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立方体细胞纳米制剂可提高非瑟酮在A549肺癌细胞中的溶解度和抗癌活性。

Cubosomal nanoformulation increase dissolution and anticancer activity of Fisetin in A549 lung cancer cells.

作者信息

Kedar Tukaram, Jalalpure Sunil, Kurangi Bhaskar

机构信息

KLE College of Pharmacy, Belagavi, KLE Academy of Higher Education & Research, Nehru Nagar, Belagavi-590010, Karnataka, India.

Dr Prabhakar Kore Basic Science Research Center, KLE Academy of Higher Education & Research, Nehru Nagar, Belagavi-590010, Karnataka, India.

出版信息

Ther Deliv. 2024 Apr 19;15(5):355-69. doi: 10.4155/tde-2023-0146.

Abstract

To prepare fisetin (FIS) cubosomal nanoformulation to increase aqueous solubility and anticancer activity. Top-down method using glyceryl monooleate (GMO) and Pluronic F-127. Optimized using 2% GMO and 1% Pluronic F-127, reported 93.07 nm particle size, 80.10% drug entrapment, and reports more than 50% enhanced drug release than native FIS. MTT assay reports IC Values of FIS 16.59 μg/ml and optimized cubosomal FIS nanoformulation (FISCUB) 12.18 μg/ml. The colony numbers observed in clonogenic assay for FISCUB were 8.33 ± 0.58 and FIS 11.67 ± 1.15. In flow cytometry study, apoptotic cells in FISCUB and FIS-treated A549 cells were found to be 33.4 and 6.83% respectively. A stable cubosomal nanoformulation of FIS showed enhanced aqueous solubility and anticancer activity.

摘要

制备漆黄素(FIS)立方液晶纳米制剂以提高其水溶性和抗癌活性。采用自上而下的方法,使用单油酸甘油酯(GMO)和泊洛沙姆F - 127。使用2%的GMO和1%的泊洛沙姆F - 127进行优化,报道其粒径为93.07纳米,药物包封率为80.10%,且与天然FIS相比,药物释放增强超过50%。MTT试验报道FIS的IC值为16.59μg/ml,优化后的立方液晶FIS纳米制剂(FISCUB)的IC值为12.18μg/ml。在克隆形成试验中观察到FISCUB的集落数为8.33±0.58,FIS的集落数为11.67±1.15。在流式细胞术研究中,发现FISCUB和FIS处理的A549细胞中的凋亡细胞分别为33.4%和6.83%。稳定的FIS立方液晶纳米制剂显示出增强的水溶性和抗癌活性。

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