On the Pharmaceutical Development of a Liposomal Dosage Form of a Tyrosine Kinase Inhibitor

IF 0.8 Q3 Engineering

Nanotechnologies in Russia Pub Date : 2025-08-25 DOI:10.1134/S263516762560066X

Z. S. Shprakh, A. R. Kovaleva, E. V. Sanarova, D. A. Kozin, L. L. Nikolaeva

{"title":"On the Pharmaceutical Development of a Liposomal Dosage Form of a Tyrosine Kinase Inhibitor","authors":"Z. S. Shprakh, A. R. Kovaleva, E. V. Sanarova, D. A. Kozin, L. L. Nikolaeva","doi":"10.1134/S263516762560066X","DOIUrl":null,"url":null,"abstract":"<p>Pazopanib is a multitargeted tyrosine kinase inhibitor that suppresses angiogenesis and proliferation of tumor cells. To increase its bioavailability, a model of a liposomal dosage form of pazopanib is developed and its main pharmaceutical and technological characteristics are determined. It is found that a composition including the active substance, egg phosphatidylcholine, cholesterol, and poly(ethylene glycol) lipid in a mass ratio of 1 : 75 : 7.5 : 0.75 possesses the best properties (size, polydispersity index, and surface charge). To determine the pazopanib concentration in model mixtures, ultraviolet (UV) spectrophotometry is used, which demonstrates the specificity of the method and its linearity (the ability to obtain results within a specified range that are directly proportional to the concentration of the analyte in the sample). The liposomal dispersion is stabilized by lyophilization, and a 10%-aqueous sucrose solution is selected as a cryoprotectant. Pazopanib in the final product is determined by high-performance liquid chromatography. The stability of the lyophilized liposomal dosage form for six months at a storage temperature of no higher than –18°C is shown.</p>","PeriodicalId":716,"journal":{"name":"Nanotechnologies in Russia","volume":"20 3","pages":"366 - 372"},"PeriodicalIF":0.8000,"publicationDate":"2025-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Nanotechnologies in Russia","FirstCategoryId":"1085","ListUrlMain":"https://link.springer.com/article/10.1134/S263516762560066X","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Engineering","Score":null,"Total":0}

引用次数: 0

Abstract

Pazopanib is a multitargeted tyrosine kinase inhibitor that suppresses angiogenesis and proliferation of tumor cells. To increase its bioavailability, a model of a liposomal dosage form of pazopanib is developed and its main pharmaceutical and technological characteristics are determined. It is found that a composition including the active substance, egg phosphatidylcholine, cholesterol, and poly(ethylene glycol) lipid in a mass ratio of 1 : 75 : 7.5 : 0.75 possesses the best properties (size, polydispersity index, and surface charge). To determine the pazopanib concentration in model mixtures, ultraviolet (UV) spectrophotometry is used, which demonstrates the specificity of the method and its linearity (the ability to obtain results within a specified range that are directly proportional to the concentration of the analyte in the sample). The liposomal dispersion is stabilized by lyophilization, and a 10%-aqueous sucrose solution is selected as a cryoprotectant. Pazopanib in the final product is determined by high-performance liquid chromatography. The stability of the lyophilized liposomal dosage form for six months at a storage temperature of no higher than –18°C is shown.

Abstract Image

查看原文本刊更多论文

酪氨酸激酶抑制剂脂质体剂型的研制

Pazopanib是一种多靶点酪氨酸激酶抑制剂，可抑制肿瘤细胞的血管生成和增殖。为了提高帕唑帕尼的生物利用度，建立了一种帕唑帕尼脂质体剂型模型，并确定了其主要的药物和工艺特性。发现含有活性物质、卵磷脂酰胆碱、胆固醇和聚乙二醇脂的组合物，其质量比为1:75:7.5:0.75，具有最佳的性能（尺寸、多分散性指数和表面电荷）。为了确定模型混合物中的pazopanib浓度，使用了紫外分光光度法，这证明了该方法的特异性及其线性（在特定范围内获得与样品中分析物浓度成正比的结果的能力）。通过冻干稳定脂质体分散体，选择10%的蔗糖水溶液作为冷冻保护剂。用高效液相色谱法测定最终产品中的帕唑帕尼。冻干脂质体剂型在不高于-18°C的储存温度下可保持6个月的稳定性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Nanotechnologies in Russia NANOSCIENCE & NANOTECHNOLOGY-

CiteScore

1.20

自引率

0.00%

发文量

期刊介绍： Nanobiotechnology Reports publishes interdisciplinary research articles on fundamental aspects of the structure and properties of nanoscale objects and nanomaterials, polymeric and bioorganic molecules, and supramolecular and biohybrid complexes, as well as articles that discuss technologies for their preparation and processing, and practical implementation of products, devices, and nature-like systems based on them. The journal publishes original articles and reviews that meet the highest scientific quality standards in the following areas of science and technology studies: self-organizing structures and nanoassemblies; nanostructures, including nanotubes; functional and structural nanomaterials; polymeric, bioorganic, and hybrid nanomaterials; devices and products based on nanomaterials and nanotechnology; nanobiology and genetics, and omics technologies; nanobiomedicine and nanopharmaceutics; nanoelectronics and neuromorphic computing systems; neurocognitive systems and technologies; nanophotonics; natural science methods in a study of cultural heritage items; metrology, standardization, and monitoring in nanotechnology.