School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, 200240, China.
J Mater Chem B. 2019 Feb 14;7(6):974-985. doi: 10.1039/c8tb02673d. Epub 2019 Jan 23.
To prevent premature drug release from nanoparticles, it is vital to design and prepare controlled and site-specific drug release systems. We investigated a new controllable drug release mesoporous carbon nanoparticle (MCN)-based nano-system with the advantages of enhanced permeability and retention effect (EPR) to target tumors followed by the NIR-induced heat-triggered release of a chemotherapeutic drug to show anti-tumor effects. The pores of MCN with photo-thermal effects were filled with the chemotherapeutic agent doxorubicin (DOX) and the phase change material (PCM) 1-tetradecanol was used as a gatekeeper to trap DOX inside the pores of the mesoporous carbon nanoparticles and the release of DOX inside tumor cells was triggered using NIR irradiation. The surface of MCN was coated with natural sophorolipid (SLPD) to obtain nanoparticles (DOX-PCM@MCN-SLPD) with good biocompatibility, dispersibility and stability in aqueous solutions. The MCN-based nano-system had the ability to load 24% DOX trapped with the PCM before coating with SLPD. It was observed that the release of DOX was temperature-dependent above the melting point of PCM. Once DOXPCM@MCN-SLPD was delivered into MCF-7/ADR cells, the release of DOX was triggered by MCN-borne photo-thermal effects under NIR irradiation. The amount of DOX inside the tumor was visualized via confocal laser scanning microscopy, which showed a higher amount of DOX at a higher temperature compared to that at normal body temperature, further confirming the minimization of premature drug release at 37 °C.
为了防止纳米颗粒中药物过早释放,设计和制备可控的、靶向释放的药物释放系统至关重要。我们研究了一种新的基于介孔碳纳米粒子(MCN)的可控药物释放纳米系统,该系统具有增强的通透性和保留效应(EPR),可靶向肿瘤,随后通过近红外(NIR)诱导的热触发释放化疗药物来发挥抗肿瘤作用。具有光热效应的 MCN 的孔中填充了化疗药物阿霉素(DOX),相变材料(PCM)十四醇被用作守门员,将 DOX 困在介孔碳纳米粒子的孔内,并用近红外辐射触发 DOX 在肿瘤细胞内的释放。MCN 的表面用天然槐糖脂(SLPD)进行包覆,得到具有良好生物相容性、分散性和在水溶液中稳定性的纳米粒子(DOX-PCM@MCN-SLPD)。基于 MCN 的纳米系统在包覆 SLPD 之前能够负载 24%的被 PCM 捕获的 DOX。结果表明,在 PCM 的熔点以上,DOX 的释放是温度依赖的。一旦 DOX-PCM@MCN-SLPD 被递送到 MCF-7/ADR 细胞中,在近红外辐射下,MCN 携带的光热效应就会触发 DOX 的释放。通过共聚焦激光扫描显微镜可以观察到肿瘤内 DOX 的含量,与正常体温相比,在更高的温度下 DOX 的含量更高,进一步证实了在 37°C 时可以最大限度地减少药物过早释放。