文献：mPEG-PDLLA ＆ mPEG-DSPE 载奥沙利铂复合胶束的制备及性能 

作者赵文豪; 龚婷; 熊迎新; 霍美蓉

文献链接：https://openurl.ebsco.com/EPDB%3Agcd%3A8%3A31831176/detailv2?sid=ebsco%3Aplink%3Ascholar&id=ebsco%3Agcd%3A180319522&crl=c&link_origin=scholar.google.com

摘要

Objective: To address the challenges associated with the low encapsulation efficiency of water-soluble drugs, poor stability and negligible endocytosis in micelles. Method: mPEG-DSPE and mPEG-PDLLA were used as carrier materials and oxaliplatin as model drug to prepare mPEG-DSPE&mPEG-PDLLA/OXA mixed NPs by flash nanoprecipitation. The performances of mixed NPs were compared with mPEG-PDLLA/OXA NPs and LPHNP/OXA NPs. Results: The optimal preparation process of mixed NPs obtained by single factor screening was as follows: the total flow rate was 4 mL/min with a flow rate ratio of 1∶3, the total material concentration was 3.75 mg/mLwith a material ratio was 1∶2, and the anti-solvent was acetonitrile. The three kinds of NPs had uniform particle sizes and all of their encapsulation efficiencies were more than 70%. The in vitro drug release test showed that the release rate of the mixed micelles which could be completely released was slower than that of the ordinary micelles. The results of uptake and apoptosis assay showed that the mixed micelles had the best uptake performance and cytotoxicity efficacy among the three NPs. Conclusions: The preparation of mixed micelles by flash nanoprecipitation which is a simple and convenient preparation method for commercialization, can achieve high encapsulation of water-soluble drugs. At the same time, the designed mixed micelles mPEG-DSPE&mPEG-PDLLA/OXA exhibits excellent abilities including favorable stability, superior uptake and robust cytotoxicity efficacy. This research provides a new idea for the application and transformation of micelles.

目的：解决水溶性药物包封率低、稳定性差和胶束内吞作用可忽略不计的挑战。

方法：以mPEG-DSPE和mPEG-PDLLA为载体材料，奥沙利铂为模型药物制备mPEG-DSPE&amp；mPEG-PDLLA/OXA混合纳米颗粒的快速纳米沉淀。将混合NP的性能与mPEG-PDLLA/OXA NP和LPHNP/OXA NP进行了比较。

结果：通过单因素筛选获得的混合NP的最佳制备工艺如下：总流速为4 mL/min，流速比为1∶3，总物质浓度为3.75 mg/mL，物质比为1比2，抗溶剂为乙腈。

三种NP的粒径均匀，包封率均在70%以上。体外药物释放试验表明，混合胶束可以完全释放的释放速率比普通胶束慢。

摄取和凋亡分析结果表明，混合胶束在三种NP中具有最佳的摄取性能和细胞毒性功效。

结论：快速纳米沉淀制备混合胶束是一种简单方便的商业化制备方法，可以实现水溶性药物的高度包封。

同时，设计了混合胶束mPEG-DSPE&amp；mPEG-PDLLA/OXA表现出优异的能力，包括良好的稳定性、优异的摄取和强大的细胞毒性功效。  

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DSPE-PEG-SH

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DSPE-PEG-SP2-AA

DSPE-PEG-SS

DSPE-PEG-TCO

DSPE-PEG-Tetrazine

DSPE-PEG-TMS

DSPE-PEG-TPP

DSPE-PEG-Transferrin 

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