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首页> 外文期刊>Artificial cells, nanomedicine, and biotechnology. >Folic acid conjugated nanoliposomes as promising carriers for targeted delivery of bleomycin
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Folic acid conjugated nanoliposomes as promising carriers for targeted delivery of bleomycin

机译：叶酸偶联的纳米脂质体作为博莱霉素靶向递送的有希望的载体

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Abstract Targeted drug delivery has received considerable attention due to its key role in improving therapeutic efficacy and reducing the side effects of anticancer drugs. Bleomycin (BLM) is an anticancer antibiotic with short half-life, low therapeutic and high side effects that limit its clinical applications. This study aims to evaluate the anticancer potential of folate-targeted liposomal bleomycin (FL-BLM) and its free-folate form (L-BLM) on two different cancer cell lines including human cervix carcinoma HeLa, and human breast carcinoma MCF-7 cells. Furthermore, the effect of FL-BLM in induction of apoptosis and cell cycle arrest was studied by flow cytometry. FL-BLM was prepared by thin film hydration method and folic acid was conjugated to nanoliposomes by post insertion technique. Anticancer activity was evaluated by MTT assay. The cytotoxicity of FL-BLM against HeLa cells was significantly increased compared to L-BLM and conventional BLM. Flow cytometry and annexin-V analysis indicated that FL-BLM effectively induced apoptosis and cell-cycle arrest in HeLa cells especially at G2/M phase. In addition, the uptake of FL-BLM by Hela cells was significantly increased as compared to the MCF-7 cells. Overall, our findings indicated that FL-BLM may be promising formulation for targeted drug delivery to folate receptor-positive tumour cells.
机译：摘要靶向药物递送由于其在提高治疗功效和减少抗癌药物副作用方面的关键作用而受到了广泛的关注。博来霉素（BLM）是一种抗癌抗生素，具有半衰期短，治疗效果差和副作用大等特点，限制了其临床应用。这项研究旨在评估针对叶酸的脂质体博来霉素（FL-BLM）及其游离叶酸形式（L-BLM）在两种不同的癌细胞系（包括人宫颈癌HeLa和人乳腺癌MCF-7细胞）上的抗癌潜力。此外，通过流式细胞术研究了FL-BLM在诱导凋亡和细胞周期停滞中的作用。通过薄膜水化法制备FL-BLM，并通过后插入技术将叶酸与纳米脂质体结合。通过MTT分析评估抗癌活性。与L-BLM和常规BLM相比，FL-BLM对HeLa细胞的细胞毒性显着增加。流式细胞仪和膜联蛋白-V分析表明，FL-BLM特别是在G2 / M期有效诱导HeLa细胞凋亡和细胞周期停滞。另外，与MCF-7细胞相比，Hela细胞对FL-BLM的摄取显着增加。总体而言，我们的研究结果表明，FL-BLM有望成为靶向药物向叶酸受体阳性肿瘤细胞递送的制剂。

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