We study βLAP and its derivative nor-β-Lapachone (NβL) complexes with 2-hydroxypropyl-β-cyclodextrin to increase the solubility and bioavailability. The formation of true inclusion complexes between βLAP or NβL in 2-HP-β-CD in solid solution was characterization by FT-IR, DSC, powder X-ray was and was confirmed by one- and two-dimensional ¹H NMR experiments. Additionally, the biological activities of βLAP, NβL, ICβLAP, and ICNβL were investigated through trypanocidal assays with T. cruzi and cytotoxicity studies with mouse peritoneal macrophages. Originally, we tested these complexes against T. cruzi viability and observed higher biological activities and lower cytotoxicity when compared to βLAP and NβL. Thus, the complexation of βLAP and NβL with 2-HP-β-CD increases the drug solubility, in addition vectorization was observed, increasing the biological activity against epimastigotes and trypomastigotes T. cruzi forms. Reduced the toxicity of the compounds against mammalian cells. In addition, the selectivity indices higher of the inclusion complexes comparing to substance free and those of benznidazole.

我们研究了 βLAP 及其衍生物 nor-β-Lapachone (NβL) 与 2-羟丙基-β-环糊精的复合物，以提高溶解度和生物利用度。通过 FT-IR、DSC、粉末 X 射线表征了固溶体中 2-HP-β-CD 中 βLAP 或 NβL 之间形成真正的包合配合物，并通过一维和二维¹ H NMR 实验证实。此外，βLAP、NβL、ICβLAP 和 ICNβL 的生物学活性通过对克氏锥虫的杀锥虫测定和对小鼠腹腔巨噬细胞的细胞毒性研究进行了研究。最初，我们针对T. cruzi测试了这些复合物与βLAP和NβL相比，活性并观察到更高的生物活性和更低的细胞毒性。因此，βLAP 和 NβL 与 2-HP-β-CD 的络合增加了药物溶解度，此外还观察到矢量化，增加了针对外鞭毛体和锥鞭毛体T. cruzi形式的生物活性。降低了化合物对哺乳动物细胞的毒性。此外，包合物的选择性指数高于无物质和苯并硝唑的选择性指数。