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An Apigenin-Based Bone-Targeted System Enhances Antioxidant Capacity of Bone Marrow Mesenchymal Stem Cells via the

Daihui Liu1, Yi Wang1, Can Zhu1

  • 1Department of Orthopedics, the First Affiliated Hospital of Soochow University, Orthopedic Institute of Soochow University, 899 Pinghai Road, Suzhou 215031, Jiangsu, China.

ACS Biomaterials Science & Engineering
|February 25, 2026
PubMed

Insights

This study developed a novel bone-targeting delivery system for apigenin (API) to treat osteoporosis. The system enhances API

Area of Science:

  • Biomaterials Science
  • Pharmacology
  • Cell Biology

Background:

  • Osteoporosis (OP) arises from bone homeostasis imbalance, leading to reduced bone formation and increased resorption.
  • Current OP treatments have systemic toxicities; the osteoporotic microenvironment worsens oxidative stress, impairing bone marrow mesenchymal stem cells (BMSCs) osteogenic differentiation.
  • Apigenin (API), a natural flavonoid, has antioxidant and regulatory properties but suffers from poor bioavailability and rapid metabolism, hindering clinical use.

Purpose of the Study:

  • To develop a bone-targeted delivery system to overcome apigenin's pharmacokinetic limitations for osteoporosis treatment.
  • To investigate the mechanism of apigenin in promoting osteogenic differentiation of osteoporotic BMSCs (OP-BMSCs).
  • To evaluate the efficacy of the novel delivery system in an in vivo osteoporosis model.

Main Methods:

  • In vitro assessment of API's effects on OP-BMSCs, including osteogenic differentiation, reactive oxygen species (ROS) levels, and mitochondrial membrane potential.
  • RNA sequencing analysis to elucidate the molecular mechanism of API action, focusing on the PI3K/Akt signaling pathway.
  • Development and in vivo evaluation of a BMSC-affinitive E7 peptide-based liposomal system for apigenin delivery (API@Lipo-E7) in ovariectomized (OVX) mice.

Main Results:

  • Apigenin significantly enhanced OP-BMSC osteogenic differentiation, reduced ROS levels, and increased mitochondrial membrane potential in vitro.
  • The study identified the PI3K/Akt signaling axis as a key mediator of apigenin's protective effects on OP-BMSCs, restoring redox homeostasis.
  • The API@Lipo-E7 system demonstrated excellent bone-targeting capability and significantly increased bone mineral density in OVX mice compared to API alone.

Conclusions:

  • Apigenin holds therapeutic potential for osteoporosis by restoring redox balance and promoting osteogenic differentiation in BMSCs via the PI3K/Akt pathway.
  • A novel BMSC-affinitive liposomal system (API@Lipo-E7) effectively overcomes apigenin's pharmacokinetic limitations, enhancing bone targeting and therapeutic efficacy.
  • This bone-targeted delivery strategy offers a promising new approach for the precise and effective treatment of osteoporosis.
Keywords:
PI3K/AKT signaling pathwayapigeninbone marrow mesenchymal stem cellsoxidative stresspostmenopausal osteoporosis

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