Absorption Study of Genistein Using Solid Lipid Microparticles and Nanoparticles: Control of Oral Bioavailability by Particle Sizes

Abstract

In this study, the effect of particle size of genistein-loaded solid lipid particulate systems on drug dissolution behavior and oral bioavailability was investigated. Genistein-loaded solid lipid microparticles and nanoparticles were prepared with glyceryl palmitostearate. Except for the particle size, other properties of genistein-loaded solid lipid microparticles and nanoparticles such as particle composition and drug loading efficiency and amount were similarly controlled to mainly evaluate the effect of different particle sizes of the solid lipid particulate systems on drug dissolution behavior and oral bioavailability. The results showed that genistein-loaded solid lipid microparticles and nanoparticles exhibited a considerably increased drug dissolution rate compared to that of genistein bulk powder and suspension. The microparticles gradually released genistein as a function of time while the nanoparticles exhibited a biphasic drug release pattern, showing an initial burst drug release, followed by a sustained release. The oral bioavailability of genistein loaded in solid lipid microparticles and nanoparticles in rats was also significantly enhanced compared to that in bulk powders and the suspension. However, the bioavailability from the microparticles increased more than that from the nanoparticles mainly because the rapid drug dissolution rate and rapid absorption of genistein because of the large surface area of the genistein-solid lipid nanoparticles cleared the drug to a greater extent than the genistein-solid lipid microparticles did. Therefore, the findings of this study suggest that controlling the particle size of solid-lipid particulate systems at a micro-scale would be a promising strategy to increase the oral bioavailability of genistein.

Transmucosal Solid Lipid Nanoparticles to Improve Genistein Absorption via Intestinal Lymphatic Transport

“…This may be attributed to the presence of a small amount of GEN in the external matrix of SLN, as previously hypothesized based on the zeta potential results. This is in disagreement with the previous work of Kim et al, which reported that GEN-loaded SLN rapidly release GEN, which could then be absorbed into the upper part of the intestine and could undergo first-pass metabolism in the liver [ 38 ]. The difference in this behaviour could be attributed to the lipid and surfactant composition affecting GEN entrapment.…”

Recent developments in solid lipid nanoparticle and surface-modified solid lipid nanoparticle delivery systems for oral delivery of phyto-bioactive compounds in various chronic diseases

“…Smaller SLNs can be extensively absorbed in mesenteric vessels, leading to a higher absorption of the bioactive compounds rather than reaching the colon. 63 In another study, curcumin-loaded SLNs were studied for their antitumor activity through intravenous administration, and curcumin showed a 1.25 times enhanced bioavailability. 62 Other research groups compared curcumin-loaded SLNs administered via intravenous or oral routes and showed 30 or 16.4 times higher bioavailability of curcumin, respectively.…”

Nanodelivery of Natural Antioxidants: An Anti-aging Perspective

“…According to the authors, this effect could be due to higher solubility and gastrointestinal release of nanomicelle-loaded genistein. The oral bioavailability was also found to be improved in genistein loaded in solid lipid nanoparticles compared to that for its suspensions or bulk powders (Kim J. T. et al, 2017). Recently, Pool et al (2018) found in studies with HT29 human colon cancer cells that incorporation of genistein into small (∼33 nm) PEGylated silica nanoparticles may substantially potentiate its antioxidant effects.…”