National Cancer Institute, Frederick, MD, USA.
Biomacromolecules. 2012 Oct 8;13(10):3388-94. doi: 10.1021/bm301143d. Epub 2012 Sep 26.
Biopolymers bearing hydrophobic side-chains, such as hydrophobically modified chitosan (hmC), can connect liposomes into a gel network via hydrophobic interactions. In this paper, we show that such liposome gels possess an attractive combination of properties for certain drug delivery applications. Their shear-thinning property allows these gels to be injected at a particular site, while their gel-like nature at rest ensures that the material will remain localized at that site. Moreover, drugs can be encapsulated in the interior of the liposomes and delivered at the local site for an extended period of time. The presence of two transport resistances - from the liposomal bilayer and the gel network - is shown to be responsible for the sustained release; in turn, disruption of the liposomes both weakens the gel and causes a faster release. We have monitored release kinetics from liposome gels of a cationic anticancer drug doxorubicin (Dox) encapsulated in liposomes. Sustained release of Dox from these gels and the concomitant cytotoxic effect could be observed for over a week.
具有疏水性侧链的生物聚合物,如疏水性改性壳聚糖(hmC),可以通过疏水性相互作用将脂质体连接成凝胶网络。在本文中,我们表明,这种脂质体凝胶具有某些药物输送应用的吸引力的组合性质。它们的剪切稀化性质允许这些凝胶在特定部位注射,而在休息时的凝胶状性质确保材料将保留在该部位。此外,可以将药物封装在脂质体的内部,并在局部部位长时间递送。显示存在两种传输阻力 - 来自脂质体双层和凝胶网络 - 负责持续释放; 反过来,破坏脂质体既削弱了凝胶并导致更快的释放。我们已经监测了包封在脂质体中的阳离子抗癌药物阿霉素(Dox)的脂质体凝胶的释放动力学。可以观察到这些凝胶中 Dox 的持续释放和伴随的细胞毒性作用超过一周。