Bio-guided fractionation of the total MeOH extract (TME) of the aerial parts of Blepharis ciliaris (L.) B.L. Burtt. (Acanthaceae) growing in Saudi Arabia was carried out to evaluate its hepatoprotective activity against CCl4-induced hepatotoxicity in rats. Successive chromatographic separations of the potent hepatoprotective n-BuOH fraction afforded two new flavonol glycosides, blepharisides A (1) and B (2), along with quercetin 3-O-rutinoside (3). Their structures were established by UV, IR, 1D, 2D NMR, and HRESIMS spectral data, in addition to comparison with literature data. Co-treatment of CCl4 hepatic injured rats with the total MeOH extract (TME) and its fractions significantly restored the hepatic marker enzymes and total bilirubin to near-normal values compared to silymarin (reference drug). The isolated compounds were evaluated for their antioxidant and anti-inflammatory activities. They displayed significant antioxidant activity (DPPH assay) in relation to propyl gallate (positive control) (% inhibition of 88.2, 87.9, and 74.2, respectively). Compounds 1 and 2 demonstrated anti-inflammatory effects in the carrageenin induced paw edema method at a dose of 10 mg/kg.

Bio-guided fractionation of the total MeOH extract (TME) of the aerial parts of Blepharis ciliaris (L.) B.L. Burtt. (Acanthaceae) growing in Saudi Arabia was carried out to evaluate its hepatoprotective activity against CCl4-induced hepatotoxicity in rats. Successive chromatographic separations of the potent hepatoprotective n-BuOH fraction afforded two new flavonol glycosides, blepharisides A (1) and B (2), along with quercetin 3-O-rutinoside (3). Their structures were established by UV, IR, 1D, 2D NMR, and HRESIMS spectral data, in addition to comparison with literature data. Co-treatment of CCl4 hepatic injured rats with the total MeOH extract (TME) and its fractions significantly restored the hepatic marker enzymes and total bilirubin to near-normal values compared to silymarin (reference drug). The isolated compounds were evaluated for their antioxidant and anti-inflammatory activities. They displayed significant antioxidant activity (DPPH assay) in relation to propyl gallate (positive control) (% inhibition of 88.2, 87.9, and 74.2, respectively). Compounds 1 and 2 demonstrated anti-inflammatory effects in the carrageenin induced paw edema method at a dose of 10 mg/kg.

Bio-guided fractionation of the total MeOH extract (TME) of the aerial parts of Blepharis ciliaris (L.) B.L. Burtt. (Acanthaceae) growing in Saudi Arabia was carried out to evaluate its hepatoprotective activity against CCl4-induced hepatotoxicity in rats. Successive chromatographic separations of the potent hepatoprotective n-BuOH fraction afforded two new flavonol glycosides, blepharisides A (1) and B (2), along with quercetin 3-O-rutinoside (3). Their structures were established by UV, IR, 1D, 2D NMR, and HRESIMS spectral data, in addition to comparison with literature data. Co-treatment of CCl4 hepatic injured rats with the total MeOH extract (TME) and its fractions significantly restored the hepatic marker enzymes and total bilirubin to near-normal values compared to silymarin (reference drug). The isolated compounds were evaluated for their antioxidant and anti-inflammatory activities. They displayed significant antioxidant activity (DPPH assay) in relation to propyl gallate (positive control) (% inhibition of 88.2, 87.9, and 74.2, respectively). Compounds 1 and 2 demonstrated anti-inflammatory effects in the carrageenin induced paw edema method at a dose of 10 mg/kg.

Bio-guided fractionation of the total MeOH extract (TME) of the aerial parts of Blepharis ciliaris (L.) B.L. Burtt. (Acanthaceae) growing in Saudi Arabia was carried out to evaluate its hepatoprotective activity against CCl4-induced hepatotoxicity in rats. Successive chromatographic separations of the potent hepatoprotective n-BuOH fraction afforded two new flavonol glycosides, blepharisides A (1) and B (2), along with quercetin 3-O-rutinoside (3). Their structures were established by UV, IR, 1D, 2D NMR, and HRESIMS spectral data, in addition to comparison with literature data. Co-treatment of CCl4 hepatic injured rats with the total MeOH extract (TME) and its fractions significantly restored the hepatic marker enzymes and total bilirubin to near-normal values compared to silymarin (reference drug). The isolated compounds were evaluated for their antioxidant and anti-inflammatory activities. They displayed significant antioxidant activity (DPPH assay) in relation to propyl gallate (positive control) (% inhibition of 88.2, 87.9, and 74.2, respectively). Compounds 1 and 2 demonstrated anti-inflammatory effects in the carrageenin induced paw edema method at a dose of 10 mg/kg.

Purpose: Dry powder vaccine delivery via the pulmonary route has gained significant attention as an alternate route to parenteral delivery. In this study, we investigated bovine serum albumin (BSA) adsorbed poly(glycerol adipate-co-ω-pentadecalactone), PGA-co-PDL polymeric nanoparticles (NPs) within L-leucine (L-leu) microcarriers for dry powder inhalation. Methods: NPs were prepared by oil-in-water single emulsion-solvent evaporation and particle size optimised using Taguchi’s design of experiment. BSA was adsorbed onto NPs at different ratios at room temperature. The NPs were spray-dried in aqueous suspension of L-leu (1:1.5) using a Büchi-290 mini-spray dryer. The resultant nanocomposite microparticles (NCMPs) were characterised for toxicity (MTT assay), aerosolization (Next Generation Impactor), in vitro release study and BSA was characterized using SDS-PAGE and CD respectively. Results: NPs of size 128.50±6.57 nm, PDI 0.07±0.03 suitable for targeting lung dendritic cells were produced. BSA adsorption for 1 h resulted in 10.23±1.87 μg of protein per mg of NPs. Spray-drying with L-leu resulted in NCMPs with 42.35±3.17% yield. In vitro release study at 37°C showed an initial burst release of 30.15±2.33% with 95.15±1.08% over 48 h. Aerosolization studies indicated fine particle fraction (FPF%) dae4.46 μm as 76.95±5.61% and mass median aerodynamic diameter (MMAD) of 1.21±0.67 μm. The cell viability was 87.01±14.11% (A549 cell line) and 106.04±21.14% (16HBE14o-cell line) with L-leu based NCMPs at 1.25 mg/ml concentration after 24 h treatment. The SDS-PAGE and CD confirmed the primary and secondary structure of the released BSA. Conclusions: The results suggest that PGA-co-PDL/L-leu NCMPs may be a promising carrier for pulmonary vaccine delivery due to excellent BSA adsorption and aerosolization behaviour. KEY WORDS: Dry powder inhalation, nanoparticles, pulmonary delivery, spray drying, vaccines.