Yang Rui, Chen Daozhen, Li Mengfei, Miao Fengqin, Liu Peidang, Tang Qiusha
School of Medicine, Southeast University, Nanjing 210009, China.
Department of Obstetrics, Affiliated Wuxi Maternity and Child Health Care Hospital, Nanjing Medical University, Wuxi 214002, Jiangsu Province, China.
Biomed Mater Eng. 2014;24(6):1991-8. doi: 10.3233/BME-141008.
20(s)-ginsenoside Rg3 is extracted from traditional Chinese medicine, red ginseng. However, due to its poor aqueous solubility and low oral bioavailability, the use of 20(s)-Rg3 is limited. This study aimed to explore a method of preparing nano-sized 20(s)-ginsenoside Rg3 particle named 20(s)-ginsenoside Rg3-loaded magnetic human serum albumin nanospheres (20(s)-Rg3/HSAMNP) to change dosage form to improve its aqueous solubility and bioavailability. 20(s)-Rg3/HSAMNP were prepared by the desolvation-crosslinking method. The character of 20(s)-Rg3/HSAMNP was detected. An antiproliferative effect and cell apoptosis rates of 20(s)-Rg3/HSAMNP on human cervical cancer cells were determined by the MTT assay and flow cytometry, respectively. TEM analysis showed that 20(s)-Rg3/HSAMNP were approximately spherical and uniform in size. Thermodynamic testing showed that the corresponding magnetic fluid of a specific concentration rosed to a steady temperature of 42-65○C. Iron content was approximately 3 mg/mL. Drug encapsulation efficiency was approximately 70%. The potential of 20(s)-Rg3/HSAMNP combined with magnetic hyperthermia therapy to inhibit cell growth and induce apoptosis was much more prominent than that of the other groups. A new dosage form of 20(s)-Rg3 was prepared, which effectively induced apoptosis in HeLa cervical cancer cells in vitro when combined with hyperthermia.
20(S)-人参皂苷Rg3是从传统中药红参中提取的。然而,由于其水溶性差和口服生物利用度低,20(S)-Rg3的应用受到限制。本研究旨在探索一种制备纳米级20(S)-人参皂苷Rg3颗粒的方法,即载20(S)-人参皂苷Rg3磁性人血清白蛋白纳米球(20(S)-Rg3/HSAMNP),以改变剂型,提高其水溶性和生物利用度。采用去溶剂交联法制备20(S)-Rg3/HSAMNP。检测20(S)-Rg3/HSAMNP的性质。分别通过MTT法和流式细胞术测定20(S)-Rg3/HSAMNP对人宫颈癌细胞的抗增殖作用和细胞凋亡率。透射电镜分析表明,20(S)-Rg3/HSAMNP近似球形,大小均匀。热力学测试表明,特定浓度的相应磁流体升温至42-65℃的稳定温度。铁含量约为3mg/mL。药物包封率约为70%。20(S)-Rg3/HSAMNP联合磁热疗抑制细胞生长和诱导凋亡的潜力比其他组更为突出。制备了20(S)-Rg3的新剂型,其与热疗联合时可有效诱导体外HeLa宫颈癌细胞凋亡。