Preparation And Evaluation Of Emodin Loaded CSO-SA Nanomicelles

Polymeric micelles is a popular form of new drug formulations. Polymeric micelles can be enriched in the tumor site by EPR effect, achieve good passive targeting. In this research, to enhance solubility and anti-tumor activity of EMO, stearic acid-g-chitosan oligosaccharide polymer which was self-synthesized was used to prepare emodin loaded CSO-SA nano-micelles. I chose chitosanase to degrade macromolecule chitosan into small molecule chitosan. I used carbodiimide as crosslinking agent to prepared CSO-SA, then synthesised EMO loaded CSO-SA nano-micelles.The SD%, CMC, particle size, Zeta potential of CSO-SA were evaluated with different experimental methods. It was not difficult to find that the CSO-SA polymer was a kind of nanometer micelle with good dispersion and small particle size. FITC was used to label CSO-SA micelles, to evaluate the uptake of nano-micelles in gastric cancer cells. In order to observe distribution of CSO-SA micelles in vivo, nude mice were used as model animal and DiR as tracer, then photographed in small animal live imager. The results was that CSO-SA could be fully taken up by gastric cancer cells within 12 hours and enrich in the tumor site in vivo.The CSO-SA/EMO micelles were prepared with dialysis method, which was with slightly decreased potential and slightly increased particle size. CSO-SA could efficiently encapsulate EMO, whose encapsulation efficiency was up to 96.0%, and the drug loading was as high as 21.2%. The cumulative release of CSO-SA/EMO at different time was determined by HPLC, we could found that compared with free EMO, the release rate of CSO-SA/EMO was more moderate within 72 hours. MTT assay and FCM demonstrated that CSO-SA micelles were a safe drug carrier, and the effect of CSO-SA/EMO on gastric cancer cells apoptosis was significantly higher than that of free EMO. In summary, the polymer micelles which I synthesised was biocompatible and low toxicity. It could efficiently encapsulate EMO and improve the antitumor activity, CSO-SA was a promising new preparation.