Self-Assembling Cyclodextrin-Based Nanoparticles Enhance the Cellular Delivery of Hydrophobic Allicin

Most chemotherapeutics are hydrophobic molecules and need to be converted into hydrophilic formulations before administration. To address this issue, a novel cyclodextrin-based nanoparticle was proposed as a versatile carrier for cellular delivery of hydrophobic molecules. First, the effect of the polylysine (PL)/NH₂-β-cyclodextrin (NH₂-β-CD) ratio on particle size and encapsulation efficiency in prepared complexes was investigated. Subsequently, transmission electron microscopy images showed that the sizes of PL/NH₂-β-CD nanoparticles ranging from 10 to 260 nm decreased with the reduction in the PL/NH₂-β-CD ratio, which was completely consistent with the findings of size distributions. At a PL/NH₂-β-CD ratio of 10, the surface charge on the PL/NH₂-β-CD nanoparticle was maximized at (+52.8 mV), and encapsulation efficiency was optimal (47.2%), which revealed a great advantage in delivery of hydrophobic allicin. In addition, the positive charge of PL chains facilitated the cellular uptake of the PL/NH₂-β-CD-DOX by interacting with the negatively charged cell membrane. Conclusively, this study suggests that the combination of allicin and PL/NH₂-β-CD nanoparticles acting on the S and G2/M phases in cell cycle regulation induces apoptosis and exhibits substantial application in killing cancer cells.