Use of surfactant-based amorphous solid dispersions for BDDCS class II drugs to enhance oral bioavailability: A case report of resveratrol

This paper aimed to improve in vitro dissolution/solubility as well as inhibit intestinal metabolism and thus enhance oral bioavailability for a BDDCS class II drug by constructing surfactant-based amorphous solid dispersions using resveratrol (RES) as a model drug. After preliminary screening of polymers and surfactants, and subsequent prescription optimization, two optimized spray-drying RES-polymer-surfactant ASDs were obtained and exhibited a significant increase in solubility of RES by 2.69–3.45-fold compared to crystalline RES, and by 1.13–1.56-fold compared to corresponding RES-polymer ASDs, maintaining a higher concentration in the dissolution process.

A metabolism study using everted sacs showed that two optimized ASDs reduced the concentration ratio of RES-G to RES to 51.66%–52.05% of crystalline RES on the serosal side of the rat everted intestinal sac at 2 h. Consequently, these two RES-polymer-surfactant ASDs achieved significantly higher exposure of RES in the plasma with significant enhancements in Cmax (2.33–2.35-fold higher than crystalline RES, and 1.72–2.04-fold higher than corresponding RES-polymer ASDs), and in AUC 0–∞ (3.51–3.56-fold higher than crystalline RES, and 1.38–1.41-fold higher than corresponding RES-polymer ASDs).

These advantages of the RES-polymer-surfactant ASDs in oral absorption of RES were attributed to solubilization by ASDs and metabolic inhibition by UGT inhibitors. The introduction of surfactants including EL and Lab to ASDs plays an important role in inhibiting glucuronidation and further improving solubility. This study demonstrated that such surfactant-based amorphous solid dispersions may serve as a new approach to increase the oral absorption of BDDCS class II drugs.

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Resveratrol (RES, purity > 99%), caprylcaproyl macrogol glycerides (Labrasol, Lab), uridine-diphosphate glucuronic acid trisodium salt (UDPGA), D-glucaric acid 1,4-lactone, polyethoxylated castor oil (Cremophor EL, EL), polyoxyl hydrogenated 40 castor oil (Cremophor RH40, RH40) and polyoxyethylene 80 (Tween 80, TW-80) were obtained from Shanghai Yuanye Bio-Technology Co., Ltd. (Shanghai, China). Resveratrol 3-O-glucuronide (RES-G, purity > 99%) was purchased from Shanghai Zzbio Co., Ltd.

Xiaoshun Jia, Jinfeng Chen, Hongqing Cheng, Xinxin Pan, Yixin Ke, Tingming Fu, Hongzhi Qiao, Xiaobing Cui, Wen Li, Lisi Zou, Jianming Cheng, Junsong Li, Use of surfactant-based amorphous solid dispersions for BDDCS class II drugs to enhance oral bioavailability: A case report of resveratrol, International Journal of Pharmaceutics, 2023, 123059, ISSN 0378-5173,

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