Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, PR China.
Drug Deliv. 2011 Feb;18(2):131-42. doi: 10.3109/10717544.2010.520353. Epub 2010 Oct 12.
The interest in nanosuspensions by the pharmaceutical industry is increasing given several nanosuspension products currently on the market for poorly soluble drugs. In this study, a novel dosage form for curcumin (CUR), CUR nanosuspension (CUR-NS), was successfully prepared by high pressure homogenization to improve CUR's cytotoxicity, as well as improve its application via intravenous injection. Characterization of the CUR-NS was evaluated by morphology, size, zeta potential, solubility, dissolution rate, and crystal state of drug. The nanoparticles for CUR-NS presented a sphere-like shape under transmission electron microscopy with an average diameter of 250.6 nm and the zeta potential of CUR-NS was -27.92 mV. Solubility and dissolution rate of CUR in the form of CUR-NS were significantly increased due to the small particle size and the crystalline state of CUR was preserved to increase its stability against degradation. Superior cytotoxicity in Hela and MCF-7 cells was obtained for CUR-NS compared with CUR solution. The safety evaluation showed that, compared with the CUR solution, CUR-NS provided less local irritation and phlebitis risks, lower rate of erythrocyte hemolysis. These findings suggest that CUR-NS may represent a promising new drug formulation for intravenous administration in the treatment of certain cancers.
鉴于目前市场上有几种用于难溶性药物的纳米混悬剂产品,制药行业对纳米混悬剂的兴趣日益增加。在这项研究中,通过高压匀质成功制备了姜黄素(CUR)的新型剂型——CUR 纳米混悬剂(CUR-NS),以提高 CUR 的细胞毒性,并通过静脉注射改善其应用。通过形态、粒径、Zeta 电位、溶解度、溶出度和药物晶体状态对 CUR-NS 进行了表征。透射电子显微镜下 CUR-NS 的纳米粒子呈球形,平均直径为 250.6nm,CUR-NS 的 Zeta 电位为-27.92mV。由于粒径小,CUR-NS 中 CUR 的溶解度和溶出度显著提高,同时保持了 CUR 的晶体状态,提高了其对降解的稳定性。与 CUR 溶液相比,CUR-NS 在 Hela 和 MCF-7 细胞中表现出更强的细胞毒性。安全性评价表明,与 CUR 溶液相比,CUR-NS 引起局部刺激和静脉炎的风险较低,红细胞溶血率较低。这些发现表明,CUR-NS 可能代表一种有前途的新型静脉给药药物制剂,可用于治疗某些癌症。