Department of Nutrition and Health Sciences, Chang Gung University of Science and Technology, Kweishan, Taoyuan 33302, Taiwan.
Research Center for Food and Cosmetic Safety and Research Center for Chinese Herbal Medicine, Chang Gung University of Science and Technology, Kweishan, Taoyuan 33302, Taiwan.
Nutrients. 2019 Jan 1;11(1):68. doi: 10.3390/nu11010068.
The chemical environment and enzymes in the gastrointestinal (GI) membrane limit the oral absorption of some vitamins. The GI epithelium also contributes to the poor permeability of numerous antioxidant agents. Thus, lipophilic vitamins do not readily dissolve in the GI tract, and therefore they have low bioavailability. Nanomedicine has the potential to improve the delivery efficiency of oral vitamins. In particular, the use of lipid nanocarriers for certain vitamins that are administered orally can provide improved solubility, chemical stability, epithelium permeability and bioavailability, half-life, nidus targeting, and fewer adverse effects. These lipid nanocarriers include self-emulsifying drug delivery systems (SEDDSs), nanoemulsions, microemulsions, solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs). The use of nontoxic excipients and sophisticated material engineering of lipid nanosystems allows for control of the physicochemical properties of the nanoparticles and improved GI permeation via mucosal or lymphatic transport. In this review, we highlight recent progress in the development of lipid nanocarriers for vitamin delivery. In addition, the same lipid nanocarriers used for vitamins may also be effective as carriers of vitamin derivatives, and therefore enhance their oral bioavailability. One example is the incorporation of d-α-tocopheryl polyethylene glycol succinate (TPGS) as the emulsifier in lipid nanocarriers to increase the solubility and inhibit P-glycoprotein (P-gp) efflux. We also survey the concepts and discuss the mechanisms of nanomedical techniques that are used to develop vitamin-loaded nanocarriers.
胃肠道(GI)膜中的化学环境和酶限制了某些维生素的口服吸收。GI 上皮也导致许多抗氧化剂的通透性差。因此,亲脂性维生素不易溶解在胃肠道中,因此生物利用度较低。纳米医学有潜力提高口服维生素的递送效率。特别是,某些口服给予的维生素的脂质纳米载体的使用可以提供改善的溶解度、化学稳定性、上皮通透性和生物利用度、半衰期、病灶靶向和更少的不良反应。这些脂质纳米载体包括自乳化药物递送系统(SEDDS)、纳米乳液、微乳液、固体脂质纳米粒(SLN)和纳米结构脂质载体(NLC)。使用无毒赋形剂和脂质纳米系统的复杂材料工程可以控制纳米颗粒的物理化学性质,并通过粘膜或淋巴转运改善 GI 通透性。在这篇综述中,我们强调了用于维生素递送的脂质纳米载体的最新进展。此外,用于维生素的相同脂质纳米载体也可以作为维生素衍生物的载体有效,从而提高其口服生物利用度。一个例子是将 d-α-生育酚聚乙二醇琥珀酸酯(TPGS)用作脂质纳米载体中的乳化剂,以提高溶解度并抑制 P 糖蛋白(P-gp)外排。我们还调查了纳米医学技术的概念,并讨论了用于开发载有维生素的纳米载体的机制。