Predictive selection and evaluation of appropriate functional peptides for intestinal delivery with a porous silica gel.

Bioactive peptides have a positive impact on body functions and conditions and may influence health. However, peptides are degraded by digestive enzymes, such as pepsin in the stomach when ingested orally. In order to solve this problem, we previously focused on porous silica gel and found that by using calcined silica gel, hydrophobic and negatively charged peptides could be efficiently delivered into the intestine, because peptides adsorbed on the cavity of the silica gel could be protected from enzymatic degradation. Therefore, in this study, we attempted to develop peptides whose physicochemical properties were suitable for intestinal delivery without lowering their activity. We also proposed guidelines of predictive selection of such peptides. For that purpose, we selected hypercholesterolemic peptides as a model and re-designed the peptides based on the previously reported color map, in which intestinal delivery degree was predictively depicted as contour lines. As a result, we succeeded in getting five different re-designed peptides from 1265 substituted peptide derivatives. These peptides showed a dual function of being suitable for intestinal delivery with silica gel and for disruption of bile acid micelles. The release amount of IYEYMY was 2.09 times the parent peptide, which was the highest.

Sugarcane bagasse lignin, and silica gel and magneto-silica as drug vehicles for development of innocuous methotrexate drug against rheumatoid arthritis disease in albino rats.

The present study clarifies co-therapy action of deliveries from their textural changes point of view. Methotrexate (MTX) was immobilized onto biodegradable lignin, silica gel and iron/silica nanocomposite. Loaded-MTX was i.p. injected into albino rats at doses of 0.25 and 0.5mg/kg/week for 2.5months, after which spleen, liver, testes and knee joint tissues were collected for tests. IFN-γ and IL-17A mRNA gene expressions in spleen in all biological samples were determined by RT-PCR. Physicochemical features of drug carriers were monitored by XRD, BET-PSD, SEM and TEM. Drug inflammatory-site targeting was found to be closely related to the physico-features of deliverers. The interlayered lignin of micro- and meso-pore channels directed MTX toward concealed infected cells in liver and testes tissues, while meso-structured silica flacks satisfied by gathering MTX around knee joints. The magneto-silica nanocomposite targeted MTX toward spleen tissue, which is considered as a lively factory for the production of electron rich compounds.