Prednisolone in phospholipid nanoparticles: prolonged circulation and increased antiinflammatory effect

Prozorovskii V.N.1, Ipatova O.M.1, Tikhonova E.G.1, Zakharova T.S.1, Druzhilovskaya O.S.1, Korotkevich E.I.1, Torkhovskaya T.I.1

1. Institute of Biomedical Chemistry, Moscow, Russia
Section: Experimental Study
DOI: 10.18097/PBMC20196503222      PubMed Id: 31258145
Year: 2019  Volume: 65  Issue: 3  Pages: 222-226
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.
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Keywords: prednisolone, phospholipid nanoparticles, bioavailability, inflammation model

Prozorovskii, V. N., Ipatova, O. M., Tikhonova, E. G., Zakharova, T. S., Druzhilovskaya, O. S., Korotkevich, E. I., Torkhovskaya, T. I. (2019). Prednisolone in phospholipid nanoparticles: prolonged circulation and increased antiinflammatory effect. Biomeditsinskaya Khimiya, 65(3), 222-226.
This paper is also available as the English translation: 10.1134/S1990750820010126
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