关键词: Anesthetic Bupivacaine Controlled drug delivery Iontophoresis Lidocaine

来  源:   DOI:10.1007/s13346-024-01627-5

Abstract:
Postoperative pain management is an important aspect of the overall surgical care process. Effective pain management not only provides patient comfort but also promotes faster recovery and reduces the risk of complications. Bupivacaine (BUP) and Lidocaine (LID) transdermal drug deliveries via thermoplastic polyurethane matrix (TPU) and iontophoresis technique are proposed here as alternative routes for postoperative pain instead of the injection route. Under applied electric field, the amounts of BUP and LID released were 95% and 97% from the loaded amounts, which were higher than the passive patch of 40%. The time to equilibrium of BUP turned out to be faster than the time to equilibrium of LID by approximately 1.5 times. This was due to 2 factors namely the drug molecular weight and the drug pKa value; they play an important role in the selection of a suitable drug for fast-acting or long-acting for the postoperative patients. By using this transdermal patch via iontophoresis system, BUP was deemed as the suitable drug for fast-acting due to the shorter time to equilibrium, whereas LID was the suitable drug for long-acting. The in-vitro drug release - permeation study through a porcine skin indicated the efficiency and potential of the system with the amounts of drug permeated up to 76% for BUP and 81% for LID. The TPU transdermal system was demonstrated here as potential to deliver BUP and LID for postoperative patients.
摘要:
术后疼痛管理是整个外科护理过程的重要方面。有效的疼痛管理不仅为患者提供舒适,而且还促进更快的恢复并降低并发症的风险。本文提出了通过热塑性聚氨酯基质(TPU)和离子电渗疗法技术的布比卡因(BUP)和利多卡因(LID)透皮药物递送作为术后疼痛的替代途径,而不是注射途径。在外加电场下,BUP和LID的释放量分别为加载量的95%和97%,高于被动贴片的40%。BUP的平衡时间比LID的平衡时间快约1.5倍。这是由于2个因素,即药物分子量和药物pKa值;它们在为术后患者选择合适的速效或长效药物中起重要作用。通过离子电渗系统使用这种透皮贴剂,由于达到平衡的时间较短,BUP被认为是快速起效的合适药物,而LID是适合长效的药物。通过猪皮肤的体外药物释放-渗透研究表明了该系统的效率和潜力,BUP的药物渗透量高达76%,LID的药物渗透量高达81%。这里证明了TPU透皮系统具有为术后患者递送BUP和LID的潜力。
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