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LIPID-BASED NANOCARRIERS FOR THE LOCAL ANESTHETIC TETRACAINE

Grant number: 18/12121-0
Support type:Scholarships in Brazil - Post-Doctorate
Effective date (Start): September 01, 2018
Effective date (End): November 30, 2019
Field of knowledge:Biological Sciences - Pharmacology - Biochemical and Molecular Pharmacology
Principal researcher:Eneida de Paula
Grantee:Fernando Freitas de Lima
Home 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.

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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)
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, . (17/26687-3, 18/12121-0, 17/02201-4, 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, . (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, . (19/17784-0, 21/02617-1, 18/12121-0, 20/01237-8, 17/15174-5)

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