Sodium Alginate-Quaternary Polymethacrylate Composites: Characterization of Dispersions and Calcium Ion Cross-Linked Gel Beads.

The objective of this work was to examine the effect of quaternary polymethacrylate (QPM), a water-insoluble polymer with a positive charge, on the characteristics of the sodium alginate (SA) dispersions and the calcium alginate (CA) gel beads containing propranolol HCl (PPN). The SA-QPM composite dispersions presented the formation of flocculates with a negative charge due to the electrostatic interaction of both substances. The QPM addition did not affect the SA dispersions' Newtonian flow, but the composite dispersions' viscosity enhancement was found. The PPN-loaded CA-QPM gel beads had more spherical than the PPN-loaded CA gel beads. The incorporation of QPM caused a bigger particle size, higher drug entrapment efficiency, and greater particle strength of the gel beads. Despite the similar water uptake property, the PPN-loaded CA-QPM gel beads displayed lower burst release and slower drug release rate than the PPN-loaded CA gel beads. However, the drug release from the PPN-loaded CA-QPM gel beads involved drug diffusion and matrix swelling mechanisms. This study demonstrated that adding QPM into the SA dispersions leads to a viscosity synergism. The CA-QPM gel beads display a good potential for use as a bioactive compound delivery system.

Anticariogenic Activities of Derris reticulata Ethanolic Stem Extract Against Streptococcus mutans.

BACKGROUND AND OBJECTIVE: Streptococcus mutans is a dominant causative pathogen of dental caries, which is a major oral health problem affecting million people worldwide. Derris reticulata is a medicinal plant possessing antimicrobial activity against several Gram-positive pathogenic bacteria. None the less, its effects on growth and cariogenic properties of S. mutans has not been clearly established. This study aimed to investigate the antibacterial and anti cariogenic activities of the D. reticulata ethanolic stem extract. MATERIALS AND METHODS: The TLC analysis was performed to authenticate the D. reticulata sample. Minimum inhibition concentration and minimum bactericidal concentration were determined by using broth dilution and drop plate methods, respectively. Sucrose dependent and sucrose independent-adherences, biofilm formation and glycolytic pH drop assays were performed to evaluate the anticariogenic activity. RESULTS: The ethanolic stem extract of D. reticulata possessed the antibacterial activity against S. mutans with the MIC and MBC of 0.875±0.250 and 1.750±0.500 mg mL-1, respectively. The extract at the lower concentrations of sub-MIC also had significant inhibitory actions against the cariogenic properties of S. mutans, including surface adherence, biofilm formation and glycolytic acid production. CONCLUSION: The D. reticulata stem extract had a substantial anticariogenic activities and thus potentially be developed as an oral health care product for dental caries prevention in the near future.

Characterization of chitosan-magnesium aluminum silicate nanocomposite films for buccal delivery of nicotine.

The objective of this study was to prepare and characterize chitosan-magnesium aluminum silicate (CS-MAS) nanocomposite films as a buccal delivery system for nicotine (NCT). The effects of the CS-MAS ratio on the physicochemical properties, release and permeation, as well as on the mucoadhesive properties, were investigated. Molecular interactions between the components of the film were also investigated. The results indicated that NCT-loaded CS-MAS films provided a higher NCT content than NCT-loaded films containing only CS. The greater the MAS ratio in the films, the higher the NCT content that was observed because intercalated nanocomposites could be formed by electrostatic interactions of MAS with NCT and CS. These interactions caused an insignificant loss of NCT by evaporation during film drying. The release and permeation of NCT were related to the square root of time, indicating that a diffusion-controlled mechanism via the NCT-MAS complex particles and the film matrix controls NCT release. NCT release and permeation rates decreased with as the MAS ratio of the films was increased. However, the NCT-loaded CS-MAS films may have a potential adhesion to the mucosal membrane. These findings suggest that NCT-loaded CS-MAS films can be used as a buccal NCT delivery system.

Novel chitosan-magnesium aluminum silicate nanocomposite film coatings for modified-release tablets.

