SN-38 is a chemotherapeutic compound with potent antitumor effects. However, its 9 clinical application is currently limited due to its poor solubility and low stability at physiological 10 pH. Liposomes and cyclodextrins have been long studied for the solubilization and delivery of 11 hydrophobic compounds. Aiming to combine the advantages from both systems, we attempted 12 to develop an SN-38-in-cyclodextrin-in-liposome formulation. We found that the encapsulation 13 of SN-38-SBE-β-CD inclusion complexes in the lumen of liposomes was not possible, owing to 14 the disassembly of liposomes and the formation of lipid nanoparticles, as revealed by size 15 exclusion chromatography and single nanoparticle fluorescence microscopy. Interestingly, the 16 retention time of SN-38 inside SN-38-SBE-β-CD-lipid nanoparticles is higher than in liposomes, 17 whereby SN-38 was directly loaded into the lipid film. The toxicity of purified SN-38-SBE-β-CD-18 lipid nanoparticles was assayed in cultured cancer cells, showing no therapeutic advantage 19 compared to bulk SN-38-SBE-β-CD complexes. Further formulation optimization, in particular an 20 increased concentration of the nanoparticles, will be necessary to obtain cytotoxicity effects. 21 Moreover, the results highlight the value of fluorescence imaging of single, surface-immobilized 22 nanoparticles, in the development of liposomal delivery systems such as drug-in-cyclodextrin-23 in-liposomes. 24
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