Redispersible nanosuspensions as a plausible oral delivery system for curcumin
Redispersible nanosuspensions as a plausible oral delivery system for curcumin
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可再分散纳米混悬剂作为姜黄素的合理口服给药系统
DOI：
10.1016/j.foodhyd.2021.107005
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发表时间：
2021
影响因子：
10.7
通讯作者：
Elbaz N
中科院分区：
文献类型：
--
作者：
Elbaz N
姜黄素被广泛用作食品和饮料产品的营养成分。据报道，姜黄素具有广泛的生物活性，如抗癌、抗炎、抗氧化、抗菌等。尽管姜黄素有很强的治疗作用，但它的低水溶性、稳定性和口服生物利用度限制了它的有效性。为了改善姜黄素的理化性质，我们采用乳化模板冷冻干燥技术，将姜黄素制成纳米悬浮剂。这种方法产生的固体可以根据需要分散，形成纳米悬浮。在使用不同赋形剂的筛选过程中对这些处方进行了研究，结果鉴定了一个仅含有聚乙二醇(PEG)作为赋形剂的姜黄素纳米悬浮液。该制剂具有较小的直径(2 11 Nm)、低的多分散性(0.0 6)和−2 5 mV的zeta电位，因此被选作进一步的体外研究。改变各种实验参数，如活化剂和赋形剂浓度，以及超声作用时间，以调整所选配方的尺寸和多分散性。由此得到的纳米悬浮液在模拟胃肠道的pH值下显示出更好的化学稳定性。Anin体外生物可及性实验表明，纳米混悬剂导致姜黄素的溶出度增加，但这也伴随着稳定性的降低。细胞毒性研究表明，与所研究的两种细胞系上溶解的姜黄素相比，纳米悬浮液提供了更低的细胞毒性曲线。这种可再分散的姜黄素纳米混悬剂可能为姜黄素的口服剂量提供新的机会。
Curcumin is widely used as a nutraceutical ingredient in food and beverage products. It has been reported that curcumin has a broad spectrum of biological activities such as anticancer, anti-inflammatory, antioxidant, and antibacterial effects. Despite the potent therapeutic effect of curcumin, its low aqueous solubility, stability, and oral bioavailability limits its effectiveness. In order to improve the physical and chemical properties of curcumin, we have formulated curcumin as a nanosuspension by using the emulsion templated freeze-drying technique. This approach produces a solid that can be dispersed as required to form a nanosuspension. The formulations were investigated in a screening process using various excipients, resulting in the identification of one curcumin nanosuspension sample which contained only polyethylene glycol (PEG) as the excipient. This formulation exhibited a small diameter (211 nm), low polydispersity (0.06) and zeta potential of −25 mV and was therefore chosen for furtherin vitroinvestigations. Various experimental parameters such as active agent and excipient concentrations, and sonication time were varied to tune the size and polydispersity of the chosen formulation. The resulting nanosuspension showed an improved chemical stability at pH values that mimic the gastrointestinal tract. Anin vitrobioaccessibility experiment showed that the nanosuspension formulation resulted in more dissolution of the curcumin but this was also coupled with reduced stability. Cytotoxicity studies showed that the nanosuspension offered a reduced cytotoxicity profile compared to the solubilised curcumin on both cell lines investigated. This redispersible curcumin nanosuspension formulation may provide new opportunities for the oral dosing of curcumin.
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DOI：
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期刊：
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