• Rev Bras Anestesiol · Sep 2003

    Drug-delivery systems for local anesthetics: therapeutic applications.

    • Daniele Ribeiro de Araújo, Luciana de Matos Alves Pinto, Angélica de Fátima de Assunção Braga, and Eneida de Paula.
    • Departamento de Bioquímica, Instituto de Biologia da Universidade Estadual de Campinas, UNICAMP, Campinas, SP. daraujo@unicamp.br
    • Rev Bras Anestesiol. 2003 Sep 1; 53 (5): 663-71.

    Background And ObjectivesMany 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.ContentsLiposomes 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.ConclusionsAlthough studies are still in progress, drug-delivery systems are flagging a new direction for the development of safer and more effective local anesthetic formulations.

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