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Targeting Epirubicin Plus Quinacrine Liposomes Modified with DSPE-PEG2000-C(RGDfK) Conjugate for Eliminating Invasive
Abstract:
Recurrence of invasive breast cancer could arise from the residual cancer cells after comprehensive treatment. It is possible that residual invasive cancer cells are capable of forming highly patterned vasculogenic mimicry (VM) channels, leading to relapse and metastasis. In the present study, a new type of targeting epirubicin plus quinacrine liposomes was developed by modifying functional DSPE-PEG2000 with C(RGDfK), a cyclic peptide containing Arg-Gly-Asp. These liposomes could potentially eliminate invasive breast cancer and destroy VM channels. Evaluations were made in human invasive breast cancer cells and their xenografts in nude mice. The results showed that the targeting epirubicin plus quinacrine liposomes could enhance the accumulation and uptake of the drugs in cancer tissues, kill cancer cells directly, activate apoptotic enzymes, destroy the VM channels and downregulate the VM channel-forming marker molecules (EphA2, FAK, PI3K, MMP 9, MMP 14, VE-Cad and HIF-α), thereby exhibiting a strong overall anticancer efficacy. The targeting epirubicin plus quinacrine liposomes provided a promising strategy to treat invasive breast cancer and to prevent the relapse arising from VM channels after chemotherapy.
Insights
Targeted liposomes carrying epirubicin and quinacrine effectively eliminate invasive breast cancer cells and destroy vasculogenic mimicry (VM) channels, preventing cancer recurrence after chemotherapy.
Area of Science:
- Oncology
- Nanomedicine
- Cancer Biology
Background:
- Invasive breast cancer recurrence can stem from residual cancer cells.
- These residual cells may form vasculogenic mimicry (VM) channels, promoting relapse and metastasis.
Purpose of the Study:
- To develop and evaluate novel targeted epirubicin plus quinacrine liposomes.
- To assess their efficacy in eliminating invasive breast cancer and destroying VM channels.
Main Methods:
- Liposomes were functionalized with C(RGDfK) peptide for targeting.
- Evaluations were conducted in human invasive breast cancer cells and xenografts in nude mice.
Main Results:
- Targeted liposomes enhanced drug accumulation and uptake in cancer tissues.
- They directly killed cancer cells, activated apoptotic enzymes, and destroyed VM channels.
- Downregulation of VM channel markers (EphA2, FAK, PI3K, MMP-9, MMP-14, VE-Cad, HIF-α) was observed.
Conclusions:
- Targeted epirubicin plus quinacrine liposomes show strong anticancer efficacy.
- This strategy holds promise for treating invasive breast cancer and preventing relapse associated with VM channels.
