Zhai Yingjie, Xu Rui, Wang Yi, Liu Jiyong, Wang Zimin, Zhai Guangxi
a Department of Pharmaceutics, College of Pharmacy , Shandong University , Jinan , China .
b Department of Orthopedics, Changhai Hospital , Second Military Medical University , Shanghai , China , and.
J Liposome Res. 2015;25(4):316-24. doi: 10.3109/08982104.2014.999686. Epub 2015 Jan 27.
Ropivacaine, a novel long-acting local anesthetic, has been proved to own superior advantage. However, Naropin® Injection, the applied form in clinic, can cause patient non-convenience. The purpose of this study was to formulate ropivacaine (RPV) in ethosomes and evaluate the potential of ethosome formulation in delivering RPV transdermally. The RPV-loaded ethosomes were prepared with thin-film dispersion technique and the formulation was characterized in terms of size, zeta potential, differential scanning calorimetry (DSC) analysis and X-ray diffraction (XRD) study. The results showed that the optimized RPV-ethosomes displayed a typical lipid bilayer structure with a narrow size distribution of 73.86 ± 2.40 nm and drug loading of 8.27 ± 0.37%, EE of 68.92 ± 0.29%. The results of DSC and XRD study indicated that RPV was in amorphous state when encapsulated into ethosomes. Furthermore, the results of ex vivo permeation study proved that RPV-ethosomes could promote the permeability in a high-efficient, rapid way (349.0 ± 11.5 μg cm(-2) at 12 h and 178.8 ± 7.1 μg cm(-2) at 0.5 h). The outcomes of histopathology study forecasted that the interaction between ethosomes and skin could loosen the tight conjugation of corneocyte layers and weaken the permeation barrier. In conclusion, RPV-ethosomes could be a promising delivery system to encapsulate RPV and deliver RPV for transdermal administration.
罗哌卡因是一种新型长效局麻药，已被证明具有显著优势。然而，临床应用的耐乐品®注射液给患者带来不便。本研究旨在制备罗哌卡因脂质体，并评估脂质体制剂经皮递送罗哌卡因的潜力。采用薄膜分散技术制备了载罗哌卡因脂质体，并对其粒径、ζ电位、差示扫描量热法（DSC）分析和X射线衍射（XRD）研究等方面进行了表征。结果表明，优化后的载罗哌卡因脂质体呈现典型的脂质双分子层结构，粒径分布窄，为73.86±2.40 nm，载药量为8.27±0.37%，包封率为68.92±0.29%。DSC和XRD研究结果表明，罗哌卡因包封于脂质体中时呈无定形状态。此外，体外渗透研究结果证明，载罗哌卡因脂质体能够高效、快速地促进药物渗透（12 h时为349.0±11.5 μg/cm²，0.5 h时为178.8±7.1 μg/cm²）。组织病理学研究结果预测，脂质体与皮肤之间的相互作用可使角质形成细胞层紧密结合松弛，削弱渗透屏障。总之，载罗哌卡因脂质体可能是一种有前途的给药系统，可用于包封罗哌卡因并实现其经皮给药。
