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一种用于增强全反式维甲酸口服吸收的新型微乳剂的研制。

Development of a novel microemulsion for oral absorption enhancement of all-trans retinoic acid.

作者信息

Subongkot Thirapit, Ngawhirunpat Tanasait

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Burapha University, Chonburi, Thailand.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand.

出版信息

Int J Nanomedicine. 2017 Aug 3;12:5585-5599. doi: 10.2147/IJN.S142503. eCollection 2017.

Abstract

This study was aimed to develop a novel microemulsion that contained oleth-5 as a surfactant to enhance the oral absorption of all-trans retinoic acid (ATRA). The prepared microemulsion was evaluated for its particle size, shape, zeta potential, in vitro release, in vitro intestinal absorption, intestinal membrane cytotoxicity and stability. The obtained microemulsion was spherical in shape with a particle size of <200 nm and a negative surface charge. The in vitro release of the ATRA-loaded microemulsion was best fit with the zero-order model. This microemulsion significantly improved the intestinal absorption of ATRA. Confocal laser scanning microscopy analysis using a fluorescent dye-loaded microemulsion also confirmed the intestinal absorption result. The intestinal membrane cytotoxicity of the ATRA-loaded microemulsion did not differ from an edible oil (fish oil). Stability testing showed that the ATRA-loaded microemulsion was more stable at 25°C than 40°C.

摘要

本研究旨在开发一种新型微乳剂,其含有油醇聚醚-5作为表面活性剂,以提高全反式维甲酸(ATRA)的口服吸收。对制备的微乳剂进行了粒径、形状、ζ电位、体外释放、体外肠道吸收、肠膜细胞毒性和稳定性评估。所获得的微乳剂呈球形,粒径<200nm,表面带负电荷。载有ATRA的微乳剂的体外释放最符合零级模型。这种微乳剂显著提高了ATRA的肠道吸收。使用载有荧光染料的微乳剂进行的共聚焦激光扫描显微镜分析也证实了肠道吸收结果。载有ATRA的微乳剂的肠膜细胞毒性与食用油(鱼油)无差异。稳定性测试表明,载有ATRA的微乳剂在25°C比在40°C更稳定。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/359b/5548273/74767a044fd1/ijn-12-5585Fig1.jpg

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