Synthesis of ginsenoside Rb1-imprinted magnetic polymer nanoparticles for the extraction and cellular delivery of therapeutic ginsenosides.

Background: Panax ginseng (ginseng) is a traditional medicine that is reported to have cardioprotective effects; ginsenosides are the major bioactive compounds in the ginseng root. Methods: Magnetic molecularly imprinted polymer (MMIP) nanoparticles might be useful for both the extraction of the targeted (imprinted) molecules, and for the delivery of those molecules to cells. In this work, plant growth regulators were used to enhance the adventitious rooting of ginseng root callus; imprinted polymeric particles were synthesized for the extraction of ginsenoside Rb1 from root extracts, and then employed for subsequent particle-mediated delivery to cardiomyocytes to mitigate hypoxia/reoxygenation injury. Results: These synthesized composite nanoparticles were first characterized by their specific surface area, adsorption capacity, and magnetization, and then used for the extraction of ginsenoside Rb1 from a crude extract of ginseng roots. The ginsenoside-loaded MMIPs were then shown to have protective effects on mitochondrial membrane potential and cellular viability for H9c2 cells treated with CoCl2 to mimic hypoxia injury. The protective effect of the ginsenosides was assessed by staining with JC-1 dye to monitor the mitochondrial membrane potential. Conclusion: MMIPs can play a dual role in both the extraction and cellular delivery of therapeutic ginsenosides.

Porous Biphasic Calcium Phosphate Granules from Oyster Shell Promote the Differentiation of Induced Pluripotent Stem Cells.

Oyster shells are rich in calcium, and thus, the potential use of waste shells is in the production of calcium phosphate (CaP) minerals for osteopathic biomedical applications, such as scaffolds for bone regeneration. Implanted scaffolds should stimulate the differentiation of induced pluripotent stem cells (iPSCs) into osteoblasts. In this study, oyster shells were used to produce nano-grade hydroxyapatite (HA) powder by the liquid-phase precipitation. Then, biphasic CaP (BCP) bioceramics with two different phase ratios were obtained by the foaming of HA nanopowders and sintering by two different two-stage heat treatment processes. The different sintering conditions yielded differences in structure and morphology of the BCPs, as determined by scanning electron microscopy (SEM), X-ray diffraction (XRD), and Brunauer-Emmett-Teller (BET) surface area analysis. We then set out to determine which of these materials were most biocompatible, by co-culturing with iPSCs and examining the gene expression in molecular pathways involved in self-renewal and differentiation of iPSCs. We found that sintering for a shorter time at higher temperatures gave higher expression levels of markers for proliferation and (early) differentiation of the osteoblast. The differences in biocompatibility may be related to a more hierarchical pore structure (micropores within macropores) obtained with briefer, high-temperature sintering.

Preparation of curcumin microemulsions with food-grade soybean oil/lecithin and their cytotoxicity on the HepG2 cell line.

The choice of surfactants and cosurfactants for preparation of oral formulation in microemulsions is limited. In this report, a curcumin-encapsulated phospholipids-based microemulsion (ME) using food-grade ingredients soybean oil and soybean lecithin to replace ethyl oleate and purified lecithin from our previous study was established and compared. The results indicated soybean oil is superior to ethyl oleate as the oil phase in curcumin microemulsion, as proven by the broadened microemulsion region with increasing range of surfactant/soybean oil ratio (approx. 1:1-12:1). Further preparation of two formula with different particle sizes of formula A (30nm) and B (80nm) exhibited differential effects on the cytotoxicity of hepatocellular HepG2 cell lines. At 15µM of concentration, curcumin-ME in formula A with smaller particle size resulted in the lowest viability (approx. 5%), which might be explained by increasing intake of curcumin, as observed by fluorescence microscopy. In addition, the cytotoxic effect of curcumin-ME is exclusively prominent on HepG2, not on HEK293, which showed over 80% of viability at 15µM. The results from this study might provide an innovative applied technique in the area of nutraceuticals and functional foods.

Comparison of the antioxidant and transmembrane permeative activities of the different Polygonum cuspidatum extracts in phospholipid-based microemulsions.

The main purpose of this study was to investigate the transmembrane permeability of polyphenol-containing Polygonum cuspidatum extracts (PCE) encapsulated in phospholipid-based o/w microemulsion system. First, preparations of several PCEs using solid- or liquid-phase extraction or a combination of both, as well as evaluation of their antioxidant activities, were conducted and compared. In the antioxidant study, results indicated that PC-1 with the least extraction process exhibited the best antioxidant activity. By comparing the permeability coefficient (K(p)) among all tested PCEs in microemulsions (ME-PCs), ME-PC1 also possessed the largest permeability coefficients of both resveratrol and emodin. In addition, comparison of the transmembrane permeability of several polyphenol-encapsulated microemulsions showed that resveratrol had the most competitive advantage in the microemulsion formula for the control-release process. Taken together, it can be concluded that the matrix removed from the solid-phase extraction in PC-1 not only possesses antioxidant activity but also acts as an enhancer in transmembrane permeation. The structure specificity of the polyphenol plays important roles in the mechanism of the transmembrane permeation process. These findings might provide scientific evidence for the value of developing polyphenol-containing PCEs as nutraceuticals and cosmoceutical products.

Enhancement of the encapsulation and transmembrane permeation of isoflavone-containing red clover extracts in phospholipid-based microemulsions using different extraction processes.

Several isoflavone-enriched red clover extracts (RCE) prepared by using solid- or liquid-phase extraction or a combination of both were studied for their encapsulation into a phospholipid-based microemulsion system. The optimization process with regard to the bioactive ingredient-encapsulated amounts and transmembrane efficiency of various RCE micelles was demonstrated. The results indicated that the encapsulated amounts of isoflavones in RCE-encapsulated microemulsions (ME) of ME-RC5, ME-RC6, and ME-RC7 were increased by >10-fold when compared with that of the raw red clover extracts. Comparison of the permeability coefficient K(p) of the formononetin among the ME-RCs from the in vitro skin permeation study showed that ME-RC5 significantly exhibited the least permeability, whereas ME-RC6 exhibited enhanced permeability after two-stage solid-phase extraction, indicating the potential role of the matrix material as a barrier or enhancer in the transmembrane study.