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壳聚糖/甘露醇微球作为螺旋藻生物活性肽提取物口服给药传递系统的研制。

Development of Chitosan/Mannitol Microparticles as Delivery System for the Oral Administration of a Spirulina Bioactive Peptide Extract.

机构信息

Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, I-84084 Fisciano (SA), Italy.

出版信息

Molecules. 2020 Apr 29;25(9):2086. doi: 10.3390/molecules25092086.

Abstract

contains several compounds showing nutritional and therapeutic benefits. Recently, a series of peptides able to reduce the blood pressure level and to enhance the endothelial vasorelaxation was isolated from the hydrolyzed highly water-soluble extract (HSE). However, HSE shows critical organoleptic characteristics also having poor intestinal permeability, limiting absorption when orally delivered. This research aims to overcome the critical issues through the encapsulation of HSE in Chitosan/Mannitol-(CM)-based microparticles by spray drying. The produced powders (CM-HSE) showed good process yield (≈70%) and encapsulation efficiency (≈100%) also having good derived flow properties as well as stability up to six months storage. The microparticles constituting the spray-dried powder resulted in an amorphous micrometric state (d ≈ 14 µm) able to retain dark colour and unpleasant smell of raw HSE. Moreover, the in vitro permeation study by Franz cell indicated that the engineered microparticles are able to enhance the permeation of HSE through an intestinal biomimetic barrier (551.13 μg/cm CM-HSE vs. 315.46 μg/cm HSE at 270 min).

摘要

含有多种具有营养和治疗功效的化合物。最近,从高度水溶性提取物(HSE)的水解产物中分离出了一系列能够降低血压水平并增强内皮血管舒张功能的肽。然而,HSE 具有关键的感官特性,同时肠道通透性差,口服给药时吸收受限。本研究旨在通过喷雾干燥将 HSE 包封在壳聚糖/甘露醇(CM)基微球中克服这些关键问题。所制备的粉末(CM-HSE)具有良好的工艺收率(约 70%)和包封效率(约 100%),具有良好的衍生流动性能以及长达六个月的储存稳定性。喷雾干燥粉末中的微球形成无定形的微尺度状态(d ≈ 14 µm),能够保留 HSE 原始的深色和难闻气味。此外,通过 Franz 细胞进行的体外渗透研究表明,工程化的微球能够增强 HSE 通过肠道仿生屏障的渗透(270 分钟时,CM-HSE 的渗透量为 551.13 μg/cm,而 HSE 的渗透量为 315.46 μg/cm)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a59b/7248919/79a8329a9f1e/molecules-25-02086-g001.jpg

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