索拉非尼负载重封红细胞治疗肝细胞癌。

Raj M Desai, Neha Desai, Munira Momin, Lokesh Kumar Bhatt
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引用次数: 0

摘要

背景:本研究旨在制备和表征负载索拉非尼的重封红细胞(sorafenib- reseal erythrocytes, sor),并研究其在大鼠肝细胞癌模型中的抗癌活性。方法:采用含药透析介质(2 ~ 10 mg/ml)和渗透时间(30 ~ 240 min)对Wistar大鼠红血球进行低渗透析。对优化后的体外释放酶(8mg /mL, 240 min)的大小、形态、稳定性、包封效率、体外释放谱和体内疗效评价进行了表征。为了进行疗效研究,我们将优化后的sov静脉注射给黄曲霉毒素B诱导肝细胞病变的Wistar大鼠,并监测其体内抗肿瘤活性。结果:索拉非尼的包封量与透析介质中药物浓度和渗透时间成正比;10 mg/mL和240分钟时最高,2 mg/mL和30分钟时最低。优化后的膜为双凹型,尺寸为112.7 nm, zeta电位为-11.95±2.25 mV。渗透性和湍流脆性与天然红细胞相当。结论:药物释放符合一级模式。体内研究显示,与索拉非尼标准制剂相比,sorafenib制剂具有更好的抗癌活性。负载索拉非尼的重封红细胞在肝细胞癌大鼠模型中显示出一级体外释放和有希望的抗癌活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Sorafenib Loaded Resealed Erythrocytes for the Treatment of Hepatocellular Carcinoma.

Background: This study aims to formulate and characterize sorafenib-loaded resealed erythrocytes (SoRE) and investigate their anticancer activity in a rat model of hepatocellular carcinoma.

Methods: SoRE were prepared by hypotonic dialysis of red blood cells obtained from Wistar rats using a range of drug-containing dialysis mediums (2-10 mg/ml) and osmosis time (30-240 mins). Optimized SoRE (8 mg/mL and 240 mins) were characterized for size, morphology, stability, entrapment efficiency, in vitro release profiles, and in vivo efficacy evaluations. For efficacy studies, optimized SoRE were intravenously administered to Wistar rats having hepatocellular lesions induced by aflatoxin B and monitored for in vivo antineoplastic activity.

Results: The amount of sorafenib entrapped was directly proportional to the drug concentration in the dialysis medium and duration of osmosis; highest for 10 mg/mL and 240 minutes and lowest for 2 mg/mL and 30 minutes, respectively. Optimized SoRE were biconcave with a size of 112.7 nm and zeta potential of -11.95 ± 2.25 mV. Osmotic and turbulence fragility were comparable with native erythrocytes.

Conclusion: Drug release follows the first-order pattern. In vivo investigations reveal better anticancer activity of SoRE formulation compared to sorafenib standard preparation. Resealed erythrocytes loaded with sorafenib displayed first-order in vitro release and promising anticancer activity in a rat model of hepatocellular carcinoma.

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