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CC BY-NC-ND 4.0 · Planta Medica International Open 2021; 8(03): e122-e130
DOI: 10.1055/a-1543-1190
Original Papers

Thymol and Piperine-Loaded Poly(D,L-lactic-co-glycolic acid) Nanoparticles Modulate Inflammatory Mediators and Apoptosis in Murine Macrophages

Jean Paul Dzoyem
1   Department of Biochemistry, Faculty of Science, University of Dschang, Dschang, Cameroon
2   School of Pharmaceutical Sciences, University of Geneva, Geneva, Switzerland
3   Institute of Pharmaceutical Sciences of Western Switzerland, University of Geneva, Geneva, Switzerland
,
Nathalie Boulens
2   School of Pharmaceutical Sciences, University of Geneva, Geneva, Switzerland
3   Institute of Pharmaceutical Sciences of Western Switzerland, University of Geneva, Geneva, Switzerland
,
Eric Allémann
2   School of Pharmaceutical Sciences, University of Geneva, Geneva, Switzerland
3   Institute of Pharmaceutical Sciences of Western Switzerland, University of Geneva, Geneva, Switzerland
,
Florence Delie
2   School of Pharmaceutical Sciences, University of Geneva, Geneva, Switzerland
3   Institute of Pharmaceutical Sciences of Western Switzerland, University of Geneva, Geneva, Switzerland
› Author Affiliations Funding This work was supported by the Swiss National Foundation through the grant project n ° IZSEZO_180383/1 and the Laboratory of Pharmaceutical Technology, Institute of Pharmaceutical Sciences of Western Switzerland, University of Geneva.
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Abstract

This study aimed at preparing and characterizing thymol, eugenol, and piperine-loaded poly(D,L-lactic-co-glycolic acid) nanoparticles and evaluating the effect on inflammatory mediators secretion and apoptosis in Raw 264.7 macrophage cells. Nanoparticles were produced by the solvent evaporation technique. Dynamic light scattering and scanning electron microscopy were used to study the physicochemical characteristics. Raw 264.7 macrophage cells were used as a model for in vitro assays. The 2-(4-iodophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium assay was used to determine the cytotoxicity of the formulated nanoparticles. An annexin V apoptosis detection kit was used to assess apoptosis. Nitric oxide production was determined using the Griess reagent, and the inflammatory mediators level was evaluated with Th1/Th2 cytokine and fluorometric cyclooxygenase kits. The loaded nanoparticles showed a particle size around 190 nm with a low polydispersity between 0.069 and 0.104 and a zeta potential between–1.2 and–9.5 mV. Reduced cytotoxicity of nanoparticles compared to free molecules against Raw 264.7 macrophage cells was observed and seemed to occur through a mechanism associated with apoptosis. A decrease in cyclooxygenase enzyme activity with an increasing concentration was observed. Both free molecules and nanoparticles showed their capacity to modulate the inflammatory process mostly by inhibiting the investigated inflammatory cytokines. The data presented in this study indicate that thymol and piperine-loaded poly(D,L-lactic-co-glycolic acid nanoparticles could serve as a novel anti-inflammatory colloidal drug delivery system with reduced toxicity. However, further study should be considered to optimize the formulation’s loading capacity and thereby probably enhance their bioactivity in treating inflammatory diseases.

Key words

thymol - piperine - nanoparticles - anti-inflammatory activity - cytokines - apoptosis

Supplementary Material



Publication History

Received: 02 March 2021
Received: 08 June 2021

Accepted: 21 June 2021

Article published online:
21 September 2021

© 2021. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution-NonDerivative-NonCommercial-License, permitting copying and reproduction so long as the original work is given appropriate credit. Contents may not be used for commercial purposes, or adapted, remixed, transformed or built upon. (https://creativecommons.org/licenses/by-nc-nd/4.0/).

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