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Liposomal formulations of protein proteinase inhibitors: Preparation and specific activity

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

Abstract

Possibility of encapsulation of water-soluble proteins into multilayer liposomes of soybean zwitterionic phospholipid mixtures (phosphatidylcholine (PC) and phosphatidylethanolamine (PE)) was investigated. The influence of the PC/PE ratio (w/w) on efficiency of incorporation of the Bowman-Birk soybean proteinase inhibitor (BBI) and aprotinin (BPTI) into liposomes was studied. Protein encapsulation did not affect liposome sizes. Confocal laser scanning microscopy demonstrated that proteins were located in the central part of the spherical particle and also between bilayers. The study of biological (antitrypsin and antichymotrypsin) activity demonstrated partial spatial shielding of active sites of proteins entrapped in liposomes. The effect of an ionic detergent on the activity of the encapsulated BBI and BPTI is consistent with this hypothesis and suggests that this shielding is reversible. Stability of liposomes was examined using three various media modeling gastrointestinal fluids (gastric and intestinal juices and fluids). Data obtained indicate that the prepared liposomes seem to be promising formulations for BBI and BPTI delivery.

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Authors and Affiliations

  1. School of Chemistry, Moscow State University, Moscow, 119992, Russia

    A. S. Balkina & N. I. Larionova

  2. School of Biology, Moscow State University, Moscow, 119992, Russia

    A. A. Selischeva

Authors
  1. A. S. Balkina
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  2. A. A. Selischeva
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  3. N. I. Larionova
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Correspondence to A. S. Balkina.

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Original Russian Text © A.S. Balkina, A.A. Selischeva, N.I. Larionova, 2009, published in Biomeditsinskaya Khimiya.

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Balkina, A.S., Selischeva, A.A. & Larionova, N.I. Liposomal formulations of protein proteinase inhibitors: Preparation and specific activity. Biochem. Moscow Suppl. Ser. B 3, 48–53 (2009). https://doi.org/10.1134/S1990750809010065

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  • DOI: https://doi.org/10.1134/S1990750809010065

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