PEGylated Water‐Soluble Organic Nanoparticles with Chlorin Derivative for Biocompatible Photodynamic Therapy In Vitro and In Vivo,ChemNanoMat

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PEGylated Water‐Soluble Organic Nanoparticles with Chlorin Derivative for Biocompatible Photodynamic Therapy In Vitro and In Vivo
ChemNanoMat ( IF 2.6 ) Pub Date : 2020-11-06 , DOI: 10.1002/cnma.202000535
Yang Liu ₁ , Min Seob Lee ₂ , Sang Hyeob Lee ₁ , Hyeon Ho Song ₁ , Bo Sun Baek ₁ , Woo Kyoung Lee ₁ , Yeon‐Jeong Kim _{2,

3} , Il Yoon ₁

Affiliation

Photodynamic therapy (PDT) is a non‐invasive and highly selective therapeutic approach. Photosensitizers (PSs) are an essential ingredient in PDT. However, many PSs are hydrophobic and insoluble, seriously restraining their clinical use. In this study, we prepared biocompatible PSs using water‐soluble organic nanoparticles (WSONs) with a chlorin derivative, pyropheophorbide a (PPa), and polyethylene glycol (PEG) to overcome the limited clinical applications of PDT. Among the PEGylated WSONs (WSON‐PEGs), WSON‐PEG 3400 and 2000 exhibited good water solubility and stability, with no aggregation in aqueous media, a high photoactivity, and low dark toxicity in vitro against A549 and HeLa cells. An in vivo application of WSON‐PEG 3400 using A549 tumour‐bearing BALB/c nude mice demonstrated a three‐fold higher PDT efficacy compared with the control and drug only groups, without treatment‐induced toxicity or toxic side effects. These results demonstrate that WSON‐PEG (3400) is a biocompatible PS with a high PDT efficacy and reduced dark toxicity, suitable for use in clinical trials.

中文翻译：

含氯衍生物的聚乙二醇化水溶性有机纳米颗粒，用于体内外生物相容性光动力疗法

光动力疗法（PDT）是一种非侵入性且高度选择性的治疗方法。光敏剂（PSs）是PDT中必不可少的成分。但是，许多PS疏水且不溶，严重限制了其临床应用。在这项研究中，我们使用水溶性有机纳米颗粒（WSON）与二氢卟酚衍生物，焦脱镁叶绿素a（PPa）和聚乙二醇（PEG）制备了生物相容性PS，以克服PDT在临床上的有限应用。在PEG化WSON（WSON-PEG）中，WSON-PEG 3400和2000表现出良好的水溶性和稳定性，在水性介质中没有聚集，在体外对A549和HeLa细胞具有高光活性和低暗毒性。一个在体内将WSON‐PEG 3400与A549荷瘤BALB / c裸鼠一起使用，显示PDT功效比对照组和仅药物组高三倍，而没有治疗诱导的毒性或毒性副作用。这些结果表明，WSON-PEG（3400）是一种生物相容性PS，具有较高的PDT功效和降低的暗毒性，适合用于临床试验。

更新日期：2020-11-06

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