Two-step emulsification for the fabrication of homogeneous PCL microspheres encapsulating geniposidic acid with antioxidant properties--颗粒学报PARTICUOLOGY

Wang, H., Ye, P., Song, R., Chen, G., Zhang, L., Zhu, H., . . . He, J. (2024). Two-step emulsification for the fabrication of homogeneous PCL microspheres encapsulating geniposidic acid with antioxidant properties. Particuology, 94, 305-313. https://doi.org/10.1016/j.partic.2024.08.015

Two-step emulsification for the fabrication of homogeneous PCL microspheres encapsulating geniposidic acid with antioxidant properties

Hongyu Wang, Peng Ye, Ran Song, Guiru Chen, Limei Zhang, Huatai Zhu, Yuting Ren, Jiandu Lei^*, Jing He^*

Beijing Key Laboratory of Lignocellulosic Chemistry, College of Material Science and Technology, Beijing Forestry University, Beijing, 100083, China

10.1016/j.partic.2024.08.015

Volume 94, November 2024, Pages 305-313

Received 12 July 2024, Revised 25 July 2024, Accepted 22 August 2024, Available online 7 September 2024, Version of Record 16 September 2024.

E-mail: hejing2008@sina.com; ljd2012@bjfu.edu.cn

Highlights

• Developed a two-step emulsification method that produces more uniform microspheres compared to traditional methods.

• Encapsulating GPA in PCL microspheres protects it from degradation, thereby enhancing its efficacy.

• PCL microspheres efficiently load GPA and provide sustained release in vitro.

• GPA-loaded PCL microspheres are biocompatible and protect neuronal cells from oxidative damage by scavenging ROS.

Abstract

The mortality rate of neurological disorders is increasing globally, and natural antioxidant geniposidic acid (GPA) holds great potential in the treatment of neuronal oxidative damage. Nevertheless, its inherent instability constrains its pragmatic utilization. Herein, we introduced a drug delivery system capable of protecting unstable natural active compounds from degradation. Among the various methods for preparing drug-loaded microspheres, the emulsification-solvent evaporation technique is one of the most commonly employed due to its efficiency and simplicity. Nevertheless, this method results in microspheres with heterogeneous particle sizes. To address this limitation, we developed a two-step emulsification method involving stirring and homogenization. Using the biocompatible, synthetic, biodegradable polymer polycaprolactone (PCL) as the drug delivery carrier, we prepared GPA-loaded PCL microspheres via the two-step emulsification method. The results demonstrated that the microspheres possessed uniform particle size (polydispersity index = 0.12), excellent drug loading capacity (∼4.86%), sustained drug release profiles (∼68.55% in 264 h), and biocompatibility (cell viability >85%). The in vitro tests showed that the microspheres exerted antioxidant effects by scavenging reactive oxygen species (ROS) induced by oxidative stress, thereby protecting neuronal cells from oxidative damage. This work presents a promising new approach for the treatment of neuronal oxidative damage.

Graphical abstract

Keywords

Eucommia ulmoides Oliv.; Polycaprolactone; Geniposidic acid; Two-step emulsification; Neuronal oxidative damage; Antioxidant

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