Department of Anesthesiology, Weifang Medical University, Weifang, China.
Department of Gynecology, Affiliated Hospital of Weifang Medical University, Weifang, China.
Drug Deliv. 2022 Dec;29(1):263-269. doi: 10.1080/10717544.2021.2023695.
Combination therapy combining two drugs in one modified drug delivery system is used to achieve synergistic analgesic effect, and bring effective control of pain management, especially postoperative pain management. In the present study, a combination of drug delivery technologies was utilized. Transcriptional transactivator (TAT) peptide modified, transdermal nanocarriers were designed to co-deliver ropivacaine (RVC) and meloxicam (MLX) and anticipated to achieve longer analgesic effect and lower side effect. TAT modified nanostructured lipid carriers (TAT-NLCs) were used to co-deliver RVC and MLX. RVC and MLX co-loaded TAT-NLCs (TAT-NLCs-RVC/MLX) were evaluated through skin permeation and treatment studies. NLCs-RVC/MLX showed uniform and spherical morphology, with a size of 133.4 ± 4.6 nm and a zeta potential of 20.6 ± 1.8 mV. The results illustrated the anesthetic pain relief ability of the present constructed system was significantly improved by the TAT modification through the enhanced skin permeation efficiency and the co-delivery of MLX along with RVC that improved pain management by reducing inflammation at the injured area. This study provides an efficient and facile method for preparing TAT-NLCs-RVC/MLX as a promising system to achieve synergistic analgesic effect.
联合疗法将两种药物结合在一个改良的药物传递系统中，以达到协同的镇痛效果，并有效控制疼痛管理，特别是术后疼痛管理。在本研究中，联合使用了药物传递技术。设计了经转录激活物（TAT）肽修饰的透皮纳米载体来共递送罗哌卡因（RVC）和美洛昔康（MLX），并预期实现更长的镇痛效果和更低的副作用。TAT 修饰的纳米结构脂质载体（TAT-NLCs）用于共递送 RVC 和 MLX。通过皮肤渗透和治疗研究评估了共载有 RVC 和 MLX 的 TAT-NLCs（TAT-NLCs-RVC/MLX）。NLCs-RVC/MLX 呈均匀的球形形态，粒径为 133.4±4.6nm，zeta 电位为 20.6±1.8mV。结果表明，通过 TAT 修饰增强了皮肤渗透效率，并与 RVC 共递送 MLX，改善了损伤部位的炎症，从而提高了疼痛管理水平，显著提高了本构建系统的麻醉止痛能力。本研究为制备 TAT-NLCs-RVC/MLX 提供了一种高效简便的方法，作为一种实现协同镇痛效果的有前途的系统。
