Abstract
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.
Highlights
Gliomas mainly occur in middle-aged people, and they are the most malignant primary brain tumors, representing 70% of primary adult malignant brain tumors with a yearly incidence of ∼0.06% (Schulte et al, 2020; Hartanto et al, 2021; Miyake et al, 2021)
PLGA MBs carrying Gambogic acid (GA) were prepared through water/oil/water (W1/O/W2) dual emulsion
GA was better distributed in the U251 region and inhibited its growth
Summary
Gliomas mainly occur in middle-aged people, and they are the most malignant primary brain tumors, representing 70% of primary adult malignant brain tumors with a yearly incidence of ∼0.06% (Schulte et al, 2020; Hartanto et al, 2021; Miyake et al, 2021). Chemotherapies or chemoradiotherapies can reduce the tumor size and improve the prognosis, but these treatments have significant side effects, especially in the aged patients (Festuccia et al, 2020; Smith-Cohn et al, 2021). It is GA Lipid/PLGA Microbubbles on Human Glioma essential to develop safe and effective treatments with fewer side effects. One of these treatment methods is ultrasound (US)targeted microbubble destruction (UTMD) (Anderson et al, 2021; Zhao et al, 2021). Selective blood–tumor barrier opening is an effective method to improve the chemotherapeutic efficacy for brain glioma (Anderson et al, 2021)
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