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Antirheumatic activity of methotrexate in phospholipid nanoparticles (Phosphogliv)

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Biochemistry (Moscow) Supplement Series B: Biomedical Chemistry Aims and scope Submit manuscript

Abstract

The efficiency of methotrexate use in the basic therapy of rheumatoid arthritis is limited because of risk of side effects and fast drug efflux from zone of joints as well. We have developed a new stabilized form of methotrexate using phospholipid micelles of the injection form of the Phosphogliv preparation as a carrier. Phosphogliv has recently been developed in the Institute of Biomedical Chemistry (Moscow), as the emulsion of 50 nm phospholipid nanoparticles stabilized by glycyrrhizic acid. The conditions of maximal methotrexate incorporation into the phospholipid nanoparticles were optimized under control of HPLC (60% of total methotrexate was associated with nanoparticles). Methotrexate in phospholipid nanoparticles exhibited higher therapeutic efficiency in experimental adjuvant arthritis in rats than with free methotrexate. (This was evaluated by the decrease of edema and swelling of joints and inhibition of secondary inflammatory reaction.) The increase of antirheumatic activity of the developed preparation may also be attributed to the influence of glycyrrhizic acid, possessing both anti-inflammatory and immune properties. It is suggested to use a new form of methotrexate for intra-articular administration for rheumatoid arthritis treatment.

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Authors and Affiliations

  1. Orekhovich Institute of Biomedical Chemistry, Russian Academy of Medical Sciences, Pogodinskaya ul. 10, Moscow, Russia, 119121

    M. G. Zykova, V. N. Prozorovskii, O. M. Ipatova, T. I. Torkhovskaya & V. V. Glazatov

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  1. M. G. Zykova
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  2. V. N. Prozorovskii
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  3. O. M. Ipatova
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  4. T. I. Torkhovskaya
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  5. V. V. Glazatov
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Correspondence to M. G. Zykova.

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Original Russian Text © M.G. Zykova, V.N. Prozorovskii, O.M. Ipatova, T.I. Torkhovskaya, V.V. Glazatov, 2008, published in Biomeditsinskaya Khimiya.

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Zykova, M.G., Prozorovskii, V.N., Ipatova, O.M. et al. Antirheumatic activity of methotrexate in phospholipid nanoparticles (Phosphogliv). Biochem. Moscow Suppl. Ser. B 2, 71–74 (2008). https://doi.org/10.1007/s11828-008-1007-y

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  • DOI: https://doi.org/10.1007/s11828-008-1007-y

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