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基于牛血清白蛋白和鞣酸多层微胶囊的乳铁蛋白口服递药制剂。

Formulation for Oral Delivery of Lactoferrin Based on Bovine Serum Albumin and Tannic Acid Multilayer Microcapsules.

机构信息

Institute of Materials Research and Engineering, Agency for Science, Technology and Research (A*STAR), 2 Fusionopolis Way, Innovis, #08-03, 138634, Singapore.

Food Science and Technology Programme, Department of Chemistry, National University of Singapore, 3 Science Drive 3, 117543, Singapore.

出版信息

Sci Rep. 2017 Mar 10;7:44159. doi: 10.1038/srep44159.

DOI:10.1038/srep44159
PMID:28281573
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5344998/
Abstract

Lactoferrin (Lf) has considerable potential as a functional ingredient in food, cosmetic and pharmaceutical applications. However, the bioavailability of Lf is limited as it is susceptible to digestive enzymes in gastrointestinal tract. The shells comprising alternate layers of bovine serum albumin (BSA) and tannic acid (TA) were tested as Lf encapsulation system for oral administration. Lf absorption by freshly prepared porous 3 μm CaCO particles followed by Layer-by-Layer assembly of the BSA-TA shells and dissolution of the CaCO cores was suggested as the most efficient and harmless Lf loading method. The microcapsules showed high stability in gastric conditions and effectively protected encapsulated proteins from digestion. Protective efficiency was found to be 76 ± 6% and 85 ± 2%, for (BSA-TA) and (BSA-TA) shells, respectively. The transit of Lf along the gastrointestinal tract (GIT) of mice was followed in vivo and ex vivo using NIR luminescence. We have demonstrated that microcapsules released Lf in small intestine allowing 6.5 times higher concentration than in control group dosed with the same amount of free Lf. Significant amounts of Lf released from microcapsules were then absorbed into bloodstream and accumulated in liver. Suggested encapsulation system has a great potential for functional foods providing lactoferrin.

摘要

乳铁蛋白(Lf)作为食品、化妆品和制药应用中的功能性成分具有很大的潜力。然而,由于它易受胃肠道消化酶的影响,Lf 的生物利用度有限。牛血清白蛋白(BSA)和鞣酸(TA)交替层组成的壳被测试为口服给药的 Lf 封装系统。通过新制备的多孔 3μm CaCO 颗粒吸收 Lf,然后进行 BSA-TA 壳的层层组装和 CaCO 核的溶解,被认为是最有效和无害的 Lf 加载方法。微胶囊在胃条件下表现出高稳定性,并有效地保护包封的蛋白质免受消化。保护效率分别为(BSA-TA)和(BSA-TA)壳的 76±6%和 85±2%。使用近红外发光在体内和体外跟踪乳铁蛋白在小鼠胃肠道(GIT)中的转运。我们已经证明,微胶囊在小肠中释放 Lf,允许释放的 Lf 浓度比用相同量的游离 Lf 给药的对照组高 6.5 倍。然后,大量从微胶囊中释放的 Lf 被吸收到血液中并在肝脏中积累。所提出的封装系统对于提供乳铁蛋白的功能性食品具有很大的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0803/5344998/3d517eb36c65/srep44159-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0803/5344998/3d517eb36c65/srep44159-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0803/5344998/3d517eb36c65/srep44159-f1.jpg

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