Abstract The therapeutic applications of curcumin, a phenolic compound extracted from Curcuma species, is limited due to poor bioavailability. To enhance the bioavailability, self-microemulsifying drug delivery systems (SMEDDS) with curcumin were prepared. Ethyl oleate, Tween 80, and Transcutol® P with surfactant: co-surfactant ratio of 2:1 w/w was selected based on the solubility and pseudo-ternary phase diagrams. The optimized formulation (S-Eo3) was evaluated for use of spice oleoresins as curcumin bioenhancers. The oleophilic phase of curcumin containing SMEDDS formulations was then successfully modified by using bioactive oleoresins extracted from two Curcuma species, viz. C. longa (S-CL1) and C. aromatica (S-CA1). The curcumin content in S-Eo3, S-CL1, and S-CA1 were 69.6 ± 0.23, 82.4 ± 0.62, and 88.8 ± 0.46 mg/g, respectively. Thus, by the partial modification of oleophilic phase of SMEDDS with spice oleoresin (acting as bioenhancer) resulted in ∼88 k improvement of curcumin aqueous solubility. The pharmacokinetic study in male Wistar rats showed that the relative bioavailability of curcumin in S-CL1 and S-CA1 were 26- and 29-fold vis-à-vis 22-fold in S-Eo3 compared to curcumin suspension. All the SMEDDS formulations were stable for three months as established by ICH guidelines.

中文翻译：

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使用姜黄树脂增强负载姜黄素的自微乳化脂质载体的负载和口服生物利用度

摘要 姜黄素是一种从姜黄属植物中提取的酚类化合物，由于生物利用度差，其治疗应用受到限制。为了提高生物利用度，制备了含有姜黄素的自微乳化给药系统（SMEDDS）。根据溶解度和假三元相图选择油酸乙酯、吐温 80 和 Transcutol® P，表面活性剂：助表面活性剂的比例为 2:1 w/w。使用香料油树脂作为姜黄素生物增强剂对优化的配方 (S-Eo3) 进行了评估。然后通过使用从两种姜黄属植物中提取的生物活性油树脂成功地修饰了含有姜黄素的 SMEDDS 制剂的亲油相，即。C. longa (S-CL1) 和 C.aromatica (S-CA1)。S-Eo3、S-CL1 和 S-CA1 中的姜黄素含量分别为 69.6 ± 0.23、82.4 ± 0.62 和 88.8 ± 0.46 mg/g。因此，通过用香料油树脂（作为生物增强剂）对 SMEDDS 的亲油相进行部分改性，姜黄素的水溶性提高了约 88 k。雄性 Wistar 大鼠的药代动力学研究表明，与姜黄素悬浮液相比，S-CL1 和 S-CA1 中姜黄素的相对生物利用度分别是 S-Eo3 中的 22 倍和 26 倍。根据 ICH 指南的规定，所有 SMEDDS 制剂在三个月内都是稳定的。