The incorporation of drugs in liposomes provides the potential for delivery to mucosal surfaces on a localized and sustained basis. Liposomes are lipid vesicles which contain or incorporate into their shell an aqueous solution of the active substance in their inner space. The inclusion of the echinochrome A carrageenan matrix ((Ech) - the active substance of the drug Histochrome) in liposomes has been studied. Ech was not oxidized according to spectral characteristics and maintained stability after encapsulation in the liposomes and the lyophilization process. The loading of liposomes with a negatively charged polysaccharide results in an increase of the zeta potential to more negative values (from -14.6 to -24.4 mV), which, along with an increase in liposome sizes (from 124.7 to 2.2 to 159.3 to 5.8 nm), implies the development of a polymer coating on liposomes. The DLS and SEM methods determined the interactions of liposomes with porcine stomach mucin. As a consequence of the interaction of liposomes with mucin, changes in the zeta-potential and size of the mucin particles were observed. A fresh-frozen inner surface of the pig's small intestine as a model of mucous tissue was used to determine the mucoadhesive properties of liposomes and the penetration of Ech into the mucosa. There are very strong mucoadhesive properties in polysaccharide-coated liposomes; 50 percent of Ech remains on the mucosa.
Author (s) DetailsV. I. Gorbach
G. B. Elyakov Pacific Institute of Bioorganic Chemistry, Far-Eastern Branch of the Russian Academy of Sciences, 100 Let Vladivostoku Prosp., 159, 690022, Vladivostok, Russian Federation.
V. P. Glazunov
G. B. Elyakov Pacific Institute of Bioorganic Chemistry, Far-Eastern Branch of the Russian Academy of Sciences, 100 Let Vladivostoku Prosp., 159, 690022, Vladivostok, Russian Federation.
V. N. Davydova
G. B. Elyakov Pacific Institute of Bioorganic Chemistry, Far-Eastern Branch of the Russian Academy of Sciences, 100 Let Vladivostoku Prosp., 159, 690022, Vladivostok, Russian Federation.
I. M. Yermak
G. B. Elyakov Pacific Institute of Bioorganic Chemistry, Far-Eastern Branch of the Russian Academy of Sciences, 100 Let Vladivostoku Prosp., 159, 690022, Vladivostok, Russian Federation.
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