Articaine in functional NLC show improved anesthesia and anti-inflammatory activity in zebrafish
Autor: | Lígia Nunes de Morais Ribeiro, Gabriela Geronimo, Márcia Cristina Breitkreitz, Juan P. García-López, Eneida de Paula, Gustavo Henrique Rodrigues da Silva, Ludmilla David de Moura, Carmen G. Feijóo |
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Jazyk: | angličtina |
Rok vydání: | 2020 |
Předmět: |
0301 basic medicine
Cetyl Palmitate medicine.drug_class Anti-Inflammatory Agents lcsh:Medicine Carticaine 02 engineering and technology Pharmacology Articaine Article Anti-inflammatory Copaiba Oil Excipients 03 medical and health sciences chemistry.chemical_compound In vivo Bradycardia medicine Zeta potential Animals Anesthesia Anesthetics Local lcsh:Science Tristearin Zebrafish Inflammation Drug Carriers Multidisciplinary Cetyl palmitate lcsh:R Factorial experiment Polydispersity 021001 nanoscience & nanotechnology Nanostructures Drug Liberation 030104 developmental biology chemistry Dentistry Drug delivery Anesthetic lcsh:Q 0210 nano-technology medicine.drug |
Zdroj: | Scientific Reports, Vol 10, Iss 1, Pp 1-13 (2020) Scientific Reports |
ISSN: | 2045-2322 |
Popis: | Indexación Scopus Anesthetic failure is common in dental inflammation processes, even when modern agents, such as articaine, are used. Nanostructured lipid carriers (NLC) are systems with the potential to improve anesthetic efficacy, in which active excipients can provide desirable properties, such as anti-inflammatory. Coupling factorial design (FD) for in vitro formulation development with in vivo zebrafish tests, six different NLC formulations, composed of synthetic (cetyl palmitate/triglycerides) or natural (avocado butter/olive oil/copaiba oil) lipids were evaluated for loading articaine. The formulations selected by FD were physicochemically characterized, tested for shelf stability and in vitro release kinetics and had their in vivo effect (anti-inflammatory and anesthetic effect) screened in zebrafish. The optimized NLC formulation composed of avocado butter, copaiba oil, Tween 80 and 2% articaine showed adequate physicochemical properties (size = 217.7 ± 0.8 nm, PDI = 0.174 ± 0.004, zeta potential = − 40.2 ± 1.1 mV, %EE = 70.6 ± 1.8) and exhibited anti-inflammatory activity. The anesthetic effect on touch reaction and heart rate of zebrafish was improved to 100 and 60%, respectively, in comparison to free articaine. The combined FD/zebrafish approach was very effective to reveal the best articaine-in-NLC formulation, aiming the control of pain at inflamed tissues. © 2020, The Author(s). https://www-nature-com.recursosbiblioteca.unab.cl/articles/s41598-020-76751-6 |
Databáze: | OpenAIRE |
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