ABC Federal University, Natural and Human Science Center , Av dos Estados 5001 Bloco A, Torre 3, Sala 624-3, Santo André, 09210-580 , Brazil
Expert Opin Drug Deliv. 2013 Nov;10(11):1551-63. doi: 10.1517/17425247.2013.828031. Epub 2013 Aug 13.
Dermal and transdermal drug delivery systems offer the possibility to control the release of the drug for an extended period of time. In particular, skin-delivery of local anesthetics (LA) is one of the most important strategies to increase the local drug concentration and to reduce systemic adverse reactions.
During the development phase of new formulations for skin-delivery of LA one should consider a set of desirable features such providing suitable adhesion, easy application/removal and also to be biocompatible, biodegradable and non-toxic. This review emphasizes the main strategies for skin-delivery of LA considering those features in relation to the composition of the delivery systems described. The topics highlight the relationships between physico-chemical studies and pharmaceutical applications for liposomes and solid lipid nanoparticles as well as the formulation and clinical applications for hydrogels and patches.
The development of LA skin-delivery systems using hydrogels and different permeation enhancers, liposomes or lipid nanoparticles (as isolated carrier systems or as their dispersion in a gel-base) and patches have been explored as alternatives to commercial formulations, modifying the release rate of LA, increasing bioadhesive properties and reducing toxicity, resulting in an improved therapeutic efficacy. This review should provide to the reader a special emphasis on four delivery-systems, comprising the group of liposomes and lipid nanoparticles, hydrogels and patches technologies looking forward their application for skin anesthesia.
皮肤和透皮药物递送系统为延长药物的释放时间提供了可能。特别是,局部麻醉剂(LA)的皮肤递送是增加局部药物浓度和减少全身不良反应的最重要策略之一。
在 LA 的皮肤递药新制剂的开发阶段,应考虑一系列理想的特性,如提供适当的附着力、易于涂抹/去除、生物相容性、可生物降解性和低毒性。本综述强调了 LA 皮肤递药的主要策略,考虑到与所描述的递药系统组成相关的这些特性。这些主题突出了脂质体和固体脂质纳米粒作为独立载体系统或其在凝胶基质中的分散体以及水凝胶和贴剂的制剂和临床应用之间的物理化学研究和药物应用之间的关系。
使用水凝胶和不同的渗透增强剂、脂质体或脂质纳米粒(作为独立载体系统或其在凝胶基质中的分散体)以及贴剂开发 LA 皮肤递药系统已被探索为商业制剂的替代品,可调节 LA 的释放速度、增加生物黏附特性和降低毒性,从而提高治疗效果。本文综述重点介绍了四种递药系统,包括脂质体和脂质纳米粒、水凝胶和贴剂技术,以期将其应用于皮肤麻醉。