The chitosan-folate conjugate was synthesized initially and confirmed by FTIR and NMR spectroscopic studies. Following, docetaxel (DXL) loaded non-targeted, single receptor and dual receptor (folate and EGFR) targeted chitosan nanoparticles were prepared and their shape, particle size, zeta-potential, surface morphology and texture were screened by SEM, TEM, AFM analyses. Surface chemistry analysis by XPS indeed confirmed the successful conjugation of folate and cetuximab on the targeted formulations. In-vitro analysis of dual-targeted chitosan nanoparticles has revealed their superior cytotoxicity against A-549 cells. The IC₅₀ of dual receptor-targeted chitosan NP was almost 34 times lower than DXL control. In-vivo pharmacokinetic study on Wistar rats has demonstrated improved relative bioavailability of all NP in comparison to DXL control. The results illustrated that EGFR and folate dual targeted NP enhanced the cytotoxicity of DXL towards A-549 lung cancer cells and substantially improved DXL pharmacokinetics in rats.

最初合成壳聚糖-叶酸缀合物，并通过 FTIR 和 NMR 光谱研究证实。随后，制备了负载多西紫杉醇（DXL）的非靶向、单受体和双受体（叶酸和EGFR）靶向壳​​聚糖纳米颗粒，并通过SEM、TEM、AFM分析筛选了它们的形状、粒径、zeta电位、表面形态和纹理。 . XPS 的表面化学分析确实证实了叶酸和西妥昔单抗在目标制剂上的成功结合。双靶向壳聚糖纳米颗粒的体外分析显示它们对 A-549 细胞具有优异的细胞毒性。IC ₅₀双受体靶向壳聚糖 NP 的含量几乎比 DXL 对照低 34 倍。对 Wistar 大鼠的体内药代动力学研究表明，与 DXL 对照相比，所有 NP 的相对生物利用度都有所提高。结果表明，EGFR和叶酸双重靶向NP增强了DXL对A-549肺癌细胞的细胞毒性，并显着改善了DXL在大鼠中的药代动力学。