STUDY OF THE EFFECT OF CRYOPROTECTORS ON THE SIZE AND SHAPE OF CINNARIZINE AND POLY-D,L-LACTIDE-CO-GLYCOLIDE MICROPARTICLES.

Sorokoumova M.V., Kompantsev D.V., Blinov A.V.
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Abstract

In a traditional drug delivery system, it is difficult to achieve precise control of the drug release rate and the drug release site. Poly-D,L-lactide-co-glycolide is one of the most frequently studied biodegradable polymeric drug carriers for drug delivery to target organs. Biodegradable polymers must have good biocompatibility. Targeted delivery of drugs obtained using modern technologies can provide a new therapeutic strategy for more localized treatment of diseases, potentially provide systemic delivery of drugs, reduce the dose of the administered drug and its possible side effects on the patient. In the experiment, we obtained microparticles based on cinnarizine with poly-D,L-lactide-co-glycolide using the co-precipitation method. The physicochemical characteristics of microparticles are of key importance for understanding their properties for further use in pharmaceuticals, since they can have different effects on the target organ due to their unique properties. The study of the dispersed composition of the obtained samples of cinnarizine microparticles based on poly-D,L-lactide-co-glycolide was carried out using photon correlation spectroscopy on a Photocor-Complex installation (Antek-97, Russia). The size and shape of microparticles explain their ability to penetrate blood vessels, tissues and target cells of target organs. The purpose of this work was to determine the effect of various cryoprotectants on the size and shape of cinnarizine microparticles at different ratios to poly-D,L-lactide-co-glycolide. Under experimental conditions, a cryoprotector was selected. As a result of the tests, it was determined that the nature of the cryoprotector affects the size and shape of the resulting particles - the optimal ratio of cinnarizine and poly-D,L-lactide-co-glycolide is 1:3, which produces microparticles 104 nm in size, spherical in shape, having a uniform distribution in the sample.
研究低温保护剂对西奈利嗪和聚-d,l-内酯-共聚乙二醇微粒的大小和形状的影响。
在传统的给药系统中,很难实现对药物释放速率和释放部位的精确控制。聚-D,L-内酰胺-共聚乙二醇是研究最多的生物可降解聚合物药物载体之一,用于向靶器官给药。生物可降解聚合物必须具有良好的生物相容性。利用现代技术进行靶向给药可以为疾病的局部治疗提供一种新的治疗策略,并有可能提供全身给药,减少给药剂量及其对患者可能产生的副作用。在实验中,我们采用共沉淀法获得了基于辛那利嗪与聚-D,L-内酯-共聚乙二醇的微颗粒。微颗粒因其独特的性质会对靶器官产生不同的影响,因此了解微颗粒的理化特性对于了解其进一步用于制药的性质至关重要。在 Photocor-Complex 设备(俄罗斯,Antek-97)上使用光子相关光谱法研究了基于聚-D,L-内酯-共聚乙二醇的朱那利嗪微颗粒样品的分散成分。微粒子的大小和形状决定了其穿透血管、组织和靶器官靶细胞的能力。这项工作的目的是确定各种低温保护剂对不同比例的朱砂苷微粒的大小和形状的影响。在实验条件下,选择了一种低温保护剂。试验结果表明,低温保护剂的性质会影响所产生微粒的大小和形状--朱鹭碱和聚-D,L-内酰胺-共聚乙二醇的最佳比例为 1:3,这样产生的微粒大小为 104 nm,呈球形,在样品中分布均匀。
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