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. 2021 Mar 7;26(5):1455.
doi: 10.3390/molecules26051455.

In Vitro Cytotoxic Protective Effect of Alginate-Encapsulated Capsaicin Might Improve Skin Side Effects Associated with the Topical Application of Capsaicin

Ariana Hudita  1 , Bianca Galateanu  1 , Marieta Costache  1 , Carolina Negrei  2 , Rodica-Mariana Ion  3 , Lorena Iancu  3 , Octav Ginghina  4   5
Affiliations

In Vitro Cytotoxic Protective Effect of Alginate-Encapsulated Capsaicin Might Improve Skin Side Effects Associated with the Topical Application of Capsaicin

Ariana Hudita et al. Molecules. .

Abstract

Chronic neuropathic pain, particularly peripheral pain, is a cause of great concern for diabetic patients. Current treatments include numerous agents such as capsaicinoids, a known deterrent of neuropathic pain despite the inconvenience associated with local side effects. In this context, the current work aims to elucidate the potential mechanisms involved in cytotoxicity by capsaicin and proposes an efficient formulation of capsaicin in alginate microcapsules, which significantly reduces side effects from capsaicin topical administration. For this, human dermal fibroblast cells were treated with alginate-microencapsulated capsaicin extracts and screened for potential cytotoxic effects produced by the treatment. Cell viability and morphology were examined, as well as oxidative stress status and anti-inflammatory potential. Our results show that the alginate encapsulated formulation of capsaicin exerted lower cytotoxic effects on human dermal fibroblasts as measured by cell viability and reactive oxygen species (ROS) production. Furthermore, the expression profiles of inflammatory cytokines were significantly altered by the treatment as compared with the control culture.

Keywords: alginate encapsulation; capsaicin; cytotoxicity; inflammation; neuropathic pain.

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Conflict of interest statement

The authors declare no conflict of interest. The funders had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, or in the decision to publish the results.

Figures

Figure 1
Figure 1
Microscopy image of alginate microcapsules loaded with capsaicin.
Figure 2
Figure 2
Measurement of cell viability after 24 h of exposure to different treatments as revealed by MTT assay (*** p ≤ 0.001 treated vs. control; **** p ≤ 0.0001 treated vs. control).
Figure 3
Figure 3
Quantification of LDH release after 24 h of exposure to different experimental conditions (** p ≤ 0.01 treated vs. control; **** p ≤ 0.0001 treated vs. control).
Figure 4
Figure 4
Fluorescence micrographs of live/dead stained CCD-1070Sk cells after 24 h exposure to different solutions of capsaicin and various extracts collected from simple AM or capsaicin-loaded AM (green fluorescence: live cells; red fluorescence: dead cells).
Figure 5
Figure 5
CCD-1070Sk cell morphology after 24 h of exposure to 5.88 × 10−3 M capsaicin, AM extract, and 5.88 × 10−3 M capsaicin AM extract as revealed by phalloidin staining of actin filaments (green). Cellular nuclei are stained with 2-(4-amidinophenyl)-1H-indole-6-carboxamidine (DAPI) (blue).
Figure 6
Figure 6
Effects of capsaicin and microencapsulated capsaicin treatment on ROS production after 6 h and 24 h of treatment in CCD-1070Sk cells as revealed by the ROS–Glo H2O2 assay. (**** p ≤ 0.001 treated vs. control).
Figure 7
Figure 7
Effects of capsaicin and microencapsulated capsaicin treatment on NO production after 1 h, 3 h, 6 h, and 24 h of treatment in LPS-stimulated RAW 264.7 cells as revealed by Griess reagent assay (**** p ≤ 0.0001 treated vs. control).
Figure 8
Figure 8
Effects of capsaicin and microencapsulated capsaicin treatment on IL-1β, IL-6, IL-10, IL-12p70, MCP-1, MIP-1α, RANTES, and TNF-α production after 3 h and 24 h of treatment in LPS-stimulated RAW 264.7 cells (* p ≤ 0.05 treated vs. control; ** p ≤ 0.01 treated vs. control; *** p ≤ 0.001 treated vs. control; **** p ≤ 0.0001 treated vs. control).
Figure 9
Figure 9
The chemical structure of capsaicin (CAS No.: 404-86-4).
See this image and copyright information in PMC

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