Abstract
Objective. Aim of this work was to create a stable liposomal dosage form of native hydrophobic antitumor compound from the group of indolocarbazoles - LHS-1208. Materials and methods. Quantitative analysis of the drug content in liposomes was determined by spectrophotometry with a standard sample at X = 320 ± 2 nm. The encapsulation was investigated as the ratio of LHS-1208 concentration in the liposomal dispersion after extrusion through nylon membrane filters 0.22 ^m “Pall” to concentration LHS-1208 in liposomal dispersions before filtration. pH of the liposome was determitaned by the method of potentiometry. The size of liposomes was evaluated by nanosizer. Cytotoxic activity was studied by MTT-test. Results. Experimental liposomal models of LHS-1208 with different molar ratios of the components were obtained and analyzed. Composition with the molar ratios LHS-1208: lecithin 1:150, and lecithin : cholesterol: PEG-2000 - 1:0,2:0,003 was selected. Encapsulation percentage of LHS-1208 was 94 % and size of the vesicles was 185±10 nm. Cytotoxic activity of liposomal LHS-1208 was studied, IC 0 was 1.24 ^g/ml. Conclusion. As a result of complex pharmaceutical research determined the optimum composition of the components and the technology for production of liposomal dosage form LHS-1208.
Highlights
As a result of complex pharmaceutical research determined the optimum composition of the components and the technology for production of liposomal dosage form LHS-1208
Разработка наноструктурированной модели лекарственной формы производного индолокарбазола ЛХС-1208
Summary
Цель исследования – создание стабильной липосомальной лекарственной формы отечественного гидрофобного противоопухолевого соединения из группы производных индолокарбазолов – ЛХС-1208. Количественное содержание препарата в липосомах определяли спектрофотометрическим методом с использованием стандартного образца при λ = 320 ± 2 нм. Были получены и проанализированы экспериментальные модели составов липосомальной лекарственной формы ЛХС-1208 с различными молярными соотношениями компонентов. Выбран состав со следующими молярными соотношениями ЛХС-1208: лецитин – 1:150 и лецитин : холестерин : PEG-2000 – 1:0,2:0,003. Изучена цитотоксическая активность липосомальной лекарственной формы ЛХС-1208, концентрация вещества, вызывающая гибель 50 % клеток (ИК50), составила 1,24 мкг/мл. В результате проведения комплекса фармацевтических исследований определен оптимальный состав компонентов и разработана технология получения липосомальной лекарственной формы ЛХС-1208. Blokhin Russian Cancer Research Center, Ministry of Health of Russia; 24 Kashyrskoe Shosse, Moscow, 115478, Russia
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