Key result
CAM/DOX-PEGylated liposomes significantly reduced the IC50 value to 0.13 µM compared to free DOX (0.21 µM) against MCF-7 breast cancer cells.
Why the study?
Doxorubicin effectiveness in breast cancer is often diminished by resistance mechanisms, particularly P-glycoprotein-mediated drug efflux, which clarithromycin might counter.
Absolute Event Rate: 0.13% vs 0.21%
Co-encapsulation of clarithromycin and doxorubicin in PEGylated liposomes enhances doxorubicin cytotoxicity against MCF-7 breast cancer cells in vitro.
Clarithromycin may potentiate doxorubicin in resistant MCF-7 cells in vitro; hypothesis-generating and requires in vivo validation before any clinical consideration.
Background Doxorubicin (DOX) is a potent chemotherapeutic agent for breast cancer, but its effectiveness is often diminished by resistance mechanisms, particularly through p-glycoprotein (P-gp) mediated drug efflux. Clarithromycin (CAM), a macrolide antibiotic, inhibits multiple metabolic pathways including CYP3A and P-gp, potentially countering DOX resistance. Objective This study aimed to evaluate the potentiation of DOX and its effectiveness against the MCF-7 breast cancer cell line by encapsulating both DOX and CAM in PEGylated liposomes. Methods PEGylated liposomes containing DOX and CAM were prepared using the thin film hydration method. The physicochemical properties of the liposomes, including average particle size, polydispersity index (PDI), and zeta potential, were characterized. Encapsulation efficiencies for CAM and DOX were assessed, and stability of the liposomes was evaluated over 9 days at room temperature. Cell viability was measured using an IC 50 assay, and P-gp expression levels were determined by ELISA. Results The CAM/DOX-PEGylated liposomes exhibited optimal average particle size (238 ± 26.7 nm), PDI (0.29 ± 0.107), and zeta potential (−20.9 ± 2.17 mV). These liposomes maintained good stability regarding size and charge over 9 days. Encapsulation efficiencies were 81.05% for CAM and 78.13% for DOX. The IC50 value for CAM/DOX-PEGylated liposomes was 0.13 µM, representing a significant reduction compared to the physical mixture of CAM and DOX (0.25 µM) and free DOX (0.21 µM) against MCF-7 cells. ELISA analysis showed a reduction in P-gp expression of approximately 5% with CAM/DOX-PEGylated liposomes compared to 1.61% with free DOX. Conclusion The results indicate that CAM encapsulated in PEGylated liposomes enhances the effectiveness of DOX against breast cancer cells, likely through the inhibition of p-glycoprotein. This approach may offer a promising strategy to overcome DOX resistance and improve chemotherapy outcomes.
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Alfreahat et al. (2025) studied Breast cancer (MCF-7 cell line). CAM/DOX-PEGylated liposomes vs. Free DOX and physical mixture of CAM and DOX was evaluated on IC50 value against MCF-7 cells. CAM/DOX-PEGylated liposomes significantly reduced the IC50 value to 0.13 µM compared to free DOX (0.21 µM) against MCF-7 breast cancer cells.
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