de Araújo Daniele Ribeiro, Pinto Luciana de Matos Alves, Braga Angélica de Fátima de Assunção, de Paula Eneida
Departamento de Bioquímica, Instituto de Biologia da Universidade Estadual de Campinas, UNICAMP, Campinas, SP.
Rev Bras Anestesiol. 2003 Sep;53(5):663-71.
Many researchers in the last four decades have been devoted to the development of drug-delivery systems. Since its first application in the pharmaceutical industry, many results have been obtained especially in the molecular manipulation of carriers and their interaction with encapsulated drugs. These new carriers have the advantage of bypassing encapsulated drugs restraining physicochemical properties (such as water or membrane solubility), thus improving pharmacodynamics (therapeutic effect potentiation), pharmacokinetics (control of tissue absorption and distribution) and toxic effects (lower local and systemic toxicity). Liposomes and cyclodextrins are among the most important carriers which have shown to be quite advantageous in the development of drug-delivery systems for local anesthetics. This study aimed at reviewing the interaction of local anesthetics with liposomes and cyclodextrins, the development of basic and applied research on the field, in addition to therapeutic applicability of these formulations.
Liposomes have the ability to control drug delivery to target tissues, fractionating drug release in its site of action. Cyclodextrins, on the other hand, change intensity and duration of effects due to low systemic drug absorption. Basic and clinical studies have pointed out that the administration of local anesthetics in liposome or cyclodextrin formulations induces slow release of the drugs, prolonging the anesthetic action and decreasing cardiac and nervous systems toxicity.
Although studies are still in progress, drug-delivery systems are flagging a new direction for the development of safer and more effective local anesthetic formulations.
在过去的四十年里，许多研究人员致力于药物递送系统的开发。自其首次应用于制药行业以来，已取得了许多成果，尤其是在载体的分子操控及其与包封药物的相互作用方面。这些新型载体具有绕过包封药物限制其理化性质（如水溶性或膜溶性）的优势，从而改善药效学（增强治疗效果）、药代动力学（控制组织吸收和分布）以及毒性作用（降低局部和全身毒性）。脂质体和环糊精是最重要的载体，在局部麻醉药药物递送系统的开发中已显示出相当大的优势。本研究旨在综述局部麻醉药与脂质体和环糊精的相互作用、该领域基础和应用研究的进展，以及这些制剂的治疗适用性。
脂质体能够控制药物向靶组织的递送，在其作用部位实现药物的分级释放。另一方面，由于药物的全身吸收较低，环糊精会改变药物作用的强度和持续时间。基础和临床研究指出，以脂质体或环糊精制剂形式给予局部麻醉药可使药物缓慢释放，延长麻醉作用并降低心脏和神经系统毒性。
尽管研究仍在进行中，但药物递送系统正在为开发更安全、更有效的局部麻醉药制剂指明新的方向。
