Preparation and evaluation of oleoyl-carboxymethy-chitosan (OCMCS) nanoparticles as oral protein carriers.

Oleoyl-carboxymethy chitosan (OCMCS) nanoparticles based on chitosan with different molecular weights (50, 170 and 820 kDa) were prepared by self-assembled method. The nanoparticles had spherical shape, positive surface charges and the mean diameters were 157.4, 274.1 and 396.7 nm, respectively. FITC-labeled OCMCS nanoparticles were internalized via the intestinal mucosa and observed in liver, spleen, intestine and heart following oral deliverance to carps (Cyprinus carpio). Extracellular products (ECPs) of Aeromonas hydrophila as microbial antigen was efficiently loaded to form OCMCS-ECPs nanoparticles and shown to be sustained release in PBS. Significantly higher (P < 0.05) antigen-specific antibodies were detected in serum after orally immunized with OCMCS-ECPs nanoparticles than that immunized with ECPs alone and non-immunized in control group in carps. These results implied that amphiphilic modified chitosan nanoparticles had great potential to be applied as carriers for the oral administration of protein drugs.

Physical and turbidimetric properties of cholecalciferol- and menaquinone-loaded lipid nanocarriers emulsified with polysorbate 80 and soy lecithin.

The present study aimed to investigate the physical and turbidimetric properties of cholecalciferol- and menaquinone-loaded lipid nanocarriers emulsified with different ratios of polysorbate 80 and soy lecithin. The lipid nanocarriers were subjected to three different heat treatments, LTLT (low temperature long time), HTST (high temperature short time), and autoclave treatments. Both cholecalciferol and menaquinone were successfully encapsulated in lipid nanocarriers and there was little loss of them during preparation. The droplet size of lipid nanocarriers emulsified with only polysorbate 80 increased and its PDI became larger than 0.3 after autoclave treatment. Moreover, 30.9% and 49.4% of cholecalciferol and menaquinone, respectively, were lost. In turbidimetric analysis, the destabilization by creaming formation in the upper layer of the lipid nanocarriers emulsified with a high polysorbate ratio was observed. However, the use of combination of both emulsifiers inhibited destabilization by flocculation as well as retained the cholecalciferol and menaquinone after all heat treatments.

Enhancing oral bioavailability using preparations of apigenin-loaded W/O/W emulsions: In vitro and in vivo evaluations.

We analyzed the physical properties and digestibility of apigenin-loaded emulsions as they passed through a simulated digestion model. As the emulsion passed through the simulated stages of digestion, the particle size and zeta potential of all the samples changed, except for the soybean oil-Tween 80 emulsion, in which zeta potential remained constant, through all stages, indicating that soybean oil-Tween 80 emulsions may have an effect on stability during all stages of digestion. Fluorescence microscopy was used to observe the morphology of the emulsions at each step. The in vivo pharmacokinetics revealed that apigenin-loaded soybean oil-Tween 80 emulsions had a higher oral bioavailability than did the orally administrated apigenin suspensions. These results suggest that W/O/W multiple emulsions formulated with soybean oil and tween 80 have great potential as targeted delivery systems for apigenin, and may enhance in vitro and in vivo bioavailability when they pass through the digestive tract.