Department of Pharmaceutical and Fine Chemicals, School of Chemical Engineering, Nanjing University of Science and Technology, Nanjing, People's Republic of China.
Drug Dev Res. 2020 Aug;81(5):585-592. doi: 10.1002/ddr.21657. Epub 2020 Mar 12.
To improve water solubility, reduce phototoxicity and increase the tumor-targeting ability of hematoporphyrin (Hp) as a sonosensitizer for sonodynamic therapy under ultrasonic conditions, a novel folate receptor (FR)-targeted, folate-conjugated ethylenediamine-β-cyclodextrin (FA-EN-β-CD) containing Hp (FA-EN-β-CD-Hp) was constructed. β-Cyclodextrin containing Hp (β-CD-Hp) was also established as a nontargeted control. The inclusion efficiencies of Hp in FA-EN-β-CD-Hp and β-CD-Hp were determined to be 90.4 ± 2.7% (wt/wt) and 92.5 ± 3.4% (wt/wt), respectively. Growth inhibition rates in HepG-2 cells in vitro were assessed upon ultrasound exposure. The results indicated that the growth inhibition rates of FA-EN-β-CD-Hp, β-CD-Hp, and F-Hp (Hp: 150 μg/ml) reached 96.4 ± 3.6%, 53.4 ± 3.4%, and 48.2 ± 2.8%, respectively. These results indicated that FA-EN-β-CD-Hp is a promising drug delivery system in the field of sonodynamic cancer therapy.
为提高血卟啉（Hp）作为声动力学治疗超声条件下的声敏剂的水溶性、降低光毒性和增加肿瘤靶向能力，构建了一种新型叶酸受体（FR）靶向、叶酸偶联的乙二胺-β-环糊精（FA-EN-β-CD）载Hp（FA-EN-β-CD-Hp）。还建立了β-环糊精载Hp（β-CD-Hp）作为非靶向对照。测定了 FA-EN-β-CD-Hp 和β-CD-Hp 中 Hp 的包封效率分别为 90.4 ± 2.7%（wt/wt）和 92.5 ± 3.4%（wt/wt）。体外超声暴露后评估 HepG-2 细胞的生长抑制率。结果表明，FA-EN-β-CD-Hp、β-CD-Hp 和 F-Hp（Hp：150μg/ml）的生长抑制率分别达到 96.4 ± 3.6%、53.4 ± 3.4%和 48.2 ± 2.8%。这些结果表明，FA-EN-β-CD-Hp 是声动力学癌症治疗领域有前途的药物传递系统。
