文獻(xiàn)：mPEG-PDLLA ＆ mPEG-DSPE 載奧沙利鉑復(fù)合膠束的制備及性能 

作者趙文豪; 龔婷; 熊迎新; 霍美蓉

文獻(xiàn)鏈接：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：解決水溶性藥物包封率低、穩(wěn)定性差和膠束內(nèi)吞作用可忽略不計(jì)的挑戰(zhàn)。

方法：以mPEG-DSPE和mPEG-PDLLA為載體材料，奧沙利鉑為模型藥物制備mPEG-DSPE&amp；mPEG-PDLLA/OXA混合納米顆粒的快速納米沉淀。將混合NP的性能與mPEG-PDLLA/OXA NP和LPHNP/OXA NP進(jìn)行了比較。

結(jié)果：通過(guò)單因素篩選獲得的混合NP的最佳制備工藝如下：總流速為4 mL/min，流速比為1∶3，總物質(zhì)濃度為3.75 mg/mL，物質(zhì)比為1比2，抗溶劑為乙腈。

三種NP的粒徑均勻，包封率均在70%以上。體外藥物釋放試驗(yàn)表明，混合膠束可以完全釋放的釋放速率比普通膠束慢。

攝取和凋亡分析結(jié)果表明，混合膠束在三種NP中具有最佳的攝取性能和細(xì)胞毒性功效。

結(jié)論：快速納米沉淀制備混合膠束是一種簡(jiǎn)單方便的商業(yè)化制備方法，可以實(shí)現(xiàn)水溶性藥物的高度包封。

同時(shí)，設(shè)計(jì)了混合膠束mPEG-DSPE&amp；mPEG-PDLLA/OXA表現(xiàn)出優(yōu)異的能力，包括良好的穩(wěn)定性、優(yōu)異的攝取和強(qiáng)大的細(xì)胞毒性功效。  

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