Encapsulation of synthesized purpurin-18-N-aminoimide methyl ester in lipid nanovesicles for use as agents in photodynamic cancer therapy.

IF 3.7 3区 医学 Q2 CHEMISTRY, MEDICINAL Journal of pharmaceutical sciences Pub Date : 2025-01-19 DOI:10.1016/j.xphs.2025.01.001
Sooho Yeo, Huiqiang Wu, Young Kyu Song, Il Yoon, Woo Kyoung Lee
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Abstract

This study aimed to synthesize purpurin-18-N-aminoimide methyl ester (P18 N AI ME) and encapsulate it into lipid nanovesicles (LNVs) for potential application as photodynamic therapy (PDT) agents in cancer therapy. PDT, a light-induced treatment, offers several advantages over conventional cancer treatments, such as minimal invasiveness and localized action. P18 N AI ME, a chlorine class photosensitizer model drug, was synthesized in an attempt to treat tumor in deeper tissues by interacting long-wavelength light. LNVs were introduced to improve anticancer effect and photostability of P18 N AI ME. LNVs using glycerol monostearate demonstrated smaller particle sizes and more sustained release profiles than those using lauric acid. In photocytotoxicity against HeLa (human cervical carcinoma) and A549 (human lung carcinoma) cell lines, P18 N AI ME-LNVs demonstrated safety under dark conditions and enhanced anticancer effects under light conditions compared to P18 N AI ME alone. The inhibitory concentration values (IC50) were 0.86 μM (P18 N AI ME) and 0.68 μM (LNVs) in HeLa cell line and 0.85 μM (P18 N AI ME) and 0.64 μM (LNVs) in A549 cell line. These findings suggest that P18 N AI ME-LNVs hold promise as PDT agents in cancer therapy.

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合成紫嘌呤-18- n-氨基亚胺甲酯在脂质纳米囊泡中的包封及其在光动力癌症治疗中的应用。
本研究旨在合成紫嘌呤-18-N-氨基酰亚胺甲酯(P18 N AI ME)并将其包封于脂质纳米囊泡(LNVs)中,作为光动力治疗(PDT)药物在癌症治疗中的潜在应用。PDT是一种光诱导治疗方法,与传统的癌症治疗方法相比,它有几个优点,比如微创和局部作用。合成氯类光敏剂模型药物P18 N AI ME,试图通过长波光相互作用治疗深层组织肿瘤。引入LNVs来提高p18nai ME的抗癌效果和光稳定性。使用单硬脂酸甘油的LNVs比使用月桂酸的LNVs显示出更小的颗粒尺寸和更持久的释放曲线。在对HeLa(人宫颈癌)和A549(人肺癌)细胞株的光毒性实验中,与单独使用P18 N AI ME相比,P18 N AI ME- lnvs在黑暗条件下表现出安全性,在光照条件下表现出更强的抗癌作用。对HeLa细胞株的IC50分别为0.86 μM (P18 N AI ME)和0.68 μM (LNVs),对A549细胞株的IC50分别为0.85 μM (P18 N AI ME)和0.64 μM (LNVs)。这些发现表明P18 N AI ME-LNVs有望成为癌症治疗中的PDT药物。
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来源期刊
CiteScore
7.30
自引率
13.20%
发文量
367
审稿时长
33 days
期刊介绍: The Journal of Pharmaceutical Sciences will publish original research papers, original research notes, invited topical reviews (including Minireviews), and editorial commentary and news. The area of focus shall be concepts in basic pharmaceutical science and such topics as chemical processing of pharmaceuticals, including crystallization, lyophilization, chemical stability of drugs, pharmacokinetics, biopharmaceutics, pharmacodynamics, pro-drug developments, metabolic disposition of bioactive agents, dosage form design, protein-peptide chemistry and biotechnology specifically as these relate to pharmaceutical technology, and targeted drug delivery.
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