文獻(xiàn)：聚乙二醇單甲醚-聚D,L-乳酸-聚谷氨酸/聚賴氨酸三嵌段復(fù)合膠束的制備及穩(wěn)定性

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

作者：唐麗丹， 沉艷， 屠家勝

節(jié)選：

為了提高原有聚乙二醇單甲醚-聚D, L-乳酸（mPEG-PLA）共聚物膠束的結(jié)構(gòu)穩(wěn)定性，制備了等比例聚乙二醇單甲醚-聚D, L-乳酸-聚谷氨酸（mPEG-PLA-PLG）和聚乙二醇單甲醚-聚D, L-乳酸-聚賴氨酸（mPEG-PLA-PLL）電中性聚離子復(fù)合膠束。新膠束穩(wěn)定性的提高歸因于靜電引力。mPEG-PLA氨基鍵合的端羥基分別與谷氨酸和賴氨酸的環(huán)狀羧酸酐發(fā)生開環(huán)反應(yīng)，再脫去保護(hù)基，得到目標(biāo)產(chǎn)物。采用核磁共振氫譜（1H NMR）和紅外光譜（IR）對(duì)結(jié)構(gòu)進(jìn)行表征，熒光法測(cè)定mPEG-PLA與改性聚合物的臨界膠束濃度（CMC）差異，采用透析法制備脫氧鬼臼毒素聚合物膠束，用高效液相色譜（HPLC）測(cè)定mPEG-PLA膠束和電中性聚離子復(fù)合膠束的載藥量和包封率，用激光粒度儀（動(dòng)態(tài)光散射）和HPLC分別測(cè)定25℃水浴中粒徑和藥物含量的變化。

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pg電子官方生物提供相關(guān)產(chǎn)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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