Isolation, characterisation and complement fixation activity of acidic polysaccharides from Argemone mexicana used as antimalarials in Mali.

CONTEXT: Global studies on Argemone mexicana L. (Papaveraceae) traditionally used against malaria in Mali are limited to its low-mass compounds activities, and little information on its bioactive polysaccharides is available. OBJECTIVE: This study determines the structure and the immunomodulatory activity of polysaccharides from aerial parts of A. mexicana. MATERIALS AND METHODS: Acidic polysaccharides from this plant material named HMAmA1 and HMAmA2 were isolated from water extracts. Their monosaccharide composition was determined by gas chromatography. Glycosidic linkages were determined using GC-MS. NMR was also applied. The polymers were tested for effects on the human complement system in vitro at different doses. RESULTS: The monosaccharide composition showed that the two polysaccharides contained in different amounts the following monomers: arabinose, rhamnose, galactose, and galacturonic acid. Overall structural analysis showed the presence of a low ratio of 1,2-linked rhamnose compared to 1,4-linked galacturonic acid with arabinogalactans substituted on position 4 of rhamnose. NMR data showed the presence of galacturonans alternated by rhamnogalacturonans bearing arabinose and galactose units. α-Linkages were found for l-arabinose, l-rhamnose and d-galacturonic acid, while ß-linkages were found for d-galactose. The two polysaccharides exhibited strong complement fixation activities, with HMAmA1 being the highest potent fraction. ICH50 value of HMAmA1 was 5 µg/mL, compared to the control BPII being 15.9 µg/mL. DISCUSSION AND CONCLUSIONS: Polysaccharides form A. mexicana presented a complement fixation effect. The complement system is an important part of the immune defense, and compounds acting on the cascade are of interest. Therefore, these polymers may be useful as immunodulatory agents.

Effects of Autoclaving and Freeze-Drying on Physicochemical Properties of Plectranthus esculentus Starch Derivatives.

The goal of this research was to assess the effects of autoclaving followed by freeze-drying on acetylated xerogel (AXS) and carboxymethylated (CMS) derivatives of Plectranthus esculentus starch as potential vaccine stabilizers. Starch extracted from tubers of P. esculentus were modified by single (carboxymethylation) and dual (acetylation followed by xerogel formation) methods. The derivatives were formulated into vaccine stabilizer suspensions, autoclaved, and freeze-dried without additives or antigen. The derivatives and freeze-dried products were assessed by physical appearance, titration, moisture content (MC), TGA, DSC, XRD, SEM, and FTIR analyses. The degrees of substitution (DS) of the CMS and AXS derivatives were 0.345 and 0.033, respectively. Modification significantly reduced the MC of the derivatives. Freeze-dried AXS (FAXS) had lower MC than freeze-dried CMS (FCMS). The lower degree of hydrophilicity/MC of AXS and FAXS was confirmed by TGA and FTIR band intensities and shifts. Reduction in DSC water desorption/evaporation enthalpies (ΔH) from - 1168.8 mJ (NaS) to - 407.48 mJ (AXS) confirmed the influence of modification on moisture. FTIR confirmed acetylation and carboxymethylation of the derivatives by the presence of 1702.9 cm-1 and 1593 cm-1 bands, respectively (FTIR). Increasing concentrations of the derivatives yielded uncollapsed/unshrunken lyophilisates. SEM and XRD showed that modification, autoclaving, and freeze-drying yielded beehive-like microstructures of FCMS and FAXS that were completely amorphous. Processing (autoclaving and freeze-drying), therefore, enhanced the amorphousness of the starch derivatives which is required in vaccine stability during processing and storage. These findings indicate that these starch derivatives have potential as novel vaccine stabilizers.

Starch-based xerogels: Effect of acetylation on Physicochemical and rheological properties.

This study was aimed at evaluating the physicochemical and rheological properties of starch-based xerogels. The starch from the shoots of Borassus aethiopium was physically modified by xerogelization, and chemically by acetylation, and combination of acetylation and xerogelization. The solubility, swelling and syneresis of the starches were determined by gravimetric techniques. Evaluation of the native starch and derivatives was done using microscopy, Fourier transform infra-red (FTIR), x-ray diffractometry (XRD), and 1H NMR spectroscopy. Rheological evaluation was done on 10%w/v dispersions using a Bohlin Gemini rheometer (fitted with a 55mm and 2° cone and plate geometry with gap of 70). The diffractograms displayed three peaks, centered on 2θ=15.3, 17.2 and 23.1° for the native and the starch acetate while the xerogel and the starch acetate xerogel were amorphous. The 1H NMR and FTIR confirmed the presence of acetyl groups at about 2.05ppm and 1720cm-1, respectively. Acetylation of the native starch resulted in improvement of solubility. The starch acetate-xerogel sample formed viscoelastic gels without the need for heating. Acetylation and/or xerogelization of the native starch inhibited syneresis. Starch acetate-xerogels, may find application as stabilizer or suspending agent in liquid food and pharmaceutical formulations.

Drug release from E chemistry hypromellose tablets using the Bio-Dis USP type III apparatus: An evaluation of the effect of systematic agitation and ionic strength.

The aim of the study was to evaluate the effect of systematic agitation, increasing ionic strength and gel strength on drug release from a gel-forming matrix (HPMC E10M, E4M and E50LV) using USP type III Bio-Dis apparatus with theophylline as a model drug. The triboelectric charging; particle sizing, water content, true density and SEM of all the hypromellose grades, theophylline and formulated blends were characterised. The results showed that balanced inter-particulate forces exist between drug particles and the excipient surface and this enabled optimum charge to mass ratio to be measured. Agitation and ionic strength affected drug release from E50LV and E4M tablet matrices in comparison to the E10M tablet matrices. Drug release increased substantially when water was used as the dissolution media relative to media at pH 1.2 (containing 0.4M NaCl). The results showed all f2 values for the E10M tablet matrices were above 50 suggesting the drug release from these tablet matrices to be similar. Rheological data also explained the different drug release behaviour with the stress required to yield/erode being 1Pa, 150Pa, and 320Pa, for the E50LV, E4M and E10M respectively. The stiffness of the gel was also found to be varied from 2.5Pa, 176.2Pa and 408.3Pa for the E50LV, E4M and E10M respectively. The lower G' value can be explained by a softer gel being formed after tablet introduction into the dissolution media thereby indicating faster drug release.