Kedar Tukaram, Jalalpure Sunil, Kurangi Bhaskar
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.
Ther Deliv. 2024 Apr 19;15(5):355-69. doi: 10.4155/tde-2023-0146.
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.
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。