Desenvolvimento e avaliação farmacologica de formulações de liberação controlada com anestesicos locais amino-amidas ciclicos : bupivacaina, mepivacaina e ropivacaina / Development and pharmacological evaluation of drug-delivery systems for cyclic amino-amide local anesthetics: bupivacaine, mepivacaine and ropivacaine

AUTOR(ES)

Daniele Ribeiro de Araujo

DATA DE PUBLICAÇÃO

2005

RESUMO

Local anesthetics (LA) are among the different classes of pharmacological compounds used to attenuate or to eliminate pain. These drugs, which are able to reversibly block the excitation/transmission of the nerve impulse in axons have a relatively short action and a significant toxicity to the Central Nervous and Cardiovascular systems. In order to prolong the time of action and to reduce the systemic toxicity of LA, many investigations have been carried out with LA in drug-delivery systems. These novel formulations, called long-acting local anesthetics, allow the controlled release - avoiding high plasmatic concentrations to be reached ? in such a way that they prolong analgesia as well as they reduce LA?s intrinsic toxicity. Our aim was to prepare, to characterize (the encapsulation, stability and drug-release) and to evaluate - both in vitro (cellular toxicity) and in vivo (latency, intensity and duration of anesthesia as well as local toxicity) the pharmacological activity of new drug-delivery systems for LA, in comparison to the commercially available anesthetics. We have chosen the cyclic amino-amide anesthetics Bupivacaine (BVC), Mepivacaine (MVC) and Ropivacaine (RVC), since they are largely used in medicine and dentistry. The drug-carrier systems used were large unilamellar liposomes (400 nm LUV, composed by phosphathidylcholine and cholesterol) and cyclodextrins: ?-CD and hydroxypropyl (HP?-CD). Stability tests showed that liposomes were able to keep their content and that LA incorporation did not change their permeability at different times and temperatures. Partition coefficients were measured and indicated the profile expected from the substitution degree, i.e. MVC

ASSUNTO(S)

anesthesia ciclodextrinas local anesthesia analgesia anestesia local ciclodextrins lipossomos anestesia analgesia liposomes

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