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口服维生素C递送稳定性增强:一种通过动态高压微流化制备和包封脂质体的新型大规模方法。

Enhanced Stability of Oral Vitamin C Delivery: A Novel Large-Scale Method for Liposomes Production and Encapsulation through Dynamic High-Pressure Microfluidization.

作者信息

Romano Eugenia, Palladino Roberta, Cannavale Mariagabriella, Lamparelli Erwin Pavel, Maglione Barbara

机构信息

Farmaceutici Damor SpA, Via E. Scaglione 27, 80125 Napoli, NA, Italy.

Department of Medicine, Surgery and Dentistry, University of Salerno, Via S. Allende, 84081 Baronissi, SA, Italy.

出版信息

Nanomaterials (Basel). 2024 Mar 14;14(6):516. doi: 10.3390/nano14060516.

Abstract

In recent years, nanocarriers have been widely used as an effective solution for oral administration of pharmaceuticals. However, there is still an urgent need to speed up their translation to clinical practice. Cost-effective and industrially scalable methodologies are still needed. Herein, the production of vitamin C-loaded liposomes for nutraceutical purposes has been investigated and optimized by adopting a High-Pressure Homogenizer. Initially, the impact of process parameters on particles size, distributions, and morphology was explored. The findings document that the pressure and cycle manipulation allow for control over liposome size and polydispersity, reaching a maximum encapsulation efficiency exceeding 80%. This significantly improves the storage stability of vitamin C, as demonstrated by monitoring its antioxidant activity. Furthermore, the in vitro simulation of gastrointestinal digestion shows that liposomes could protect the active substance from damage and control its release in the gastrointestinal fluid. Thus, the whole nanodelivery system can contribute to enhancing vitamin C bioavailability. In conclusion, the results indicate that this innovative approach to producing vitamin C liposomes holds promise for clinical translation and industrial scale-up. Indeed, by utilizing food-grade materials and straightforward equipment, it is possible to produce stable and functional liposomes suitable for health products.

摘要

近年来,纳米载体已被广泛用作药物口服给药的有效解决方案。然而,仍迫切需要加快其向临床实践的转化。仍需要具有成本效益且可在工业上扩展的方法。在此,通过采用高压均质机对用于营养保健品目的的负载维生素C的脂质体的生产进行了研究和优化。最初,探索了工艺参数对颗粒大小、分布和形态的影响。研究结果表明,通过压力和循环操作可以控制脂质体的大小和多分散性,最大包封效率超过80%。通过监测其抗氧化活性表明,这显著提高了维生素C的储存稳定性。此外,胃肠道消化的体外模拟表明,脂质体可以保护活性物质免受损伤,并控制其在胃肠液中的释放。因此,整个纳米递送系统有助于提高维生素C的生物利用度。总之,结果表明这种生产维生素C脂质体的创新方法有望实现临床转化和工业放大。事实上,通过使用食品级材料和简单的设备,可以生产出适用于健康产品的稳定且功能性的脂质体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eff0/10975307/9e3e1c2129ed/nanomaterials-14-00516-g001.jpg

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