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作 者:林超 袁于民 LIN Chao;YUAN Yumin(School of Materials Science&Engineering,Zhejiang Sci-Tech University,Hangzhou 310018,China;Institute of Smart Biomedical Materials,Zhejiang Sci-Tech University,Hangzhou 310018,China;Biomatrik Inc.,Jiaxing 314001,China)
机构地区:[1]浙江理工大学材料科学与工程学院,杭州310018 [2]浙江理工大学智能生物材料研究所,杭州310018 [3]浙江博美生物技术有限公司,浙江嘉兴314001
出 处:《浙江理工大学学报(自然科学版)》2024年第6期743-752,共10页Journal of Zhejiang Sci-Tech University(Natural Sciences)
摘 要:聚乙二醇(Polyethylene glycol,PEG)化胶束在体外的稳定性是其作为纳米药物载体的重要参考指标。将不同分散性和结构的PEG,与十八烷酸、十四烷酸、1,2-二硬脂酸-3-磷脂酰乙醇、胆固醇、维生素E琥珀酸酯、N,N-双十四烷基胺和抗癌药物紫杉醇等合成一系列两亲性聚合物;分析在相同疏水段的条件下,PEG的分散性和结构对其胶束临界胶束浓度(Critical micelle concentration,CMC)、粒径以及在牛血清白蛋白(BSA)溶液中的稳定性的影响。结果显示:PEG的分散性对线形PEG化胶束的CMC和粒径影响不明显,分支结构的PEG化胶束在CMC和粒径上均显著小于线形PEG化胶束;在BSA溶液中,分支结构的PEG化胶束的稳定性显著优于线形单分散的,多分散PEG化胶束的稳定性最差,PEG结构和分散性影响胶束的体外稳定性。该文结果为开发单分散PEG化胶束的药物递送系统提供了重要的理论依据。The in vitro stability of polyethylene glycol(PEG)-modified micelles is a crucial factor for their application as nanocarriers for drug delivery.A series of amphiphilic polymers were synthesized by using PEGs with different dispersities and structures,combined with octadecanoic acid,tetradecanoic acid,1,2-distearoyl-sn-glycero-3-phosphoethanolamine,cholesterol,vitamin E succinate,N,N-ditetradecylamine,and the anticancer drug paclitaxel.The study investigated the effects of PEG′s dispersity and structure on the critical micelle concentration(CMC),particle size,and stability in bovine serum albumin(BSA)solutions under the same hydrophobic segment conditions.The results show that the dispersion of PEG has little effect on the CMC and particle size of linear PEGylated micelles,while the branched PEGylated micelles are significantly smaller in CMC and particle size than linear PEGylated micelles;the stability of branched PEGylated micelles in BSA solutions is superior to that of their linear monodisperse counterparts,while the stability of polydisperse PEGylated micelles is unsatisfactory.PEG structure and dispersity affect the in vitro stability of micelles.The results of this paper provide important reference for the development of drug delivery systems with monodisperse PEG micelles.
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