Abstract：
This work aimed to develop amphiphilic nanocarriers such as polymersome based diblock copolymer of Kollicoat ® IR -block-poly(ε-caprolactone) (Kollicoat ® IR-b-PCL) for potential co-delivery of Nisin (Ni) and Curcumin (CUR) for treatment of breast cancer. To generate multi-layered nanocarriers of uniform size and morphology, microfluidics was used as a new technology. In order to characterise and optimize polymersome, design of experiments (Design-Expert) software with three levels full factorial design (3-FFD) method was used. Finally, the optimized polymersome was produced with a spherical morphology, small particle size (dH < 200 nm), uniform size distribution (PDI < 0.2), and high drug loading efficiency (Ni 78 % and CUR 93 %). Furthermore, the maximum release of Ni and CUR was found to be roughly 60 % and 80 % in PBS, respectively. Cytotoxicity assays showed a slight cytotoxicity of Ni and CUR -loaded polymersome (N- Ni /CUR) towards normal cells while demonstrating inhibitory activity against cancer cells compared to the free drugs. Also, the apoptosis assays and cellular uptake confirmed the obtained results from cytotoxic analysis. In general, this study demonstrated a microfluidic approach for preparation and optimization of polymersome for co-delivery of two drugs into cancer cells.
摘要：
这项工作旨在开发两亲性纳米载体，例如Kollicoat®IR-嵌段-聚（ε-己内酯）（Kollicoat®IR-b-PCL）的基于聚合物的二嵌段共聚物，用于Nisin（Ni）和姜黄素（CUR）的潜在共递送，用于治疗乳腺癌。为了产生均匀尺寸和形态的多层纳米载体，微流控技术是一种新技术。为了表征和优化聚合物，实验设计（Design-Expert）软件采用三级全因子设计（3-FFD）方法。最后,优化的聚合物囊具有球形形态，小粒径（dH<200nm），均匀的尺寸分布（PDI<0.2），和高的载药率(Ni78%和CUR93%)。此外，在PBS中，Ni和CUR的最大释放量约为60％和80％，分别。细胞毒性测定显示Ni和CUR负载的聚合物体(N-Ni/CUR)对正常细胞具有轻微的细胞毒性,同时与游离药物相比显示对癌细胞的抑制活性。此外，细胞凋亡测定和细胞摄取证实了从细胞毒性分析获得的结果。总的来说,这项研究证明了一种微流控方法，用于制备和优化聚合物小体，用于将两种药物共递送到癌细胞中。
