Department of Pharmacy, Hebei North University, Zhangjiakou 075000, China.
Hebei Key Laboratory of Neuropharmacology, Zhangjiakou 075000, China.
Molecules. 2022 Jan 27;27(3):860. doi: 10.3390/molecules27030860.
Due to the remarkable anti-tumor activities of oridonin (Ori), research on has attracted more and more attention in the pharmaceutical field. The purpose of this study was to extract Ori from by ultrasound-assisted extraction (UAE) and prepare Ori liposomes as a novel delivery system to improve the bioavailability and biocompatibility. Response surface methodology (RSM), namely Box-Behnken design (BBD), was applied to optimize extraction conditions, formulation, and preparation process. The results demonstrated that the optimal extraction conditions were an ethanol concentration of 75.9%, an extraction time of 35.7 min, and a solid/liquid ratio of 1:32.6. Under these optimal conditions, the extraction yield of Ori was 4.23 mg/g, which was well matched with the predicted value (4.28 mg/g). The optimal preparation conditions of Ori liposomes by RSM, with an ultrasonic time of 41.1 min, a soybean phospholipids/drug ratio of 9.6 g/g, and a water bath temperature of 53.4 °C, had higher encapsulation efficiency (84.1%). The characterization studies indicated that Ori liposomes had well-dispersible spherical shapes and uniform sizes with a particle size of 137.7 nm, a polydispersity index (PDI) of 0.216, and zeta potential of -24.0 mV. In addition, Ori liposomes presented better activity than free Ori. Therefore, the results indicated that Ori liposomes could enhance the bioactivity of Ori, being proposed as a promising vehicle for drug delivery.
由于冬凌草甲素（Ori）具有显著的抗肿瘤活性，其在制药领域的研究受到了越来越多的关注。本研究旨在通过超声辅助提取（UAE）从 中提取 Ori，并制备 Ori 脂质体作为一种新型给药系统，以提高其生物利用度和生物相容性。响应面法（RSM），即 Box-Behnken 设计（BBD），被应用于优化提取条件、配方和制备工艺。结果表明，最佳提取条件为乙醇浓度 75.9%、提取时间 35.7 min、固液比 1:32.6。在这些最佳条件下，Ori 的提取率为 4.23 mg/g，与预测值（4.28 mg/g）吻合较好。通过 RSM 优化的 Ori 脂质体的最佳制备条件为超声时间 41.1 min、大豆磷脂/药物比 9.6 g/g、水浴温度 53.4°C，包封率较高，为 84.1%。表征研究表明，Ori 脂质体具有良好的分散性和球形形状，粒径为 137.7nm，多分散指数（PDI）为 0.216，Zeta 电位为-24.0 mV。此外，Ori 脂质体的活性优于游离 Ori。因此，结果表明 Ori 脂质体可以增强 Ori 的生物活性，有望成为一种有前途的药物传递载体。
