Anesthetic efficacy of bupivacaine complexed in sulfobutylether-²-cyclodextrin in the infraorbital nerve block

• Grant number: 21/02197-2
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Effective date (Start): July 01, 2021
• Effective date (End): June 30, 2022
• Field of knowledge: Biological Sciences - Pharmacology - General Pharmacology
• Principal Investigator: Luiz Eduardo Nunes Ferreira
• Grantee: Maria Fernanda de Queiroz Laranjeira
• Host Institution: Universidade Universus Veritas Guarulhos (Univeritas UNG). Guarulhos , SP, Brazil

Abstract

The development of drugs able to produce long-lasting analgesia, with lower systemic toxicity and few adverse effects would be of great benefit for acute and chronic pain control. Bupivacaine is a long-acting local anesthetic with strong action, however, it has lower solubility and higher toxicity. The complexation of LA in cyclodextrin has shown improvements in aqueous solubility, reduced systemic toxicity, and other biopharmaceutical properties. This study aims to prepare a formulation of bupivacaine complexed in sulfobutylether-²-cyclodextrin (SBE²CD) and test the anesthetic efficacy in relation to plain bupivacaine in an infraorbital nerve block model. An inclusion complex of bupivacaine in SBE²CD will be prepare. The formulation will be tested in 20 rats (Rattus norvegicus albinus) from Wistar lineage, adults, weighing between 250-400 g. The animal will be treated with the formulation on the right side. The contralateral side will be used for control. The study will be blind and the groups and injections will be randomized. The anesthesia will be measured at 5 minutes to determine the anesthetic efficacy of the formulations. Data will be submitted to analysis of variance with the appropriate posthoc test. (AU)