| Wedelolactone, a naturally occurring coumestan generally isolated from Eclipta prostrata L. or Eclipta alba L., has been reported to possess multiple biological effects, including antivenom, anti-inflammatory, anti-fibrotic and anti-hepatotoxic activities. In recent years, the anti-tumor effect of wedelolactone has been found, bringing forth new hope for patients suffering from cancer. However, due to poor water solubility and low bioavailability, wedelolactone is restricted to clinical administration.In this study, PEGylated liposomal wedelolactone was synthesized by the ethanol injection method. With the aim of achieving the optimized prescription for higher entrapment efficiency, orthogonal experiments had been done. The optimized prescription was determined as follows: the mass ratios of wedelolactone to soybean phosphatidylcholine, wedelolactone to cholesterol, and wedelolactone to PEG-2000 were 1:65, 1:6, and 1:2, respectively; and the optimum hydration temperature was 38 °C. Besides, transmission electron microscopy(TEM), atomic force microscopy(AFM), UV-Vis spectrophotometry and FTIR spectrometry were used to characterize the liposomes. On the other hand, a new type of DDS called as Au shell-liposomal wedelolactone and ICG-liposomal wedelolactone was successfully synthesized to integrate photothermotherapy with the traditional chemotherapy. Upon laser irradiation, this kind of DDS would convert an NIR absorption into heat, thus inducing the release of wedelolactone and hyperthermia for cancer cells. Therapeutic effect against cancer cells was evaluated by MTT cell assays. And the results showed that a synergistic effect of chemotherapy and photothermotherapy was achieved. All these studies on wedelolactone and liposomes would be of great value for future cancer therapy. |
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