To develop an injectable formulation and improve the stability of disulfiram (DSF), DSF was encapsulated into mixed nanoparticles (DSF-NPs) through a high-pressure homogenization method. The Flory-Huggins interaction parameters (χ_FH) were calculated to predict the miscibility between DSF and the hydrophobic core, resulting in PCL₅₀₀₀ selected as the hydrophobic block to encapsulate the DSF, as PCL₅₀₀₀ had a lower χ_FH 3.39 and the drug loading of the nanoparticles prepared by mPEG₅₀₀₀-PCL₅₀₀₀ was relatively higher. mPEG₅₀₀₀-PCL₅₀₀₀ and PCL₅₀₀₀ were blended to reduce the leakage of DSF during preparation, as well as increase the stability of the nanoparticles. The cargo-loading capacity of the nanoparticles was improved from 3.35% to 5.50% by reducing the crystallinity of the PCL nanoparticle core, and the crystallinity decreased from 51.13% to 25.15% after adding medium chain triglyceride (MCT). The DSF-NPs prepared by the above method had a small particle size of 98.1 ± 10.54 nm, with a polydispersity index (PDI) of 0.036, as well as drug loading of 5.50%. Furthermore, DSF-NPs containing MCT showed higher stability than DSF-NPs without MCT and DSF-sol (DSF dissolved in Cremophor EL and ethanol) in water and 90% plasma-containing PBS. The pharmacokinetics proved that DSF-NPs containing MCT enhanced the DSF concentration in the blood. Finally, DSF-NPs effectively inhibited H22 xenograft tumor growth in vivo.

为了开发可注射制剂并提高双硫仑（DSF）的稳定性，通过高压均质方法将DSF封装到混合纳米颗粒（DSF-NPs）中。的弗洛里-赫金斯相互作用参数（χ _FH）进行了计算，预测DSF和疏水核心之间的互溶性，从而导致PCL ₅₀₀₀选择作为疏水性嵌段以包封DSF，如PCL ₅₀₀₀具有更低的χ _FH 3.39，载药量由mPEG ₅₀₀₀ -PCL ₅₀₀₀制备的纳米颗粒的相对较高。mPEG ₅₀₀₀ -PCL ₅₀₀₀和PCL ₅₀₀₀将其掺混以减少制备过程中DSF的泄漏，并增加纳米颗粒的稳定性。通过降低PCL纳米颗粒核的结晶度，纳米颗粒的载物能力从3.35％提高到5.50％，加入中链甘油三酸酯（MCT）后，结晶度从51.13％降低到25.15％。通过上述方法制备的DSF-NP具有98.1±10.54nm的小粒径，0.036的多分散指数（PDI）以及5.50％的载药量。此外，含有MCT的DSF-NP比没有MCT和DSF-sol（DSF-sol溶解在Cremophor EL和乙醇中的DSF）在水和含90％血浆的PBS中显示出更高的稳定性。药代动力学证明，含有MCT的DSF-NP可增强血液中的DSF浓度。最后，