Wang Chuanjin, Wei Yunyang, Yu Li, Zhang Liang
Department of Pharmaceutical Engineering, Institute of Chemical Engineering, Nanjing University of Science and Technology, Nanjing 210094, PR China.
PDA J Pharm Sci Technol. 2009 Sep-Oct;63(5):409-16.
High-purity oridonin was isolated and identified from Rabdosia rubescens hemsl by preparative high-performance liquid chromatography (HPLC). Stealth liposomes of oridonin were prepared by thin-film ultrasonic dispersion using polyethylene glycol-distearoylphosphatidyleth-anolamine(PEG2000-DSPE) as the surface-coating material. A reversed-phase HPLC method was developed and validated to determine the concentrations of oridonin in the serum and tissues of mice. The tissue distribution and pharmacokinetics of oridonin stealth liposomes and oridonin solution in mice were investigated. The results showed that the distribution and pharmacokinetics of oridonin stealth liposomes in mice were changed as compared to the distribution and pharmacokinetics of oridonin solution. The levels of stealth liposomal oridonin in the heart tissues were reduced, while the levels of stealth liposomal oridonin in the blood were increased. The stealth liposomes were very effective at inhibiting the rate of solid tumor growth. The PEG2000-DSPE of liposomes prolonged the circulation time of oridonin in mouse blood, reduced accumulation in the reticuloendothelial system and increased the anti-tumor activity of oridonin.
采用制备型高效液相色谱法（HPLC）从溪黄草中分离并鉴定出高纯度冬凌草甲素。以聚乙二醇-二硬脂酰磷脂酰乙醇胺（PEG2000-DSPE）作为表面包覆材料，通过薄膜超声分散法制备冬凌草甲素隐形脂质体。建立并验证了一种反相HPLC方法，用于测定小鼠血清和组织中冬凌草甲素的浓度。研究了冬凌草甲素隐形脂质体和冬凌草甲素溶液在小鼠体内的组织分布和药代动力学。结果表明，与冬凌草甲素溶液相比，冬凌草甲素隐形脂质体在小鼠体内的分布和药代动力学发生了变化。心脏组织中隐形脂质体冬凌草甲素的含量降低，而血液中隐形脂质体冬凌草甲素的含量增加。隐形脂质体对抑制实体瘤生长速率非常有效。脂质体的PEG2000-DSPE延长了冬凌草甲素在小鼠血液中的循环时间，减少了在网状内皮系统中的蓄积，并增强了冬凌草甲素的抗肿瘤活性。
