Enhanced Antioxidant and Anti-Inflammatory Effects of Self-Nano and Microemulsifying Drug Delivery Systems Containing Curcumin

• Published in: Molecules (Basel, Switzerland) Switzerland), 2022-10, Vol.27 (19), p.6652
• Main Authors: Józsa, Liza, Vasvári, Gábor, Sinka, Dávid, Nemes, Dániel, Ujhelyi, Zoltan, Vecsernyés, Miklós, Váradi, Judit, Fenyvesi, Ferenc, Lekli, István, Gyöngyösi, Alexandra, Bácskay, Ildikó, Fehér, Pálma
• Format: Article
• Language: English
• Subjects: Adenocarcinoma; Analysis; Anti-inflammatory drugs; anti-inflammatory effect; antioxidant effect; Antioxidants; Assaying; Bioavailability; Colorectal cancer; Curcumin; Cytotoxicity; Database industry; Drug delivery; Drug delivery systems; Drug dosages; Drugs; Enzyme-linked immunosorbent assay; Enzymes; Formulations; IL-1β; Inflammation; Interleukin 1; Lipophilic; Mediation; Microemulsions; Nanoparticles; Nonionic surfactants; self-emulsifying systems; Solubility; Superoxide dismutase; Surface active agents; Surfactants; Thermodynamics; Tumor necrosis factor-TNF; Tumor necrosis factor-α; Vehicles
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules27196652

Turmeric has been used for decades for its antioxidant and anti-inflammatory effect, which is due to an active ingredient isolated from the plant, called curcumin. However, the extremely poor water-solubility of curcumin often limits the bioavailability of the drug. The aim of our experimental work was to improve the solubility and thus bioavailability of curcumin by developing self-nano/microemulsifying drug delivery systems (SN/MEDDS). Labrasol and Cremophor RH 40 as nonionic surfactants, Transcutol P as co-surfactant and isopropyl myristate as the oily phase were used during the formulation. The average droplet size of SN/MEDDS containing curcumin was between 32 and 405 nm. It was found that the higher oil content resulted in larger particle size. The drug loading efficiency was between 93.11% and 99.12% and all formulations were thermodynamically stable. The curcumin release was studied at pH 6.8, and the release efficiency ranged between 57.3% and 80.9% after 180 min. The results of the MTT cytotoxicity assay on human keratinocyte cells (HaCaT) and colorectal adenocarcinoma cells (Caco-2) showed that the curcumin-containing preparations were non-cytotoxic at 5 w/v%. According to the results of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide dismutase (SOD) assays, SNEDDS showed significantly higher antioxidant activity. The anti-inflammatory effect of the SN/MEDDS was screened by enzyme-linked immunosorbent assay (ELISA). SNEDDS formulated with Labrasol as surfactant, reduced tumor necrosis factor-alpha (TNF-α) and interleukin-1 beta (IL-1β) levels below 60% at a concentration of 10 w/w%. Our results verified the promising use of SN/MEDDS for the delivery of curcumin. This study demonstrates that the SN/MEDDS could be promising alternatives for the formulation of poorly soluble lipophilic compounds with low bioavailability.