A Pegylated Liposome Loaded with Raddeanin A for Prostate Cancer Therapy.

INTRODUCTION

Raddeanin A (RA), a potent triterpenoid extracted from Anemone raddeana Regel, has a moderate therapeutic effect on prostate cancer (PCa), correlating with serious biological toxicity. Therefore, a RA-loaded PEGylated liposome drug delivery system was devised in this study.

METHODS

Hydrogenated soybean phospholipids (HSPC), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-Polyethyleneglycol-2000 (sodium salt) (DSPE-PEG2k), cholesterol (CHO), and RA were utilised to prepare a RA-loaded liposome (LRA) drug delivery system via the thin film hydration technique., The drug loading content was confirmed by high performance liquid chromatography. Dynamic light scattering was employed to evaluate the drug's particle size and stability. Methyl tetrazolium, colony formation, and Western blot (WB) were used in vitro to elucidate the inhibitory effect and mechanism of LRA on prostate cancer cells. Finally, xenograft model was used to confirm the tumor-inhibiting efficacy, clarify the mechanism, and determine the biosafety in mice.

RESULTS

LRA has stable physicochemical properties and a diameter of 173.5 15.3 nm. LRA inhibited the growth of prostate cancer cells in a dose- and time-dependent manner. LRA can substantially reduce the expression of AR and HMGB1, induce apoptosis, regulate the expression of cell cycle-related proteins in vitro and in vivo. The results of the biosafety tests demonstrated that LRA effectively reduced the adverse effects of RA.

CONCLUSION

As a drug delivery system, LRA could effectively and safely inhibit the progression of prostate cancer.