The biggest challenge in colorectal cancer therapy is to avoid intestinal drug absorption before reaching the colon, while focusing on tumor specific delivery with high local concentration and minimal toxicity. In our work, thymoquinone (TQ)-loaded polymeric nanocapsules were prepared using the nanoprecipitation technique using Eudragit S100 as polymeric shell. Conjugation of anisamide as a targeting ligand for sigma receptors overexpressed by colon cancer cells to Eudragit S100 was carried out via carbodiimide coupling reaction, and was confirmed by thin layer chromatography and ¹H-NMR. TQ nanocapsules were characterized for particle size, surface morphology, zeta potential, entrapment efficiency % (EE%), in vitro drug release and physical stability. A cytotoxicity study on three colon cancer cell lines (HT-29, HCT-116, Caco-2) was performed. Results revealed that the polymeric nanocapsules were successfully prepared, and the in vitro characterization showed a suitable size, zeta potential, EE% and physical stability. TQ exhibited a delayed release pattern from the nanocapsules in vitro. Anisamide-targeted TQ nanocapsules showed higher cytotoxicity against HT-29 cells overexpressing sigma receptors compared to their non-targeted counterparts and free TQ after incubation for 48 h, hence delineating anisamide as a promising ligand for active colon cancer targeting.

大肠癌治疗的最大挑战是在到达结肠之前要避免肠道药物的吸收，同时要关注高局部浓度和最小毒性的肿瘤特异性递送。在我们的工作中，使用Eudragit S100作为聚合物外壳的纳米沉淀技术制备了载有胸腺醌（TQ）的聚合物纳米胶囊。通过碳二亚胺偶联反应，将茴香酰胺作为结肠癌细胞过度表达的sigma受体的靶向配体与Eudragit S100的缀合，并通过薄层色谱法和¹1 H-NMR。TQ纳米胶囊的粒径，表面形态，ζ电位，包封率％（EE％），体外药物释放和物理稳定性均经过表征。对三种结肠癌细胞系（HT-29，HCT-116，Caco-2）进行了细胞毒性研究。结果表明，已成功制备了聚合物纳米胶囊，并且体外表征显示出合适的尺寸，ζ电势，EE％和物理稳定性。TQ在体外显示出从纳米胶囊的延迟释放模式。与无靶标的TQ纳米胶囊和无靶标的TQ纳米胶囊相比，在孵育48小时后，其对过表达sigma受体的HT-29细胞和游离TQ的细胞毒性更高，因此，它被认为是有希望的主动结肠癌靶向配体。