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<p>Betulin (BT) is a pentacyclic triterpene with antibacterial, antiviral, and antitumor activity. However, it is insoluble in water and lacks targeting in the in vivo distribution. To improve this situation, this study aims to formulate betulin into nanoparticles (NPs) and further modify it with folic acid (FA) to develop a novel drug-targeting delivery system (FA-BT@NPs). Based on a single-factor experiment, the central composite design was used to optimize the formulation of BT@NPs which was prepared by an emulsion dispersion method. The conjugate of n-hydroxy succinimide with folic acid was used to decorate BT@NPs to prepare the final formulation of FA-BT@NPs. Further, in terms of the nanoparticles with aqueous form, it is still not as convenient and stable as the dry powder form for application and storage, the lyophilization technique was employed to stabilize the preservation of FA-BT@NPs. The results demonstrated the successful preparation of FA-BT@NPs with uniform spherical shapes and good encapsulation efficiency. The lyophilization formulation could preserve the structural integrity and activity of the nanodrugs and facilitate their long-term storage and immediate usability. Our work may lay a solid foundation for the clinical translation of FA-BT@NPs as a potential therapeutic agent for clinical application, highlighting the crucial roles of prescription optimization and advanced formulation technologies in enhancing nanomedicine efficacy.</p> Graphical Abstract <p>Folic acid (FA) was activated to form the conjugate with n-hydroxysuccinmide (FA-NHS). The betulin-loaded nanoparticles (BT@NPs) were prepared by emulsion dispersion method. Finally, BT@NPs was conjugated with FA-NHS to form the novel drug-targeting delivery system FA-BT@NPs.</p> <p></p>

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Development of the Folic Acid-Coated Nanoparticles Based on Human Serum Albumin for the Targeting Delivery of Betulin

  • 期刊论文

  • 发表日期：

    2025年10月20日

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  • Shihua Fu,
  • Zaiyi Luo,
  • Xin Chen,
  • Lingling Yang,
  • Xingjie Du,
  • Kexin Chai,
  • Yujie Zhang,
  • Zhongbing Liu,
  • Pei Jing,
  • Changguang Wang,
  • Yan Lin,
  • Ruilin Lu,
  • Zhirong Zhong

摘要

Betulin (BT) is a pentacyclic triterpene with antibacterial, antiviral, and antitumor activity. However, it is insoluble in water and lacks targeting in the in vivo distribution. To improve this situation, this study aims to formulate betulin into nanoparticles (NPs) and further modify it with folic acid (FA) to develop a novel drug-targeting delivery system (FA-BT@NPs). Based on a single-factor experiment, the central composite design was used to optimize the formulation of BT@NPs which was prepared by an emulsion dispersion method. The conjugate of n-hydroxy succinimide with folic acid was used to decorate BT@NPs to prepare the final formulation of FA-BT@NPs. Further, in terms of the nanoparticles with aqueous form, it is still not as convenient and stable as the dry powder form for application and storage, the lyophilization technique was employed to stabilize the preservation of FA-BT@NPs. The results demonstrated the successful preparation of FA-BT@NPs with uniform spherical shapes and good encapsulation efficiency. The lyophilization formulation could preserve the structural integrity and activity of the nanodrugs and facilitate their long-term storage and immediate usability. Our work may lay a solid foundation for the clinical translation of FA-BT@NPs as a potential therapeutic agent for clinical application, highlighting the crucial roles of prescription optimization and advanced formulation technologies in enhancing nanomedicine efficacy.

Graphical Abstract

Folic acid (FA) was activated to form the conjugate with n-hydroxysuccinmide (FA-NHS). The betulin-loaded nanoparticles (BT@NPs) were prepared by emulsion dispersion method. Finally, BT@NPs was conjugated with FA-NHS to form the novel drug-targeting delivery system FA-BT@NPs.