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Topotecan (TPT), a potent anticancer agent, suffers from rapid hydrolysis of its active lactone ring under physiological conditions, severely limiting its clinical efficacy. To address this challenge, it was developed a novel pH-responsive, magnetic drug delivery system integrating β-cyclodextrin-functionalized Fe3O4 nanoparticles (Fe3O4@β-CD) and liposomes. Fe3O4@β-CD nanoparticles were synthesized via chemical co-precipitation and then loaded with TPT via host-guest complexation. The resulting Fe3O4@β-CD@TPT complexes were encapsulated into liposomes using the sonication method to increase drug stability, maintain the stable lactone form, and achieve controlled release.
In vitro drug release studies demonstrated a diffusion-controlled release profile, while the pH responsiveness of the system was primarily governed by pH-dependent drug stabilization and loading efficiency rather than pronounced differences in release kinetics. Cytotoxicity assays against MCF-7 breast cancer cells showed that the Fe3O4@β-CD@TPT@Liposome formulation exhibited significantly lower IC50 values compared to free TPT and Fe3O4@β-CD@TPT complexes. These results highlight the potential of the magnetic cyclodextrin-liposome hybrid platform as an effective strategy for the targeted and controlled delivery of pH-sensitive chemotherapeutics such as topotecan.
Bilsen Tural, Erdal Ertaş, Ali Kuruçay, Burhan Ateş, Servet Tural (2026) pH-responsive magnetic cyclodextrin-liposome nanoplatforms for stabilization and targeted delivery of topotecan. Journal of Drug Delivery Science and Technology 116, 107976. https://doi.org/10.1016/j.jddst.2026.107976.