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自乳化双药物递送系统提高低聚原花青素的口服生物利用度。

Enhanced oral bioavailability of oligomeric proanthocyanidins by a self-double-emulsifying drug delivery system.

作者信息

Tian Yuan, Mao Xinyu, Sun Rui, Zhang Ming, Xia Qiang

机构信息

School of Biological Sciences and Medical Engineering Southeast University Nanjing China.

State Key Laboratory of Bioelectronics School of Biological Sciences and Medical Engineering Southeast University Nanjing China.

出版信息

Food Sci Nutr. 2020 Jun 1;8(7):3814-3825. doi: 10.1002/fsn3.1673. eCollection 2020 Jul.

Abstract

The present study aims at the formulation and evaluation of solid self-double-emulsifying drug delivery system (SDEDDS) to increase the bioavailability of oligomeric proanthocyanidin (OPC). The formulation is prepared through two-step method and is able to form water-in-oil-in-water (W/O/W) double emulsions after diluted with aqueous medium while keeping the drug in inner water phase. Solid-state characterization is performed by DSC and X-ray powder diffraction. Furthermore, antioxidant capacity shows that OPC is preserved by the solid SDEDDS. OPC-SDEDDS exhibit sustained release of OPC under the conditions mimicking gastrointestinal tract. The result shows that bioaccessibility of OPC is improved after incorporating into SDEDDS formulation compared to pure drug. The proposed SDEDDS is a promising carrier strategy for delivering the hydrophilic compounds with low-oral bioavailability.

摘要

本研究旨在制备和评价固体自乳化药物递送系统(SDEDDS),以提高低聚原花青素(OPC)的生物利用度。该制剂通过两步法制备,在用水性介质稀释后能够形成水包油包水(W/O/W)双重乳液,同时将药物保留在内水相中。通过差示扫描量热法(DSC)和X射线粉末衍射进行固态表征。此外,抗氧化能力表明固体SDEDDS可保留OPC。OPC-SDEDDS在模拟胃肠道的条件下呈现OPC的缓释特性。结果表明,与纯药物相比,将OPC掺入SDEDDS制剂后其生物可及性得到改善。所提出的SDEDDS是一种用于递送口服生物利用度低的亲水性化合物的有前景的载体策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e8c/7382205/0ebd84f4cb26/FSN3-8-3814-g001.jpg

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