文獻：Folate-targeted etoposide-encapsulated lipid nanospheres

作者：Ram Reddy Patlolla &Venkateswarlu Vobalaboina

文獻鏈接：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.

脂質納米球（LN）是一種簡單的膠體藥物遞送系統，已被證明可用于親脂性抗癌藥物的全身遞送。工作表明，在LN中包封依托泊苷可以提高活性，進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的循環時間和穩定性。

本研究主要葉酸-PEG-DSPE對LN的靶向能力。在大豆油、雞蛋磷脂酰膽堿和PEG-DSPE的幫助下，制備了葉酸靶向（Fol-LNE）和非靶向（SLNE）依托泊苷包封的脂質納米球，有和沒有葉酸-PEG-DSPE。

使用不含依托泊苷的熒光標記靶向（Fol-LN）和非靶向（SLN）脂質納米球在KB細胞系中進行細胞攝取研究。共聚焦顯微鏡和流式細胞術結果發現，Fol-LN被KB細胞選擇性吸收，添加1 mM葉酸完全阻斷了這種吸收。

細胞毒性結果支持上述發現，依托泊苷溶液、Fol-LNE和Fol-LNE comp（與1 mM葉酸競爭）的IC50值分別為33、5和19μM。比較Fol-LNE與SLNE和依托泊苷商業制劑（ETP）在正常小鼠體內的組織分布。

研究表明，Fol-LNE給藥后腎臟中的依托泊苷濃度高于SLNE和ETP。

相關推薦：

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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