Brazilian Journal of Anesthesiology
https://app.periodikos.com.br/journal/rba/article/doi/10.1590/S0034-70942008000100003
Brazilian Journal of Anesthesiology
Scientific Article

Preparação, caracterização e avaliação in vitro de microesferas de bupivacaína em excesso enantiomérico de 50% (S75-R25)

Preparation, characterization and in vitro evaluation of 50% enantiomeric excess bupivacaine (S75-R25)-loaded microspheres

Pedro Paulo Tanaka; Jean Pierre Estèbe; Richard Campos; François Chevanne; Pascal Le Corre; Sérgio Bernardo Tenório; Maria Fernanda Torres

http://dx.doi.org/10.1590/S0034-70942008000100003 Braz J Anesthesiol, vol.58, n1, p.15-22, 2008
PDF Português
PDF English
Downloads: 0
Views: 943

Resumo

JUSTIFICATIVA E OBJETIVOS: As microesferas podem ser utilizadas como um sistema de liberação controlada para prolongar a ação de anestésicos locais. Esse estudo teve como objetivo a preparação, caracterização e análise da liberação in vitro de microesferas de bupivacaína em excesso enantiomérico de 50% (S75-R25). MÉTODO: As micropartículas foram preparadas utilizando o co-polímero de ácido poliláctico-co-glicólico contendo bupivacaína em excesso enantiomérico de 50% pelo método spray-dryed. RESULTADOS: A caracterização das microesferas em relação ao seu tamanho e conteúdo foram similares aos valores teóricos. A liberação in vitro apresentou um padrão bifásico. CONCLUSÕES: O processo de fabricação de microesferas contendo bupivacaína em excesso enantiomérico de 50% pelo método spray-dryed é factível de ser realizado, com resultados semelhantes aos encontrados com microesferas de bupivacaína.

Palavras-chave

ANESTÉSICOS, Local

Abstract

BACKGROUND AND OBJECTIVES: Microspheres can be used as a controlled delivery system to prolong the duration of action of local anesthetics. The objective of this study was the preparation, characterization and analysis of the in vitro release of 50% enantiomeric excess bupivacaine (S75-R25)-loaded microspheres. METHODS: Microspheres were prepared using the copolymer of polylactide-co-glycolic acid by the spray-dryed method. RESULTS: Characterization of microspheres regarding their size and content were similar to the theoretical values. The in vitro release demonstrated a biphasic pattern. CONCLUSIONS: Manufacturing of 50% enantiomeric excess bupivacaine-loaded microspheres by the spray-dryed method with results similar to bupivacaine-loaded microspheres can be done.

Keywords

ANESTHETICS, Local

Referencias

Borgeat A, Ekatodramis G, Schenker CA. Postoperative nausea and vomiting in regional anesthesia: A review. Anesthesiology. 2003;98:530-547.

Mulroy MF, Larkin KL, Batra MS. Femoral nerve block with 0,25% or 0,5% bupivacaine improves postoperative analgesia following outpatient arthroscopy anterior cruciate ligament repair. Reg Anesth Pain Med. 2001;26:24-29.

Neal JM, Hebl JR, Gerancher JC. Brachial plexus anesthesia: Essentials of our current understanding. Reg Anesth Pain Med. 2002;27:402-428.

Blanco MD, Bernardo MV, Gomez C. Bupivacaine-loaded comatrix formed by albumin microspheres included in a poly (lactide-co-glycolide) film: in vivo biocompatibility and drug release studies. Biomaterials. 1999;20:1919-1924.

Araújo DR, Pinto LM, Braga AFA. Formulações de anestésicos locais de liberação prolongada: Aplicações terapêuticas. Rev Bras Anestesiol. 2003;53:663-671.

Araújo DR, Fraceto LF, Braga AFA. Sistemas de liberação controlada com bupivacaína racêmica (S50-R50) e mistura enantiomérica de bupivacaína (S75-R25): Efeitos da complexação com ciclodextrinas no bloqueio do nervo ciático em camundongos. Rev Bras Anestesiol. 2005;55:316-328.

Le Corre P, Le Guevello P, Gajan V. Preparation and characterization of bupivacaine-loaded polylactide and polylactide-co-glycolide microspheres. Int J Pharm. 1994;107:41-49.

Le Guevello P, Le Corre P, Chevanne F. High-performance liquid chromatographic determination of bupivacaine in plasma samples for biopharmaceutical studies and applications to seven other local anesthetics. J Chromatogr. 1993;622:284-290.

Curley J, Castillo J, Hotz J. Prolonged regional nerve block: Injectable biodegradable bupivacaine polyester microspheres. Anesthesiology. 1996;84:1401-1410.

Malinovsky JM, Bernard JM, Le Corre P. Motor and blood pressure effects of epidural sustained-release bupivacaine from polymer microspheres: A dose-response study in rabbits. Anesth Analg. 1995;81:519-524.

Le Corre P, Estebe JP, Clement R. - Spray-dryed bupivacaine-loaded microspheres: in vitro evaluation and biopharmaceutics of bupivacaine following brachial plexus administration in sheep. Int J Pharm. 2002;238:191-203.

5dd6cef00e88254f6113f287 rba Articles
Links & Downloads
2352-2291 (Electrónico) 0104-0014 (Impreso)
Braz J Anesthesiol ©2024 Todos los derechos reservados.

Braz J Anesthesiol

Share this page
Page Sections