Rachmawati Heni, Rahma Annisa, Al Shaal Loaye, Müller Rainer H, Keck Cornelia M
Pharmaceutics Research Group, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, Indonesia.
Research Center for Nanosciences and Nanotechnology, Bandung Institute of Technology, Bandung 40132, Indonesia.
Sci Pharm. 2016 Oct 18;84(4):685-693. doi: 10.3390/scipharm84040685.
We have successfully developed curcumin nanosuspension intended for oral delivery. The main purpose is to improve bioavailability through enhancing its solubility. The nanoparticles were stabilized using various stabilizers, including polyvinyl pyrrolidone (PVP), polyvinyl alcohol (PVA), sodium carboxymethylcellulose (Na-CMC), d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), and sodium dodecyl sulfate (SDS). The average diameter of particles, microscopic appearance, and sedimentation of each preparation was observed and compared. Each stabilizer demonstrated a different degree of inhibition of particle aggregation under electrolyte-containing simulated gastrointestinal (GIT) fluid. Non-ionic stabilizers (PVA, PVP, and TPGS) were shown to preserve the nanosuspension stability against electrolytes. In contrast, strong ionic surfactants such as SDS were found to be very sensitive to electrolytes. The results can provide useful information for the formulators to choose the most suitable stabilizers by considering the nature of stabilizers and physiological characteristics of the target site of the drug.
我们已成功开发出用于口服给药的姜黄素纳米混悬液。主要目的是通过提高其溶解度来改善生物利用度。使用包括聚乙烯吡咯烷酮（PVP）、聚乙烯醇（PVA）、羧甲基纤维素钠（Na-CMC）、d-α-生育酚聚乙二醇1000琥珀酸酯（TPGS）和十二烷基硫酸钠（SDS）在内的各种稳定剂使纳米颗粒稳定。观察并比较了每种制剂的颗粒平均直径、微观外观和沉降情况。在含电解质的模拟胃肠（GIT）液中，每种稳定剂对颗粒聚集的抑制程度不同。非离子型稳定剂（PVA、PVP和TPGS）显示出能保持纳米混悬液对电解质的稳定性。相比之下，发现强离子型表面活性剂如SDS对电解质非常敏感。这些结果可为配方设计师通过考虑稳定剂的性质和药物靶部位的生理特性来选择最合适的稳定剂提供有用信息。
