Department of Chemistry and ‡School of Pharmacy, University of Wisconsin-Madison , Madison, Wisconsin 53705, United States.
Mol Pharm. 2017 Nov 6;14(11):3916-3926. doi: 10.1021/acs.molpharmaceut.7b00624. Epub 2017 Oct 10.
The presence of a perfluorocarbon block in a multiblock polymer has been shown to be an additional driving force toward nanoparticle assembly. In the preparation of nanoemulsions, this perfluorocarbon block also provides enhanced particle stability. Herein, the synthesis of a new triphilic, semifluorinated copolymer, M2F8H18, is introduced. This ABC type block copolymer can be used to formulate extremely stable nanoemulsions, assembled around a lipophilic droplet, with lifetimes of one year or more. The central oil droplet can stably solubilize high concentrations of hydrophobic drugs, making this system an ideal drug delivery vehicle. The incorporation of the perfluorocarbon block modulates drug release from the lipophilic core via the surrounding fluorous shell. Fluorous imaging agents incorporated into the fluorous shell prolong drug release even further as well as provide potent F-MRI contrast ability. In vitro studies show that these nanoemulsions efficiently inhibit cancer cell growth, thus providing a theranostic drug delivery system.
多嵌段聚合物中存在全氟碳块被证明是纳米颗粒组装的额外驱动力。在制备纳米乳液时,这种全氟碳块还提供了增强的颗粒稳定性。本文介绍了一种新型三亲性、半氟化共聚物 M2F8H18 的合成。这种 ABC 型嵌段共聚物可用于配制极为稳定的纳米乳液,围绕亲脂性液滴组装,其寿命可达一年或更长时间。中心油滴可以稳定地溶解高浓度的疏水性药物,使该系统成为理想的药物输送载体。全氟碳块的掺入通过周围的氟相壳调节疏水性核心内药物的释放。掺入氟相壳中的氟成像剂进一步延长药物释放时间,并提供强大的 F-MRI 对比能力。体外研究表明,这些纳米乳液能有效抑制癌细胞生长,从而提供一种治疗诊断药物输送系统。