State Key Laboratory of Natural and Biomimetic Drugs, the School of Pharmaceutical Sciences, Peking University, No. 38, Xueyuan Rd., Beijing 100191, China.
Langmuir. 2012 Jun 26;28(25):9387-94. doi: 10.1021/la301534h. Epub 2012 Jun 15.
Light-responsive drug delivery systems are particularly appealing that are capable of releasing active molecules at the appropriate site and rate. We synthesized a series of photodegradable polymers that can form nanoparticles for drug encapsulation. These particles in aqueous solutions are stable in buffers with different pHs or at evaluated temperatures, while light can trigger the crash of particles and the release of encapsulated substances. The release efficiency can reach up to 90% based on Nile red fluorescence intensity upon 15 min light irradiation. Nanoparticle uptake by phagocytic cells and light-triggered release in cells were observed by fluorescence emission of the hydrolyzed fluorescein diacetate upon photoinduced degradation of these nanoparticles. No significant toxicity of these nanoparticles was found at the concentrations up to 1000 μg/mL before or after light irradiation. Further encapsulation and triggered release of a bioactive model drug (Tagalsin G) was evaluated for RAW 264.7 cells. Tagalsin G encapsulated in nanoparticles did not show cytotoxity to cells, while light triggered the release of Tagalsin G increasing cell death dramatically from 9% to 67%. Our model studies show a new promising strategy to trigger drug release in cells.
光响应药物递送系统特别吸引人,因为它们能够在适当的部位和速率下释放活性分子。我们合成了一系列可形成用于药物包封的纳米颗粒的光降解聚合物。这些在不同 pH 值缓冲液或评估温度下的水溶液中的颗粒是稳定的,而光可以触发颗粒的崩溃和包裹物质的释放。基于尼罗红荧光强度,在 15 分钟的光照射下,释放效率可达 90%。通过荧光素二乙酸酯的光诱导降解,观察到吞噬细胞对纳米颗粒的摄取和细胞内的光触发释放。在光照射前后,浓度高达 1000μg/ml 时,这些纳米颗粒没有表现出明显的毒性。进一步评价了 RAW 264.7 细胞中生物活性模型药物(Tagalsin G)的包封和触发释放。Tagalsin G 包封在纳米颗粒中对细胞没有细胞毒性,而光触发了 Tagalsin G 的释放,使细胞死亡从 9%急剧增加到 67%。我们的模型研究表明了一种在细胞中触发药物释放的新的有前途的策略。