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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

The effect of two drug delivery systems in ropivacaine cytotoxicity and cytokine release by human keratinocytes and fibroblasts

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Author(s):
Nunes Ferreira, Luiz Eduardo ; Muniz, Bruno Vilela ; Burga-Sanchez, Jonny ; Volpato, Maria Cristina ; de Paula, Eneida ; Ribeiro Rosa, Edvaldo Antonio ; Groppo, Francisco Carlos
Total Authors: 7
Document type: Journal article
Source: Journal of Pharmacy and Pharmacology; v. 69, n. 2, p. 161-171, FEB 2017.
Web of Science Citations: 5
Abstract

ObjectivesModified drug delivery systems have been developed to improve pharmacological properties of local anaesthetics. However, the inflammatory potential of these formulations was not investigated. This study compared the in-vitro effects of ropivacaine (ropi) in plain, liposomal (MLV) or 2-hydroxypropyl--cyclodextrin (HP--CD) formulations on cell viability, apoptosis and cytokine (IL-1, TNF-, IL-6 and IL-10) release. MethodsHuman immortalized keratinocytes (HaCaT) and human immortalized gingival fibroblasts (HGF) were exposed to 1-100m ropi concentrations. The cell viability was measured by XTT and LIVE/DEAD assay. Apoptosis was performed by flow cytometry, and cytokine release was measured by ELISA assay. Key findingsHuman immortalized keratinocyte viability was reduced by ropi and both drug delivery systems. However, none of the formulations induced apoptosis. Results showed a differential regulation of IL-1 TNF-, IL-6 and IL-10 by HaCaT and HGF. Ropi-HP--CD increased twofold the IL-6 release by HGF in comparison with the control, while 100m ropi-MLV led to an increased release of all pro-inflammatory cytokines by HGF. ConclusionThe loss in cell viability was not related to cellular apoptosis. Ropi complexed with HP--CD showed a similar cytokine release pattern when compared to the plain formulation. Thus, the HP--CD form was a better drug carrier than the MLV form for ropivacaine drug delivery. (AU)

FAPESP's process: 12/07310-2 - Modulatory effects of local anesthetics associated with carriers on the production of inflammatory mediators and cell viability in oral epithelial cells and human gingival fibroblasts
Grantee:Francisco Carlos Groppo
Support Opportunities: Regular Research Grants
FAPESP's process: 11/12666-8 - Effects of local anesthetic associated with carriers in the modulation of inflammatory mediators, cell viability and apoptosis induction
Grantee:Luiz Eduardo Nunes Ferreira
Support Opportunities: Scholarships in Brazil - Doctorate (Direct)