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Information × Registration Number 0219U005014, 0117U006587 , R & D reports Title Development and preclinical studies of liposomal nitric oxide popup.stage_title Head Soloviev Anatoly I., Доктор медичних наук Registration Date 11-04-2019 Organization State Institution "Institute of Pharmacology and Toxicology of National Academy of Medical Sciences of Ukraine" popup.description2 Report of research work: 208 p., 22 figures, 43 tables, 14 appendixes,26 sources. LIPOSOMES, NITROGEN OXIDES, LIPOSOMAL MEDICINAL PRODUCTS, HYPOTENSIVE ACTION, SMOOTH MUSCLE OF BLOOD VESSELS, CORPORA CAVERNOSA, MYOMETRIUM, POTASSIUM CA2 + -DEPENDENT CHANNELS Objects of research - liposomal form of nitric oxide (LFNO), specific activity (dilatating and anti-ischemic action) and mechanisms of its implementation, determination of toxicological parameters of liposomal form of nitric oxide. Purpose and tasks of work: Development of liposomal form of nitric oxide, which is intended for correction of peripheral blood circulation disorders. Methods of research - physico-chemical, pharmaceutical, pharmacological, electrophysiological, toxicological, statistical. Several series of liposomal nitrous oxide forms were constructed. As a result of screening studies, it was shown that a single intravenous injection of a test sample of the series c030717 causes a dose-dependent and prolonged hypotensive reaction. Studies of the specific effect of the test sample of the liposomal form of nitric oxide have been shown to have an extremely high dilatatory, anti-ischemic and, possibly, antiarrhythmic activity of the liposomal form of nitrogen oxide: a) addition of an aqueous suspension of a liposomal form of nitric oxide into a solution for perfusion of an isolated heart reduces the coronary perfusion pressure due to decreased coronary artery tone; b) perfusion of an isolated heart with a suspension of a liposomal form of nitric oxide, both during ischemia and reperfusion, and only by reperfusion, prevents the development of critical violations of the pumping function of the heart and promotes the preservation of its contractile activity. Antiarrhythmic action is confirmed by the absence of heart rate abnormalities during both ischemia and reperfusion period. In favor of this, the lack of prolongation of the interval QTC; c) the liposomal form of nitric oxide causes a pronounced dose-dependent relaxation of the intact segments of the rat aorta; d) the action of the liposomal form of nitric oxide is manifested by a significant dose-dependent relaxation of the strips of inflamed cells of the penis and myometrium; e) dilatatory action of liposomal form of nitric oxide due to its ability to efficiently open potassium Ca2 + -dependent channels of high conductivity of plasma membranes; e) the liposomal form of nitrogen oxide can significantly increase the probability of finding channels in open state. Pharmacotoxicological characteristics (acute and subacute toxicity) of the experimental portion of the liposomal form of nitrogen oxide indicate that the tested test sample is assigned to a class of low toxicity pharmacologically active compounds. The quality control of the lyophilizate to prepare the emulsion of the liposomal form of nitrogen oxide confirms the stability of the test sample during the year when stored at a temperature from minus 20 oC to minus 10 oC. Product Description popup.authors Іванова І.В. Добреля Н.В. Дринь Д.О. Жолос О.В. Мельник М.І. Мончак І.Л. Мороз О.Ф. Прохоров В.В. Хромов О.С. Червінська Т.М. popup.nrat_date 2020-04-02 Close