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脂基质:一种新型基于抗坏血酸棕榈酸酯的脂质基质,可增强锯棕榈油的肠内吸收。

Lipomatrix: A Novel Ascorbyl Palmitate-Based Lipid Matrix to Enhancing Enteric Absorption of Serenoa Repens Oil.

机构信息

Nutraceutical Research and Innovation Technology Department, Labomar Research, Via Fabio Filzi, 55, 31036 Istrana (TV), Italy.

Head, Nutraceutical Research and Innovation Technology Department, Labomar Research, 31036 Istrana (TV), Italy.

出版信息

Int J Mol Sci. 2019 Feb 4;20(3):669. doi: 10.3390/ijms20030669.

DOI:10.3390/ijms20030669
PMID:30720739
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6386960/
Abstract

The class of lipophilic compounds coming from vegetal source represents a perspective in the adjuvant treatment of several human diseases, despite their poor bioavailability in humans. These compounds are generally soluble in fats and poorly soluble in water. The major reason for the poor bioavailability of lipophilic natural compounds after oral uptake in humans is related to their reduced solubility in enteric water-based fluids, leading to an ineffective contact with absorbing epithelium. The main goal to ensure efficacy of such compounds is then creating technological conditions to deliver them into the first enteric tract as hydro-dispersible forms to maximize epithelial absorption. The present work describes and characterizes a new technological matrix (Lipomatrix, Labomar Research, Istrana, TV, Italy) based on a molten fats core in which Ascorbyl Palmitate is embedded, able to deliver lipophilic compounds in a well-dispersed and emulsified form once exposed to duodenal fluids. Authors describe and quantify Lipomatrix delivery of oil through an innovative in vitro model of human gastro-enteric digestion, reporting results of its improved bioaccessibility, enteric absorption and efficacy compared with not formulated oil-containing commercial products using in vitro models of human intestine and prostatic tissue.

摘要

来自植物源的亲脂性化合物类代表了一类有前景的辅助治疗多种人类疾病的物质,尽管它们在人类中的生物利用度较差。这些化合物通常在脂肪中溶解,而在水中溶解度较差。亲脂性天然化合物在人类口服吸收后生物利用度较差的主要原因与它们在肠内水性流体中的溶解度降低有关,导致与吸收上皮的接触效果不佳。确保此类化合物疗效的主要目标是创造技术条件,使它们以水可分散的形式递送至第一道肠内途径,以最大限度地提高上皮吸收。本工作描述并表征了一种新的基于熔融脂肪核的技术基质(Lipomatrix,Labomar Research,Istrana,TV,意大利),其中嵌入了棕榈酸抗坏血酸,一旦暴露于十二指肠流体中,它能够以良好分散和乳化的形式递送亲脂性化合物。作者描述并定量了 Lipomatrix 对油的递送,通过一种创新性的人体胃肠消化体外模型,报告了与未配方含油商业产品相比,其生物利用度、肠内吸收和疗效的改善结果,这些结果使用了人体肠道和前列腺组织的体外模型。

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