Studies On The PLA Nanoparticles Loaded With Anticancer Drug Oridonin

Oridonin, a diterpenoid compound, is isolated from the well known Chinese herb Rabdosia rubescens, which has been used in the treatment of esophageal and hepatic carcinoma for decades. The results of pharmacological research show that oridonin exhibits apoptosis-inducing activities on a wide variety of cancer cells including those from liver(BEL-7402), non-small cell lung(NCI-H520, NCI-H460, NCI-H1299), leukemia (HL-60), esophagus (CaES-17), colon(HCT8), etc.The synthesis of oridonin is still unsatisfied, therefore, oridonin is mainly obtained by extracting from the natural plant. However, its low content in plants and the complexity of its extraction procedure restrict its investigation, exploitation and utilization greatly. Besides, its poor water-solubility and short biological half-life limited its successful use in clinic.In order to solve the problems mentioned above, we established a novel method for the extraction and separation of oridonin, which combined the supercritical CO₂ fluid extraction technology to the column chromatography technology. The research on modifier category and the extraction time showed that the best modifier was ethanol with the concentration of 95%, and the suitable extraction time was 3 h. Orthogonal experiment was applied to optimize the process parameters of the supercritical CO₂ fluid extraction. The optimized conditions were as follows: pressure-38.5 MPa, temperature -40 ℃, modifier-1.5 ml·g^-1. The extractant was purified by the further separation of column chromatography and recrystallization. The crystal product was proved to be...