Along with modern new drugs, many therapeutic schemes also include known effective drugs, particularly, glucocorticoids. One of the most distributed of them is prednisolone that has pronounced anti-inflammatory properties. Its disadvantage is short-term circulation, resulting in a number of side effects. For this reason the development of its more effective and safe formulations is carried out. We have obtained the formulation of prednisolone included in nanoparticles from soy phosphatidylcholine with an average diameter of 20 nm. With oral administration to rats and analysis by HPLC an increase in prednisolone maximal concentration in of plasma and the duration of circulation as compared with free drug administration were shown. The experiment with mice with conconavalin A induced inflammation was also carried out: conconavalin A was injected subplantary in an hour after oral administration of both prednisolone formulations in several doses. The index of the inflammatory reaction (determined by the edema degree) was suppressed more effectively in the case of prednisolone in nanoparticles. Maximal suppression (62.2% as compared with 49.6% for free prednisolone) was observed even at a minimal dose (2.5 mg/kg), at which the free drug did not act at all. The results indicate an increase in the efficiency of prednisolone included in phospholipid nanoparticles, that makes it possible to diminish its administered doses and thereby reduce the risk of side effects.
Nariadu s novymi lekarstvennymi preparatami, mnogie terapevticheskie skhemy ispol\'zuiut izvestnye éffektivnye lekarstvennye sredstva, v chastnosti, gliukokortikoidy. Sredi nikh odnim iz naibolee rasprostranennykh iavliaetsia prednizolon, obladaiushchiĭ vyrazhennymi protivovospalitel\'nymi svoĭstvami. Nedostatkom étogo lekarstva iavliaetsia kratkovremennaia tsirkuliatsiia v krovi, trebuiushchaia povtornykh vvedeniĭ i privodiashchaia k riadu pobochnykh éffektov. V sviazi s étim provodiatsia razrabotki bolee éffektivnykh i bezopasnykh lekarstvennykh form étogo preparata. Nami poluchena kompozitsiia prednizolona, vkliuchennogo v nanochastitsy iz soevogo fosfatidilkholina, so srednim diametrom 20 nm. Pri peroral\'nom vvedenii étoĭ kompozitsii pokazano uvelichenie maksimal\'noĭ kontsentratsii prednizolona v plazme i dlitel\'nosti ego tsirkuliatsii po sravneniiu so svobodnym lekarstvom. Na myshakh s model\'iu vospaleniia, indutsirovannogo vvedeniem konkonavalina A, indeks reaktsii vospaleniia (opredeliaemyĭ po oteku konechnosti) snizhalsia v sluchae kompozitsii prednizolona v nanochastitsakh sushchestvenno aktivnee, chem pri vvedenii svobodnogo lekarstva: maksimal\'noe snizhenie indeksa (62,2% po sravneniiu s 49,6%) nabliudalos\' uzhe pri minimal\'noĭ doze vvodimogo prednizolona (2,5 mg/kg), pri kotoroĭ svobodnoe lekarstvo voobshche ne deĭstvovalo. Poluchennye rezul\'taty ukazyvaiut na povyshenie éffektivnosti prednizolona pri vkliuchenii v fosfolipidnye nanochastitsy, chto daet vozmozhnost\' umen\'sheniia vvodimykh doz i snizhaet risk pobochnogo deĭstviia.