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叶酸-PEG-DSPE赋予脂质纳米球对FR+细胞的选择性摄取能力
发布时间:2025-07-18     作者:zyl   分享到:
期刊论文:Folate-targeted etoposide-encapsulated lipid nanospheres我:Ram Reddy Patlolla &Venkateswarlu Vobalaboina参考文献联接: 论文摘要:Lipid nanospheres (LN) are simple colloidal drug delivery systems, which are proven to be useful for the systemic delivery of lipophilic anticancer drugs. Our previous work shows that the encapsulation of etoposide in LN improved the anticancer activity and a further inclusion of polyethylene glycol-distearoylphosphatidylethanolamine (DSPE-PEG) increased the circulation time and stability of LN. The present study is focused on the targeting ability of LN using Folate-PEG-DSPE. Folate-targeted (Fol-LNE) and non-targeted (SLNE) etoposide-encapsulated lipid nanospheres were prepared with the help of soybean oil, egg phosphatidylcholine, and PEG-DSPE with and without Folate-PEG-DSPE. The anticancer activity of these formulations was assessed in KB cell line. Cell uptake studies were carried out in KB cell lines using fluorescent-labeled targeted (Fol-LN) and non-targeted (SLN) lipid nanospheres without etoposide. Confocal microscopy and flow cytometry results found that, Fol-LN was selectively taken up by the KB cells and the addition of 1 mM folic acid completely blocked this uptake. Cytotoxicity results support the above finding, the IC50 values of etoposide solution, Fol-LNE, and Fol-LNE-comp (competition with 1 mM folic acid) were 33, 5, and 19 μM, respectively. Tissue distribution of Fol-LNE was compared with that of SLNE and etoposide commercial formulation (ETP) in normal mice. The studies show that in the kidney etoposide concentration was higher following Fol-LNE administration than SLNE and ETP.

脂质纳米级球(LN)有的是种很简单的电解质溶液药品递送系统性,已被验证能够 使用于亲脂性治癌药品的下半身递送。工作上证明,在LN中包封依托于泊苷能够 提高自己抗逆性,提高认识骤包封聚乙二醇二硬脂酰磷脂酰酒精胺(DSPE-PEG)能够 加入LN的重复日期和比较稳确定。本的研究常见备孕备孕孕妇叶酸-PEG-DSPE对LN的靶向疗法治疗疗法水平。在玉米油、章鱼磷脂酰胆碱和PEG-DSPE的关心下,化学合成了备孕备孕孕妇叶酸靶向疗法治疗疗法(Fol-LNE)和非靶向疗法治疗疗法(SLNE)推进泊苷包封的脂质纳米级球,有和没了备孕备孕孕妇叶酸-PEG-DSPE。便用不含有助推泊苷的荧光标签靶向药物治疗(Fol-LN)和非靶向药物治疗(SLN)脂质纳米技术球在KB神经元系中进行神经元摄取量探究。共焦聚电子显微镜和流式生殖癌细胞神经元术最终结果感觉,Fol-LN被KB神经元确定性挥发,“添加1 mMDHA非常抑制了这样的挥发。团队细胞致癌性但是认可上述所说发觉,充分发挥泊苷盐溶液、Fol-LNE和Fol-LNE comp(与1 mMDHA行业竞争)的IC50值差别为33、5和19μM。相对Fol-LNE与SLNE和充分发挥泊苷行业药物制剂(ETP)在正常情况小鼠休内的团队区域。深入分析是因为,Fol-LNE给药后肾脏中的依附泊苷质量浓度高过SLNE和ETP。相关推送:4-Arm PEG-DSPEC12-PEG-COOHC18-PEG-COOHC18-PEGn-COOHC18-PEGn-HydrazideC18-PEGn-MaleimideC18-PEGn-N3 (N3: Azide)C18-PEGn-NH2 (NH2: Amine)C18-PEGn-NHSC18-PEGn-OHC18-PEGn-OPSSC18-PEGn-SH (SH: Thiol)mPEG-Cholesterol (mPEG-CLS)mPEG-CONH-C12


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