Dual-targeted Dox delivery assessedThe effect of addition of two targeted vectors, cRGD peptide and folic acid, with the same linker length on the properties of the doxorubicin phospholipid composition: a study of properties in vitro.
We investigated the impact of using folate, in conjunction with a specific peptide known as cRGD, in a targeted delivery system for the chemotherapy drug doxorubicin (Dox) in breast cancer treatment. Our approach involved a composition called NPh-Dox-cRGD-Fol(2.0), which effectively combined both targeting agents with the same linker length.
The results revealed that the dual-vector system significantly improved the internalization and accumulation of doxorubicin in breast cancer cells that express the folate receptor as well as integrin αvβ3. In fact, when we compared this dual approach to the single-vector system featuring only folate, the dual composition showed enhanced release rates of the drug in various pH conditions, particularly in acidic environments typical of tumor tissues.
However, it is important to note that we did not isolate the effects of folate alone in this study, which makes it difficult to pinpoint its individual contribution. While the dual-vector system was effective, in experiments with a different breast cancer cell line that expresses only the folate receptor, we noted similar outcomes when using compositions just containing folate. This highlights that while folate can play a role in drug delivery, its exclusive impact could not be firmly established.
We also observed varying results with normal cells, indicating that the targeted compositions did not demonstrate a significant difference in drug uptake compared to free doxorubicin. Ultimately, while we saw encouraging results with the dual-targeted approach, we must clarify that the specific benefits of folate on its own were not conclusively determined from our findings.