Wang Mingchao, Malfanti Alessio, Bastiancich Chiara, Préat Véronique
Université Catholique de Louvain, Louvain Drug Research Institute, Advanced Drug Delivery and Biomaterials, Brussels, Belgium.
Aix-Marseille Univ, CNRS, INP, Inst Neurophysiopathol, Marseille, France.
Int J Pharm X. 2022 Dec 21;5:100147. doi: 10.1016/j.ijpx.2022.100147. eCollection 2023 Dec.
We hypothesized that tocopherol succinate (TOS) and D-α-tocopherol polyethylene2000 succinate (TPGS) micelles could work as a drug delivery system while enhancing the anti-cancer efficacy of doxorubicin lauryl hydrazone derivative (DOXC) for the treatment of glioblastoma. The DOXC-TOS-TPGS micelles were formulated with synthesized DOXC and TPGS. They showed a high drug loading of hydrophobic DOXC (29%), a size of <100 nm and a pH sensitive drug release behaviour. , fast uptake of DOXC-TOS-TPGS micelles by GL261 cells was observed. For cytotoxicity, DOXC-TOS-TPGS micelles were evaluated on two glioblastoma cell lines and showed synergism between DOXC and TOS-TPGS The higher cytotoxicity of DOXC-TOS-TPGS micelles was mainly caused by necrosis. The DOXC-TOS-TPGS micelles seem to be a promising delivery system for enhancing the anticancer efficacy of doxorubicin in glioblastoma (GBM).
我们推测,琥珀酸生育酚(TOS)和聚乙二醇2000琥珀酸D-α-生育酚(TPGS)胶束可作为一种药物递送系统,同时增强阿霉素月桂酰腙衍生物(DOXC)治疗胶质母细胞瘤的抗癌疗效。DOXC-TOS-TPGS胶束由合成的DOXC和TPGS配制而成。它们显示出对疏水性DOXC的高载药量(29%)、小于100纳米的粒径以及pH敏感的药物释放行为。观察到GL261细胞对DOXC-TOS-TPGS胶束的快速摄取。对于细胞毒性,在两种胶质母细胞瘤细胞系上评估了DOXC-TOS-TPGS胶束,结果显示DOXC与TOS-TPGS之间具有协同作用。DOXC-TOS-TPGS胶束较高的细胞毒性主要由坏死引起。DOXC-TOS-TPGS胶束似乎是一种有前景的递送系统,可增强阿霉素在胶质母细胞瘤(GBM)中的抗癌疗效。
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