Gambogic acid (GA) is a highly effective antitumor agent, and it is used for the treatment of a wide range of cancers. It is challenging to deliver drugs to the central nervous system due to the inability of GA to cross the blood–brain barrier (BBB). Studies have shown that ultrasound-targeted microbubble destruction can be used for transient and reversible BBB disruption, significantly facilitating intracerebral drug delivery. We first prepared GA–loaded porous-lipid microbubbles (GA porous-lipid/PLGA MBs), and an in vitro BBB model was established. The cell viability was detected by CCK-8 assay and flow cytometry. The results indicate that U251 human glioma cells were killed by focused ultrasound (FUS) combined with GA/PLGA microbubbles. FUS combined with GA/PLGA microbubbles was capable of locally and transiently enhancing the permeability of BBB under certain conditions. This conformational change allows the release of GA to extracellular space. This study provides novel targets for the treatment of glioma.

藤黄酸 (GA) 是一种高效的抗肿瘤剂，可用于治疗多种癌症。由于 GA 无法穿过血脑屏障 (BBB)，因此将药物输送到中枢神经系统具有挑战性。研究表明，超声靶向微泡破坏可用于瞬时和可逆的 BBB 破坏，显着促进脑内给药。我们首先制备了负载 GA 的多孔脂质微泡（GA 多孔脂质 / PLGA MBs），并体外BBB模型建立。通过CCK-8测定和流式细胞术检测细胞活力。结果表明，U251 人脑胶质瘤细胞被聚焦超声 (FUS) 结合 GA/PLGA 微泡杀死。FUS 结合 GA/PLGA 微泡能够在某些条件下局部和瞬时提高 BBB 的渗透性。这种构象变化允许 GA 释放到细胞外空间。该研究为胶质瘤的治疗提供了新的靶点。