当前位置：
X-MOL 学术
›
Int. J. Nanomed.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Cationic Solid Lipid Nanoparticles of Resveratrol for Hepatocellular Carcinoma Treatment: Systematic Optimization, in vitro Characterization and Preclinical Investigation
International Journal of Nanomedicine ( IF 6.6 ) Pub Date : 2020-11-23 , DOI: 10.2147/ijn.s277545 Mahfoozur Rahman 1 , Waleed H Almalki 2 , Obaid Afzal 3 , Abdulmalik Saleh Alfawaz Altamimi 3 , Imran Kazmi 4 , Fahad A Al-Abbasi 4 , Hani Choudhry 5 , Sattam K Alenezi 6 , Md Abul Barkat 7 , Sarwar Beg 8 , Vikas Kumar 1 , Abdulsalam Alhalmi 9
International Journal of Nanomedicine ( IF 6.6 ) Pub Date : 2020-11-23 , DOI: 10.2147/ijn.s277545 Mahfoozur Rahman 1 , Waleed H Almalki 2 , Obaid Afzal 3 , Abdulmalik Saleh Alfawaz Altamimi 3 , Imran Kazmi 4 , Fahad A Al-Abbasi 4 , Hani Choudhry 5 , Sattam K Alenezi 6 , Md Abul Barkat 7 , Sarwar Beg 8 , Vikas Kumar 1 , Abdulsalam Alhalmi 9
Affiliation
Aim: The present study focuses on the development and evaluation of the resveratrol (RV)-loaded cationic solid lipid nanoparticles (RV-c-SLNs) for the management of hepatocellular carcinoma (HCC).
Materials and Methods: Optimization of formulation was performed using factorial design, and further in vitro drug release, cytotoxicity, biodistribution, in vivo preclinical, and biochemical evaluation were carried out.
Results: The optimized formulation exhibited uniform size, homogeneous disparity, positive zeta potential, and stability over 12-week storage at 25°C/60% RH. The in vitro drug release and cytotoxicity study showed 60% drug release within the first 6 hours and comparatively higher cytotoxicity on HepG2 cell line by resveratrol-solid lipid nanoparticle (RV-SLN) as compared to the RV solution. In addition, an anticancer action and biodistribution study on a rat model of HCC showed significant reduction of tumor volume and higher accumulation in the tumor tissue from RV-c-SLN (P< 0.01) over RV solution and RV-SLN. Furthermore, RV-c-SLN showed significant down-regulation in the levels of pro-inflammatory cytokines and balancing of antioxidant enzymes. Histopathological investigation showed reduced occurrence of hepatic nodules, necrosis formation, infiltration of inflammatory cells, blood vessels inflammation, and cell swelling.
Conclusion: Overall, the obtained results construed that RV-c-SLN with improved antitumor activity as clearly evident from in vitro, in vivo, and biochemical investigations.
Keywords: resveratrol, cationic solid lipid, solid lipid nanoparticles, inflammatory biomarkers, hepatocellular carcinoma, diethyl nitrosamine
中文翻译：
用于治疗肝细胞癌的白藜芦醇阳离子固体脂质纳米颗粒：系统优化、体外表征和临床前研究
目的：本研究的重点是开发和评估负载白藜芦醇 (RV) 的阳离子固体脂质纳米颗粒 (RV-c-SLNs) 用于治疗肝细胞癌 (HCC)。
材料与方法：采用析因设计对制剂进行优化，进一步进行体外药物释放、细胞毒性、生物分布、体内临床前和生化评价。
结果：优化后的配方在 25°C/60% RH 下储存 12 周后表现出均匀的尺寸、均匀的差异、正 zeta 电位和稳定性。体外药物释放和细胞毒性研究表明，与 RV 溶液相比，白藜芦醇固体脂质纳米颗粒 (RV-SLN) 在前 6 小时内释放了 60% 的药物，并且对 HepG2 细胞系的细胞毒性相对较高。此外，一项针对 HCC 大鼠模型的抗癌作用和生物分布研究表明，RV-c-SLN 可显着减少肿瘤体积，并在肿瘤组织中积累更多（P< 0.01) 在 RV 溶液和 RV-SLN 上。此外，RV-c-SLN 在促炎细胞因子水平和抗氧化酶平衡方面表现出显着下调。组织病理学检查显示肝结节、坏死形成、炎性细胞浸润、血管炎症和细胞肿胀的发生减少。
结论：总体而言，所获得的结果表明 RV-c-SLN 具有改善的抗肿瘤活性，这在体外、体内和生化研究中是显而易见的。
关键词：白藜芦醇，阳离子固体脂质，固体脂质纳米粒，炎症生物标志物，肝细胞癌，二乙基亚硝胺
更新日期：2020-11-23
Materials and Methods: Optimization of formulation was performed using factorial design, and further in vitro drug release, cytotoxicity, biodistribution, in vivo preclinical, and biochemical evaluation were carried out.
