Myat Yin Yin, Ngawhirunpat Tanasait, Rojanarata Theerasak, Opanasopit Praneet, Bradley Mark, Patrojanasophon Prasopchai, Pornpitchanarong Chaiyakarn
Pharmaceutical Development of Green Innovations Group (PDGIG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
School of Chemistry, University of Edinburgh, David Brewster Road, Edinburgh EH9 3FJ, UK.
Pharmaceutics. 2022 Feb 22;14(3):479. doi: 10.3390/pharmaceutics14030479.
Doxorubicin (Dox) is known for its potential to deliver desirable anticancer effects against various types of cancer including colorectal cancer. However, the adverse effects are serious. This study aimed to synthesize polyethylene glycol diacrylate (PEGDA)/acrylic acid (AA)-based nanoparticles (PEGDA/AA NPs) for Dox delivery to colorectal cancer cells. The NPs were synthesized using free-radical polymerization reaction using the monomers PEGDA and AA with their physical properties, drug loading and release, biocompatibility, and anticancer effect evaluated. The NPs were spherical with a size of around 230 nm, with a 48% Dox loading efficiency and with loading capacity of 150 µg/mg. Intriguingly, the NPs had the ability to prolong the release of Dox in vitro over 24 h and were non-toxic to intestinal epithelial cells. Dox-loaded PEGDA/AA NPs (Dox-NPs) were able to effectively kill the colorectal cancer cell line (HT-29) with the Dox-NPs accumulating inside the cell and killing the cell through the apoptosis pathway. Overall, the synthesized PEGDA/AA NPs exhibit considerable potential as a drug delivery carrier for colon cancer-directed, staged-release therapy.
阿霉素（Dox）以其对包括结直肠癌在内的多种癌症具有理想的抗癌效果而闻名。然而，其副作用严重。本研究旨在合成基于聚乙二醇二丙烯酸酯（PEGDA）/丙烯酸（AA）的纳米颗粒（PEGDA/AA NPs），用于将阿霉素递送至结直肠癌细胞。通过自由基聚合反应，使用单体PEGDA和AA合成纳米颗粒，并对其物理性质、药物负载与释放、生物相容性以及抗癌效果进行评估。纳米颗粒呈球形，尺寸约为230 nm，阿霉素负载效率为48%，负载量为150 µg/mg。有趣的是，纳米颗粒能够在体外将阿霉素的释放延长超过24小时，并且对肠上皮细胞无毒。负载阿霉素的PEGDA/AA纳米颗粒（Dox-NPs）能够有效杀死结直肠癌细胞系（HT-29），Dox-NPs在细胞内积累并通过凋亡途径杀死细胞。总体而言，合成的PEGDA/AA NPs作为结肠癌定向、缓释治疗的药物递送载体具有相当大的潜力。
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