Hsu Wen-Chan, Ng Lean-Teik, Wu Tzu-Hui, Lin Liang-Tzung, Yen Feng-Lin, Lin Chun-Ching
School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
J Nanosci Nanotechnol. 2012 Mar;12(3):2022-7. doi: 10.1166/jnn.2012.5173.
Silymarin, a well known hepatoprotective drug, has been routinely used in treating liver disorders. However, its bioavailability and therapeutic efficiency are limited by the poor aqueous solubility. In this study, we used the nanoprecipitation technique to develop a nanoparticles system to improve the solubility of silymarin. The newly developed silymarin nanoparticles were characterized for mean particle size, morphology, intermolecular interaction, crystalline features and dissolution property, as well as assessing for antioxidant activities. Results indicated that a drastic change in the physiochemical properties of silymarin was noted in the form of nanoparticles, as displayed by the extremely small particle size (46.1 +/- 1.73 nm), the formation of intermolecular hydrogen bonding between silymarin and matrix of nanoparticles, and the rendering of amorphous state. These phenomena have contributed to the enhanced dissolution property of silymarin nanoparticles, as well as a greater potency in DPPH radical scavenging, anti-superoxide anion formation, and superoxide anion scavenging activities than the crude silymarin. The present study concludes that silymarin nanoparticles have an improved physicochemical property as demonstrated by an increased solubility and enhanced antioxidant activities.
水飞蓟素是一种著名的保肝药物,一直被常规用于治疗肝脏疾病。然而,其生物利用度和治疗效果受到水溶性差的限制。在本研究中,我们采用纳米沉淀技术开发了一种纳米颗粒系统,以提高水飞蓟素的溶解度。对新开发的水飞蓟素纳米颗粒进行了平均粒径、形态、分子间相互作用、晶体特征和溶解性能的表征,并评估了其抗氧化活性。结果表明,水飞蓟素以纳米颗粒的形式呈现出理化性质的剧烈变化,表现为粒径极小(46.1±1.73 nm)、水飞蓟素与纳米颗粒基质之间形成分子间氢键以及呈现无定形状态。这些现象有助于提高水飞蓟素纳米颗粒的溶解性能,并且在清除DPPH自由基、抗超氧阴离子形成和超氧阴离子清除活性方面比粗水飞蓟素具有更高的效力。本研究得出结论,水飞蓟素纳米颗粒具有改善的理化性质,表现为溶解度增加和抗氧化活性增强。