Katz Joshua S, Levine Dalia H, Davis Kevin P, Bates Frank S, Hammer Daniel A, Burdick Jason A
Department of Bioengineering, University of Pennsylvania, Philadelphia, PA 19104, USA.
Langmuir. 2009 Apr 21;25(8):4429-34. doi: 10.1021/la803769q.
Biodegradable polymersomes are promising vehicles for a range of applications. Their stabilization would improve many properties, including the retention and controlled release of polymersome contents, yet this has not been previously accomplished. Here, we present the first example of stabilizing fully biodegradable polymersomes through acrylation of the hydrophobic terminal end of polymersome-forming poly(caprolactone-b-ethylene glycol). Exposure of the resulting polymersomes loaded with a hydrophobic photoinitiator to ultraviolet light polymerized the acrylates, without affecting polymersome morphology or cell cytotoxicity. These stabilized polymersomes were more resistant to surfactant disruption and degradation. As an example of stabilized polymersome utility, the unintended release of doxorubicin (DOX) due to leakage from polymersomes decreased with membrane stabilization and slower sustained release was observed. Finally, DOX-loaded polymersomes retained their cytotoxicity following stabilization.
可生物降解的聚合物囊泡是一系列应用中很有前景的载体。它们的稳定性改善将提升许多性能，包括聚合物囊泡内容物的保留和控释，但此前尚未实现这一点。在此，我们展示了第一个通过对形成聚合物囊泡的聚（己内酯 -b-乙二醇）的疏水末端进行丙烯酸化来稳定完全可生物降解聚合物囊泡的例子。将负载有疏水光引发剂的所得聚合物囊泡暴露于紫外线下会使丙烯酸酯聚合，而不会影响聚合物囊泡的形态或细胞毒性。这些稳定的聚合物囊泡对表面活性剂破坏和降解更具抗性。作为稳定聚合物囊泡实用性的一个例子，由于聚合物囊泡泄漏导致的阿霉素（DOX）意外释放随着膜稳定性的提高而减少，并且观察到缓释更慢。最后，负载DOX的聚合物囊泡在稳定后仍保留其细胞毒性。
