文献：聚乙二醇单甲醚-聚D,L-乳酸-聚谷氨酸/聚赖氨酸三嵌段复合胶束的制备及稳定性

链接：https://jcpu.cpu.edu.cn/en/article/doi/10.11665/j.issn.1000-5048.20140309

作者：唐丽丹， 沉艳， 屠家胜

节选：

为了提高原有聚乙二醇单甲醚-聚D, L-乳酸（mPEG-PLA）共聚物胶束的结构稳定性，制备了等比例聚乙二醇单甲醚-聚D, L-乳酸-聚谷氨酸（mPEG-PLA-PLG）和聚乙二醇单甲醚-聚D, L-乳酸-聚赖氨酸（mPEG-PLA-PLL）电中性聚离子复合胶束。新胶束稳定性的提高归因于静电引力。mPEG-PLA氨基键合的端羟基分别与谷氨酸和赖氨酸的环状羧酸酐发生开环反应，再脱去保护基，得到目标产物。采用核磁共振氢谱（1H NMR）和红外光谱（IR）对结构进行表征，荧光法测定mPEG-PLA与改性聚合物的临界胶束浓度（CMC）差异，采用透析法制备脱氧鬼臼毒素聚合物胶束，用高效液相色谱（HPLC）测定mPEG-PLA胶束和电中性聚离子复合胶束的载药量和包封率，用激光粒度仪（动态光散射）和HPLC分别测定25℃水浴中粒径和药物含量的变化。

In order to improve the structural stability of the original polymeric micelles based on poly(ethylene glycol)monomethyl ether-poly(D, L-lactic acid)(mPEG-PLA)copolymer conjugate, the electroneutral polyion complex micelles with equal proportion of poly(ethylene glycol)monomethyl ether-poly(D, L-lactic acid)-poly(glutamic acid)(mPEG-PLA-PLG)and poly(ethylene glycol)monomethyl ether-poly(D, L-lactic acid)-poly lysine(mPEG-PLA-PLL)were prepared. The enhanced stability of the new micelle was attributed to electrostatic attraction. The target products were obtained by reacting the amino boded terminal hydroxyl group of mPEG-PLA with cyclic carboxylic acid anhydridesof glutamic acid and lysine, respectively through ring opening reaction, and subsequent protecting group removal. Their structures were identified by 1H NMR and IR, and the differences of the critical micelle concentration(CMC)between mPEG-PLA and the modified polymers were measured by fluorescence. Dialysis was empolyed to prepare deoxypodophyllotoxin loaded polymeric micelles. The drug-loading capacity and encapsulation efficiency of mPEG-PLA micelles and electroneutral polyion complex micelle were determined by HPLC. The change of their particle size and drug content in 25 °C water bath were assessed by laser particle analyzer(dynamic light scattering)and HPLC, respectively. Both micelles had low CMC value and similar drug-loading capacity and encapsulation efficiency. However, the stability of the polymer complex micelles was two times higher than that of mPEG-PLA, which represented a significant enhancement. 

西安齐岳生物提供相关产品：

PLL(30)-g[3.5]-PEG(4)

PLL(30)-g[5]-PEG(4)

PLL-Azide(N3)

PLL-Alkyne (ALK)

PLL-Biotin (Bio)

PLL-Thiol(SH)

PLL-aldehyde

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