Transdermal Sustained Release Properties and Anti-Photoaging Efficacy of Liposome-Thermosensitive Hydrogel System.

Drug delivery systems have become a research priority in the biomedical field. The incorporation of liposomes to hydrogels further forms more robust multifunctional systems for more effective and sustained topical drug delivery. In this study, carboxymethyl-modified chitosan/hyaluronic acid (CMC/HA, CMH) thermosensitive hydrogel is developed for sustained transdermal delivery of liposomes. Hydrogels are crosslinked by hydrogen bonding, hydrophobic interaction and electrostatic interaction. The gel properties can be regulated by substitution degree (DS), and when DS = 18.20 ± 0.67% (CMH2), the gel temperature is 37.8 °C, allowing rapid gelation at body temperature (315 s). Moreover, CMH2 hydrogel has suitable spreadability (17.7-57.2 cm2 ), viscosity (2133.4 mPa s) and porous structure, which facilitated its adhesion and application on the skin and liposomes delivery. The hydrogel can retard the liposomes release, and the release rate of ascorbyl glucoside (AA2G) is 33.92-49.35% in 24 h. Hydrogel avoids the rapid clearance of liposomes from the skin and improved the skin retention, achieving the long-term release of bioactive components. Liposome-hydrogel system more efficiently promotes the anti-photoaging effect of AA2G on skin, reducing epidermal thickness, melanin deposition and lipid oxidative damage and increasing collagen density. Therefore, liposome-hydrogel systems are proposed as multifunctional delivery systems for sustained transdermal delivery.

Regulation of Nanoliposome Rigidity and Bioavailability of Oligomeric Proanthocyanidin with Phytosterols Containing Different C3 Branches.

The rigidity of nanoliposomes significantly influences their physical stability and in vitro and in vivo behaviors (e.g., cellular uptake, blood circulation, biodistribution, etc.). This study aimed to quantify the rigidity of the nanoliposomes composed of phytosterol with varying C3 branches and phospholipids (DPPC, DOPC) using atomic force microscopy. Young's modulus, determined by the Shell model, effectively differentiated between mechanical differences in nanoliposomes with varying components and component structure and phase states. FTIR results indicated that P-SG exhibited the highest Young's modulus (175.98 ± 10.53 MPa) due to the hydrogen bond between the glucose residue of steryl glycosides (SGs) and the phospholipid polar head. However, the rigidity of DOPC nanoliposomes was not significantly different due to the unsaturated bond. The addition of oligomeric proanthocyanidin (OPC) did not change the order of rigidity among the nanoliposomes, with P-SG-OPC having the highest Young's modulus (126.27 ± 2.06 MPa). In the simulated gastrointestinal tract experiment, P-SG-OPC exhibited the greatest stability, with minimal particle aggregation. Cellular uptake experiments revealed that DPPC nanoliposomes with high rigidity had optimal endocytosis, while DOPC nanoliposome uptake was independent of rigidity. In melanin production inhibition tests, the inhibitory effect correlated directly with Young's modulus and P-SG-OPC had the best inhibitory effect on melanin generation. Our findings in this study provide valuable insights into the design and optimization of nanoliposomes for the efficient delivery of active substances, offering potential solutions for improving the efficacy of drug delivery systems.

Extraction and identification of steroidal saponins from Polygonatum cyrtonema Hua using natural deep eutectic solvent-synergistic quartz sand-assisted extraction method.

In this study, quartz sand with particularly sharp nanoscale edges acted like a nanoscale knife physically cut cells of Polygonatum cyrtonema Hua into nanosized particles and was synergized with natural deep eutectic solvent to extract steroidal saponins of Polygonatum cyrtonema Hua. The natural deep eutectic solvent (choline chloride-lactic acid)-synergistic quartz sand-assisted extraction was optimized using response surface methodology. The steroidal saponins purified with AB-8 macroporous resin were identified using ultra-high-performance liquid chromatography-triple time of flight mass spectrometry. The results showed that the experimental total saponins content value (36.97 ± 0.12 mg dioscin equivalent/g dry weight) at optimal extraction conditions with a temperature of 68°C, a rotational speed of 20 400 rpm, shear time of 4.3 min, the liquid-solid ratio of 38 ml/g, was close to the maximum possible theoretical value (36.64 mg dioscin equivalent/g dry weight). A total of 20 steroidal saponins were identified, among which the content of (25R)-Kingianoside E was the highest (102.66 ± 3.47 mg/g). Furthermore, a new steroid saponin (3ß,25S)-26-(ß-D-glucopyranosyloxy)-22-hydroxyfurost-5-en-3-yl 4-O-ß-D-glucopyranosyl-ß-D-galactopyranoside+Glc was found for the first time. These results revealed that natural deep eutectic solvent-synergistic quartz sand-assisted extraction was an efficient and green method to extract a variety of steroidal saponins.

Deep eutectic solvent on extraction of flavonoid glycosides from Dendrobium officinale and rapid identification with UPLC-triple-TOF/MS.

In this study, ultrasonic-assisted deep eutectic solvent (DES) method was used to extract flavonoids from Dendrobium officinale. The mechanism of DESs extraction differences was investigated by physicochemical characterization and molecular dynamics simulation experiments. Moreover, flavonoids from Dendrobium officinale were rapidly identified and quantitatively analyzed by UPLC-Triple-TOF/MS without removing DES. The results showed choline chloride-lactic acid (Chol-Lac) had the best extraction effect among forty groups of DESs, the extraction yield was up to 35.23 ± 2.12 mg/g. It was speculated that the tight hydrogen bond structure was the key to the better extraction ability of Chol-Lac. Meanwhile, the viscosity was the main physical parameter reflecting the hydrogen bond structure of DES. Fourteen flavonoid glycosides were identified, among which the content of rutin (1.94 ± 0.24 mg/g) was the highest. And the results of cluster analysis showed that different DESs had great differences in the extraction of flavonoid glycosides.

Antidiabetic potential of polysaccharides from Brasenia schreberi regulating insulin signaling pathway and gut microbiota in type 2 diabetic mice.

This study aimed to investigate the hypoglycemic activities and gut microbial regulation effects of polysaccharides from Brasenia schreberi (BS) in diabetic mice induced by high-fat diet and streptozotocin. Our data indicated that BS polysaccharides not only improved the symptoms of hyperglycemia and relieved metabolic endotoxemia-related inflammation but also optimized the gut microbiota composition of diabetic mice with significantly decreased Firmicutes/Bacteroidetes ratios. More importantly, altered gut microbiota components may affect liver glycogen and muscle glycogen by increasing the mRNA expression of phosphatidylinositol-3-kinase (PI3K) and protein kinase B (Akt) in the liver of mice through modulated the abundance of beneficial bacteria (Lactobacillus). Altogether, our findings, for the first time, demonstrate that BS polysaccharides may be used as a beneficial probiotic agent that reverses gut microbiota dysbiosis and the hypoglycemic mechanisms of BS polysaccharides may be related to enhancing the abundance of Lactobacillus to activate PI3K/Akt-mediated signaling pathways in T2DM mice.