Self-Assembling Cyclodextrin-Based Nanoparticles Enhance the Cellular Delivery of Hydrophobic Allicin
Xu Chen, Hongyu Li, Wentao Xu, Kunlun Huang, Baiqiang Zhai, Xiaoyun He
Abstract
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)/NH 2 -β-cyclodextrin (NH 2 -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/NH 2 -β-CD nanoparticles ranging from 10 to 260 nm decreased with the reduction in the PL/NH 2 -β-CD ratio, which was completely consistent with the findings of size distributions. At a PL/NH 2 -β-CD ratio of 10, the surface charge on the PL/NH 2 -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/NH 2 -β-CD-DOX by interacting with the negatively charged cell membrane. Conclusively, this study suggests that the combination of allicin and PL/NH 2 -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.