Abstract
Background
Ovarian cancer is a major threat to women's lives. Chinese medicine honokiol (HK) is a polyphenol isolated from Magnolia, which can effectively suppress the growth of ovarian cancer. However, low water solubility and lack of tumor-targeting ability have greatly hindered the clinical application of HK.
Results
Herein, a glutathione (GSH) sensitive HK polyprodrug was prepared by using HK as the backbone. Then, an EpCAM-specific aptamer and poly(ethylene glycol) (PEG) were conjugated to HK polyprodrug, and the obtained polyprodrug was assembled into nanoparticles in water. The HK polyprodrug-formed nanoparticles achieved high drug loading and GSH-responsiveness drug release. Moreover, after optimization, HK polyprodrug nanoparticles (A/P-PHK NP40) formed by aptamer-modified and PEG-modified prodrug at feed molar ratio at 2: 3 had the highest ability to target EpCAM overexpression ovarian cancer cells. A/P-PHK NP40 also exhibited a higher cell growth inhibition effect in ovarian cancer cells than free HK and control HK nanoparticles.
Conclusion
All in all, this work reported a novel strategy for HK delivery based on microenvironment responsiveness polyprodrug, which provided a potential method for ovarian cancer targeting therapy.