文献：Folate-targeted etoposide-encapsulated lipid nanospheres

作者：Ram Reddy Patlolla &Venkateswarlu Vobalaboina

文献链接：https://www.tandfonline.com/doi/abs/10.1080/10611860801945400

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.

脂质纳米球（LN）是一种简单的胶体药物递送系统，已被证明可用于亲脂性抗癌药物的全身递送。工作表明，在LN中包封依托泊苷可以提高活性，进一步包封聚乙二醇二硬脂酰磷脂酰乙醇胺（DSPE-PEG）可以增加LN的循环时间和稳定性。

本研究主要叶酸-PEG-DSPE对LN的靶向能力。在大豆油、鸡蛋磷脂酰胆碱和PEG-DSPE的帮助下，制备了叶酸靶向（Fol-LNE）和非靶向（SLNE）依托泊苷包封的脂质纳米球，有和没有叶酸-PEG-DSPE。

使用不含依托泊苷的荧光标记靶向（Fol-LN）和非靶向（SLN）脂质纳米球在KB细胞系中进行细胞摄取研究。共聚焦显微镜和流式细胞术结果发现，Fol-LN被KB细胞选择性吸收，添加1 mM叶酸完全阻断了这种吸收。

细胞毒性结果支持上述发现，依托泊苷溶液、Fol-LNE和Fol-LNE comp（与1 mM叶酸竞争）的IC50值分别为33、5和19μM。比较Fol-LNE与SLNE和依托泊苷商业制剂（ETP）在正常小鼠体内的组织分布。

研究表明，Fol-LNE给药后肾脏中的依托泊苷浓度高于SLNE和ETP。

相关推荐：

4-Arm PEG-DSPE

C12-PEG-COOH

C18-PEG-COOH

C18-PEGn-COOH

C18-PEGn-Hydrazide

C18-PEGn-Maleimide

C18-PEGn-N3 (N3: Azide)

C18-PEGn-NH2 (NH2: Amine)

C18-PEGn-NHS

C18-PEGn-OH

C18-PEGn-OPSS

C18-PEGn-SH (SH: Thiol)

mPEG-Cholesterol (mPEG-CLS)

mPEG-CONH-C12

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