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使用载有新型抗肿瘤药物 LA67 的纳米胶束提高结肠癌的抗肿瘤效果。

Improved Antitumor Outcomes for Colon Cancer Using Nanomicelles Loaded with the Novel Antitumor Agent LA67.

机构信息

Department of Gastroenterology, Yanbian University Hospital, Yanji 133000, Jilin, People's Republic of China.

State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.

出版信息

Int J Nanomedicine. 2020 May 19;15:3563-3576. doi: 10.2147/IJN.S241577. eCollection 2020.

DOI:10.2147/IJN.S241577
PMID:32547014
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7245463/
Abstract

BACKGROUND

LA67 is a derivative of triptolide that exhibits strong antitumor activity. This derivative has a better safety profile than triptolide, but is limited by poor aqueous solubility.

AIM AND METHODS

To improve solubility and further increase therapeutic efficacy, we prepared LA67-loaded polymeric micelles (LA67-PMs) using a film hydration method. The physicochemical properties of LA67-PMs were investigated, and the antitumor activity of this formulation against Colon26 (C26) cancer cell line was evaluated in vitro and in vivo with LA67 as a control.

RESULTS

Polymeric micelles containing LA67 had a particle size of 17.88 nm and a drug entrapment efficiency of 94.84%. This formulation dispersed completely in aqueous solution and exhibited slow, sustained release of LA67. Cellular uptake assay showed that LA67-PMs delivered LA67 to cancer cells with greater efficiency than free LA67, which resulted in increased LA67 accumulation in cancer cells. Cell counting kit 8 (CCK-8) assay showed that blank polymeric micelles (PMs) exhibited low toxicity and LA67-PMs exerted pronounced anti-proliferation effects against C26 cells. Furthermore, LA67-PMs induced apoptosis and repressed migration more effectively than free LA67. In vivo evaluation of antitumor activity showed that LA67-PMs inhibited tumor growth and distant organ metastasis to a greater extent than LA67, which resulted in improved survival rate. The potential mechanisms of these effects may have been induction of apoptosis, inhibition of cell proliferation, and neovascularization.

CONCLUSION

Our study showed that LA67-PMs may be a promising formulation for treatment of colon cancer.

摘要

背景

LA67 是雷公藤内酯醇的衍生物，具有很强的抗肿瘤活性。该衍生物比雷公藤内酯醇安全性更好，但由于水溶性差而受到限制。

目的和方法

为了提高溶解度并进一步提高治疗效果，我们使用薄膜水化法制备了 LA67 载药聚合物胶束（LA67-PMs）。研究了 LA67-PMs 的理化性质，并以 LA67 为对照，评价了该制剂对 Colon26（C26）癌细胞系的体内外抗肿瘤活性。

结果

载有 LA67 的聚合物胶束粒径为 17.88nm，药物包封率为 94.84%。该制剂在水溶液中完全分散，表现出 LA67 的缓慢、持续释放。细胞摄取实验表明，LA67-PMs 比游离 LA67 更有效地将 LA67 递送到癌细胞中，从而导致癌细胞中 LA67 的积累增加。细胞计数试剂盒 8（CCK-8）试验表明，空白聚合物胶束（PMs）毒性低，LA67-PMs 对 C26 细胞表现出明显的抗增殖作用。此外，LA67-PMs 诱导凋亡和抑制迁移的效果比游离 LA67 更有效。体内抗肿瘤活性评价表明，LA67-PMs 比 LA67 更能抑制肿瘤生长和远处器官转移，从而提高了生存率。这些作用的潜在机制可能是诱导细胞凋亡、抑制细胞增殖和新生血管形成。

结论

本研究表明，LA67-PMs 可能是治疗结肠癌的一种有前途的制剂。

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