Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil.
Department of Structural and Functional Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil.
Mater Sci Eng C Mater Biol Appl. 2020 Apr;109:110608. doi: 10.1016/j.msec.2019.110608. Epub 2019 Dec 28.
Finding an ideal anesthetic agent for postoperative pain control, with long action and low side effects, is still a challenge. Local anesthetics have potential for such application if their time of action is improved. This work introduces a new hybrid formulation formed by the association of a nanostructured lipid carrier with a biopolymeric system to encapsulate bupivacaine (BVC). The hybrid formulation was physicochemical and structurally characterized by DLS, TEM, DSC, XRD and FTIR-ATR, and it remained stable for 12 months at room temperature. In vivo analgesia and imaging tests showed that the hybrid system was able to modulate the release, and to increase the concentration of BVC at the site of action, by forming a nanogel in situ. Such nanogel improved over 5 times (>24 h) the anesthesia duration, when compared to free BVC at clinical (0.5%) doses. Therefore, this novel in situ-forming nanogel shows great potential to be used in postsurgical pain control, improving the action of BVC, without losing its versatility of (infiltrative) application.
寻找一种理想的术后镇痛麻醉剂，作用时间长、副作用低，仍然是一个挑战。局部麻醉剂如果能延长其作用时间，就有应用的潜力。本工作介绍了一种新的混合制剂，由纳米结构脂质载体与生物聚合体系结合，包封布比卡因（BVC）形成。通过 DLS、TEM、DSC、XRD 和 FTIR-ATR 对混合制剂进行了理化和结构表征，其在室温下稳定 12 个月。体内镇痛和成像试验表明，该混合体系能够通过原位形成纳米凝胶来调节释放，并增加作用部位 BVC 的浓度。与临床（0.5%）剂量的游离 BVC 相比，这种纳米凝胶将麻醉持续时间延长了 5 倍以上（>24 小时）。因此，这种新型的原位形成纳米凝胶具有很大的潜力，可用于术后疼痛控制，改善 BVC 的作用，而不丧失其（浸润性）应用的多功能性。
