Department of Pharmaceutics, State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing 210009 , PR China.
Faculty of Pharmaceutical Sciences , Government College University Faisalabad , Faisalabad 38040 , Pakistan.
J Agric Food Chem. 2019 Aug 21;67(33):9371-9381. doi: 10.1021/acs.jafc.9b02272. Epub 2019 Aug 13.
A major obstacle to the clinical use of curcumin (CUR) is its reduced bioavailability because of the drug's hydrophobic nature, low intestinal absorption, and rapid metabolism. In this study, a novel oral drug delivery system was constructed for improving the stability and enhancing mucoadhesion of CUR in the gastrointestinal (GI) tract. First, CUR was encapsulated in the bovine serum albumin nanoparticles (CUR-BSA-NPs). Then, -acetyl cysteine (NAC)-modified CUR-BSA-NPs (CUR-NBSA-NPs) were obtained. The average particle size and zeta potential of CUR-NBSA-NPs were 251.6 nm and -30.66 mV, respectively; encapsulation efficiency and drug loading were 85.79 and 10.9%, respectively. CUR-NBSA-NPs exhibited a sustained release property and prominently enhanced stability in simulated GI conditions. Additionally, enhanced mucoadhesion of CUR-NBSA-NPs was also observed. An MTT study showed that the CUR-NBSA-NPs were safe for oral administration. Overall, NAC-modified BSA-NPs may potentially serve as an oral vehicle for improving CUR stability in the GI tract and enhancing mucoadhesion.
姜黄素（CUR）的疏水性、低肠道吸收和快速代谢使其生物利用度降低，这是其临床应用的主要障碍。在这项研究中，构建了一种新型口服药物传递系统，以提高 CUR 在胃肠道（GI）中的稳定性和增强其粘膜粘附性。首先，将 CUR 包封在牛血清白蛋白纳米粒（CUR-BSA-NPs）中。然后，获得了 -乙酰半胱氨酸（NAC）修饰的 CUR-BSA-NPs（CUR-NBSA-NPs）。CUR-NBSA-NPs 的平均粒径和 Zeta 电位分别为 251.6nm 和-30.66mV；包封效率和载药量分别为 85.79%和 10.9%。CUR-NBSA-NPs 表现出持续释放特性，并在模拟 GI 条件下显著提高了稳定性。此外，还观察到 CUR-NBSA-NPs 增强的粘膜粘附性。MTT 研究表明，CUR-NBSA-NPs 口服给药安全。总的来说，NAC 修饰的 BSA-NPs 可能作为一种口服载体，提高 CUR 在 GI 道中的稳定性并增强其粘膜粘附性。
