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Etodolac (ET) (poorly soluble drug) nanosuspensions were prepared by both pH shift method and antisolvent techniques in order to increase its dissolution rate. Various stabilizers were used, namely, Tween 20 and 80, HPMC, PVP K44, PVA, PEG 400, NaCMC, and β-cyclodextrin. The prepared nanosuspensions were characterized by Fourier transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM) and evaluated for their particle size, particle size distribution, and in vitro dissolution rate. In general, it was found that the antisolvent method for the preparation of ET nanosuspensions reduced the drug particle size to a higher extent compared to the pH shift method. The dissolution rate of ET in distilled water was markedly enhanced in the nanosized system, as more than 65% of drug dissolved in 10 min from all the nanosuspension formulations except F5 (stabilized with PVP K44) and F8 (stabilized with Tween 20), as compared to less than 20% of crude drug. Nanoparticles prepared by antisolvent method using Tween 80 as a stabilizer were selected for further in vivo study. The in vivo test demonstrated that nanoparticles of ET were well absorbed with a percentage drug absorption value 2.7 times more than that of micrometric size of crude ET.

Nimesulide is a poorly soluble drug, the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. There are several techniques to enhance the dissolution of poorly soluble drugs. Among them the technique of liquisolid compacts which is a promising one. The liquisolid compacts were prepared using 20 mg nimesulide, Avicel PH102 as a carrier, and Aerosil 200 as a coating material in a ratio of 20:1, as well as AC-DI-SOL as a disintegrant in a concentration of 5% from the total weight of the compact. The liquids used include PEG400, PG, and a mixture of these solvents with Tween 80. From the results obtained it is concluded that the suitable loading factor (Lf) is 0.2 which gave good flowability and compressibility. Friability, hardness, disintegration time and the dissolution rate were carried out. All the liquisolid compacts showed higher dissolution rate than the conventional tablets. The liquisolid compacts containing the PEG400 showed the highest dissolution rate than the other preparations. The effect of different concentrations of drug on the dissolution rate was studied, and it was observed that 20% of drug gave the maximum dissolution rate, and no significant increase of the dissolution rate with increasing the drug concentration. Conventional tablets and liquisolid compacts containing PG and PEG400 were tested for their anti-inflammatory effects using paw oedema test. liquisolid compacts exhibited a pronounced inhibition of swelling than that of conventional tablets. In conclusion liquisolid compact of nimesulide can be used as a technique to improve the dissolution rate and the anti-inflammatory effect of nimesulide.

Anisotes trisulcus (Forssk.) Nees. (family Acanthaceae) aerial part is used in folk medicine in the Arabian peninsula for treatment of hepatic conditions. It showed different activities such as antibacterial, hepatoprotective, and cytotoxicity. It is a rich source of alkaloids and is used as an antidiabetic, bronchodilator, hypotensive, and local anesthetic. To the best of our knowledge, there is no report on the phenolic constituents of A. trisulcus. Therefore, this study aims to identify the constituents and establish antioxidant and anti-inflammatory activities of the total methanolic extract and different fractions. One new benzoyl flavonol: 7,8,3'-trihydroxy-5-methoxy-4'-benzoyl flavonol (5), along with eight known compounds: -amyrin (1), -sitosterol (2), stigmasterol (3), (2S,3S,4R)-2[(2'R)-2'-hydroxytetracosanoyl amino]-octadecane-1,3,4-triol (4), allopateuletin (6), veratric acid (7), vanillic acid (8), and -sitosterol-3-O--D-glucopyranoside (9) were isolated from A. trisulcus aerial parts. Their structures were established by physical, chemical, and spectral data (UV, IR, MS, and 1D NMR), as well as comparison with authentic samples. The anti-inflammatory activity of the total methanolic extract and different fractions was evaluated using carrageenan-induced paw edema method at a dose of 400 mg/kg. Also, the antioxidant activity was determined using DPPH assay at concentrations 0.25, 0.5, and 1 mg/mL. The total MeOH extract and EtOAc fraction showed high antioxidant activity 75% and 68% (Conc. 1 mg/mL), respectively while, the n-hexane and EtOAc fractions exhibited significant anti-inflammatory effects.

Anisotes trisulcus (Forssk.) Nees. (family Acanthaceae) aerial part is used in folk medicine in the Arabian peninsula for treatment of hepatic conditions. It showed different activities such as antibacterial, hepatoprotective, and cytotoxicity. It is a rich source of alkaloids and is used as an antidiabetic, bronchodilator, hypotensive, and local anesthetic. To the best of our knowledge, there is no report on the phenolic constituents of A. trisulcus. Therefore, this study aims to identify the constituents and establish antioxidant and anti-inflammatory activities of the total methanolic extract and different fractions. One new benzoyl flavonol: 7,8,3'-trihydroxy-5-methoxy-4'-benzoyl flavonol (5), along with eight known compounds: -amyrin (1), -sitosterol (2), stigmasterol (3), (2S,3S,4R)-2[(2'R)-2'-hydroxytetracosanoyl amino]-octadecane-1,3,4-triol (4), allopateuletin (6), veratric acid (7), vanillic acid (8), and -sitosterol-3-O--D-glucopyranoside (9) were isolated from A. trisulcus aerial parts. Their structures were established by physical, chemical, and spectral data (UV, IR, MS, and 1D NMR), as well as comparison with authentic samples. The anti-inflammatory activity of the total methanolic extract and different fractions was evaluated using carrageenan-induced paw edema method at a dose of 400 mg/kg. Also, the antioxidant activity was determined using DPPH assay at concentrations 0.25, 0.5, and 1 mg/mL. The total MeOH extract and EtOAc fraction showed high antioxidant activity 75% and 68% (Conc. 1 mg/mL), respectively while, the n-hexane and EtOAc fractions exhibited significant anti-inflammatory effects.