索拉非尼药物递送载体Niosome的制备、理化性质研究及其对HepG2细胞系的体外作用

IF 3.1 Q2 PHARMACOLOGY & PHARMACY
Advanced pharmaceutical bulletin Pub Date : 2024-12-30 Epub Date: 2024-10-02 DOI:10.34172/apb.43228
Mohammad Amin Raeisi Estabragh, Behzad Behnam, Masoud Torkzadeh-Mahani, Abbas Pardakhty
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引用次数: 0

摘要

目的:众所周知,索拉非尼是用于治疗肝癌的口服抗癌药物之一。然而,索拉非尼的亲脂性可能会导致副作用、药代动力学多变和吸收不良。使用新型给药系统(如niosomes)可能有助于解决这些问题并提高索拉非尼的疗效:方法:制备了不同的索拉非尼niosomal制剂。方法:制备了不同的索拉非尼niosomal制剂,对其形态、粒度分析和物理稳定性进行了研究。采用透析法测量了所选制剂的包封效率百分比,并使用弗朗兹扩散池检测了索拉非尼四小时的释放情况。使用 MTT 法和流式细胞术研究了对 HepG2 细胞株的细胞毒性和体外效应:结果:Span 60/Tween 60/cholesterol (45/45/10 mole%) niosomal 配方的平均体积直径为 6 微米,尺寸变化极小,储存 6 个月后稳定性良好。该制剂的封装效率为 66.40±1.11%,61.43±1.42%的药物在 4 小时内释放。体外释放遵循樋口动力学。细胞毒性测试表明,与索拉非尼溶液的 15.96 微克/毫升相比,niosomal 制剂的 IC50 为 7.5 微克/毫升:含有司盘 60/ 吐温 60/ 胆固醇(45/45/10 摩尔%)的niosomes具有装载和持续释放索拉非尼的前景。使用niosome作为载体可以增强索拉非尼对HepG2细胞系的疗效。这种索拉非尼的niosomal制剂显示了未来研究的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Niosome as a Drug Delivery Carrier for Sorafenib: Preparation, Investigation of Physicochemical Properties, and In Vitro Effects on HepG2 Cell Line.

Purpose: 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.

Methods: 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 in vitro effect on the HepG2 cell line was investigated using the MTT assay and flow cytometry.

Results: 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. In vitro release followed Higuchi kinetics. Cytotoxicity tests showed an IC50 of 7.5 µg/mL for the niosomal formulation, compared to 15.96 µg/mL for the sorafenib solution.

Conclusion: 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.

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来源期刊
Advanced pharmaceutical bulletin
Advanced pharmaceutical bulletin PHARMACOLOGY & PHARMACY-
CiteScore
6.80
自引率
2.80%
发文量
51
审稿时长
12 weeks
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