制备虾青素/玉米黄质纳米结构脂质载体以提高生物利用度:特性、稳定性和渗透性研究。

IF 2.1 4区 医学 Q3 PHARMACOLOGY & PHARMACY Acta Pharmaceutica Pub Date : 2023-12-26 Print Date: 2023-12-01 DOI:10.2478/acph-2023-0038
Kristina Radić, Ana Isabel Barbosa, Salette Reis, Marijan Marijan, Sofia Antunes Costa Lima, Dubravka Vitali Čepo
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引用次数: 0

摘要

虾青素(ASTA)和玉米黄质(ZEA)是类黄素胡萝卜素,具有广泛的促进健康的特性。然而,它们的利用率有限,主要原因是水溶性差、生物利用率有限、易氧化以及光热不稳定性。这项工作的目的是开发载入 ASTA 和 ZEA 的纳米结构脂质载体(NLCs),以防止它们降解并提高其肠道稳定性/渗透性。获得的 NLC 的特征是:ASTA-NLC 的有效直径为 294 nm,ZEA-NLC 的有效直径为 280 nm;多分散指数(PDI)低于 0.2;ZETA 电位分别为 -29.4 mV 和 -29.0 mV。有趣的是,尽管理化特性相似,但我们的研究发现 ASTA-NLC 和 ZEA-NLC 的封装效率存在差异(分别为 58.0% 和 75.5%)。获得的 NLC 在室温或 4 °C 黑暗环境中储存 21 天后保持稳定。胃肠道稳定性调查显示,有效直径和 PDI 在胃部条件下没有变化,而在肠道条件下这两个参数都发生了显著变化。我们的研究结果首次表明,在体外模型中研究的 ASTA 和 ZEA-NLCs 的肠道吸收率都明显增加(与纯化合物相比),并受到粘液存在的影响。这项研究提供了有关使用 NLC 作为 ASTA 和 ZEA 输送系统的优势的有用数据,这可能会促进它们在食品和制药行业的应用。
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Preparation of astaxanthin/zeaxanthin-loaded nanostructured lipid carriers for enhanced bioavailability: Characterization-, stability-and permeability study.

Astaxanthin (ASTA) and zeaxanthin (ZEA) are xanthophyll carotenoids showing a wide spectrum of health-promoting properties. However, their utilization is limited, mostly due to poor water solubility, limited bioavailability, and a tendency to oxidate, as well as photo- and thermal instability. The aim of this work was to develop ASTA- and ZEA-loaded nano-structured lipid carriers (NLCs) that would protect them against degradation and improve their intestinal stability/permeability. Obtained NLCs were characterized by an effective diameter of 294 nm for ASTA-NLC and 280 nm for ZEA-NLC; polydispersity index (PDI) lower than 0.2; and zeta potential of -29.4 mV and -29.0 mV, respectively. Interestingly, despite similar physicochemical characteristics, our investigation revealed differences in the encapsulation efficiency of ASTA-NLC and ZEA-NLC (58.0 % vs. 75.5 %, respectively). Obtained NLCs were stable during a 21 day-storage period in the dark at room temperature or at 4 °C. Investigation of gastrointestinal stability showed no change in effective diameter and PDI under gastric conditions while both parameters significantly changed under intestinal conditions. Our results showed for the first time that both ASTA- and ZEA-NLCs intestinal absorption investigated in the in vitro model is significantly increased (in relation to pure compounds) and is affected by the presence of mucus. This study provides useful data about the advantages of using NLC as a delivery system for ASTA and ZEA that might facilitate their applications in the food and pharmaceutical industry.

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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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