Diethylene glycol monoethyl ether-mediated nanostructured lipid carriers enhance trans-ferulic acid delivery by Caco-2 cells superior to solid lipid nanoparticles.

IF 2.1 4区 医学 Q3 PHARMACOLOGY & PHARMACY
Hongyu Zhang, Jingwen Guo, Zhi Wang, Na Wang, Nianping Feng, Yongtai Zhang
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Abstract

This work aimed to compare the performance of trans-ferulic acid-encapsulated nanostructured lipid carriers (NLCs) and solid lipid nanoparticles (SLNs) for transport by Caco-2 cells. The NLC particles (diameter: 102.6 nm) composed of Compritol® 888 ATO, ethyl oleate, Cremophor® EL, and Transcutol® P were larger than the SLNs (diameter: 86.0 nm) formed without liquid lipid (ethyl oleate), and the former had a higher encapsulation efficiency for trans-ferulic acid (p < 0.05). In vitro cultured Caco-2 cell transport was used to simulate intestinal absorption, and the cellular uptake of NLCs was higher than that of SLNs (p < 0.05). Compared to SLNs, NLCs greatly enhanced trans-ferulic acid permeation through the MillicellTM membrane (p < 0.05). This work confirms that NLCs have better properties than SLNs in terms of increasing drug transport by Caco-2 cells. This helps to comprehend the approach by which NLC-mediated oral bioavailability of trans-ferulic acid is better than that mediated by SLNs, as shown in our previous report.

二乙二醇单乙醚介导的纳米结构脂质载体比固体脂质纳米颗粒更能增强Caco-2细胞对反式阿魏酸的传递。
本研究旨在比较反式阿魏酸封装的纳米结构脂质载体(NLCs)和固体脂质纳米颗粒(SLNs)在Caco-2细胞运输中的性能。由Compritol®888 ATO、油酸乙酯、Cremophor®EL和Transcutol®P组成的NLC颗粒(直径:102.6 nm)大于不含液体脂质(油酸乙酯)形成的sln(直径:86.0 nm),且前者对反式阿威酸的包封效率更高(P < 0.05)。体外培养Caco-2细胞转运模拟肠道吸收,NLCs的细胞吸收量高于sln (p < 0.05)。与sln相比,NLCs显著增强了反式阿魏酸通过MillicellTM膜的渗透(p < 0.05)。这项工作证实,在增加Caco-2细胞的药物转运方面,NLCs比sln具有更好的特性。这有助于理解nlc介导的反式阿魏酸口服生物利用度优于sln介导的方法,如我们之前的报告所示。
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来源期刊
Acta Pharmaceutica
Acta Pharmaceutica PHARMACOLOGY & PHARMACY-
CiteScore
5.20
自引率
3.60%
发文量
20
审稿时长
>12 weeks
期刊介绍: AP is an international, multidisciplinary journal devoted to pharmaceutical and allied sciences and contains articles predominantly on core biomedical and health subjects. The aim of AP is to increase the impact of pharmaceutical research in academia, industry and laboratories. With strong emphasis on quality and originality, AP publishes reports from the discovery of a drug up to clinical practice. Topics covered are: analytics, biochemistry, biopharmaceutics, biotechnology, cell biology, cell cultures, clinical pharmacy, drug design, drug delivery, drug disposition, drug stability, gene technology, medicine (including diagnostics and therapy), medicinal chemistry, metabolism, molecular modeling, pharmacology (clinical and animal), peptide and protein chemistry, pharmacognosy, pharmacoepidemiology, pharmacoeconomics, pharmacodynamics and pharmacokinetics, protein design, radiopharmaceuticals, and toxicology.
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