Department of Medical Life Sciences, Department of Biomedicine & Health Sciences, Catholic Photomedicine Research Institute, College of Medicine, The Catholic University of Korea, 222 Banpo-daero, Seocho-gu, 06591, Seoul, Republic of Korea.
J Nanobiotechnology. 2021 Dec 7;19(1):411. doi: 10.1186/s12951-021-01160-4.
Combination therapy using more than one drug can result in a synergetic effect in clinical treatment of cancer. For this, it is important to develop an efficient drug delivery system that can contain multiple drugs and provide high accumulation in tumor tissue. In particular, simultaneous and stable loading of drugs with different chemical properties into a single nanoparticle carrier is a difficult problem.
We developed rhamnolipid-coated double emulsion nanoparticles containing doxorubicin and erlotinib (RL-NP-DOX-ERL) for efficient drug delivery to tumor tissue and combination chemotherapy. The double emulsion method enabled simultaneous loading of hydrophilic DOX and hydrophobic ERL in the NPs, and biosurfactant RL provided stable surface coating. The resulting NPs showed fast cellular uptake and synergetic tumor cell killing in SCC7 cells. In real-time imaging, they showed high accumulation in SCC7 tumor tissue in mice after intravenous injection. Furthermore, enhanced tumor suppression was observed by RL-NP-DOX-ERL in the same mouse model compared to control groups using free drugs and NPs containing a single drug.
The developed RL-NP-DOX-ERL provided efficient delivery of DOX and ERL to tumor tissue and successful tumor therapy with a synergetic effect. Importantly, this study demonstrated the promising potential of double-emulsion NPs and RL coating for combination therapy.
联合使用多种药物的治疗方法在癌症的临床治疗中可以产生协同作用。为此，开发一种能够包含多种药物并在肿瘤组织中实现高积累的高效药物输送系统非常重要。特别是，将具有不同化学性质的药物同时且稳定地装载到单个纳米颗粒载体中是一个难题。
我们开发了载有多柔比星和厄洛替尼的鼠李糖脂包裹的双重乳液纳米颗粒（RL-NP-DOX-ERL），用于高效递送至肿瘤组织和联合化疗。双重乳液法能够同时将亲水性 DOX 和疏水性 ERL 装载到 NPs 中，生物表面活性剂 RL 提供了稳定的表面涂层。所得 NPs 在 SCC7 细胞中表现出快速的细胞摄取和协同的肿瘤细胞杀伤作用。在实时成像中，它们在静脉注射后在小鼠的 SCC7 肿瘤组织中表现出高积累。此外，与使用游离药物和仅含单种药物的 NPs 的对照组相比，RL-NP-DOX-ERL 在相同的小鼠模型中观察到增强的肿瘤抑制作用。
所开发的 RL-NP-DOX-ERL 能够将 DOX 和 ERL 高效递送至肿瘤组织，并通过协同作用成功进行肿瘤治疗。重要的是，这项研究证明了双重乳液 NPs 和 RL 涂层在联合治疗中的有前途的潜力。
