Improved intestinal absorption of calcitonin by mucoadhesive delivery of novel pectin-liposome nanocomplexes
Improved intestinal absorption of calcitonin by mucoadhesive delivery of novel pectin-liposome nanocomplexes
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DOI：
10.1016/j.jconrel.2007.10.023
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发表时间：
2008-02-11
影响因子：
10.8
通讯作者：
Sriamornsak, Pornsak
中科院分区：
文献类型：
--
作者：
Thirawong, Nartaya;Thongborisute, Jringjai;Sriamornsak, Pornsak
通过将阳离子脂质体与果胶溶液简单混合制备自组装果胶-脂质体纳米复合物（PLNs），以改善降钙素（eCT）的肠道吸收。对PLN的体外和体内评价进行了评价。结果表明，PLNs的平均粒径明显大于初始阳离子脂质体。与果胶混合后，表面电荷由正向负转移。由高酯化度（DE）果胶制成的PLN比由低DE果胶制成的PLN显示出更少的负电荷值。即使载药量增加，阳离子脂质体的包封率也在相同范围内。通过共聚焦激光扫描显微镜对果胶进行的体内粘膜粘附试验表明，与阳离子脂质体和由其他果胶制成的PLN相比，由低DE果胶制成的PLN具有更强的粘膜粘附特性。此外，在整个小肠（即十二指肠、空肠和回肠）中可以观察到高强度的荧光标记物，并且即使在施用由低DE果胶制成的PLN 6小时后仍保持在粘膜粘附部位。与eCT溶液和eCT负载脂质体相比，负载eCT的PLN表现出较强的药理作用，其中观察到大鼠血浆钙浓度的增强和延长的降低。这归因于果胶粘附于粘液层并延长在肠粘膜中的滞留的能力。(C)2007 Elsevier B. V.保留所有权利。
Self-assembling pectin-liposome nanocomplexes (PLNs) were prepared by a simple mixing of cationic liposomes with pectin solution, in order to improve intestinal absorption of calcitonin (eCT). Both in-vitro and in-vivo evaluations for PLNs were evaluated. The results showed that average particle size of PLNs was significantly larger than that of initial cationic liposomes. The surface charges were shifted from positive to negative after mixing with pectin. The PLNs made of high degree of esterification (DE) pectin showed less negatively charged values than those made of low DE pectin. The entrapment efficiency in cationic liposomes was in the same range even if the drug loading was increased. The in-vivo mucoadhesive test of pectin by confocal laser scanning microscopy demonstrated stronger mucoadhesive properties of PLNs made of low DE pectin, compared to cationic liposomes and PLNs made of other pectins. Moreover, high intensities of a fluorescent marker could be observed throughout the small intestines (i.e. duodenum, jejunum and ileum) and remained at the site of mucoadhesion even after 6 h of administration of PLNs made of low DE pectin. The eCT-loaded PLNs demonstrated a strong pharmacological action over the eCT solution and eCT-loaded liposomes, in which an enhanced and prolonged reduction in plasma calcium concentration of rats was observed. This was attributed to the ability of pectin to adhere to the mucus layer and prolong retention in the intestinal mucosa. (C) 2007 Elsevier B.V. All rights reserved.