A chitosan/alginate coated nano-liposome to improve intestinal absorption of curcumin for oral administration.

Attempts to improve low absorption and rapid metabolic conversion of curcumin were made by developing curcumin-loaded bilayer nanoliposomes coated with chitosan and alginate for intestinal-specific drug delivery. A curcumin-loaded nano-liposome was prepared with optimized formulations with phosphatidylcholine, curcumin, chitosan, and alginate. The particle size of the optimized formulation was approximately 400 nm, and the encapsulation efficiency was more than 99%. In the in vitro release study, curcumin release from the curcumin-loaded nanoliposome with double layers of chitosan/alginate (CNL-CH/AL) was suppressed in the simulated gastric fluid (SGF, pH 1.2) and enhanced in the simulated intestinal fluid (SIF, pH 6.8). In the in vivo pharmacokinetic study in rats, the CNL-CH/AL-treated group showed a prolonged absorption pattern of curcumin and the area under the plasma concentration-time curve from 0 to 24 h (AUC0-24) was improved 109-fold compared to the control group treated with a curcumin solution without a nanocarrier.

A self-emulsifying omega-3 fatty acids delivery system for enhanced gastro-intestinal absorption in rats.

Omega-3 fatty acids have many health benefits as they help to prevent and treat coronary artery disease, hypertension, diabetes mellitus, arthritis, and autoimmune disorders. Omega-3 fatty acids miscible in lecithin were found to spontaneously form microemulsions in water. The particle sizes of emulsions ranged from 300 to 800 nm and their morphologies were observed by optical microscopy. In vitro testing showed that the amounts of omega-3 fatty acids released by self-emulsifying delivery (SED) formulations containing lecithin, were higher than that released by a commercial formulation without lecithin. The Cmax values of docosahexaenoic acid (DHA) or eicosapentaenoic acid (EPA) were approximately 1.38-1.40-fold for the optimized SED formulation than for the control group (P < 0.01). Similarly, the mean AUC0 - 48 values of DHA or EPA in the SED group were 1.27-1.29-fold higher than in the control group (P < 0.05). Phospholipids and lecithin were found to have considerable potentials as bioavailability enhancing excipients for SED systems.

Potential anticancer effect of aspirin and 2'-hydroxy-2,3,5'-trimethoxychalcone-linked polymeric micelles against cervical cancer through apoptosis.

Although early diagnosis and treatment of cancers in women are achievable through continuous diagnostic tests, cervical cancer (CVC) still has a high mortality rate. In the present study, we investigated whether certain nanoparticles (NPs), comprising aspirin conjugated 2'-hydroxy-2,3,5'-trimethoxychalcone chemicals, could induce the apoptosis of cancer cells. HeLa cells were treated with NPs and the cell viability was evaluated using WST-1 assay. Protein expression of Ki-67 was measured using immunocytochemistry. In addition, the apoptotic effect of NPs was determined using TUNEL assay. To investigate the apoptosis signaling pathways, reverse transcription quantitative PCR was performed and lipid accumulation was observed via holotomographic microscopy. The IC50 value of the NPs was 4.172 µM in HeLa cells. Furthermore, 10 µM NPs significantly inhibited the cell proliferation and stimulated the apoptosis of HeLa cells. In addition, apoptosis and mitochondrial dysfunction were induced by the NPs through lipid accumulation in HeLa cells, leading to apoptotic signaling cascades. Taken together, the results from the present study demonstrated that the NPs developed promoted apoptosis though efficient lipid accumulation in HeLa cells, suggesting that they may provide a novel way to improve the efficacy of CVC anticancer treatment.

Inhibitory effect of modified silkworm pupae oil in PDGF-BB-induced proliferation and migration of vascular smooth muscle cells.

Silkworm pupae oil (SPO) has been reported to have various biological activities in improving blood circulation. However, the protective action of SPO against vascular disorders remains unknown. A new formulation of SPO was prepared through an esterification and saponification process. The composition of unsaturated fatty acids in silkworm pupae oil sodium salt (SPOS) was then analyzed by LC/MS to show α-linolenic acid (11.0%), linoleic acid (73.2%), palmitic acid (3.1%), oleic acid (12.0%), and stearic acid (0.7%). The in vitro studies were performed to find out the efficacy of SPOS on platelet-derived growth factor (PDGF-BB) induced vascular smooth muscle cell (VSMC) migration and proliferation. PDGF-BB (10 ng/mL) induced abnormal migration and proliferation of VSMCs, whereas exposure to SPOS (30 µg/mL) significantly reduced the PDGF-BB-induced cell migration and proliferation. The extracellular signal-regulated kinase1/2 (ERK1/2) and phosphorylation of ERK1/2 were determined by immunoblot analysis and the ERK1/2 phosphorylation in PDGF-BB-stimulated VSMCs was downregulated by SPOS (30 µg/mL) treatment. These results indicate that SPOS may be a helpful and useful agent as a functional food and drug against vascular disorders.

Potential Skin Regeneration Activity and Chemical Composition of Absolute from Pueraria thunbergiana Flower.

The flower of Pueraria thunbergiana BENTH (PTBF) contains isoflavonoids and essential oil components. It has many biological and pharmacological activities, including anti-diabetes, anti-oxidant, and weight loss. However, its effect on skin regeneration remains unknown. In the present study, we isolated the absolute from PTBF through solvent extraction and determined the role of the absolute on skin regeneration-associated responses in human epidermal-keratinocytes (HaCats). The PTBF absolute, which contained 10 compounds, stimulated migration and proliferation and increased the phosphorylation of serine/threonine-specific protein kinase and extracellular signal-regulated kinasel/2 in HaCats. It induced type I and IV collagen synthesis in HaCats. In addition, treatment with PTBF absolute resulted in increased sprout outgrowth in HaCats. These findings suggest that PTBF absolute may participate in skin regeneration, probably through promotion of migration, proliferation, and collagen synthesis.

Covalent crosslinking of 1-D photonic crystals of microporous Si by hydrosilylation and ring-opening metathesis polymerization.

Free-standing porous Si multilayer dielectric mirrors, prepared by electrochemical etching of crystalline Si, are treated with a ruthenium ring-opening metathesis polymerization (ROMP) catalyst followed by norbornene to produce flexible, stable composite materials in which poly(norbornene) is covalently attached to the porous Si matrix.