Mucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia

Author(s)

Calixto, Giovana Maria Fioramonti ^[1] ; Muniz, Bruno Vilela ^[1] ; Castro, Simone R. ^[2] ; de Araujo, Jaiza Samara Macena ^[1] ; Amorim, Klinger de Souza ^[1] ; Ribeiro, Ligia N. M. ^[3] ; Ferreira, Luiz Eduardo Nunes ^[4] ; de Araujo, Daniele Ribeiro ^[5] ; de Paula, Eneida ^[2] ; Franz-Montan, Michelle ^[1]

Affiliation

^[1] Univ Campinas UNICAMP, Piracicaba Dent Sch, Dept Biosci, BR-13414903 Piracicaba - Brazil

^[2] Univ Campinas UNICAMP, Inst Biol, Dept Biochem & Tissue Biol, BR-13083872 Campinas - Brazil

^[3] Fed Univ Uberlandia UFU, Inst Biotechnol, BR-38405302 Uberlandia, MG - Brazil

^[4] Guarulhos Univ UNG, Lab Inflammat & Immunol, BR-07023070 Guarulhos - Brazil

^[5] Fed Univ ABC UFABC, Human & Nat Sci Ctr, BR-09210580 Santo Andre, SP - Brazil

• Document type: Journal article
• Source: PHARMACEUTICS; v. 13, n. 11 NOV 2021.
• Web of Science Citations: 1

Abstract

Recent advances have been reported for needle-free local anesthesia in maxillary teeth by administering a nasal spray of tetracaine (TTC) and oxymetazoline, without causing pain, fear, and stress. This work aimed to assess whether a TTC-loaded hybrid system could reduce cytotoxicity, promote sustained permeation, and increase the anesthetic efficacy of TTC for safe, effective, painless, and prolonged analgesia of the maxillary teeth in dental procedures. The hybrid system based on TTC (4%) encapsulated in nanostructured lipid carriers (NLC) and incorporated into a thermoreversible hydrogel of poloxamer 407 (TTCNLC-HG4%) displayed desirable rheological, mechanical, and mucoadhesive properties for topical application in the nasal cavity. Compared to control formulations, the use of TTCNLC-HG4% slowed in vitro permeation of the anesthetic across the nasal mucosa, maintained cytotoxicity against neuroblastoma cells, and provided a three-fold increase in analgesia duration, as observed using the tail-flick test in mice. The results obtained here open up perspectives for future clinical evaluation of the thermoreversible hybrid hydrogel, which contains TTC-loaded NLC, with the aim of creating an effective, topical, intranasal, needle-free anesthesia for use in dentistry. (AU)

• FAPESP's process: 18/25920-9 - Thermoreversible hydrogel containing tetracaine loaded in nanostructured lipid carriers for topical intranasal delivery
• Grantee: Bruno Vilela Muniz
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 19/07245-5 - Lidocaine and epinephrine co-loaded mucoadhesive liquid crystal precursor systems as a strategy for topical anesthesia in the buccal cavity
• Grantee: Giovana Maria Fioramonti Calixto Balian
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 14/14457-5 - Lipid-based nanocarriers (SLN/NLC and remote-loading liposomes) used to improve the upload and potency of local anesthetics
• Grantee: Eneida de Paula
• Support Opportunities: Research Projects - Thematic Grants