Physicochemical Characterization and <i>In Vitro</i> Dissolution Test of Quercetin-Succinic Acid Co-crystals Prepared Using Solvent Evaporation

Abstract

Objectives: Quercetin is one of the flavonoids with a polyhydroxyaromatic structure. Quercetin has been proposed to exhibit a bioWactivity against oxidative stress. However, quercetin has poor solubility in aqueous media. The purpose of this study was to investigate the physicochemical properties and dissolution rates of quercetin-succinic acid co-crystals. Materials and Methods:The quercetin-succinic acid co-crystals were prepared in 1:1 molar ratio using solvent evaporation. X-ray diffraction, differential thermal analysis, infrared spectroscopy, and scanning electron microscopy were performed to determine the physicochemical properties of quercetin-succinic acid co-crystals. Dissolution was studied in medium citrate buffer with 2% SLS for 60 min using USP II (paddle) apparatus at 100 rpm and 37°C. Results: Based on diffractogram, thermogram, infrared spectrum, and microscopic capture, the physicochemical properties of quercetin-succinic acid co-crystals showed difference to those of quercetin. In addition, the in vitro dissolution test showed that the dissolution profile of co-crystals was significantly higher than pure quercetin. Conclusion: This study suggests that the formation of quercetin-succinic acid co-crystals using solvent evaporation enhanced the physicochemical properties and dissolution rate of quercetin.

Improvement <i>in vitro</i> Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid

“…This is in agreement with previous studies on fluoxetine hydrochloride -L-tartaric acid [7] and artesunatenicotinamide [11]. [2,4] as seen on Fig. 2a.…”

“…The thermogram of Co Qu-Ma showed an endothermic peak at 277.9 °C which is higher when compared to that of Ma and is lower when compared to that of Qu. The shifting of the melting point indicates the possible interaction between components to form cocrystals [2,9,11,14]. One of the parameter used to The appearance of new melting point positioned between the melting points of cocrystals components may clarify the cocrystals formation.…”

“…Quercetin is a flavonoid, which can be found in citrus fruits, tea, onions, apple and berry [1]. These plant substances were also well known as an antioxidant, which prevent the damage made by free radicals [2]. Moreover, it is reported that quercetin exhibits other pharmacological effects such as anticancer, cardio protectant, antibacterial and antiviral activity [2][3][4][5].…”

“…These plant substances were also well known as an antioxidant, which prevent the damage made by free radicals [2]. Moreover, it is reported that quercetin exhibits other pharmacological effects such as anticancer, cardio protectant, antibacterial and antiviral activity [2][3][4][5]. The solubility of quercetin in water is 0.3 µg/mL [3], the bioavailability of quercetin is considered low due to its poor water solubility [2,5].…”

“…Moreover, it is reported that quercetin exhibits other pharmacological effects such as anticancer, cardio protectant, antibacterial and antiviral activity [2][3][4][5]. The solubility of quercetin in water is 0.3 µg/mL [3], the bioavailability of quercetin is considered low due to its poor water solubility [2,5]. In addition, this poor water solubility also limits the dissolution process, which is the rate-limiting step in the absorption process.…”