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NANOPARTICLES BASED ON BIODEGRADABLE POLYMERS WITH ANTICANCER DRUGS ENCAPSULATED THEREIN

机译:基于生物可降解聚合物的纳米颗粒及其包裹的抗癌药

摘要

FIELD: medicine.;SUBSTANCE: invention refers to medicine, namely to oncology, to nanoparticles based on biodegradable polymers with anticancer preparations encapsulated therein and can be used for treating malignant growths. Nanoparticles based on biodegradable polymers with anticancer preparations encapsulated therein are made in the form of spherical double-layer structures containing an outer insulating layer and inner spherical part made of biodegradable polymers selected from polyglycolide group, poly-DL-lactide, polylactide-glycolides (PLGA) containing 50 % of L-isomer and 50 % of D-isomer or polylactide-glycolides (PLGA), containing 85–90 % of L-isomer and 10–15 % of D-isomer, inner spherical part of two-layer structure is encapsulated in its volume with nanoparticles of anti-tumour preparations in amount of 36 to 54 wt. %. Antineoplastic preparations are selected from a group of fluorouracil, or a mixture of fluorouracil with exogenous siRNA205, or a mixture of fluorouracil with exogenous siRNA205 and cisplatin, or a mixture of fluorouracil with cisplatin. Nanoparticles of anti-tumour preparations can be adsorbed on the surface of the inner spherical part of the two-layer structure. Spherical nanoparticles are made with diameters of 10 to 200 nm, and thickness of outer insulating layer is selected depending on expected time of controlled delivery of anti-tumour preparations to affected tissue and makes 0.15–0.32 of external diameters of nanoparticles. Produced nanoparticles provide effective inhibition of growth of malignant growth, increased cytostatic activity and selective effect on tumour cells. Besides, obtained nanoparticles provide targeted effect of anti-cancer preparations on tumour cells without isolation of anticancer preparations in surrounding tissues during movement to tumour cells with simultaneous reduction of treatment time and reduced biochemical load on patient's body.;EFFECT: invention provides high clinical effectiveness with obtaining a stable therapeutic effect ensured by the inhibitory effect on malignant growth.;4 cl, 1 tbl, 3 dwg
机译:技术领域本发明涉及医学,即肿瘤学,是指基于生物可降解聚合物的纳米颗粒,其中包裹有抗癌制剂,可用于治疗恶性肿瘤。以封装有抗癌制剂的可生物降解聚合物为基础的纳米颗粒以球形双层结构的形式制成,该双层结构包含外部绝缘层和内部球形部分,该外部绝缘层和内部球形部分由可生物降解的聚合物制成,该可生物降解的聚合物选自聚乙交酯,聚-DL-丙交酯,聚丙交酯-乙交酯(PLGA) )包含50%的L-异构体和50%的D-异构体或聚丙交酯-乙交酯(PLGA),其中包含85-90%的L-异构体和10-15%的D-异构体,两层结构的内部球形部分用36至54wt。%的抗肿瘤制剂的纳米颗粒将其包裹在其体积中。 %。抗肿瘤制剂选自氟尿嘧啶,或氟尿嘧啶与外源siRNA205的混合物,或氟尿嘧啶与外源siRNA205和顺铂的混合物,或氟尿嘧啶与顺铂的混合物。抗肿瘤制剂的纳米颗粒可以吸附在两层结构的内部球形部分的表面上。球形纳米粒子的直径为10到200 nm,外部绝缘层的厚度取决于抗肿瘤制剂向受影响组织的控制递送的预期时间,纳米粒子的外径为0.15-0.32。产生的纳米颗粒可有效抑制恶性肿瘤的生长,增加细胞抑制活性以及对肿瘤细胞的选择性作用。此外,所获得的纳米颗粒提供了抗癌制剂对肿瘤细胞的靶向作用,而在向肿瘤细胞移动期间没有分离周围组织中的抗癌制剂,同时减少了治疗时间并减少了对患者身体的生化负荷。通过抑制对恶性肿瘤的生长确保获得稳定的治疗效果。; 4 cl,1 tbl,3 dwg

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