Eun Suh Kim

Nanoencapsulation of Red Ginseng Extracts Using Chitosan with Polyglutamic Acid or Fucoidan for Improving Antithrombotic Activities

The potential of nanoencapsulation using bioactive coating materials for improving antithrombotic activities of red ginseng extract (RG) was examined. RG-loaded chitosan (CS) nanoparticles were prepared using antithrombotic materials, polyglutamic acid (PGA) or fucoidan (Fu). Both CS-PGA (P-NPs, 360 ± 67 nm) and CS-Fu nanoparticles (F-NPs, 440 ± 44 nm) showed sustained ginsenoside release in an acidic environment and improved ginsenoside solubility by approximately 122.8%. Both in vitro rabbit and ex vivo rat platelet aggregation of RG (22.3 and 41.5%) were significantly (p < 0.05) decreased within P-NPs (14.4 and 30.0%) and F-NPs (12.3 and 30.3%), respectively. Although RG exhibited no effect on in vivo carrageenan-induced mouse tail thrombosis, P-NPs and F-NPs demonstrated significant effects, likely the anticoagulation activity of PGA and Fu. Moreover, in the in vivo rat arteriovenous shunt model, P-NPs (156 ± 6.8 mg) and F-NPs (160 ± 3.2 mg) groups showed significantly lower thrombus formation than that of RG (190 ± 5.5 mg). Therefore, nanoencapsulation using CS, PGA, and Fu is a potential for improving the antithrombotic activity of RG.

Calcium-alginate microparticles for sustained release of catechin prepared via an emulsion gelation technique

Catechin-loaded Ca-alginate beads and microparticles were prepared by an emulsion gelation method using sunflower oil for efficient sustained release of catechin. The emulsion was prepared by sequential mixing of alginate, oil, and oleic acid ester as an emulsifier. Encapsulation efficiency (EE) and inhibition of catechin release of the beads were significantly increased approximately to 453.83 and 148.71% by the emulsion gelation technique, respectively (p<0.05). For the microparticles, the highest inhibition of catechin release after 1 h of incubation (78.82%) was observed at the microparticles prepared by 5% (w/w) oil, 3% (w/w) alginate, 4% (w/v) CaCl2, and 200 mg catechin with the most hydrophilic emulsifier, decaglycerol mono-ester. Moreover, the catechin release was sustained at acidic conditions and increased with increase in pH of release medium. These results suggest that catechin encapsulation within Ca-alginate particles by emulsion gelation method can be an effective delivery system for catechin.

Improving the water solubility and antimicrobial activity of silymarin by nanoencapsulation

The aims of this study were to improve the water solubility and antimicrobial activity of milk thistle silymarin by nanoencapsulation and to assess the functions of silymarin nanoparticle-containing film as an antimicrobial food-packaging agent. Silymarin nanoparticles were prepared using water-soluble chitosan (WCS) and poly-γ-glutamic acid (γ-PGA). As the WCS and silymarin concentrations increased, particle size and polydispersity index (PDI) significantly increased. Nanoencapsulation significantly improved the water solubility of silymarin 7.7-fold. Antimicrobial activity of silymarin was effectively improved when silymarin was entrapped within the nanocapsule compared to when it was not entrapped. Films incorporating silymarin nanoparticles had better antimicrobial activity than films incorporating free silymarin. The results suggest that silymarin nanoparticles have applications in antimicrobial food additives and food packing.

Microencapsulation of catechin with high loading and encapsulation efficiencies using soaking methods

Catechin-loaded calcium alginate microparticles with high encapsulation and loading efficiencies were prepared using two types of soaking methods; swelling and absorption methods. The soaking methods, respectively, showed approximately 2.4× and 21.7× higher encapsulation and loading efficiencies than the conventional method. Compared with the swelling method, the absorption method showed significantly (p<0.05) higher encapsulation and loading efficiencies that were controlled in the range of 10.6-51.6 and 4.9-38.2%, respectively, under different preparation conditions, including alginate viscosity, blank particle quantity, and the catechin concentration. The absorption method also showed better sustained release in simulated gastric and intestinal fluids and a smaller particle size with uniform morphological properties than the swelling method. The absorption method is a promising method for microencapsulation of catechin.