Chitosan (CS), a positively charged polysaccharide, and magnesium aluminum silicate (MAS), a negatively charged clay with silicate layers, can electrostatically interact to form nanocomposite films. In this study, CS-MAS nanocomposite films were evaluated for use in tablet film coating. Effects of CS-MAS ratio and coating level on water uptake and drug release from the coated tablets were investigated. Surface and film matrix morphology of the coated film and the effect of enzymes in the simulated gastro-intestinal fluid on drug release were also examined. The results demonstrated that the CS-MAS coated tablets had a rough surface and a layered matrix film, whereas a smooth surface and dense matrix film on the CS coated tablets was found. However, the CS-MAS coated tablets provided fewer film defects than the CS coated tablets. Nanocomposite formation between CS and MAS could retard swelling and erosion of CS in the composite films in acidic medium. The higher MAS ratio of the CS-MAS coated tablets gave lower water uptake and slower drug release when compared with the CS coated tablets. Moreover, the CS-MAS films on the tablets presented good stability towards enzymatic degradation in simulated intestinal fluid. The release of drug from the CS-MAS coated tablets could be modulated by varying CS-MAS ratios and coating levels. Additionally, drug solubility also influenced drug release characteristics of the CS-MAS coated tablets. These findings suggest that the CS-MAS nanocomposites displays a strong potential for use in tablet film coating intended for modifying drug release from tablets.

Chitosan-magnesium aluminum silicate nanocomposite films: physicochemical characterization and drug permeability.

Chitosan-magnesium aluminum silicate (CS-MAS) films were prepared and the effects of MAS content and heat treatment of the CS-MAS dispersion before film casting on the physicochemical and drug permeability properties of the films were investigated. CS could interact with MAS via electrostatic interaction and intermolecular hydrogen bonding mechanisms, resulting in nanocomposite formation, for which it was not necessary to apply the heat treatment on the composite dispersions. The nature of the exfoliated and intercalated nanocomposite films formed was depended on the MAS content added. The heat treatment on the composite dispersions caused an increase in tensile strength, but reduced %elongation of the CS-MAS nanocomposite films. The exfoliated nanocomposite films showed higher flexibility, water uptake, and drug permeability compared to the CS and intercalated CS-MAS nanocomposite films. At higher MAS content, the CS-MAS films prepared using heat treatment had a lower water uptake, resulting in lower drug permeability when compared with those prepared using non-heated dispersions. The permeation mechanism of non-electrolyte and negatively charged drugs across the CS-MAS nanocomposite films was predominantly controlled by diffusion in water-filled microchannels, whereas both adsorption onto MAS and diffusion processes occurred concurrently for the film permeation of positively charged drugs. The findings of this study suggest that CS-MAS nanocomposite films can be formed without heating of the composite dispersion before casting. CS-MAS nanocomposites showed strong potential to be used as a film former for coated tablets intended for modulating drug release.

Chitosan-magnesium aluminum silicate composite dispersions: characterization of rheology, flocculate size and zeta potential.

Composite dispersions of chitosan (CS), a positively charged polymer, and magnesium aluminum silicate (MAS), a negatively charged clay, were prepared and rheology, flocculate size and zeta potential of the CS-MAS dispersions were investigated. High and low molecular weights of CS (HCS and LCS, respectively) were used in this study. Moreover, the effects of heat treatment at 60 degrees C on the characteristics of the CS-MAS dispersions and the zeta potential of MAS upon addition of CS at different pHs were examined. Incorporation of MAS into CS dispersions caused an increase in viscosity and a shift of CS flow type from Newtonian to pseudoplastic flow with thixotropic properties. Heat treatment brought about a significant decrease in viscosity and hysteresis area of the composite dispersions. Microscopic studies showed that flocculation of MAS occurred after mixing with CS. The size and polydispersity index of the HCS-MAS flocculate were greater than those of the LCS-MAS flocculate. However, a narrower size distribution and the smaller size of the HCS-MAS flocculate were found after heating at 60 degrees C. Zeta potentials of the CS-MAS flocculates were positive and slightly increased with increasing MAS content. In the zeta potential studies, the negative charge of the MAS could be neutralized by the addition of CS. Increasing the pH and molecular weight of CS resulted in higher CS concentrations required to neutralize the charge of MAS. These findings suggest that the electrostatic interaction between CS and MAS caused a change in flow behavior and flocculation of the composite dispersions, depending on the molecular weight of CS. Heat treatment affected the rheological properties and the flocculate size of the composite dispersions. Moreover, pH of medium and molecular weight of CS influence the zeta potential of MAS.