Polyglycerol fatty acid esters as alternatives to PEGylated lipids for liposome coating
Polyglycerol fatty acid esters as alternatives to PEGylated lipids for liposome coating
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聚甘油脂肪酸酯作为脂质体涂层聚乙二醇化脂质的替代品
DOI：
10.2217/nnm-2022-0101
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发表时间：
2022
期刊：
影响因子：
5.5
通讯作者：
Qianyu Zhang
中科院分区：
文献类型：
--
作者：
Huali Chen;Qianyu Zhang
背景资料：聚甘油（PG）是一种具有生物相容性的亲水性聚醚多元醇，被认为是聚乙二醇（PEG）改性纳米药物的潜在替代品。材料和方法：将聚甘油脂肪酸酯（PGFEs）修饰到脂质体上，并与聚乙二醇化脂质体（PEG-Lips）比较其血清稳定性、药代动力学、体内分布和诱导抗PEG IgM抗体的能力。结果如下：聚甘油10-单硬脂酸酯（PG-10-MS）具有良好的血清稳定性和与小鼠红细胞的相容性，在药代动力学研究中，与未修饰的脂质体相比，它显著延长了脂质体的血液循环，其生物分布模式与PEG-Lips相似。此外，PGFE修饰的脂质体不太可能诱导抗PEG IgM的产生。结论：PGFEs可作为制备脂质体的理想材料。
Background: Polyglycerol (PG) is a type of biocompatible hydrophilic polyether polyol, and it is considered as a potential alternative to polyethylene glycol (PEG) in modifying nanomedicines. Materials & methods: Polyglycerol fatty acid esters (PGFEs) were modified onto liposomes and their serum stability, pharmacokinetics, in vivo distribution and the capacity to induce anti-PEG IgM were compared with PEGylated liposomes (PEG-Lips). Results: Polyglycerol 10-monostearate (PG-10-MS) displayed considerable serum stability and compatibility with mice red blood cells, and it significantly prolonged the blood circulation of liposomes in the pharmacokinetics study compared with the unmodified liposomes, with a similar biodistribution pattern to that of the PEG-Lips. Moreover, PGFE-modified liposomes were less likely to induce the production of anti-PEG IgM. Conclusion: PGFEs could be considered as good candidates to replace PEG lipids for the preparation of liposomes.