Research on the loading and release kinetics of the vincristine sulfate liposomes and its anti-breast cancer activity

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Zixu Liu , Yang Liu , Zixuan Wu , Boyuan Liu , Linxuan Zhao , Tian Yin , Yu Zhang , Haibing He , Jingxin Gou , Xing Tang , Song Gao
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Abstract

Vincristine (VCR), as a cytotoxic drug, is used clinically to treat acute lymphatic leukemia and breast cancer, and commonly used clinically as vincristine sulfate (VCRS). However, its clinical use is limited by unpredictable pharmacologic characteristics, a narrow therapeutic index, and neurotoxicity. The pH gradient method was used for active drug loading of VCRS, and the process route mainly includes the preparation of blank liposomes and drug-loaded liposomes. VCRS liposomes had suitable particle size, high encapsulation efficiency and good stability. The loading and release kinetics of VCRS liposomes were explored. By calculating the changes of encapsulation efficiency with time at different temperatures, it was confirmed that the drug-loading process of liposomes exhibited a first-order kinetic feature, and the activation energy required for the reaction was determined as 20.6 kcal/mol. The release behavior at different pH was also investigated, and it was demonstrated that the release behavior conformed to the first-order model, suggesting that the release mechanism of VCRS was simple transmembrane diffusion. VCRS liposomes also enhanced in vitro and in vivo antitumor activity. Thus, VCRS liposomes showed great potential for VCRS delivery, and the loading and release kinetics were well researched to provide a reference for investigating active drug loading liposomes.

Abstract Image

硫酸长春新碱脂质体的负载和释放动力学及其抗乳腺癌活性研究
长春新碱(VCR)作为一种细胞毒性药物,在临床上用于治疗急性淋巴白血病和乳腺癌,临床上常用的药物是硫酸长春新碱(VCRS)。然而,由于其药理特性难以预测、治疗指数较窄以及神经毒性,其临床应用受到了限制。本文采用pH梯度法对VCRS进行活性药物负载,工艺路线主要包括制备空白脂质体和药物负载脂质体。VCRS脂质体具有合适的粒径、较高的包封效率和良好的稳定性。研究人员对 VCRS 脂质体的负载和释放动力学进行了探讨。通过计算不同温度下包封效率随时间的变化,证实脂质体的药物负载过程呈现一阶动力学特征,并确定反应所需的活化能为 20.6 kcal/mol。此外,还研究了不同 pH 值下的释放行为,结果表明释放行为符合一阶模型,表明 VCRS 的释放机制是简单的跨膜扩散。VCRS 脂质体还增强了体外和体内抗肿瘤活性。因此,VCRS脂质体在输送VCRS方面显示出了巨大的潜力,其负载和释放动力学研究也为研究活性药物负载脂质体提供了参考。
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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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