基于肌酵素脂质衍生物的抗肿瘤药物的制备及性能研究

Y. Tereshkina, M. A. Sanzhakov, L. Kostryukova, E. Korotkevich, A. Chistov, E. Tikhonova, V. N. Prozorovsky, O. Ipatova
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引用次数: 1

摘要

优化了以磷脂纳米颗粒包埋肌溶素脂质衍生物为基础的药物制剂的制备条件。本品为超薄乳剂,透光率80%以上,粒径不大于50nm。值得注意的是,99%的肌溶素脂质衍生物被纳入磷脂纳米颗粒中。在水生环境中,聚合稳定性至少保持了2天。体外实验表明,肌溶素作为磷脂纳米颗粒的一部分被引入,分布在血浆的脂蛋白和蛋白质组分中。此外,与在孵育培养基中使用自由形式(药理学物质)相比,在磷脂纳米颗粒组合物中使用前药给药(肌溶素的脂质衍生物)时,参与体内生物活性物质运输的所有部分中肌溶素的含量明显更高。前药转化为肌溶素的过程发生在血细胞中。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and Properties of Antitumor Drug Based on Lipid Derivative of Sarcolysin
The conditions for the preparation of a drug formulations based on the lipid derivative of sarcolysin embedded in phospholipid nanoparticles have been optimized. The drug is an ultra-thin emulsion with a light transmittance above 80% and a particle size of not more than 50 nm. It should be noted that 99% of the lipid derivative of sarcolysin are incorporated into phospholipid nanoparticles. Preservation of aggregation stability in the aquatic environment was observed for at least 2 days. In vitro experiments have shown that sarcolysin, introduced as a part of phospholipid nanoparticles, is distributed among lipoproteins and protein components of plasma. Moreover, the content of sarcolysin in all fractions involved in the transport of biologically active substances in the body, is significantly higher in case of prodrug administration (lipid derivative of sarcolysin) in the composition of phospholipid nanoparticles than, as compared with administration of a free form (pharmacological substances) to the incubation medium. The transformation of a prodrug into the drug sarcolysin occurs in the blood cells.
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