Results: The optimized formulation exhibited uniform size, homogeneous disparity, positive zeta potential, and stability over 12-week storage at 25°C/60% RH. The in vitro drug release and cytotoxicity study showed 60% drug release within the first 6 hours and comparatively higher cytotoxicity on HepG2 cell line by resveratrol-solid lipid nanoparticle (RV-SLN) as compared to the RV solution. In addition, an anticancer action and biodistribution study on a rat model of HCC showed significant reduction of tumor volume and higher accumulation in the tumor tissue from RV-c-SLN (P< 0.01) over RV solution and RV-SLN. Furthermore, RV-c-SLN showed significant down-regulation in the levels of pro-inflammatory cytokines and balancing of antioxidant enzymes. Histopathological investigation showed reduced occurrence of hepatic nodules, necrosis formation, infiltration of inflammatory cells, blood vessels inflammation, and cell swelling.
Conclusion: Overall, the obtained results construed that RV-c-SLN with improved antitumor activity as clearly evident from in vitro, in vivo, and biochemical investigations.
Keywords: resveratrol, cationic solid lipid, solid lipid nanoparticles, inflammatory biomarkers, hepatocellular carcinoma, diethyl nitrosamine
中文翻译：
用于治疗肝细胞癌的白藜芦醇阳离子固体脂质纳米颗粒：系统优化、体外表征和临床前研究
目的：本研究的重点是开发和评估负载白藜芦醇 (RV) 的阳离子固体脂质纳米颗粒 (RV-c-SLNs) 用于治疗肝细胞癌 (HCC)。
材料与方法：采用析因设计对制剂进行优化，进一步进行体外药物释放、细胞毒性、生物分布、体内临床前和生化评价。
结果：优化后的配方在 25°C/60% RH 下储存 12 周后表现出均匀的尺寸、均匀的差异、正 zeta 电位和稳定性。体外药物释放和细胞毒性研究表明，与 RV 溶液相比，白藜芦醇固体脂质纳米颗粒 (RV-SLN) 在前 6 小时内释放了 60% 的药物，并且对 HepG2 细胞系的细胞毒性相对较高。此外，一项针对 HCC 大鼠模型的抗癌作用和生物分布研究表明，RV-c-SLN 可显着减少肿瘤体积，并在肿瘤组织中积累更多（P< 0.01) 在 RV 溶液和 RV-SLN 上。此外，RV-c-SLN 在促炎细胞因子水平和抗氧化酶平衡方面表现出显着下调。组织病理学检查显示肝结节、坏死形成、炎性细胞浸润、血管炎症和细胞肿胀的发生减少。
结论：总体而言，所获得的结果表明 RV-c-SLN 具有改善的抗肿瘤活性，这在体外、体内和生化研究中是显而易见的。
关键词：白藜芦醇，阳离子固体脂质，固体脂质纳米粒，炎症生物标志物，肝细胞癌，二乙基亚硝胺
京公网安备 11010802027423号