Van Gheluwe Louise, Buchy Eric, Chourpa Igor, Munnier Emilie
EA 6295 Nanomédicaments et Nanosondes, Faculté de Pharmacie, Université de Tours, 31 Avenue Monge, 37 200 Tours, France.
Laboratoires Eriger, 39 Rue des Granges Galand, 37550 Saint-Avertin, France.
Polymers (Basel). 2020 Oct 14;12(10):2350. doi: 10.3390/polym12102350.
Smart polymeric nanocarriers have been developed to deliver therapeutic agents directly to the intended site of action, with superior efficacy. Herein, a mixture of poly(lactide) (PLA) and redox-responsive poly(ethylene glycol)--poly(lactide) (PEG--PLA) containing a disulfide bond was synthesized in three steps. The nanoprecipitation method was used to prepare an aqueous suspension of polymeric nanocarriers with a hydrodynamic diameter close to 100 nm. Retinol, an anti-aging agent very common in cosmetics, was loaded into these smart nanocarriers as a model to measure their capacity to encapsulate and to protect a lipophilic active molecule. Retinol was encapsulated with a high efficiency with final loading close to 10% . The stimuli-responsive behavior of these nanocarriers was demonstrated in vitro, in the presence of l-Glutathione, susceptible to break of disulfide bond. The toxicity was low on human keratinocytes in vitro and was mainly related to the active molecule. Those results show that it is not necessary to use 100% of smart copolymer in a nanosystem to obtain a triggered release of their content.
智能聚合物纳米载体已被开发出来，可将治疗剂直接递送至预期作用部位，具有卓越的功效。在此，通过三步合成了聚丙交酯（PLA）和含有二硫键的氧化还原响应性聚乙二醇-聚丙交酯（PEG-PLA）的混合物。采用纳米沉淀法制备了流体动力学直径接近100nm的聚合物纳米载体水悬浮液。视黄醇是化妆品中非常常见的一种抗衰老剂，被载入这些智能纳米载体中作为模型，以测量它们包封和保护亲脂性活性分子的能力。视黄醇的包封效率很高，最终载药量接近10%。在体外，在易使二硫键断裂的L-谷胱甘肽存在下，证明了这些纳米载体的刺激响应行为。在体外对人角质形成细胞的毒性较低，且主要与活性分子有关。这些结果表明，在纳米系统中不必使用100%的智能共聚物来实现其内容物的触发释放。
