초록 |
Folic Acid (FA) is one of most widely utilized targeting ligands for drug delivery systems (DDS) through binding with folate receptors (FRs). Since FRs are overexpressed on various tumor cells, active targeting of FRs and intracellular delivery of genetic materials such as pDNA and small interfering RNA (siRNA) have been investigated for many years. However, many studies revealed that the endosomal releasing was critical bottleneck for FA-mediated DDS requiring additional use of the endosomal releasing agents. In this study, we have synthesized various endolytic FA with various amine containing linkers. Targeting and effective gene silencing of FA-siRNA conjugates with an endolytic property have been verified in the green fluorescence protein (GFP) expressing KB cells. |