Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.
Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.
Int J Pharm. 2019 May 1;562:124-134. doi: 10.1016/j.ijpharm.2019.03.038. Epub 2019 Mar 18.
Curcumin is a natural active constituent of Curcuma longa from Zingiberaceae family that shows many different pharmacological effects such as anticancer, antioxidant, anti-inflammatory, antimicrobial and antiviral effect. However, its bioavailability is profoundly limited by its poor water solubility. In this study antisolvent crystallization followed by freeze drying was used for the preparation of curcumin nanoparticles. The presence of different ratios of hydrophilic polymers (poloxamer 188 & soluplus) on physicochemical properties of curcumin nanoparticles was also investigated. In addition, the effect of high pressure homogenization (HPH) on solubility and dissolution properties of curcumin was investigated. All nanoparticle formulations were examined to determine their particle size distribution, saturation solubility, morphology (SEM), solid state (DSC, XRPD and FT-IR) and dissolution behavior. It was observed that curcumin crystallized in the presence of polymers exhibited better solubility and dissolution rate in comparison with original curcumin. The results showed that the concentration of the stabilizer and the method used to prepare nanoparticles can control the dissolution of curcumin. The crystallized nanoparticles showed polymorph 2 curcumin with lower crystallinity and higher dissolution rate. Curcumin nanoparticles containing 50% soluplus prepared via HPH method presented 16-fold higher solubility than its original form. In conclusion, samples crystalized and proceed with HPH technique showed smaller particle size, better re-dispersibility, higher solubility and dissolution rate in water compared with a sample prepared using a simple antisolvent crystallization process.
姜黄素是姜科姜黄属植物姜黄的一种天然活性成分，具有多种不同的药理作用，如抗癌、抗氧化、抗炎、抗菌和抗病毒作用。然而，其生物利用度受到其较差的水溶性的极大限制。在这项研究中，反溶剂结晶后再冷冻干燥被用于制备姜黄素纳米粒子。还研究了不同比例的亲水性聚合物（泊洛沙姆 188 和 Soluplus）对姜黄素纳米粒子理化性质的影响。此外，还研究了高压均质（HPH）对姜黄素溶解度和溶解性能的影响。所有纳米粒子制剂都进行了检查，以确定它们的粒径分布、饱和溶解度、形态（SEM）、固态（DSC、XRPD 和 FT-IR）和溶解行为。结果表明，在聚合物存在下结晶的姜黄素与原姜黄素相比表现出更好的溶解度和溶解速率。结果表明，稳定剂的浓度和制备纳米粒子的方法可以控制姜黄素的溶解。结晶纳米粒子显示出具有较低结晶度和更高溶解速率的 2 型姜黄素。通过 HPH 法制备的含有 50% Soluplus 的姜黄素纳米粒子的溶解度比其原形式高 16 倍。总之，与仅通过反溶剂结晶工艺制备的样品相比，经过结晶和 HPH 技术处理的样品在水中的粒径更小、再分散性更好、溶解度和溶解速率更高。
