Capsaicin-loaded folic acid-conjugated lipid nanoparticles for enhanced therapeutic efficacy in ovarian cancers
Capsaicin-loaded folic acid-conjugated lipid nanoparticles for enhanced therapeutic efficacy in ovarian cancers
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DOI：
10.1016/j.biopha.2017.04.097
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发表时间：
2017-07-01
影响因子：
7.5
通讯作者：
Wu, Shao-yu
中科院分区：
文献类型：
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作者：
Lv, Lin;Zhuang, Yu-xin;Wu, Shao-yu
在这项研究中，成功制备了叶酸缀合的脂质纳米粒，以增强辣椒素（CAP）在卵巢癌中的主动靶向作用。这些颗粒是纳米级的，在生理条件下表现出药物的受控释放。与非靶向系统相比，叶酸（FA）缀合系统在癌细胞中表现出明显更高的纳米颗粒摄取量。叶酸缀合的 CAP 负载脂质纳米颗粒 (CFLN) 在与癌细胞相互作用后通过受体介导的内吞机制被内化，并在癌细胞中产生更高的浓度。与非靶向纳米颗粒系统相比，CFLN 始终表现出明显更高的毒性作用。 CFLN 显示出显着更高的癌细胞凋亡，凋亡室中有近 39% 的细胞（早期和晚期），而负载 CAP 的脂质纳米颗粒 (CLN) 和 CAP 的凋亡率仅为 21%，且接近 11%。脂质纳米颗粒系统中药物的负载延长了药物在血液循环中的保留，并允许主动靶向特定的癌细胞。药物循环时间的延长归因于结构中聚乙二醇分子的防污性能。总体而言，研究强调，使用靶向部分可以增强纳米药物在实体瘤治疗中的治疗反应。 (C) 2017 Elsevier Masson SAS。版权所有。
sIn this study, folic acid-conjugated lipid nanoparticles were successfully prepared to enhance the active targeting of capsaicin (CAP) in ovarian cancers. The particles were nanosized and exhibited a controlled release of drug in the physiological conditions. The folic acid (FA)-conjugated system exhibited a remarkably higher uptake of nanoparticles in the cancer cells compared to that of non-targeted system. The folate-conjugated CAP-loaded lipid nanoparticles (CFLN) upon interacting with cancer cells were internalized via receptor-mediated endocytosis mechanism and resulted in higher concentration in the cancer cells. Consistently, CFLN showed a remarkably higher toxic effect compared to that of non-targeted nanoparticle system. CFLN showed significantly higher cancer cell apoptosis with nearly 39% of cells in apoptosis chamber (early and late) compared to only similar to 21% and similar to 11% for CAP-loaded lipid nanoparticles (CLN) and CAP. The loading of drug in the lipid nanoparticle system extended the drug retention in the blood circulation and allowed the active targeting to specific cancer cells. The prolonged circulation of drug attributed to the antifouling property of polyethylene glycol molecule in the structure. Overall, study highlights that using targeting moiety could enhance the therapeutic response of nanomedicines in the treatment of solid tumors. (C) 2017 Elsevier Masson SAS. All rights reserved.