Irache Juan M, Huici María, Konecny Monica, Espuelas Socorro, Campanero Miguel Angel, Arbos Pau
Centro Galénico, Universidad de Navarra, 31080 - Pamplona (Spain).
Molecules. 2005 Jan 31;10(1):126-45. doi: 10.3390/10010126.
Bioadhesive nanoparticles have been proposed as carriers for the oral delivery of poorly available drugs and facilitate the use of this route. This work summarises some experiments describing the bioadhesive potential of Gantrez nanoparticles fluorescently labeled with rhodamine B isothiocyanate. The adhesive potential of Gantrez was found to be stronger when folded as nanoparticles than in the solubilised form. Conventional nanoparticles displayed a tropism for the upper areas of the gastrointestinal tract, with a maximum of adhesion 30 min post-administration and a decrease in the adhered fraction along the time depending on the given dose. The cross-linkage of nanoparticles with increasing amounts of 1,3-diaminopropane stabilised the resulting carriers and prolonged their half-life in an aqueous environment; although, the adhesive capacity of nanoparticles, the intensity and the relative duration of the adhesive interactions within the gut as a function of the cross-linking degree. Finally, nanoparticles were coated with either gelatin or albumin. In the first case, the presence of gelatin dramatically decreased the initial capacity of these carriers to interact with the gut mucosa and the intensity of these phenomenons. In the latter, bovine serum albumin coated nanoparticles (BSA-NP) showed an important tropism for the stomach mucosa without further significant distribution to other parts of the gut mucosa.
生物黏附性纳米颗粒已被提议作为口服递送难吸收药物的载体,并促进这种给药途径的应用。这项工作总结了一些实验,这些实验描述了用异硫氰酸罗丹明B荧光标记的甘泰兹纳米颗粒的生物黏附潜力。发现甘泰兹折叠成纳米颗粒时的黏附潜力比溶解形式时更强。传统纳米颗粒对胃肠道上部区域表现出嗜性,给药后30分钟时黏附量最大,并且随着时间推移,黏附部分会根据给定剂量而减少。纳米颗粒与越来越多的1,3 -二氨基丙烷交联可稳定所得载体,并延长其在水性环境中的半衰期;尽管如此,纳米颗粒的黏附能力、肠道内黏附相互作用的强度和相对持续时间是交联度的函数。最后,纳米颗粒用明胶或白蛋白包被。在第一种情况下,明胶的存在显著降低了这些载体与肠黏膜相互作用的初始能力以及这些现象的强度。在后一种情况下,牛血清白蛋白包被的纳米颗粒(BSA - NP)对胃黏膜表现出重要的嗜性,而不会进一步大量分布到肠黏膜的其他部位。
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