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首页> 外文期刊>RSC Advances >Paclitaxel-loaded PLGA microspheres with a novel morphology to facilitate drug delivery and antitumor efficiency
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Paclitaxel-loaded PLGA microspheres with a novel morphology to facilitate drug delivery and antitumor efficiency

机译：载有紫杉醇的PLGA微球具有新颖的形态，有助于药物递送和抗肿瘤功效

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The aim of this study was to develop a novel morphological paclitaxel (PTX) loaded poly(lactide-co-glycolide) (PLGA) microspheres (MS) delivery system to enhance drug delivery and antitumor efficiency as well as reduce drug administration frequency. Therefore, different morphological types of PTX-PLGA-MS were prepared using a modified solvent evaporation technique. Morphology analysis confirmed the successful preparation of the smooth PTX-PLGA-MS with internal sporadic porosity, and the novel rough PTX-PLGA-MS with microporous surface and porous internal structures. The PTX drugs were distributed in the readily bioavailable state (amorphous) in PTX-loaded MS, which allowed fast drug release from MS following intratumoral administration. The drug entrapment and release behaviors indicated that the rough MS could provide enough hydrophobic space for PTX-loading and deep surface folds for fast matrices degradation, thus achieving a higher drug-loading efficiency (17.8%) and a rapid sustained drug release effect. Furthermore, the rough MS showed strengthened in vitro anti-hepatoma efficiency than that of free PTX and smooth MS. The in vivo studies indicated remarkable antitumor activity of rough MS (tumor inhibition rate = 58.33%) for at least 13 days after a single injection, which was because the rapid sustained-release drugs could induce the pro-apoptosis gene and protein expressions, cause extensive tumor cell apoptosis, and reduce the toxicity to normal tissues. In conclusion, the rough PTX-PLGA-MS drug delivery system with outstanding tumor growth inhibition effect could serve as a promising treatment for liver tumor.
机译：这项研究的目的是开发一种新型的形态紫杉醇（PTX）负载的聚（丙交酯- co <​​/ em>-乙交酯）（PLGA）微球（MS）递送系统，以增强药物递送和抗肿瘤效率，以及减少给药频率。因此，使用改进的溶剂蒸发技术制备了不同形态的PTX-PLGA-MS。形态分析证实成功制备了具有内部零星孔隙的光滑PTX-PLGA-MS，以及具有微孔表面和多孔内部结构的新型粗糙PTX-PLGA-MS。 PTX药物以易于生物利用的状态（无定形）分布在载有PTX的MS中，这允许在肿瘤内给药后从MS快速释放药物。药物的截留和释放行为表明，粗糙的质谱可以为PTX装载提供足够的疏水空间，并为快速基质降解提供深层的表面折叠，从而实现更高的药物装载效率（17.8％）和快速持续的药物释放效果。此外，粗糙的MS显示出比游离PTX和光滑MS更强的体外抗肝癌功效。 体内研究表明，单次注射后至少13天，粗制MS具有显着的抗肿瘤活性（抑瘤率= 58.33％），这是因为快速持续释放药物可以诱导前体凋亡基因和蛋白质的表达，引起广泛的肿瘤细胞凋亡，并降低对正常组织的毒性。综上所述，具有显着的抑瘤作用的粗PTX-PLGA-MS给药系统可以作为治疗肝肿瘤的有前途的药物。

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