Characterization of Articaine-Loaded Poly(epsilon-caprolactone) Nanocapsules and Solid Lipid Nanoparticles in Hydrogels for Topical Formulations

Author(s)

Silva de Melo, Nathalie Ferreira ^[1] ; Ramos Campos, Estefania Vangelie ^[2] ; Franz-Montan, Michelle ^[3] ; de Paula, Eneida ^[4] ; Goncalves da Silva, Camila Morais ^[4] ; Maruyama, Cintia Rodrigues ^[2] ; Stigliani, Tatiane Pasquoto ^[5] ; de Lima, Renata ^[5] ; de Araujo, Daniele Ribeiro ^[6] ; Fraceto, Leonardo Fernandes ^[2]

Affiliation

^[1] Sao Leopoldo Mand Res Inst, Dept Immunol & Mol Biol, BR-13045755 Campinas, SP - Brazil

^[2] Sao Paulo State Univ, Dept Environm Engn, BR-18180000 Sorocaba, SP - Brazil

^[3] Univ Estadual Campinas, Piracicaba Dent Sch, Dept Physiol Sci, BR-13414018 Piracicaba, SP - Brazil

^[4] Univ Estadual Campinas, Dept Biochem, BR-13083862 Campinas, SP - Brazil

^[5] Univ Sorocaba, Dept Biotechnol, BR-18023000 Sorocaba, SP - Brazil

^[6] Fed Univ ABC, BR-09210580 Santo Andre, SP - Brazil

• Document type: Journal article
• Source: Journal of Nanoscience and Nanotechnology; v. 18, n. 6, p. 4428-4438, JUN 2018.
• Web of Science Citations: 9

Abstract

This work describes the development of poly-epsilon-caprolactone nanocapsules (PCL-NC) and solid lipid nanoparticles (SLN) aiming delivery for articaine (ATC), in order to improve its chemical stability in semi-solid preparations looking forward their use for skin delivery. The nanoparticles were characterized by size, polydispersity index, and pH. Cellular viability was evaluated using the MTT test and the in vitro release kinetics was determined using a two-compartment model. The hydrogels with nanoparticle suspensions were characterized considering their rheological aspects and in vitro permeation across artificial membranes. Colloidal stability was satisfactory, since the formulations did not present major alterations during 120 days. High ATC encapsulation was achieved (78% for PCL-NC and 65% for SLN). The release profile of PCL-NC-ATC was slower, compared to the free molecule and SLN-ATC. MTT experiments showed the nanosystems were capable to increase cellular viability compared with free ATC. The hydrogels showed good consistency, homogeneity, and stability and presented pseudoplastic behavior with thixotropy, improving drug efficacy in clinical applications. The gel based on PCL-NC showed faster onset of activity and flux of 35.68 +/- 1.98 mu g/cm(2)/h, which then continued for up to 8 h. This study opens up prospects for employment of nanoparticulate systems for modified release of ATC. (AU)

• FAPESP's process: 10/18529-0 - Modified release systems for local anesthetic articaine aim to odontological applications
• Grantee: Nathalie Ferreira Silva de Melo
• Support Opportunities: Scholarships in Brazil - Doctorate