Deng Tao, Mao Xianglan, Li Yu, Bo Shaowei, Yang Zhigang, Jiang Zhong-Xing
Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals and School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.
Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals and School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.
Bioorg Med Chem Lett. 2018 Dec 1;28(22):3502-3505. doi: 10.1016/j.bmcl.2018.10.009. Epub 2018 Oct 10.
The low water solubility of Propofol resulted in complicated formulation and adverse effects during its clinical application. To improve its water solubility and maintain its anesthetic effects, Propofol prodrugs with monodisperse oligoethylene glycols as solubility enhancer were designed and synthesized. Monodisperse oligoethylene glycols enable the concise manipulation of water solubility, biocompatibility and anesthetic effects. Through the physicochemical and biological assay, a few water soluble prodrugs of Propofol were identified as promising anesthetic to overcome the drawbacks associated with Propofol.
丙泊酚的低水溶性导致其在临床应用中制剂复杂且有不良反应。为提高其水溶性并维持其麻醉效果,设计并合成了以单分散低聚乙二醇作为增溶剂的丙泊酚前药。单分散低聚乙二醇能够精确调控水溶性、生物相容性和麻醉效果。通过理化和生物学分析,确定了几种丙泊酚水溶性前药有望成为克服丙泊酚相关缺点的麻醉剂。