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pH敏感型mPEG-Hz-PLA聚合物納米載藥膠束的制備

發(fā)布時(shí)間:2018-06-11 13:34

  本文選題:mPEG-Hz-PLA聚合物 + 膠束; 參考:《高分子學(xué)報(bào)》2017年03期


【摘要】:以合成的含有腙鍵的聚乙二醇大分子(mPEG-Hz-OH)為引發(fā)劑,以丙交酯為單體引發(fā)開(kāi)環(huán)聚合反應(yīng),并通過(guò)調(diào)整投料比,制備出3種不同分子量的含腙鍵的生物可降解嵌段聚合物(mPEG-Hz-PLA).將腙鍵引入到聚合物的骨架中,以此構(gòu)建聚合物膠束并作為pH敏感型納米藥物載體.制備的pH敏感型膠束的CMC值等于或低于5.46×10-4 mg/m L,DLS和TEM顯示粒徑均小于100 nm,且粒徑分布均勻.非pH敏感型膠束在不同pH下的粒徑變化不明顯,而pH敏感型膠束在酸性環(huán)境下(pH=4.0和pH=5.0)膠束粒徑出現(xiàn)了明顯變化.以阿霉素為模型藥物制備了pH敏感型載藥膠束,其粒徑比空白膠束大(100~200 nm),且粒徑分布均勻.藥物釋放實(shí)驗(yàn)表明pH敏感型載藥膠束隨著釋放介質(zhì)pH降低累積釋藥量增高.MTT實(shí)驗(yàn)表明空白膠束對(duì)HeLa細(xì)胞和RAW264.7細(xì)胞幾乎沒(méi)有抑制作用,而載阿霉素的膠束對(duì)2種細(xì)胞的抑制作用都隨著劑量的增大和時(shí)間的延長(zhǎng)而增強(qiáng).
[Abstract]:Three kinds of biodegradable block polymers containing Hydrazone bond were prepared by using poly (ethylene glycol) macromolecule containing Hydrazone bond as initiator, lactide as monomer to initiate ring-opening polymerization, and by adjusting the feed ratio. Hydrazone bond was introduced into the framework of polymer to construct polymer micelle and used as pH sensitive drug carrier. The mg/m values of pH sensitive micelles were equal to or less than 5.46 脳 10-4 mg/m DLS and Tem showed that the particle size of the prepared micelles was less than 100nmand the particle size distribution was uniform. The particle size of non-pH sensitive micelles did not change obviously at different pH values, but the particle size of pH sensitive micelles changed obviously in acidic environment (pH 4. 0 and pH 5. 0). The pH-sensitive drug loaded micelles were prepared using adriamycin as the model drug. The particle size of the micelles was larger than that of the blank micelles, and the particle size distribution was uniform. Drug release assay showed that pH-sensitive drug carrier micelles increased with the decrease of release medium pH. MTT assay showed that the blank micelles had little inhibitory effect on HeLa cells and RAW264.7 cells. The inhibitory effects of adriamycin-loaded micelles on both cells increased with the increase of dose and time.
【作者單位】: 河南大學(xué)藥物研究所;
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