
Promising potential of articaine-loaded poly(epsilon-caprolactone) nanocapules for intraoral topical anesthesia
Author(s) -
Camila Batista da Silva,
Maria Cristina Volpato,
Bruno Vilela Muniz,
Cleiton Pita dos Santos,
Luciano Serpe,
Luiz Eduardo Nunes Ferreira,
Nathalie Ferreira Silva de Melo,
Leonardo Fernandes Fraceto,
Francisco Carlos Groppo,
Michelle Franz-Montan
Publication year - 2021
Publication title -
plos one
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.99
H-Index - 332
ISSN - 1932-6203
DOI - 10.1371/journal.pone.0246760
Subject(s) - nanocapsules , articaine , poloxamer , local anesthetic , analgesic , anesthesia , medicine , chemistry , pharmacology , materials science , nanoparticle , polymer , nanotechnology , organic chemistry , copolymer
To determine whether the permeation capacity and analgesic efficacy of articaine (ATC) could be increased and cytotoxicity decreased by encapsulation in poly(ɛ-caprolactone) nanocapsules (ATC nano ), aiming at local or topical anesthesia in dentistry. Cellular viability was evaluated (using the MTT test and fluorescence microscopy) after 1 h and 24 h exposure of HaCaT cells to ATC, ATC nano , ATC with epinephrine (ATC epi ), and ATC in nanocapsules with epinephrine (ATC nanoepi ). The profiles of permeation of 2% ATC and 2% ATC nano across swine esophageal epithelium were determined using Franz-type vertical diffusion cells. Analgesic efficacy was evaluated with a von Frey anesthesiometer in a postoperative pain model in rats, comparing the 2% ATC, 2% ATC nano , 2% ATC epi , and 2% ATC nanoepi formulations to 4% ATC epi (a commercially available formulation). We show that use of the nanocapsules decreased the toxicity of articaine ( P <0.0001) and increased its flux ( P = 0.0007). The 2% ATC epi and 4% ATC epi formulations provided higher analgesia success and duration ( P <0.05), compared to 2% ATC, 2% ATC nano , and 2% ATC nanoepi . Articaine-loaded poly(ɛ-caprolactone) nanocapsules constitute a promising formulation for intraoral topical anesthesia (prior to local anesthetic injection), although it is not effective when injected in inflamed tissues for pain control, such as irreversible pulpitis.