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首页> 美国卫生研究院文献>Materials >Surface Modification of Liposomes by a Lipopolymer Targeting Prostate Specific Membrane Antigen for Theranostic Delivery in Prostate Cancer
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Surface Modification of Liposomes by a Lipopolymer Targeting Prostate Specific Membrane Antigen for Theranostic Delivery in Prostate Cancer

机译：脂质体靶向前列腺特异性膜抗原的脂质体的表面修饰用于前列腺癌的经皮给药

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摘要

Prostate specific membrane antigen (PSMA) is a marker for diagnosis and targeted delivery of therapeutics to advanced/metastasized prostate cancer. We report a liposome-based system for theranostic delivery to PSMA-expressing (PSMA+) LNCaP cells. A lipopolymer (P3) comprising of PSMA ligand (PSMAL), polyethylene glycol (PEG2000), and palmitate was synthesized and post-inserted into the surface of preformed liposomes. These P3-liposomes were loaded with doxorubicin and radiolabeled with 99mTc radionuclide to study their theranostic characteristics. Differential expression of PSMA on LNCaP and PC3 cells was confirmed by immunoblotting as well as by uptake of PSMAL labeled with 18F radionuclide. We found that the uptake of 99mTc-labeled P3-liposomes by LNCaP cells was >3-fold higher than 99mTc-labeled Plain-liposomes; the amount of doxorubicin delivered to LNCaP cells was also found to be >3-fold higher by P3-liposomes. Cell-based cytotoxicity assay results showed that doxorubicin-loaded P3-liposomes were significantly more toxic to LNCaP cells (p < 0.05), but not to PSMA-negative PC3 cells. Compared to doxorubicin-loaded Plain-liposomes, the IC50 value of doxorubicin-loaded P3-liposomes was reduced by ~5-fold in LNCaP cells. Together, these results suggest that surface functionalization of liposomes with small PSMA-binding motifs, such as PSMAL, can provide a viable platform for specific delivery of theranostics to PSMA+ prostate cancer.
机译：前列腺特异性膜抗原（PSMA）是诊断和靶向治疗向晚期/转移性前列腺癌的标志物。我们报告了一个基于脂质体的系统，用于向表达PSMA（PSMA + ）的LNCaP细胞进行诊断治疗。合成了由PSMA配体（PSMAL），聚乙二醇（PEG2000）和棕榈酸酯组成的脂聚合物（P 3 ），然后将其插入到预先制成的脂质体表面。这些P 3 -脂质体中装有阿霉素，并用 99m Tc放射性核素进行放射性标记，以研究其治疗学特性。免疫印迹以及 18 F放射性核素标记的PSMAL的摄取证实了PSMA在LNCaP和PC3细胞上的差异表达。我们发现，LNCaP细胞对 99m Tc标记的P 3 -脂质体的摄取是 99m Tc标记的平原的> 3倍以上-脂质体； P 3 -脂质体还发现传递给LNCaP细胞的阿霉素的量高3倍以上。基于细胞的细胞毒性测定结果表明，负载阿霉素的P 3 -脂质体对LNCaP细胞的毒性更高（p <0.05），而对PSMA阴性的PC3细胞没有毒性。与载有阿霉素的普通脂质体相比，载有阿霉素的P 3 -脂质体的IC50值在LNCaP细胞中降低了约5倍。总之，这些结果表明，具有较小PSMA结合基序的脂质体的表面功能化（例如PSMAL）可为将治疗药物特异性递送至PSMA + 前列腺癌提供可行的平台。

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