Key Laboratory of Functional Polymer Materials, Ministry of Education, Institute of Polymer Chemistry, Nankai University, Tianjin, 300071, People's Republic of China.
J Mater Sci Mater Med. 2012 Jul;23(7):1663-74. doi: 10.1007/s10856-012-4627-1. Epub 2012 Apr 27.
Four types of doxorubicin (DOX)-loaded polymeric micelles based on hydrophobically-modified sulfated chitosan (SCTS) were prepared. The hydrophobic group was composed of glycyrrhetinic acid (GA), cholic acid, stearic acid (SA) or lauric aldehyde. DOX encapsulation depended on several parameters, including the degree of substitution of the sulfate group and the hydrophobic group, and the type of hydrophobic group. Of these micelles, GA-SCTS micelles had the best capability to solubilize DOX. In addition, GA-SCTS micelles had the ability to target HepG(2) cells, and the IC50 for DOX-loaded GA-SCTS micelles was 54.7 ng/mL, which was much lower than that of the other micelles. Further studies on the DOX-loaded GA-SCTS micelles showed that they were stable in salt and protein solutions, in cell culture media, and during long-term storage (6 months). Based on these results, these micelles may be a promising DOX-encapsulated formulation, particularly, GA-SCTS as a potential vehicle for liver-targeted delivery.
四种基于疏水改性硫酸化壳聚糖（SCTS）的阿霉素（DOX）载药聚合物胶束被制备。疏水性基团由甘草次酸（GA）、胆酸、硬脂酸（SA）或十二醛组成。DOX 的包封取决于几个参数，包括硫酸根和疏水性基团的取代度以及疏水性基团的类型。在这些胶束中，GA-SCTS 胶束具有最好的 DOX 增溶能力。此外，GA-SCTS 胶束具有靶向 HepG(2)细胞的能力，载 DOX 的 GA-SCTS 胶束的 IC50 为 54.7ng/mL，明显低于其他胶束。对载 DOX 的 GA-SCTS 胶束的进一步研究表明，它们在盐和蛋白质溶液、细胞培养基中和长期储存（6 个月）中均稳定。基于这些结果，这些胶束可能是一种有前途的 DOX 包封制剂，特别是 GA-SCTS 作为肝靶向递药的潜在载体。
