Gou MaLing, Wu Lan, Yin QinQin, Guo QingFa, Guo Gang, Liu Jin, Zhao Xia, Wei YuQuan, Qian Zhiyong
State Key Laboratory of Biotherapy and Cancer Center West China Hospital, West China Medical School, Sichuan University, Chengdu, 610041, China.
J Nanosci Nanotechnol. 2009 Nov;9(11):6360-5. doi: 10.1166/jnn.2009.1343.
Rapid local transdermal anaesthetic is desirable in clinic. In this paper, lidocaine loaded poly(epsilon-caprolactone)-poly(ethylene glycol)-poly(epsilon-caprolactone) (PCL-PEG-PCL) nanoparticles were prepared, and a novel transdermal lidocaine formulation: lidocaine loaded PCL-PEG-PCL nanoparticles in F127 hydrogel (Nano-Lido Gel), was demonstrated. These lidocaine loaded PCL-PEG-PCL nanoparticles with mean particle size of ca. 200 nm had drug loading of about 40%. The efficiency of transdermal anaesthesia of four treatments: EMLA cream (E), Nano-Lido Gel (N), EMLA cream with brief focal ultrasound pretreatment (EU), and Nano-Lidocaine Gel with brief focal ultrasound pretreatment (NU), was evaluated by tail-flick latency test assay in rats. Results indicated that the topical anaesthesia onset time in NU was 5 times and 2.5 times shorter than that in E and EU. The efficiency of anaesthesia in NU, expressed as maximum possible effects (MPE) value, was significantly higher than that in other treatments. It provided a novel path to develop rapid transdermal anaesthesia by combination of ultrasound pretreatment and lidocaine nano-formulation based on polymeric nanoparticles.
临床上需要快速起效的局部透皮麻醉剂。本文制备了负载利多卡因的聚（ε-己内酯）-聚（乙二醇）-聚（ε-己内酯）（PCL-PEG-PCL）纳米颗粒，并展示了一种新型的透皮利多卡因制剂：F127水凝胶中负载利多卡因的PCL-PEG-PCL纳米颗粒（纳米利多卡因凝胶）。这些负载利多卡因的PCL-PEG-PCL纳米颗粒平均粒径约为200 nm，载药量约为40%。通过大鼠甩尾潜伏期试验评估了四种治疗方法的透皮麻醉效果：复方利多卡因乳膏（E）、纳米利多卡因凝胶（N）、经短暂聚焦超声预处理的复方利多卡因乳膏（EU）和经短暂聚焦超声预处理的纳米利多卡因凝胶（NU）。结果表明，NU的局部麻醉起效时间比E和EU分别短5倍和2.5倍。以最大可能效应（MPE）值表示，NU的麻醉效果显著高于其他治疗方法。它为基于聚合物纳米颗粒的超声预处理和利多卡因纳米制剂联合开发快速透皮麻醉提供了一条新途径。
