Department of Pharmaceutics, College of Pharmacy, Anhui University of Chinese Medicine, Hefei, China.
Department of Pharmaceutics, College of Pharmacy, Anhui University of Chinese Medicine, Hefei, China; Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei, China; Engineering Technology Research Center of Modernized Pharmaceutics, AnHui Province, China.
Int J Pharm. 2020 Mar 15;577:119046. doi: 10.1016/j.ijpharm.2020.119046. Epub 2020 Jan 23.
A rotigotine (ROT)-loaded polymer micelles thermosensitive gel (ROT-PM-TSG) delivery system was engineered to enhance the solubility of the drug, prolong the residence time, and increase the concentration of the drug in the brain tissue. First, ROT-loaded polymer micelles (ROT-PM) were tailored and optimized. The average particle size, encapsulation efficiency, and drug loading of the ROT-PM were (88.62 ± 1.47) nm, (93.5 ± 0.79) %, and (19.9 ± 0.60) %. The optimal ROT-PM-TSG formulation contained 22% P407 and 2% P188 with a gelation temperature of about 32.3 °C and a pH of 5.186. In vivo, the MRT of ROT-PM and ROT-PM-TSG nasal administration was 1.43 and 1.79 times extended than that of the intravenous. In comparison with the intravenous group, the distribution of ROT in olfactory bulb, cerebrum, cerebellum and striatum was 276.6%, 170.5%, 166.5% and 184.4%, respectively. In conclusion, the ROT-PM-TSG system has proven to be a potential application prospect as a ROT nose-to-brain delivery system.
设计了一种载罗替戈汀（ROT）聚合物胶束温敏凝胶（ROT-PM-TSG）递药系统，以提高药物的溶解度、延长滞留时间并增加脑组织中药物的浓度。首先，定制和优化了载 ROT 的聚合物胶束（ROT-PM）。ROT-PM 的平均粒径、包封效率和载药量分别为（88.62±1.47）nm、（93.5±0.79）%和（19.9±0.60）%。最佳 ROT-PM-TSG 配方含有 22%P407 和 2%P188，胶凝温度约为 32.3°C，pH 值为 5.186。在体内，ROT-PM 和 ROT-PM-TSG 鼻内给药的 MRT 分别延长了 1.43 倍和 1.79 倍，与静脉组相比，ROT 在嗅球、大脑、小脑和纹状体中的分布分别增加了 276.6%、170.5%、166.5%和 184.4%。综上所述，ROT-PM-TSG 系统已被证明具有作为 ROT 鼻内递药系统的潜在应用前景。
