Liu Dandan, Yang Zhiyuan, Lu Yue, Yang Weiwei
School of Biomedical & Chemical Engineering, Liaoning Institute of Science and Technology, Benxi, Liaoning, China.
Health Management Center, Baoji Central Hospital, Baoji, Shaanxi, China.
Pak J Pharm Sci. 2025 May-Jun;38(3):1095-1105.
Low water solubility and poor intestinal permeability hinder the oral absorption of curcumin (CUR). To address this, we designed a core-shell structured nanoparticle based on nanodiamonds (NDs) and thiolated chitosan (TCS). First, D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) covalently modified NDs were prepared and loaded with CUR (CUR@NDs-TPGS). N-acetylcysteine (NAC) was then coupled to chitosan (CS) to obtain positively charged CS-NAC, which electrostatically coated the negatively charged NDs-TPGS/CUR. Particle size (PS), zeta potential (ZP) and drug loading efficiency (DLE) were selected as screening indices to optimize the formulation and preparation process of CUR@NDs-TPGS/CS-NAC via single-factor experiments. The results showed that after coating with CS-NAC, the PS of optimized CUR@NDs-TPGS/CS-NAC increased from 183.63±5.24 nm to 245.24±3.95 nm, the ZP value flipped from -25.47±1.36 to +25.81±1.06 and the DLE value decreased slightly. Moreover, the nanoparticles adopted a spherical morphology and the cumulative release percentage of the nanocomplexes within 24 h decreased from 35.69% to 25.54% after coating. CUR@NDs-TPGS/CS-NAC remained stable within 48 h in simulated intestinal fluid. Mucin adsorption, GI retention and oral absorption of CUR@NDs-TPGS/CS-NAC were further enhanced compared to CUR@NDs-TPGS. These findings suggest that CUR@NDs-TPGS/CS-NAC is a promising carrier for oral delivery of CUR.
低水溶性和较差的肠道通透性阻碍了姜黄素（CUR）的口服吸收。为了解决这个问题，我们设计了一种基于纳米金刚石（NDs）和硫醇化壳聚糖（TCS）的核壳结构纳米颗粒。首先，制备了共价修饰有D-α-生育酚聚乙二醇1000琥珀酸酯（TPGS）的NDs并负载CUR（CUR@NDs-TPGS）。然后将N-乙酰半胱氨酸（NAC）偶联到壳聚糖（CS）上以获得带正电荷的CS-NAC，其通过静电作用包覆带负电荷的NDs-TPGS/CUR。选择粒径（PS）、zeta电位（ZP）和载药效率（DLE）作为筛选指标，通过单因素实验优化CUR@NDs-TPGS/CS-NAC的制剂和制备工艺。结果表明，用CS-NAC包覆后，优化后的CUR@NDs-TPGS/CS-NAC的PS从183.63±5.24 nm增加到245.24±3.95 nm，ZP值从-25.47±1.36变为+25.81±1.06，DLE值略有下降。此外，纳米颗粒呈球形，包覆后纳米复合物在24小时内的累积释放率从35.69%降至25.54%。CUR@NDs-TPGS/CS-NAC在模拟肠液中48小时内保持稳定。与CUR@NDs-TPGS相比，CUR@NDs-TPGS/CS-NAC的粘蛋白吸附、胃肠道滞留和口服吸收进一步增强。这些发现表明，CUR@NDs-TPGS/CS-NAC是一种有前途的CUR口服递送载体。
