Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study.

l-ascorbic acid (AA) or vitamin C is a crucial nutrient needed for optimal health. However, being unable to be synthesized by the body, it is thus necessary to be included in health care products. Moreover, AA is one of the antioxidants that occur naturally, which is used in pharmaceutical and food products as an antioxidant additive. However, AA is vulnerable to environmental settings and undergoes oxidative degradation to dehydroascorbic acid and further to inactive products. Therefore, new research strategies and approaches are required to augment its stability. The objective of this study is to develop and characterize a fiber-reinforced-phospholipid (FRP) matrix-based vehicle, Zeal-AA, for the delivery of AA and optimize the oral bioavailability of the obtained AA powder using an efficacy study by open-label, randomized, single-dose, two-treatment, two-sequence, two-period, two-way crossover. The structural and surface morphologies were analyzed by Fourier transform infrared spectroscopy, transmission electron microscopy, scanning electron microscopy, and differential scanning calorimetry studies. Encapsulation efficiency, mean particle size, size distribution, ζ-potential measurements, and ADMET profiling revealed the potential delivery system for AA. AUC0-t was found to be 55.23 (mg/dL) for Zeal-AA, whereas it was 9.38 (mg/dL) for AA, and C max was found to be 6.69 (mg/dL) for Zeal-AA, whereas it was 1.23 (mg/dL) for AA, with a fold difference of bioavailability in terms of AUC found to be 5.9 fold. The results show that a single oral dose of Zeal-AA is capable of rising the AA levels in the body relative to the control up to 24 h.

Neuropharmacological and cognitive effects of Bacopa monnieri (L.) Wettst - A review on its mechanistic aspects.

Bacopa monnieri (L.) - (BM) is a perennial, creeping herb which is widely used in traditional ayurvedic medicine as a neural tonic to improve intelligence and memory. Research into the biological effects of this plant has burgeoned in recent years, promising its neuroprotective and memory boosting ability among others. In this context, an extensive literature survey allows an insight into the participation of numerous signaling pathways and oxidative mechanism involved in the mitigation of oxidative stress, along with other indirect mechanisms modulated by bioactive molecules of BM to improve the cognitive action by their synergistic potential and cellular multiplicity mechanism. This multi-faceted review describes the novel mechanisms that underlie the unfounded but long flaunted promises of BM and thereby direct a way to harness this acquired knowledge to develop innovative approaches to manipulate its intracellular pathways.

General unknown screening, antioxidant and anti-inflammatory potential of Dendrobium macrostachyum Lindl.

CONTEXT: D. macrostachyum is an epiphytic orchid abundant in Southern India and is reported for pain relief in folklore. AIMS: The objective of the present study was to determine in vitro free radical scavenging and anti-inflammatory activity of D. macrostachyum and to perform LCMS based metabolic profiling of the plant. SETTINGS AND DESIGN: Sequential stem and leaf extracts were assessed for its antioxidant and anti-inflammatory activity by in vitro methods. MATERIALS AND METHODS: The antioxidant activity determined by assays based on the decolourization of the radical monocation of DPPH, ABTS and reducing power. Total amount of phenolics for quantitative analysis of antioxidative components was estimated. In vitro anti-inflammatory activity was evaluated using protein denaturation assay, membrane stabilization assay and proteinase inhibitory activity. Methanolic extract of plant was subjected to LCMS. RESULTS: The stem ethanolic extracts exhibited significant IC50 value of 10.21, 31.54 and 142.97 µg/ml respectively for DPPH, ABTS radical scavenging and reducing power activity. The ethanol and water extract was highly effective as albumin denaturation inhibitors (IC50 = 114.13 and 135.818 µg/ml respectively) and proteinase inhibitors (IC50 = 72.49 and 129.681 µg/ml respectively). Membrane stabilization was also noticeably inhibited by the stem ethanolic extract among other extracts (IC50 = 89.33 µg/ml) but comparatively lower to aspirin standard (IC50 = 83.926 µg/ml). The highest total phenol content was exhibited by ethanolic stem and leaf extracts respectively at 20 and 16 mg of gallic acid equivalents of dry extract. On LCMS analysis 20 constituents were identified and it included chemotaxonomic marker for Dendrobium species. CONCLUSIONS: The results showed a relatively high concentration of phenolics, high scavenger activity and high anti-inflammatory activity of the stem extract compared to the leaf extract. The results indicate that the plant can be a potential source of bioactive compounds.