Laboratory for Biomaterials and Drug Delivery, Department of Anesthesiology, Division of Critical Care Medicine, Boston Children's Hospital, Harvard Medical School, Boston, MA, USA.
Nat Commun. 2020 May 8;11(1):2323. doi: 10.1038/s41467-020-16177-w.
An on-demand anesthetic that would only take effect when needed and where the intensity of anesthesia could be easily adjustable according to patients' needs would be highly desirable. Here, we design and synthesize a macromolecular prodrug (P407-CM-T) in which the local anesthetic tetracaine (T) is attached to the polymer poloxamer 407 (P407) via a photo-cleavable coumarin linkage (CM). P407-CM-T solution is an injectable liquid at room temperature and gels near body temperature. The macromolecular prodrug has no anesthetic effect itself unless irradiated with a low-power blue light emitting diode (LED), resulting in local anesthesia. By adjusting the intensity and duration of irradiation, the anesthetic effect can be modulated. Local anesthesia can be repeatedly triggered.
一种按需麻醉剂，只有在需要时才会生效，并且可以根据患者的需求轻松调节麻醉强度，这将是非常理想的。在这里，我们设计并合成了一种大分子前药（P407-CM-T），其中局部麻醉剂盐酸丁卡因（T）通过光裂解香豆素键（CM）连接到聚合物泊洛沙姆 407（P407）上。P407-CM-T 溶液在室温下为可注射液体，在接近体温时会凝胶化。除非用低功率的蓝光发光二极管（LED）照射，否则大分子前药本身没有麻醉作用，从而产生局部麻醉。通过调整照射的强度和持续时间，可以调节麻醉效果。局部麻醉可以反复触发。
