การประเมินลักษณะและชีวประสิทธิผลของสูตรตำรับเซลฟ์ไมโครอิมัลซิฟายด์ที่บรรจุเควอซิทินและเรสเวอราทรอล

Abstract

A self-microemulsifying formulation containing quercetin and resveratrol (QR-SME) was developed to overcome the poor oral bioavailability of both compounds. QR-SME consisted of Capryol 90, Cremophor EL and Labrasol in the ratio of 10:70:20 by weight. The optimal formulation was loaded with 20 mg/g of each poor water-soluble compound and showed oil in water emulsion (o/w) droplet size smaller than 20 nanometers, the spherical shape of the particles with no signs of coalescence. More than 70% and 80% of quercetin and resveratrol, respectively, were released within 30 minutes and significantly different (p<0.05) as compared to QR-nonformulated. There was no significant alters in the self-emulsification properties, and particle size under the intermediate and accelerated condition for 12 months. Furthermore, QR-SME formulation exhibited the highest DPPH and ABTS radical scavenging capacities (IC50-1.7±0.04 and 2.95±0.04 mg/mL), and presented the ferric reducing antioxidant power activity (5.76±0.23 mM FeSO4/mg of formulation) significantly different (p<0.05) compared to Blank-SME. Also, QR-SME formulation showed the highest cytotoxicity against AGS, HT-29 and Caco-2 (IC50=48.21±0.42, 38.89±1.20 and 36.17±0.46 μM, respectively) significantly different (p<0.05) compared with Blank-SME. In addition, oral administration of QR-SME formulations in rats presented the level of quercetin and resveratrol in plasma with area under the concentration curve time 0 to 6 hours (AUC0-6 h) for 11.63 and 3.20- fold, respectively, with significant difference (p<0.05) compared with the QR- suspensions. In summary, the results of this study found that a self- microemulsifying formulation containing quercetin and resveratrol can be used to enhance the solubility and oral bioavailability of two poorly water-soluble drugs which are chance to improve the product development and other pharmaceuticals.