Release properties and cellular uptake in Caco-2 cells of size-controlled chitosan nanoparticles

The influences of particle size on the physicochemical, release, and cellular uptake properties of chitosan nanoparticles (CSNPs) were investigated. Ionotropic CSNPs of different sizes (200-1000 nm) loaded with two model core materials (resveratrol or coumarin-6) were prepared using tripolyphosphate and carrageenan as cross-linkers. With an increase of particle size, zeta potential (34.6 ± 0.5 to 51.1 ± 0.9) and entrapment efficiency (14.9 ± 1.4 to 40.9 ± 1.9) of the CSNPs were significantly (p < 0.05) increased and release rates were decreased. However, Caco-2 cellular uptake of CSNPs were significantly increased from 3.70 ± 0.03 to 5.24 ± 0.20 with an increase of particle size from 200 to 600 nm, whereas those significantly decreased from 5.24 ± 0.20 to 4.55 ± 0.2 for particles larger than 600 nm in transwell assay. Moreover, much the same uptake patterns were also observed in confocal microscopy and flow cytometry. Investigation of cellular uptake of CSNPs revealed positive correlations between ZP and EE and indicated the effects of complex factors of nanoparticles other than size. These results provide a better understanding of CSNPs absorption and raises the possibility of controlling alternative nanoparticle properties to enhance bioavailability.

Preparation and Characterization of Mucoadhesive Nanoparticles for Enhancing Cellular Uptake of Coenzyme Q10

The mucoadhesive nanoparticles (NPs) for oral delivery of coenzyme Q10 (CoQ10) were prepared using natural mucoadhesive polysaccharides, chitosan (CS), and dextran sulfate sodium salt (DS) in order to improve the solubility, cellular uptake, and thermo- and photostability of CoQ10. CoQ10-loaded NPs were prepared in the range of 340-450 nm with an entrapment efficiency of 60-98%. The mucoadhesiveness and cellular uptake of NPs were evaluated by measuring the amount of mucin adsorbed on NPs and CoQ10 absorbed in Caco-2 cells, respectively. CS/DS NPs had higher mucoadhesive strength than CS/sodium triphosphate pentabasic NPs (control group). Moreover, the solubility, cellular uptake, thermo- and photostability of CS/DS NPs were significantly improved compared with non-nanoencapsulated free CoQ10. Particularly, CS/DS NPs prepared with 0.5 mg/mL of CS and DS produced the highest mucoadhesiveness, solubility, cellular uptake, and cellular antioxidant activity. Thus, mucoadhesive CS/DS NPs may be an effective oral delivery platform for improving bioavailability of CoQ10.

Preparation, characterization, and cellular uptake of resveratrol-loaded trimethyl chitosan nanoparticles

The aim of the study was to encapsulate resveratrol (RV) in trimethyl chitosan (TMC) nanoparticles cross-linked with tripolyphosphate (TPP) and/or alginate to achieve controlled release and improved cellular uptake. TMC (degree of quaternization of 78%) was prepared by reacting purified chitosan with iodomethane. Three types of RV-loaded TMC nanoparticles were prepared: TMC–TPP (TP-NPs), TMC–alginate (TA-NPs), and TMC–alginate–TPP (TAP-NPs). TA-NPs and TAP-NPs showed lower particle size and encapsulation efficiency (EE), better distribution, and more sustained release than TP-NPs due to the high molecular weight and viscous property of alginate. Caco-2 cellular uptake of RV was improved by TMC nanoencapsulation, and TP-NPs showed the highest uptake due to its significantly higher EE. Compared with TAP-NPs, TA-NPs with higher positive surface charge showed higher cellular uptake. Moreover, Caco-2 cell growth-inhibiting activity of RV was significantly increased by TMC nanoencapsulation and TP-NPs showed the significantly highest activity with a good agreement with the permeability results.

Chitosan Nanoparticle System for Improving Blood Circulation

Research & Development Center, Dongwon F&BAbstract The principal objective of this study was to produce a chitosan nanoparticle (NP) system for improving bloodcirculation. Chitosan NPs were prepared using fucoidan and poly-γ-glutamic acid (PGA), denoted as CS/Fu and CS/Fu/PGA NPs, respectively. As the chitosan concentration was increased, the activated partial thromboplastin time (APTT) ofthe NPs significantly increased (p<0.05). When the concentration of fucoidan and γ-PGA was 5-20 and 1-10µg/mL,respectively, the size of the CS/Fu and CS/Fu/PGA NPs was approximately 200 and 100 nm, respectively. With an increasein the fucoidan and PGA concentration, the APTT of CS/Fu and CS/Fu/PGA NPs significantly increased (p<0.05). Theseresults suggest that CS/Fu and CS/Fu/PGA NPs could be used as a potent NP system for improving blood circulation.Keywords: blood circulation, activated partial thromboplastin time, nanoparticle, chitosan