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Hybrid Hydrogel Composed of Polymeric Nanocapsules Co-Loading Lidocaine and Prilocaine for Topical Intraoral Anesthesia.
Sci Rep 2018; 8(1):17972SR

Abstract

This study reports the development of nanostructured hydrogels for the sustained release of the eutectic mixture of lidocaine and prilocaine (both at 2.5%) for intraoral topical use. The local anesthetics, free or encapsulated in poly(ε-caprolactone) nanocapsules, were incorporated into CARBOPOL hydrogel. The nanoparticle suspensions were characterized in vitro in terms of particle size, polydispersity, and surface charge, using dynamic light scattering measurements. The nanoparticle concentrations were determined by nanoparticle tracking analysis. Evaluation was made of physicochemical stability, structural features, encapsulation efficiency, and in vitro release kinetics. The CARBOPOL hydrogels were submitted to rheological, accelerated stability, and in vitro release tests, as well as determination of mechanical and mucoadhesive properties, in vitro cytotoxicity towards FGH and HaCaT cells, and in vitro permeation across buccal and palatal mucosa. Anesthetic efficacy was evaluated using Wistar rats. Nanocapsules were successfully developed that presented desirable physicochemical properties and a sustained release profile. The hydrogel formulations were stable for up to 6 months under critical conditions and exhibited non-Newtonian pseudoplastic flows, satisfactory mucoadhesive strength, non-cytotoxicity, and slow permeation across oral mucosa. In vivo assays revealed higher anesthetic efficacy in tail-flick tests, compared to a commercially available product. In conclusion, the proposed hydrogel has potential for provision of effective and longer-lasting superficial anesthesia at oral mucosa during medical and dental procedures. These results open perspectives for future clinical trials.

Authors+Show Affiliations

Department of Physiological Sciences, Piracicaba Dental School, University of Campinas - UNICAMP, Piracicaba, São Paulo, Brazil.São Paulo State University - UNESP, Institute of Science and Technology of Sorocaba, Department of Environmental Engineering, Sorocaba, São Paulo, Brazil.Department of Physiological Sciences, Piracicaba Dental School, University of Campinas - UNICAMP, Piracicaba, São Paulo, Brazil.Department of Physiological Sciences, Piracicaba Dental School, University of Campinas - UNICAMP, Piracicaba, São Paulo, Brazil.Department of Physiological Sciences, Piracicaba Dental School, University of Campinas - UNICAMP, Piracicaba, São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil.Department of Physiological Sciences, Piracicaba Dental School, University of Campinas - UNICAMP, Piracicaba, São Paulo, Brazil.Department of Physiological Sciences, Piracicaba Dental School, University of Campinas - UNICAMP, Piracicaba, São Paulo, Brazil.São Paulo State University - UNESP, Institute of Science and Technology of Sorocaba, Department of Environmental Engineering, Sorocaba, São Paulo, Brazil.Department of Physiological Sciences, Piracicaba Dental School, University of Campinas - UNICAMP, Piracicaba, São Paulo, Brazil. michelle@fop.unicamp.br.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

30568251

Citation

Muniz, Bruno Vilela, et al. "Hybrid Hydrogel Composed of Polymeric Nanocapsules Co-Loading Lidocaine and Prilocaine for Topical Intraoral Anesthesia." Scientific Reports, vol. 8, no. 1, 2018, p. 17972.
Muniz BV, Baratelli D, Di Carla S, et al. Hybrid Hydrogel Composed of Polymeric Nanocapsules Co-Loading Lidocaine and Prilocaine for Topical Intraoral Anesthesia. Sci Rep. 2018;8(1):17972.
Muniz, B. V., Baratelli, D., Di Carla, S., Serpe, L., da Silva, C. B., Guilherme, V. A., ... Franz-Montan, M. (2018). Hybrid Hydrogel Composed of Polymeric Nanocapsules Co-Loading Lidocaine and Prilocaine for Topical Intraoral Anesthesia. Scientific Reports, 8(1), p. 17972. doi:10.1038/s41598-018-36382-4.
Muniz BV, et al. Hybrid Hydrogel Composed of Polymeric Nanocapsules Co-Loading Lidocaine and Prilocaine for Topical Intraoral Anesthesia. Sci Rep. 2018 12 19;8(1):17972. PubMed PMID: 30568251.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Hybrid Hydrogel Composed of Polymeric Nanocapsules Co-Loading Lidocaine and Prilocaine for Topical Intraoral Anesthesia. AU - Muniz,Bruno Vilela, AU - Baratelli,Diego, AU - Di Carla,Stephany, AU - Serpe,Luciano, AU - da Silva,Camila Batista, AU - Guilherme,Viviane Aparecida, AU - Ribeiro,Lígia Nunes de Morais, AU - Cereda,Cintia Maria Saia, AU - de Paula,Eneida, AU - Volpato,Maria Cristina, AU - Groppo,Francisco Carlos, AU - Fraceto,Leonardo Fernandes, AU - Franz-Montan,Michelle, Y1 - 2018/12/19/ PY - 2018/05/31/received PY - 2018/11/15/accepted PY - 2018/12/21/entrez PY - 2018/12/21/pubmed PY - 2019/10/24/medline SP - 17972 EP - 17972 JF - Scientific reports JO - Sci Rep VL - 8 IS - 1 N2 - This study reports the development of nanostructured hydrogels for the sustained release of the eutectic mixture of lidocaine and prilocaine (both at 2.5%) for intraoral topical use. The local anesthetics, free or encapsulated in poly(ε-caprolactone) nanocapsules, were incorporated into CARBOPOL hydrogel. The nanoparticle suspensions were characterized in vitro in terms of particle size, polydispersity, and surface charge, using dynamic light scattering measurements. The nanoparticle concentrations were determined by nanoparticle tracking analysis. Evaluation was made of physicochemical stability, structural features, encapsulation efficiency, and in vitro release kinetics. The CARBOPOL hydrogels were submitted to rheological, accelerated stability, and in vitro release tests, as well as determination of mechanical and mucoadhesive properties, in vitro cytotoxicity towards FGH and HaCaT cells, and in vitro permeation across buccal and palatal mucosa. Anesthetic efficacy was evaluated using Wistar rats. Nanocapsules were successfully developed that presented desirable physicochemical properties and a sustained release profile. The hydrogel formulations were stable for up to 6 months under critical conditions and exhibited non-Newtonian pseudoplastic flows, satisfactory mucoadhesive strength, non-cytotoxicity, and slow permeation across oral mucosa. In vivo assays revealed higher anesthetic efficacy in tail-flick tests, compared to a commercially available product. In conclusion, the proposed hydrogel has potential for provision of effective and longer-lasting superficial anesthesia at oral mucosa during medical and dental procedures. These results open perspectives for future clinical trials. SN - 2045-2322 UR - https://www.unboundmedicine.com/medline/citation/30568251/Hybrid_Hydrogel_Composed_of_Polymeric_Nanocapsules_Co_Loading_Lidocaine_and_Prilocaine_for_Topical_Intraoral_Anesthesia_ L2 - http://dx.doi.org/10.1038/s41598-018-36382-4 DB - PRIME DP - Unbound Medicine ER -