Abstract
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.
Highlights
Oral administration is often the best route for bioactive agents that have therapeutic or preventive effects in which patient compliance is important
Lipid-based nanodelivery systems, such as self-emulsifying drug delivery systems (SEDDSs), nanoemulsions, microemulsions, solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs), encapsulate bioactive compounds and increase their solubility and bioavailability when administered by the oral route (Figure 1)
We focus on studies that used different lipid nanocarriers to encapsulate vitamins, such as SEDDSs, nanoemulsions, microemulsions, SLNs, and NLCs
Summary
Oral administration is often the best route for bioactive agents that have therapeutic or preventive effects in which patient compliance is important. Chemical and enzymatic degradation reduces the amount that is available for absorption, the GI membrane prevents permeation into the systemic circulation, and molecules with low water solubility do not readily dissolve in the GI tract All of these factors contribute to the low bioavailability and bioactivity of oral drugs [2]. Lipid-based nanodelivery systems, such as self-emulsifying drug delivery systems (SEDDSs), nanoemulsions, microemulsions, solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs), encapsulate bioactive compounds and increase their solubility and bioavailability when administered by the oral route (Figure 1). Cells.The transport of delivery lipid nanoparticles into epithelium cells can involve in macropinocytosis lipid-based systems can increase the bioavailability of oral various pathways, lipid raft-dependent clathrin-mediated endocytosis, and bioactive agents byincluding numerous mechanisms (Figureendocytosis, 2). We conclude with a discussion of the emerging applications of vitamin-loaded lipid nanoparticles
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