Peptu Cristian, Rotaru Razvan, Ignat Leonard, Humelnicu Andra Cristina, Harabagiu Valeria, Peptu Catalina Anisoara, Leon Maria-Magdalena, Mitu Florin, Cojocaru Elena, Boca Andreea, Tamba Bogdan Ionel
"Petru Poni" Institute of Macromolecular Chemistry, Aleea Grigore Ghica Voda 41A, 700487 Iasi, Romania.
Curr Pharm Des. 2015;21(42):6125-39. doi: 10.2174/1381612821666151027152752.
The paper focuses on the advances in the field of pain treatment by transdermal delivery of specific drugs. Starting from a short description of the skin barrier, the pharmacodynamics and pharmacokinetics including absorption, distribution, action mechanism, metabolism and toxicity, aspects related to the use of pain therapy drugs are further discussed. Most recent results on topical anesthetic agents as well as the methods proved to overcome the skin barrier and to provide efficient delivery of the drug are also discussed. The present review is proposing to summarize the recent literature on the pharmacotherapeutic principles of local anesthetics and non-steroidal anti-inflammatory drugs, generally used to alleviate pain but also the drugs as nanoformulations with potential applications in transdermal delivery. A special attention is given to efficient formulations meant for transdermal penetration enhancement of anesthetics where the drug is encapsulated into macrocyclic molecules (cyclodextrins, cyclodextrin derivatives), liposomes or polymer nanoparticles and hydrogels.
本文重点关注通过特定药物经皮给药在疼痛治疗领域的进展。从对皮肤屏障的简短描述开始，进一步讨论了包括吸收、分布、作用机制、代谢和毒性在内的药效学和药代动力学，以及与疼痛治疗药物使用相关的方面。还讨论了局部麻醉剂的最新研究结果以及被证明可克服皮肤屏障并实现药物高效递送的方法。本综述旨在总结近期关于局部麻醉药和非甾体抗炎药的药物治疗原理的文献，这些药物通常用于缓解疼痛，同时也包括作为纳米制剂且在经皮给药中有潜在应用的药物。特别关注旨在增强麻醉剂经皮渗透的高效制剂，其中药物被封装在大环分子（环糊精、环糊精衍生物）、脂质体或聚合物纳米颗粒以及水凝胶中。
