Local anesthetic combined with capsaicin:hydroxypropyl-beta-cyclodextrin inclusion complex to selective increase the anesthetic potency

• Grant number: 15/11804-9
• Support Opportunities: Scholarships in Brazil - Doctorate
• Start date: October 01, 2015
• End date: February 28, 2019
• Field of knowledge: Biological Sciences - Pharmacology - Biochemical and Molecular Pharmacology
• Principal Investigator: Eneida de Paula
• Grantee: Verônica Muniz Couto
• Host Institution: Instituto de Biologia (IB). Universidade Estadual de Campinas (UNICAMP). Campinas , SP, Brazil
• Associated research grant: 14/14457-5 - Lipid-based nanocarriers (SLN/NLC and remote-loading liposomes) used to improve the upload and potency of local anesthetics, AP.TEM
• Associated scholarship(s): 17/13004-5 - CAPSAICIN IN A LOCAL ANESTHETIC-BASED IONIC LIQUID TO SELECTIVELY INCREASE THE ANESTHETIC POTENCY, BE.EP.DR

Abstract

Local anesthetics are often used in medical and dental practice when it is necessary to numb parts of the body. Despite all clinical demand, local anesthetics does not allow selective blockade of nociceptive fibers. And furthermore fail to anesthesia procedures as inflamed areas. In fact, it continues to search for local anesthetics agents with long duration, low systemic toxicity and motor blockade.The local anesthetic mepivacaine is in the amino amide family, mainly used in dentistry, and has an intermediate duration of anesthesia. Capsaicin is a poorly water soluble compound, extracted from chili peppers, which have analgesic action and allows the opening of TRPV1 channels, only expressed in nociceptive fibers. Recently, it was reported that the application of local anesthetic followed by capsaicin leads to a selective increase in sensory blockade in rats due to easy entry of local anesthetics in nociceptive fibers (Gerner et al., 2008).In this study, we intend to develop, characterize and evaluate the effectiveness of inclusion complex of capsaicin:cyclodextrin associated to mepivacaine. Through this approach, it is expected to improve the solubility of capsaicin, developing a single dose formulation with better sensory blocking and reduced motor blockade.

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

COUTO, V. M.; CASADEI, B. R.; RODRIGUES DA SILVA, G. H.; RISKE, K. A.; OLIVEIRA-NASCIMENTO, L.; DE PAULA, E.. Capsaicin and local anesthetics interaction with model membranes. EUROPEAN BIOPHYSICS JOURNAL WITH BIOPHYSICS LETTERS, v. 46, p. 1-pg., 2017-07-01. (15/09948-2, 14/14457-5, 15/11804-9)

COUTO, VERONICA MUNIZ; DE OLIVEIRA-NASCIMENTO, LAURA; CABECA, LUIZ FERNANDO; GERALDES, DANILO COSTA; RIBEIRO COSTA, JULIANA SOUZA; RISKE, KARIN A.; FRANZ-MONTAN, MICHELLE; YOKAYCHIYA, FABIANO; DIAS FRANCO, MARGARETH K. K.; DE PAULA, ENEIDA. Capsaicin-Cyclodextrin Complex Enhances Mepivacaine Targeting and Improves Local Anesthesia in Inflamed Tissues. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, v. 21, n. 16, AUG 2020. (14/20224-3, 15/11804-9, 14/14457-5)

Academic Publications

(References retrieved automatically from State of São Paulo Research Institutions)

COUTO, Verônica Muniz. Associação de capsaicina com anestésicos locais para aumento da analgesia. 2019. Doctoral Thesis - Universidade Estadual de Campinas (UNICAMP). Instituto de Biologia Campinas, SP.