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载紫杉醇和依托泊苷的聚(丙交酯-乙交酯)同轴电喷微球的制备及其用于双药控释。

Paclitaxel and etoposide-loaded Poly (lactic-co-glycolic acid) microspheres fabricated by coaxial electrospraying for dual drug delivery.

机构信息

a Alan G. MacDiarmid Laboratory, College of Chemistry , Jilin University , Changchun , China.

b Norman Bethune First Hospital, Jilin University , Changchun , China.

出版信息

J Biomater Sci Polym Ed. 2018 Nov;29(16):1949-1963. doi: 10.1080/09205063.2018.1485816. Epub 2018 Oct 29.

DOI:10.1080/09205063.2018.1485816
PMID:29920151
Abstract

In this study, we fabricated paclitaxel (PTX) and etoposide (ETP) loaded Poly (lactic-co-glycolic acid) (PLGA) microspheres with core-shell structures and particle sizes ranging from 1 to 4 µm by coaxial electrospraying. The microspheres were analyzed by scanning electron microscopy (SEM), transmission electron microscopy (TEM). The drug loading rate and entrapment efficiency of the microspheres were detected by high performance liquid chromatograph (HPLC). Moreover, the drug release profiles and degradation of drug-loaded PLGA microspheres in vitro were investigated, respectively. The distinct layered structure that existed in the manufactured core-shell microspheres can be observed by TEM. The in vitro release profiles indicated that the PLGA/PTX + ETP (PLGA/PE) microspheres exhibited the controlled release of two drugs in a sequential manner. Cell Counting Kit-8 was used to detect the toxic and side effects of the microspheres on bone tumor cells. PTX and ETP for combination drug therapy loaded microspheres had more cytotoxic effect on saos-2 osteosarcoma cells than the individual drugs. In conclusion, core-shell PLGA microspheres by electrospraying for combination drug therapy is promising for medicine applications, the PLGA/PE microspheres have some potential for osteosarcoma treatment.

摘要

在这项研究中,我们通过同轴静电纺丝制备了具有核壳结构和 1 至 4μm 粒径的紫杉醇(PTX)和依托泊苷(ETP)载聚乳酸-共-羟基乙酸(PLGA)微球。通过扫描电子显微镜(SEM)、透射电子显微镜(TEM)对微球进行了分析。通过高效液相色谱(HPLC)检测了微球的载药率和包封效率。此外,还研究了载药 PLGA 微球在体外的释放曲线和降解情况。TEM 可以观察到所制备的核壳微球中存在的分层结构。体外释放曲线表明,PLGA/PTX+ETP(PLGA/PE)微球以顺序方式表现出两种药物的控制释放。细胞计数试剂盒-8 用于检测微球对骨肉瘤细胞的毒性和副作用。与单独用药相比,载有联合药物治疗的 PTX 和 ETP 的微球对骨肉瘤细胞 saos-2 具有更强的细胞毒性作用。总之,用于联合药物治疗的电纺核壳 PLGA 微球具有很大的医学应用潜力,PLGA/PE 微球在骨肉瘤治疗方面具有一定的潜力。

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