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用于肠道特异性递药和肽控释的纳米结构多单位载体的构建。

Fabrication of nanostructured multi-unit vehicle for intestinal-specific delivery and controlled release of peptide.

机构信息

School of Food Science and Engineering, Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety, South China University of Technology, Guangzhou 510640, People's Republic of China.

Sericultural & Agri-Food Research Institute, Guangdong Academy of Agricultural Sciences; Key Laboratory of Functional Foods, Ministry of Agriculture, Guangdong Key Laboratory of Agricultural Products Processing, People's Republic of China.

出版信息

Nanotechnology. 2021 Mar 23;32(24). doi: 10.1088/1361-6528/abed07.

Abstract

An oral multi-unit delivery system was developed by incorporating the nanoparticle (NP) into the nanofiber mat and its efficiency for intestinal-specific delivery and controlled release of a peptide (insulin) was investigated. Initially, the influence of deacetylation degree (DD) of chitosan and ionic gelation methods on the properties of NPs was studied. High DD (95%) chitosan was attributed to higher encapsulation efficiency and stability when crosslinked with polyanion tripolyphosphate. Subsequently, the multi-unit system was fabricated using a pH-sensitive polymer (sodium alginate) as the coating layer to further encapsulate the NP. Fiber mat with an average diameter of 481 ± 47 nm could significantly decrease the burst release of insulin in acidic condition and release most amount of insulin (>60%) in the simulated intestinal medium. Furthermore, the encapsulated peptide remained in good integrity. This multi-unit carrier provides the better-designed vehicle for intestinal-specific delivery and controlled release of the peptide.

摘要

研制了一种口服多单位给药系统,即将纳米颗粒(NP)纳入纳米纤维垫中,并研究了其用于肽(胰岛素)肠道特异性递送和控制释放的效率。首先,研究了壳聚糖脱乙酰度(DD)和离子凝胶法对 NPs 性质的影响。高 DD(95%)壳聚糖与多阴离子三聚磷酸交联时,表现出更高的包封效率和稳定性。随后,使用 pH 敏感聚合物(海藻酸钠)作为涂层进一步包封 NP,制备了多单位系统。平均直径为 481 ± 47nm 的纤维垫可显著降低胰岛素在酸性条件下的突释,并在模拟肠液中释放超过 60%的胰岛素。此外,包封的肽保持良好的完整性。这种多单位载体为肽的肠道特异性递送和控制释放提供了更好设计的载体。

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