Formulações de anestésicos locais de liberação controlada: aplicações terapêuticas

Abstract

RESUMO CONCLUSÕES: Embora várias pesquisas ainda estejam em andamento, os sistemas de liberação controlada de a n e s t é s i c o s l o c a i s i n d i c a m u m a n o v a d i r e ç ã o n o desenvolvimento de formulações anestésicas mais eficazes e seguras. Unitermos: ANESTÉSICOS: Local SUMMARYAraújo DR, Pinto LMA, Braga AFA, Paula E -Drug-Delivery Systems for Local Anesthetics: Therapeutic Applications 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 advanta g e o f b y p a s s i n g e n c a p s u l a t e d d r u g s r e s t r a i n i n g 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 impor-

Physicochemical stability of poly(lactide-co-glycolide) nanocapsules containing the local anesthetic Bupivacaine

“…Bupivacaine is commercially available in formulations varying from 0.25 to 0.75% in mass of BVC. 16,17 Because the desirable characteristics for a LA include long duration of action, selectivity for sensory rather than motor nerve block and reduction of systemic toxicity, 17,18 an alternative that has proved able to promote these desirable effects is the modified release of these drugs through carrier systems. The purpose of release systems is to promote slow and continuous release, reducing the systemic toxicity of these locally active drugs.…”

“…The purpose of release systems is to promote slow and continuous release, reducing the systemic toxicity of these locally active drugs. [17][18][19] Drug release systems are, in fact, able to compartmentalize the active substance and drive it to specific active sites, as well as control the rate of release without altering the chemical structure of the transported molecule. 20 The delivery of local anesthetics, which has been studied extensively by many research groups and also by our laboratory, can be achieved by the formation of inclusion complexes with cyclodextrins, 20-30 encapsulation in liposomes, [31][32][33][34][35][36][37][38][39] association to polymer microparticles [40][41][42][43] and association to polymeric nanostructured systems.…”

“…The purpose of release systems is to promote slow and continuous release, reducing the systemic toxicity of these locally active drugs. [17][18][19] Drug release systems are, in fact, able to compartmentalize the active substance and drive it to specific active sites, as well as control the rate of release without altering the chemical structure of the transported molecule. …”

Análise do potencial citotóxico agudo da bupivacaína e bupivacaína em excesso enantiomerico de 50% (S75-R25) incorporadas a microesferas sobre o nervo ciático de ratos

“…Despite major advances in the development of these formulations, studies are needed to evaluate the local neurotoxicity in order to ensure their safe use in clinical routine 4 .…”

Caracterização físico-química de complexo de inclusão entre hidroximetilnitrofurazona e hidroxipropil-beta-ciclodextrina

“…Ciclodextrinas (CDs) são oligossacarídeos cíclicos compostos por unidades de glicose unidas por ligações α-1,4 e alteram a intensidade e a duração dos efeitos dos fármacos 14 . As β-CDs são carreadores, levando a molécula hidrofóbica em solução, mantendo-a dissolvida e transportando-a à membrana celular lipofílica 15 .…”