Novel Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Single Garlic Extract: Bio-accessibility, Cytotoxicity, and Anti-Inflammatory Studies

Abstract

Single garlic has many health benefits in which the active compound content five times higher than regular garlic. However, the utilization of the active compound in single garlic was not optimal due to its lipophilic characteristics, volatility, and low stability in gastrointestinal fluids. Self-Nanoemulsifying Drug Delivery System (SNEDDS) has the potential to control the release rate of the active compounds and lead to increase bioavailability in the digestive tract. The study aimed to formulate SNEDDS for single garlic extract (SGE) to increase its bioaccessibility and anti-inflammatory potentials. SNEDDS-SGE was formulated with Tween-80, PEG-400, canola oil, and SGE. SNEDDS-SGE was characterized by response tests including emulsification time, emulsion pH, and transmittance; morphology and droplet size of SNEDDS using TEM; and SGE stability in SNEDDS was evaluated by in vitro gastrointestinal simulation. The cytotoxicity of SNEDDS-SGE was tested using MTT assay, and its anti-inflammatory potential on IL-1ß expression was assessed by the immunocytochemistry (ICC) method on TIG-1 cells induced by methylglyoxal. Response test data and characterization of SNEDDS-SGE were analyzed descriptively, bioaccessibility data were analyzed by T-test, cytotoxicity test by linear regression, IL-1β and C/EBPα expression data by One-way ANOVA. The results showed that SNEDDS-SGE had a fast emulsification time of 41.913 seconds, a stable pH of 7.56, and a high transmittance percentage of 98.027%. The SNEDDS-SGE droplet has a uniform shape with a size of less than 100 nm. SNEDDS-SGE was able to increase the bioaccessibility of SGE by 89.34% for allicin and 89.31% for alliin, also non-toxic at concentrations below 1000 µg/ml. SNEDDS was able to significantly increase the effect of SGE in suppressing the expression of IL-1ß at all concentrations of SNEDDS-SGE 62.5 µg/ml, 125 µg/ml, and 250 µg/ml with the lowest decreased expression of 44.82 ± 4.30 AU. Our study suggested that SNEDDS has the potential to enhance the biological effects of SGE, as well as being a promising anti-inflammatory agent.