develop an O-butyryl chitosan nanoparticles (O-CTS/BAI NPs) delivery system to enhance the transdermal penetration, anti-inflammatory, antioxidant properties, and melanogenesis-inhibiting effects of baicalin (BAI), thereby improving its potential for treating hyperpigmentation disorders.</p> Methods <p>O-butyryl chitosan (O-CTS) was synthesized by the butyrylation of chitosan with butyric anhydride, and O-CTS/BAI NPs were prepared using the ionic cross-linking method. The encapsulation efficiency, particle size, zeta potential, and morphology of the nanoparticles were characterized. The skin irritation potential was evaluated in SD rats, and transdermal absorption characteristics were studied using Franz diffusion cells. In vitro release behavior was assessed in a pH 7.4 buffer. The antioxidant and anti-inflammatory activities were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays and LPS-induced <i>RAW264.7</i> macrophages, respectively. The melanogenesis-inhibiting effects were assessed in <i>B16F10</i> melanoma cells and zebrafish embryos.</p> Results <p>The O-CTS/BAI NPs exhibited an encapsulation efficiency of 98.76%, with a uniform particle size of 158.7&#xa0;nm and a positive zeta potential of 38.3 mV. The nanoparticles showed no significant skin irritation and significantly increased the transdermal penetration and skin retention of BAI compared to BAI solution. The in vitro release behavior followed first-order kinetics. O-CTS/BAI NPs demonstrated superior antioxidant and anti-inflammatory activities, effectively inhibiting the production of NO, IL-6, and TNF-α. They also significantly reduced melanin content and tyrosinase activity in <i>B16F10</i> cells and inhibited melanogenesis in zebrafish embryos more effectively than BAI alone.</p> Conclusion <p>The O-CTS/BAI NPs delivery system effectively enhanced the transdermal penetration and biological activities of BAI, showing significant advantages in inhibiting melanogenesis. This system holds great potential for treating hyperpigmentation-related disorders.</p> Graphical Abstract <p></p>

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O-Butyryl Chitosan Nanoparticles Enhance Baicalin Efficacy: A Study on Transdermal Penetration, Antioxidant, Anti-inflammatory, and Melanogenesis-Inhibiting Activities

  • 期刊论文

  • 发表日期：

    2026年3月5日

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  • Yuchen Zhang,
  • Jiaxuan Liu,
  • Chongying Wang,
  • Xiaolong Zhang,
  • Xiaowei Shi,
  • Chun Zhang,
  • Haigang Li

摘要

Purpose

The study aimed to develop an O-butyryl chitosan nanoparticles (O-CTS/BAI NPs) delivery system to enhance the transdermal penetration, anti-inflammatory, antioxidant properties, and melanogenesis-inhibiting effects of baicalin (BAI), thereby improving its potential for treating hyperpigmentation disorders.

Methods

O-butyryl chitosan (O-CTS) was synthesized by the butyrylation of chitosan with butyric anhydride, and O-CTS/BAI NPs were prepared using the ionic cross-linking method. The encapsulation efficiency, particle size, zeta potential, and morphology of the nanoparticles were characterized. The skin irritation potential was evaluated in SD rats, and transdermal absorption characteristics were studied using Franz diffusion cells. In vitro release behavior was assessed in a pH 7.4 buffer. The antioxidant and anti-inflammatory activities were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays and LPS-induced RAW264.7 macrophages, respectively. The melanogenesis-inhibiting effects were assessed in B16F10 melanoma cells and zebrafish embryos.

Results

The O-CTS/BAI NPs exhibited an encapsulation efficiency of 98.76%, with a uniform particle size of 158.7 nm and a positive zeta potential of 38.3 mV. The nanoparticles showed no significant skin irritation and significantly increased the transdermal penetration and skin retention of BAI compared to BAI solution. The in vitro release behavior followed first-order kinetics. O-CTS/BAI NPs demonstrated superior antioxidant and anti-inflammatory activities, effectively inhibiting the production of NO, IL-6, and TNF-α. They also significantly reduced melanin content and tyrosinase activity in B16F10 cells and inhibited melanogenesis in zebrafish embryos more effectively than BAI alone.

Conclusion

The O-CTS/BAI NPs delivery system effectively enhanced the transdermal penetration and biological activities of BAI, showing significant advantages in inhibiting melanogenesis. This system holds great potential for treating hyperpigmentation-related disorders.

Graphical Abstract