Thermal Degradation Kinetics and pH-Rate Profile of Verbascoside and Stability Improvement by Solid Lipid Nanoparticles.

Thermal degradation of verbascoside (VB) in Acanthus ebracteatus Vahl (AE) always affects its health benefit. Here the temperature effect on VB in both AE extract and solid lipid nanoparticles (SLNs)-encapsulated AE extract was demonstrated using the Arrhenius plot. The reaction rate constants were calculated for shelf life and plotted to obtain pH-rate profiles. VB degradation was a first-order reaction. The reaction rate in a neutral to alkaline solution was faster than in an acidic solution. VB in AE extract-loaded SLNs was more stable than in uncapped AE extract. The shelf life of VB in SLNs was 153 days with activation energy (E a) of 76.16 kJ mol-1, whereas those of VB in AE extract and in AE extract solution were 75 days with E a = 78.03 kJ mol-1 and 12 days with E a = 49.24 kJ mol-1, respectively. Therefore, we anticipate that the AE extract-loaded SLNs will be beneficial for product development.

Effects of some medicinal plant extracts on dermal papilla cells.

INTRODUCTION: Miniaturization of the hair follicles is evident on the balding scalp. Approved medications, topical minoxidil, and oral finasteride for the treatment of alopecia sometimes come with undesirable adverse effects. The study was to examine the bioactivity of medicinal plants for finding the promising source of anti-hair loss application. METHODS: Ten ethanolic extracts were prepared from Acacia concina (Willd.) DC., Acanthus ebracteatus Vahl, Bridelia ovata Decne, Cleome viscosa L., Cocos nucifera L., Hibiscus subdariffla L., Oryza sativa L., Terminalia chebula Retz., Tinospora crispa (L.) Hook. f. & Thomson and cytotoxic tested on dermal papilla cells using MTT assay. The effect of the extracts on cell cycle was also determined using flow cytometry technique. Anti-inflammatory activity was examined by determining IL-1ß inhibition in RAW 257.4 cells. In vitro study of androgenic and 5α-reductase inhibitory activities were also determined using MTT assay and enzymatic reaction couple with liquid chromatography-mass spectrometry (LC-MS), respectively. RESULTS: Our results revealed that only A. ebracteatus promoted dermal papilla cell proliferation and the S and G2/M phases in cell cycle. A. ebracteatus also showed inhibitory activity against 5α-reductase and testosterone in reducing cell viability of the dermal papilla. Moreover, A. ebracteatus extract strongly inhibited LPS-stimulating IL-1ß production in RAW 264.7 cells in a dose-dependent manner. CONCLUSION: Our finding indicated that the ethanolic extract of A. ebracteatus is a promising candidate for anti-hair loss treatment.

Effects of Acanthus ebracteatus Vahl. extract and verbascoside on human dermal papilla and murine macrophage.

Androgenic alopecia is a common type of hair loss, usually caused by testosterone metabolism generating dihydrotestosterone and hair follicular micro-inflammation. These processes induce dermal papilla cells to undergo apoptosis. Currently approved effective medications for alopecia are Finasteride, an oral 5α-reductase inhibitor, Minoxidil, a topical hair growth promoter, and Diclofenac, an anti-inflammatory agent, all of which, however, have several adverse side effects. In our study, we showed the bioactivity of Acanthus ebracteatus Vahl. (AE) extract performed by 95% ethanol, and verbascoside (VB), a biomarker of AE extract. Both AE extract and VB were studied for their effects on dermal papilla cell viability and the cell cycle by using MTT assay and flow cytometry. The effect of an anti-inflammatory activity of AE extract and VB on IL-1ß, NO, and TNF-α, released from LPS induced RAW 264.7 cells, and IL-1α and IL-6 released from irradiated dermal papilla cells were detected using ELISA technique. The preventive effect on dermal papilla cell apoptosis induced by testosterone was determined by MTT assay. In controlled in vitro assays it was found that AE extract and VB at various concentrations induced dermal papilla cell proliferation which was indicated by an increase in the number of cells in the S and G2/M phases of the cell cycle. AE extract at 250 µg/mL concentration or VB at 62.50 µg/mL concentration prevented cell apoptosis induced by testosterone at a statistically significant level. In addition, both AE extract and VB greatly inhibited the release of pro-inflammatory cytokines from RAW 264.7 and dermal papilla cells. The release of IL-1ß, TNF-α, and NO from RAW 264.7 cells, as well as IL-1α and IL-6 from dermal papilla cells, was also diminished by AE extract 250 µg/mL and VB 125 µg/mL. Our results indicate that AE extract and VB are promising ingredients for anti-hair loss applications. However, further clinical study is necessary to evaluate the effectiveness of AE extract and VB as treatment for actual hair loss.

Kinetics of CBD, Δ9-THC Degradation and Cannabinol Formation in Cannabis Resin at Various Temperature and pH Conditions.

Introduction: Cannabidiol (CBD), cannabinol (CBN), and Δ9-tetrahydrocannabinol (Δ9-THC) are major cannabinoids in cannabis resin and products. The kinetic of the chemical reaction of resin cannabis is important for product development and storage. A few reports are available in the literature on the rate of CBD and Δ9-THC degradation, and CBN formation in dried resin and solutions of various pH. Materials and Methods: Thermal degradation of CBD, Δ9-THC, and formation of CBN was studied at 50°C, 60°C, 70°C, and 80°C for dried cannabis resin. The effect of pH and temperature on cannabinoids transformation in cannabis solution was also examined at pH 2, 4, 6, 8, 10, and 12 and at 40°C, 50°C, 60°C, and 70°C. High-performance chromatography coupled with diode-array detection (HPLC-DAD) was used for the analysis of CBD, CBN, and Δ9-THC transformation. The values of activation energies (Ea), shelf-life (t90% - t110%), and rate constant (k) were calculated for the CBD, Δ9-THC, and CBN. The effect of temperature and pH on the dried cannabis resin was adequately modeled with the Arrhenius equation. Results: The results indicated that the chemical kinetics in the thermal degradation of CBD, Δ9-THC, and formation of CBN were the zero-order, pseudo-zero-order, and first-order reactions, respectively, in cannabis resin. The first-order and pseudo-first-order degradation kinetics were evidenced for CBD and Δ9-THC, respectively, in cannabis solutions, whereas the zero-order formation kinetic was detected for the CBN. The transformation rate of the CBD, CBN, and Δ9-THC increased with increasing temperature, especially as temperature increased to 70°C at pH 2.0. The optimum pH for CBD stability was between pH 4 and 6, whereas the optimum pH for Δ9-THC stability was between pH 4 and 12. Conclusion: The major cannabinoids (CBD, CBN, and Δ9-THC) reacted more quickly at high temperature and in an acidic solution. Especially, the minimum transformation of CBD, CBN, and Δ9-THC was achieved by using on a low temperature, slightly to moderately acidic pH values, and short-time processing. These results may help to improve the storage condition of CBD, CBN, and Δ9-THC products and in the manufacturing process.