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Arabinoxylans (AXs) extracted from distillers dried grains with solubles (DDGSs) were treated with amylase, amyloglucosidase, and protease, to evaluate their effect on the polysaccharide capability to form covalent electro-sprayed nanoparticles. Enzymatically treated arabinoxylans (AXPPs) presented a significant decrease in protein content and molecular weight (31 and 37%, respectively), while the ferulic acid content and the arabinose-to-xylose ratio (A/X) were not statistically modified. The Fourier transform infrared spectra of the AXPPs showed a diminution in the intensity of amide I and amide II bands concerning AXs. The AXPP gels (1% w/v) induced via laccase registered a slight increase in the dimers of ferulic acid cross-linking content (9%) and the G’ value (27%) about the AX gels. The electro-sprayed nanoparticles of AXs and AXPPs (NAXs and NAXPPs, respectively) revealed a spherical and regular morphology via transmission electron microscopy. The nanoparticle diameter was not different for the NAXs and NAXPPs, while the NAXPPs show a significant reduction in Z potential value compared to NAXs. Confocal laser microscopy observations were conducted, to analyze the protein content in the AX network, and a decrease in illuminated areas was observed in the AXPP gels and the NAXPPs. These results indicate that the enzymatical treatment of an AX improves the polysaccharide gelling capability, but does not influence the fabrication of electro-sprayed covalent nanoparticles. NAXs and NAXPPs could be attractive biomaterials for diverse pharmaceutical and biomedical applications.

Polysaccharide biomaterials have gained significant importance in the manufacture of nanoparticles used in colon-targeted drug delivery systems. These systems are a form of non-invasive oral therapy used in the treatment of various diseases. To achieve successful colonic delivery, the chemical, enzymatic and mucoadhesive barriers within the gastrointestinal (GI) tract must be analyzed. This will allow for the nanomaterials to cross these barriers and reach the colon. This review provides information on the development of nanoparticles made from various polysaccharides, which can overcome multiple barriers along the GI tract and affect encapsulation efficiency, drug protection, and release mechanisms upon arrival in the colon. Also, there is information disclosed about the size of the nanoparticles that are usually involved in the mechanisms of diffusion through the barriers in the GI tract, which may influence early drug degradation and release in the digestive tract.

Zein, the major storage protein from corn, has a GRAS (Generally Regarded as Safe) status and may be easily transformed into nanoparticles, offering significant payloads for protein materials without affecting their stability. In this work, the capability of bare zein nanoparticles (mucoadhesive) and nanoparticles coated with poly(ethylene glycol) (mucus-permeating) was evaluated as oral carriers of insulin (I-NP and I-NP-PEG, respectively). Both nanocarriers displayed sizes of around 270 nm, insulin payloads close to 80 µg/mg and did not induce cytotoxic effects in Caco-2 and HT29-MTX cell lines. In Caenorhabditis elegans, where insulin decreases fat storage, I-NP-PEG induced a higher reduction in the fat content than I-NP and slightly lower than the control (Orlistat). In diabetic rats, nanoparticles induced a potent hypoglycemic effect and achieved an oral bioavailability of 4.2% for I-NP and 10.2% for I-NP-PEG. This superior effect observed for I-NP-PEG would be related to their capability to diffuse through the mucus layer and reach the surface of enterocytes (where insulin would be released), whereas the mucoadhesive I-NP would remain trapped in the mucus, far away from the absorptive epithelium. In summary, PEG-coated zein nanoparticles may be an interesting device for the effective delivery of proteins through the oral route.

The laccase induced gelation of maize bran arabinoxylans at 2.5% (w/v) in the presence of insulin or β-lactoglobulin at 0.1% (w/v) was investigated. Insulin and β-lacto-globulin did not modify either the gel elasticity (9 Pa) or the cross-links content (0.03 and 0.015 mg di- and triferulic acids/mg arabinoxylan, respectively). The protein release capability of the gel was also investigated. The rate of protein release from gels was dependent on the protein molecular weight. The apparent diffusion coefficient was 0.99 × 10-7 and 0.79 × 10-7 cm2/s for insulin (5 kDa) and β-lactoglobulin (18 kDa), respectively. The results suggest that maize bran arabinoxylan gels can be potential candidates for the controlled release of proteins.

Several studies have described the health benefits of arabinoxylan as prebiotics; however, other authors have related them with an anti-nutrient effect as arabinoxylan increases the viscosity of the alimentary bolus. In this work, the impact of arabinoxylan and crosslinked arabinoxylan on blood serum lipids and glucose levels of Wistar rats was investigated. Arabinoxylan was extracted from maize bran, presented a Fourier Transform Infra-Red spectrum typical for this polysaccharide, and a molecular weight of 250 kDa. Arabinoxylan solution at 4% (w/v) formed covalent gels induced by laccase. Male Wistar rats were fed a standard diet supplemented with 5% (w/w) lyophilized arabinoxylan or crosslinked arabinoxylan. Blood glucose levels were determined, collecting a drop of blood from the tail vein of rats at 0, 2, and 10 h after food consumption. Total cholesterol, triglycerides, high-density lipoprotein (HDL) cholesterol, and low-density lipoprotein (LDL) cholesterol were also determined. Postprandial blood glucose of the treatment groups was maintained at the same level as the control group. The serum lipid profile levels also remained close to the control group, excepting total cholesterol and LDL-cholesterol, which were higher in crosslinked arabinoxylan treatment but in the range reported for this murine model. The obtained results revealed that consumption of arabinoxylan and crosslinked arabinoxylan at moderated levels does not interfere with the absorption of these nutrients. [ABSTRACT FROM AUTHOR]

P2Et is the standardized extract of Caesalpinia spinosa (C. spinosa), which has shown the ability to reduce primary tumors and metastasis in animal models of cancer, by mechanisms involving the increase in intracellular Ca++, reticulum stress, induction of autophagy, and subsequent activation of the immune system. Although P2Et has been shown to be safe in healthy individuals, the biological activity and bioavailability can be increased by improving the dosage form. This study investigates the potential of a casein nanoparticle for oral administration of P2Et and its impact on treatment efficacy in a mouse model of breast cancer with orthotopically transplanted 4T1 cells. Animals were treated with either free or encapsulated oral P2Et orally or i.p. Tumor growth and macrometastases were evaluated. All P2Et treatments significantly delayed tumor growth. The frequency of macrometastasis was reduced by 1.1 times with P2Et i.p., while oral P2Et reduced it by 3.2 times and nanoencapsulation reduced it by 3.57 times. This suggests that nanoencapsulation led to higher doses of effective P2Et being delivered, slightly improving bioavailability and biological activity. Therefore, the results of this study provide evidence to consider P2Et as a potential adjuvant in the treatment of cancer, while the nanoencapsulation of P2Et provides a novel perspective on the delivery of these functional ingredients.