Raeisi Estabragh Mohammad Amin, Behnam Behzad, Torkzadeh-Mahani Masoud, Pardakhty Abbas
Student Research Committee, Kerman University of Medical Sciences, Kerman, Iran.
Pharmaceutics Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran.
Adv Pharm Bull. 2024 Dec 30;14(4):836-845. doi: 10.34172/apb.43228. Epub 2024 Oct 2.
Sorafenib is known as one of the oral anti-cancer drugs used in liver cancer. However, its lipophilic nature can lead to side effects, variable pharmacokinetics, and poor absorption. The use of novel drug delivery systems, such as niosomes, may help address these issues and improve the effectiveness of sorafenib.
Different niosomal formulations of sorafenib were prepared. The morphology, size analysis, and physical stability were investigated. The encapsulation efficiency percent of the selected formulations was measured using the dialysis method, and the release of sorafenib was checked for four hours using the Franz diffusion cell. The cytotoxicity and effect on the HepG2 cell line was investigated using the MTT assay and flow cytometry.
The mean volume diameter of Span 60/Tween 60/cholesterol (45/45/10 mole%) niosomal formulation was 6 µm with minimal size changes and good stability over six months of storage. The encapsulation efficiency percent of this formulation was 66.40±1.11, and 61.43±1.42 percent of the drug was released within 4 hours. release followed Higuchi kinetics. Cytotoxicity tests showed an IC of 7.5 µg/mL for the niosomal formulation, compared to 15.96 µg/mL for the sorafenib solution.
Niosomes containing Span 60/ Tween 60/ cholesterol (45/45/10 mole%) are promising for loading and sustained release of sorafenib. The use of niosome as a carrier can enhance the effectiveness of sorafenib on the HepG2 cell line. This niosomal formulation of sorafenib shows potential for future studies.
索拉非尼是用于肝癌治疗的口服抗癌药物之一。然而，其亲脂性会导致副作用、药代动力学变异性和吸收不良。使用新型药物递送系统，如脂质体，可能有助于解决这些问题并提高索拉非尼的有效性。
制备了索拉非尼的不同脂质体制剂。研究了其形态、尺寸分析和物理稳定性。使用透析法测量所选制剂的包封率，并使用Franz扩散池检查索拉非尼4小时的释放情况。使用MTT法和流式细胞术研究对HepG2细胞系的细胞毒性和作用。
Span 60/Tween 60/胆固醇（45/45/10摩尔%）脂质体制剂的平均体积直径为6 µm，在储存6个月期间尺寸变化最小且稳定性良好。该制剂的包封率为66.40±1.11，4小时内61.43±1.42%的药物被释放。释放遵循Higuchi动力学。细胞毒性测试显示脂质体制剂的IC为7.5 µg/mL，而索拉非尼溶液为15.96 µg/mL。
含有Span 60/Tween 60/胆固醇（45/45/10摩尔%）的脂质体在索拉非尼的负载和缓释方面具有潜力。使用脂质体作为载体可增强索拉非尼对HepG2细胞系的有效性。这种索拉非尼脂质体制剂显示出未来研究的潜力。
