Aim: The aim of this investigation was to evaluate the potential of folic acid-tailored solid lipid nanoparticles (SLNs) for encapsulation as well as for in vitro cytotoxicity study of irinotecan hydrochloride trihydrate (IHT) against colorectal cancer (CRC) by using HT-29 cells.

Methods: Solvent diffusion technique was employed for the preparation of SLNs. Further, the formulations were optimised via three-level, three-factor Box–Behnken design (BBD).

Results: The uncoupled SLNs (IRSLNs) and folic acid-coupled SLNs (IRSLNFs) formulations revealed not only high %entrapment efficiency but also small particle size. Moreover, in vitro drug release results from IRSLNs and IRSLNFs confirmed that they followed sustained-release effect for up to 144 h. Whereas, in vitro cell viability study against HT-29 cell line suggested significantly (p < 0.05) higher cytotoxicity (IC₅₀ = 15 µg/ml) of IRSLNFs over IRSLNs and IHT solution.

Conclusions: Outcomes suggested that the engineered IRSLNFs hold great potential for targeting CRC for an extended period of time.

目的：这项研究的目的是评估叶酸定制的固体脂质纳米颗粒（SLN）的潜力，以及使用HT-进行盐酸伊立替康三水合物（IHT）对结直肠癌（CRC）的体外细胞毒性研究。 29个单元格。

方法：采用溶剂扩散技术制备SLN。此外，通过三级三因素Box-Behnken设计（BBD）对配方进行了优化。

结果：未偶联的SLNs（IRSLNs）和叶酸偶联的SLNs（IRSLNFs）配方不仅显示出高的包封率，而且粒径很小。此外，来自IRSLN和IRSLNF的体外药物释放结果证实，它们具有持续释放作用长达144小时。相比之下，针对HT-29细胞系的体外细胞活力研究表明 ，IRSLNF的 细胞毒性（IR ₅₀ = 15 µg / ml）明显高于IRSLN和IHT溶液（p <0.05）。

结论：结果提示，经过改造的IRSLNFs在靶向CRC方面具有很大的潜力。