Получение и изучение свойств противоопухолевого лекарственного средства на основе липидного производного сарколизина
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Аннотация
Оптимизированы условия получения лекарственного средства на основе липидного производного сарколизина, встроенного в фосфолипидные наночастицы. Препарат представляет собой ультратонкую эмульсию со светопропусканием выше 80% и размером частиц не более 50 нм. При этом 99% липидного производного сарколизина встроено в фосфолипидные наночастицы. Сохранение агрегационной устойчивости в водной среде наблюдалось как минимум в течение 2-х суток. Эксперименты in vitro показали, что сарколизин, введенный в составе фосфолипидных наночастиц, распределяется по липопротеинам и белковым компонентам плазмы крови. При этом содержание сарколизина во всех фракциях, участвующих в транспорте биологически активных веществ в организме, значительно выше при введении в виде пролекарства (липидного производного сарколизина) в составе фосфолипидных наночастиц, чем при введении сарколизина в инкубационную среду в свободном виде (т.е. фармакологической субстанции). Превращение пролекарства в лекарство сарколизин происходит в клетках форменных элементов.
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