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首页> 外文会议>Annual meeting exposition of the Controlled Release Society >Intracellular uptake of water soluble ZnPP micelles (SMA-ZnPP and PEG-ZnPP) and the unique release mechanism of the drug from their micelles.
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Intracellular uptake of water soluble ZnPP micelles (SMA-ZnPP and PEG-ZnPP) and the unique release mechanism of the drug from their micelles.

机译：水溶性ZnPP胶束（SMA-ZnPP和PEG-ZnPP）的细胞内吸收以及药物从其胶束的独特释放机制。

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SMA-ZnPP and PEG-ZnPP are miceller drugs, namely encapsulating Zinc protoporphyrin IX (ZnPP) with styrene maleic acid copolymer (SMA) and covalent conjugate of ZnPP with polyethyreneglycol (PEG) respectively. Cellular uptake rate and intracellular localization was investigated for each of them. We found SMA-ZnPP showed higher cellular uptake rate than PEG-ZnPP, although both SMA-ZnPP and PEG-ZnPP micelles were localized at endoplasmic reticulum (ER) and inhibited the target enzyme heme oxygenase 1 (HO-1) similarly. Miceller ZnPP are taken up into the tumor cells by endocytosis, and SMA-ZnPP are much efficient (about 5 times) than PEG-ZnPP. Furthermore SMA-ZnPP and PEG-ZnPP were examined for their drug releasing mechanism. Liberation of ZnPP from the SMA micelle appears to depend on cellular amphiphilic components such as lecithin, while that for PEG-ZnPP depend on hydrolytic cleavage such as esterase or proteases. These results indicate these micelle formulations make water insoluble ZnPP to water soluble practical anticancer agents.
机译：SMA-ZnPP和PEG-ZnPP是胶束药物，即分别用苯乙烯马来酸共聚物（SMA）封装原卟啉IX（ZnPP）和ZnPP与聚乙二醇（PEG）的共价共轭物。研究了它们各自的细胞摄取率和细胞内定位。我们发现，虽然SMA-ZnPP和PEG-ZnPP胶束均位于内质网（ER）并同样抑制目标酶血红素加氧酶1（HO-1），但SMA-ZnPP显示出比PEG-ZnPP更高的细胞摄取率。 Miceller ZnPP通过内吞作用被吸收到肿瘤细胞中，而SMA-ZnPP比PEG-ZnPP效率更高（约5倍）。此外，还检查了SMA-ZnPP和PEG-ZnPP的药物释放机理。从SMA胶束中释放ZnPP似乎依赖于细胞两亲性成分（例如卵磷脂），而PEG-ZnPP的释放依赖于水解裂解（例如酯酶或蛋白酶）。这些结果表明这些胶束制剂使水不溶性ZnPP成为水溶性实用抗癌剂。

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