LIPID-BASED NANOCARRIERS FOR THE LOCAL ANESTHETIC TETRACAINE

• Grant number: 18/12121-0
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• Start date: September 01, 2018
• End date: November 30, 2019
• Field of knowledge: Biological Sciences - Pharmacology - Biochemical and Molecular Pharmacology
• Principal Investigator: Eneida de Paula
• Grantee: Fernando Freitas de Lima
• 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

Abstract

The encapsulation of Local Anesthetics (LA) in ionic gradient liposomes (IGL) has been shown to increase the time of analgesia and decrease the side effects, by maintaining the drug in the site of action for a longer time. Intradermal administration of IGL prepared with (NH4)2SO4 in a human volunteer achieved up to 19, 38, and 48 h of successful anesthesia with 0.5, 1, and 2% bupivacaine respectively (Grant et al., Anesthesiol 101:133, 2004). Our group has recently reported large (up to 2%) amounts of LA ropivacaine (RVC) entrapped (%EE~70%) in egg PC/chol/alpha-tocopherol 4/3/0.07 mole % IGL with a sustained release (~25 h) (Silva et al., J Lip. Res.26:1, 2015; Plos One v.12 e0185828, 2017). Also, a significant increase in the sensory block duration (27 h) in rats was achieved with a 0.012% formulation of dibucaine in IGL (prepared with sulfate and citrate), in comparison to an equivalent DBC solution (11 h) (Couto et al., J. Pharm. Sci, in press, 2018). The aim of the present study is to develop a IGL for tetracaine (TTC), an aminoester LA extensively used in ophthalmology and topical anestesia. The formulation is expected to be suitable for the treatment of burn injuries (topical). We also intend to exploit another lipid-based nanocarrier systems, prepared with hydrogenated soy phosphatidyl-choline:TTC:NaCl. In that way we propose to prepare, to characterize and to test the activity of the lipid-based TTC formulations.

Scientific publications

(5)

(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)

LESCANO, CAROLINE HONAISER; DE LIMA, FERNANDO FREITAS; CARDOSO, CLAUDIA ANDREA LIMA; VIEIRA, SILVIA CRISTINA HEREDIA; MONICA, FABIOLA ZAKIA; DE OLIVEIRA, IVAN PIRES. Rutin present in Alibertia edulis extract acts on human platelet aggregation through inhibition of cyclooxygenase/thromboxane. FOOD & FUNCTION, v. 12, n. 2, p. 802-814, JAN 21 2021. (17/26687-3, 18/12121-0, 17/02201-4, 20/01237-8)

DE LIMA, FERNANDO FREITAS; MENDONCA, TALITA CESARIM; PINILLA, CRISTIAN MAURICIO BARRETO; ALVIM, IZABELA DUTRA; VIDO, MARIANA ALVES GRAGNANI; DE PAULA, ENEIDA; SPADOTI, LEILA MARIA; SILVA E ALVES, ADRIANA TORRES. Co-encapsulation of probiotic bacteria L. rhamnosus GG and β-carotene by a novel biphasic encapsulation technique: Stability and in vivo anti-inflammatory properties. FOOD BIOSCIENCE, v. 62, p. 9-pg., 2024-09-14. (21/04987-0, 18/12121-0)

LESCANO, CAROLINE HONAISER; DE LIMA, FERNANDO FREITAS; STEFANELLO CATELAN, TALINE BAGANHA; DANTAS GUIMARAES, VICTOR HUGO; ALVES PEREIRA, ULISSES; MARTINS AGUILAR, CHARLES; LIMA CARDOSO, CLAUDIA ANDREA; SOUSA SANTOS, SERGIO HENRIQUE; BORGES, ALEXANDRE; PIRES DE OLIVEIRA, IVAN. Campomanesia guazumifolia infusion decreases human platelet aggregation by reducing cyclooxygenase 1 activity and its underlying mechanisms. FOOD BIOSCIENCE, v. 55, p. 12-pg., 2023-10-01. (17/02201-4, 18/12121-0, 17/26687-3, 20/01237-8)

DE LIMA, FERNANDO FREITAS; DA SILVA, BIANCA BRANDAO; OLIVEIRA, JULIANA DAMASCENO; DE MOURA, LUDMILLA DAVID; DA SILVA, GUSTAVO HENRIQUE RODRIGUES; FERNANDES, PRISCILA CORDEIRO LIMA; SOUZA, ROOSEVELT ISAIAS CARVALHO; DOS SANTOS, ARIANY CARVALHO; DE PAULA, ENEIDA. Prolonged anesthesia and decreased toxicity of enantiomeric-excess bupivacaine loaded in ionic gradient liposomes. International Journal of Pharmaceutics, v. 606, SEP 5 2021. (18/12121-0, 14/14457-5)

RODRIGUES DA SILVA, GUSTAVO HENRIQUE; DE MOURA, LUDMILLA DAVID; DE CARVALHO, FABIOLA VIEIRA; GERONIMO, GABRIELA; MENDONCA, TALITA CESARIM; DE LIMA, FERNANDO FREITAS; DE PAULA, ENEIDA. Antineoplastics Encapsulated in Nanostructured Lipid Carriers. Molecules, v. 26, n. 22, NOV 2021. (19/17784-0, 21/02617-1, 18/12121-0, 20/01237-8, 17/15174-5)