Development of nanostructured lipid carriers encapsulating local anesthetics processed biopolymeric matrices for topical application at oral mucosa

• Grant number: 14/25372-0
• Support Opportunities: Scholarships in Brazil - Post-Doctorate
• Effective date (Start): April 01, 2015
• Effective date (End): February 28, 2019
• Field of knowledge: Health Sciences - Dentistry - Dental Clinics
• Principal Investigator: Eneida de Paula
• Grantee: Lígia Nunes de Morais Ribeiro
• 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 administration of local anesthetics (LA) in Dentistry still causes pain and stress, being often the reason for patients to leave treatment, with serious consequences for their oral health. Topical anesthetics were developed to minimize pain sensation caused by needle insertion and injection. However, the commercially available formulations usually show low efficiency, and little scientific progress has been achieved in the development of topical anesthetics able to eliminate any inherent local anesthesia painful sensation. This project aims the development of a sustained release system for the delivery of lidocaine and prilocaine in nanostructured lipid carriers (NLC) in chitosan and pectin biopolymers matrices, processed as a bioadhesive and a hydrogel, for topical anesthesia of the oral mucosa. Such drug-delivery system should have higher efficiency and lower toxicity, in order to fulfill this gap in Dentistry anesthesia. The characterization of beads containing LA will be carried out by: infrared spectroscopy (IR), thermal (TG/DSC) analyses, scanning electron microscopy (FE-SEM, TEM), Zeta potential, particle size distribution and polidispersity, measured by dynamic light scatter (DLS) and nanoparticle tracking analysis (NTA). The characterization of hydrogels and bioadhesives will be conducted by mechanical studies, mucoadhesiveness assays. Moreover, in vitro drug release, dissolution and permeation across the pig oral mucosa in Franz type diffusion cells will be conducted.

Scientific publications

(10)

(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)

DE MORAIS RIBEIRO, LIGIA NUNES; FRANZ-MONTAN, MICHELLE; BREITKREITZ, MARCIA CRISTINA; RODRIGUES DA SILVA, GUSTAVO HENRIQUE; DE CASTRO, SIMONE RAMOS; GUILHERME, VIVIANE APARECIDA; DE ARAUJO, DANIELE RIBEIRO; DE PAULA, ENEIDA. Nanohybrid hydrogels designed for transbuccal anesthesia. INTERNATIONAL JOURNAL OF NANOMEDICINE, v. 13, p. 6453-6463, 2018. (14/14457-5, 14/25372-0)

RODRIGUES DA SILVA, GUSTAVO H.; GERONIMO, GABRIELA; RIBEIRO, LIGIA N. M.; GUILHERME, VIVIANE A.; DE MOURA, LUDMILLA DAVID; BOMBEIRO, ANDRE L.; OLIVEIRA, JULIANA DAMASCENO; BREITKREITZ, MARCIA C.; DE PAULA, ENEIDA. Injectable in situ forming nanogel: A hybrid Alginate-NLC formulation extends bupivacaine anesthetic effect. Materials Science & Engineering C-Materials for Biological Applications, v. 109, APR 2020. (18/07100-4, 14/25372-0, 17/15174-5, 14/14457-5)

RIBEIRO, LIGIA N. M.; BREITKREITZ, MARCIA C.; GUILHERME, VIVIANE A.; DA SILVA, GUSTAVO H. R.; COUTO, VERONICA M.; CASTRO, SIMONE R.; DE PAULA, BARBARA O.; MACHADO, DAISY; DE PAULA, ENEIDA. Natural lipids-based NLC containing lidocaine: from pre-formulation to in vivo studies. European Journal of Pharmaceutical Sciences, v. 106, p. 102-112, AUG 30 2017. (14/14457-5, 14/25372-0)

ALBANO, JUAN M. R.; DE MORAIS RIBEIRO, LIGIA NUNES; COUTO, VERONICA MUNIZ; MESSIAS, MARIANA BARBOSA; RODRIGUES DA SILVA, GUSTAVO HENRIQUE; BREITKREITZ, MARCIA CRISTINA; DE PAULA, ENEIDA; PICKHOLZ, MONICA. Rational design of polymer-lipid nanoparticles for docetaxel delivery. COLLOIDS AND SURFACES B-BIOINTERFACES, v. 175, p. 56-64, MAR 1 2019. (14/14457-5, 14/25372-0)

DE MORAIS RIBEIRO, LIGIA NUNES; COUTO, VERONICA MUNIZ; FRACETO, LEONARDO FERNANDES; DE PAULA, ENEIDA. Use of nanoparticle concentration as a tool to understand the structural properties of colloids. SCIENTIFIC REPORTS, v. 8, JAN 17 2018. (14/14457-5, 14/25372-0)

RIBEIRO, LIGIA N. M.; FRANZ-MONTAN, MICHELLE; ALCANTARA, ANA C. S.; BREITKREITZ, MARCIA C.; CASTRO, SIMONE R.; GUILHERME, VIVIANE A.; MUNIZ, V, BRUNO; RODRIGUES DA SILVA, GUSTAVO H.; DE PAULA, ENEIDA. Hybrid nanofilms as topical anesthetics for pain-free procedures in dentistry. SCIENTIFIC REPORTS, v. 10, n. 1, JUL 9 2020. (14/50867-3, 14/25372-0, 14/14457-5)

CASTRO, SIMONE R.; RIBEIRO, LIGIA N. M.; BREITKREITZ, MARCIA C.; GUILHERME, VIVIANE A.; RODRIGUES DA SILVA, GUSTAVO H.; MITSUTAKE, HERY; ALCANTARA, ANA C. S.; YOKAICHIYA, FABIANO; FRANCO, MARGARETH K. K. D.; CLEMENS, DANIEL; et al. A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers. SCIENTIFIC REPORTS, v. 11, n. 1, NOV 2 2021. (14/14457-5, 14/25372-0)

RIBEIRO, LIGIA N. M.; ALCANTARA, ANA C. S.; RODRIGUES DA SILVA, GUSTAVO H.; FRANZ-MONTAN, MICHELLE; NISTA, SILVIA V. G.; CASTRO, SIMONE R.; COUTO, VERONICA M.; GUILHERME, VIVIANE A.; DE PAULA, ENEIDA. Advances in Hybrid Polymer-Based Materials for Sustained Drug Release. INTERNATIONAL JOURNAL OF POLYMER SCIENCE, 2017. (14/14457-5, 14/25372-0)

DE ARAUJO, DANIELE RIBEIRO; DE MORAIS RIBEIRO, LIGIA NUNES; DE PAULA, ENEIDA. Lipid-based carriers for the delivery of local anesthetics. Expert Opinion on Drug Delivery, v. 16, n. 7, JUN 2019. (14/14457-5, 14/25372-0)

RODRIGUES DA SILVA, GUSTAVO H.; PAES LEMES, JULIA BORGES; GERONIMO, GABRIELA; DE LIMA, FERNANDO FREITAS; DE MOURA, LUDMILLA DAVID; DOS SANTOS, ARIANY CARVALHO; CARVALHO, NATHALIA SANTOS; MALANGE, KAUE FRANCO; BREITKREITZ, MARCIA C.; PARADA, CARLOS A.; et al. Lipid nanoparticles loaded with butamben and designed to improve anesthesia at inflamed tissues dagger. BIOMATERIALS SCIENCE, v. 9, n. 9, p. 3378-3389, MAY 7 2021. (17/15174-5, 14/25372-0)