G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far-Eastern Branch of the Russian Academy of Sciences, 100 Let Vladivostoku Prosp., 159, 690022 Vladivostok, Russia.
National Scientific Center of Marine Biology, Far-Eastern Branch of the Russian Academy of Sciences, Palchevskogo, 17, 690041 Vladivostok, Russia.
Mar Drugs. 2018 Sep 10;16(9):324. doi: 10.3390/md16090324.
Inclusion of drugs in liposomes offers the potential for localized and sustained delivery to mucosal surfaces. The inclusion of the carrageenan matrix with echinochrome A ((Ech)-the active substance of the drug Histochrome) in liposomes was studied. According to the spectral characteristics, Ech was not oxidized and retained stability after encapsulation in the liposomes and the lyophilization process. Loading the liposomes with negatively charged polysaccharide results in the increase in the zeta potential to more negative values (from -14.6 to -24.4 mV), that together with an increasing in the sizes of liposomes (from 125.6 ± 2.5 nm to 159.3 ± 5.8 nm) propose of the formation of the polymer coating on liposomes. The interactions of liposomes with porcine stomach mucin was determined by the DLS and SEM methods. The changes in the zeta-potential and size of the mucin particles were observed as the result of the interaction of liposomes with mucin. To evaluate the mucoadhesive properties of liposomes and the penetration of Ech in the mucosa, a fresh-frozen inner surface of the small intestine of a pig as a model of mucous tissue was used. Polysaccharide-coated liposomes exhibit very good mucoadhesive properties -50% of Ech remains on the mucosa.
将药物包封在脂质体中为局部和持续向黏膜表面递送提供了潜力。研究了卡拉胶基质与海胆烯酮 A（Ech）（Histochrome 药物的活性物质）在脂质体中的包封情况。根据光谱特征，Ech 在包封在脂质体中和冻干过程中没有被氧化，保持稳定。将带负电荷的多糖载入脂质体中会导致 zeta 电位增加到更负的值（从-14.6 到-24.4 mV），这与脂质体粒径的增加（从 125.6±2.5nm 到 159.3±5.8nm）一起表明在脂质体上形成了聚合物涂层。通过 DLS 和 SEM 方法确定了脂质体与猪胃粘蛋白的相互作用。观察到粘蛋白颗粒的 zeta 电位和粒径的变化，这是脂质体与粘蛋白相互作用的结果。为了评估脂质体的黏膜黏附特性和 Ech 在黏膜中的渗透，使用新鲜冷冻的猪小肠内表面作为黏蛋白组织模型。多糖包被的脂质体表现出非常好的黏膜黏附特性，50%的 Ech 留在黏膜上。
