Brazilian Journal of Anesthesiology
https://bjan-sba.org/article/doi/10.1590/S0034-70942003000500014
Brazilian Journal of Anesthesiology
Miscellaneous

Formulações de anestésicos locais de liberação controlada: aplicações terapêuticas

Drug-delivery systems for local anesthetics: therapeutic applications

Daniele Ribeiro de Araújo; Luciana de Matos Alves Pinto; Angélica de Fátima de Assunção Braga; Eneida de Paula

http://dx.doi.org/10.1590/S0034-70942003000500014 Braz J Anesthesiol, vol.53, n5, p.663-671, 2003
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Resumo

JUSTIFICATIVA E OBJETIVOS: O desenvolvimento de sistemas de liberação controlada tem sido alvo de pesquisas há pelo menos quatro décadas. Desde que foi sugerida sua aplicação na indústria farmacêutica, muitos resultados foram obtidos, especialmente na manipulação molecular de carreadores e no estudo de suas interações com as drogas encapsuladas. Esses novos carreadores têm a vantagem de contornar propriedades físico-químicas limitantes (como a solubilidade aquosa ou em membranas) das drogas encapsuladas, melhorando assim a farmacodinâmica (potencialização do efeito terapêutico), farmacocinética (controle da absorção e distribuição tecidual) e os efeitos toxicológicos (redução da toxicidade local e sistêmica) das mesmas. Entre os principais carreadores, destacam-se os lipossomas e as ciclodextrinas, que vêm trazendo inúmeras vantagens no desenvolvimento de formulações para liberação controlada de anestésicos locais. Este trabalho de revisão objetiva descrever a interação de anestésicos locais com lipossomas ou ciclodextrinas, o desenvolvimento das pesquisas básica e clínica nessa área, além da aplicabilidade terapêutica dessas formulações. CONTEÚDO: Lipossomas têm a capacidade de veicular drogas em órgãos-alvo, disponibilizando apenas uma fração - liberação controlada - para o sítio de ação. Já as ciclodextrinas alteram a intensidade e a duração do efeitos das drogas através da baixa absorção sistêmica do complexo. Pesquisas básicas e clínicas apontam como vantagens do uso de anestésicos locais encapsulados em lipossomas ou complexados com ciclodextrinas a liberação lenta da droga que prolonga a duração da anestesia e reduz a toxicidade para os sistemas cardiovascular e nervoso central. CONCLUSÕES: Embora várias pesquisas ainda estejam em andamento, os sistemas de liberação controlada de anestésicos locais indicam uma nova direção no desenvolvimento de formulações anestésicas mais eficazes e seguras.

Palavras-chave

ANESTÉSICOS

Abstract

BACKGROUND AND OBJECTIVES: 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. CONTENTS: 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. CONCLUSIONS: 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.

Keywords

ANESTHETICS

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