Bilayer/multilayer tablets have been introduced to formulate incompatible components for compound preparations, but they are now more commonly used to tailor drug release. This research aimed to formulate a novel gastro-retentive tablet to deliver a combination of a fixed dose of two drugs to eliminate Helicobacter pylori (H. pylori) in the gastrointestinal tract. The bilayer tablets were prepared by means of the direct compression technique. The controlled-release bilayer tablets were prepared using various hydrophilic swellable polymers (sodium alginate, chitosan, and HPMC-K15M) alone and in combination to investigate the percent of swelling behavior and average drug release. The weight of the controlled-release floating layer was 500 mg, whereas the weight of the floating tablets of pantoprazole was 100 mg. To develop the most-effective formulation, the effects of the experimental components on the floating lag time, the total floating time, T 50%, and the amount of drug release were investigated. The drugs’ and excipients’ compatibilities were evaluated using ATR-FTIR and DSC. Pre-compression and post-compression testing were carried out for the prepared tablets, and they were subjected to in vitro characterization studies. The pantoprazole layer of the prepared tablet demonstrated drug release (95%) in 2 h, whereas clarithromycin demonstrated sustained drug release (83%) for up to 24 h (F7). The present study concluded that the combination of sodium alginate, chitosan, and HPMC polymers (1:1:1) resulted in a gastro-retentive and controlled-release drug delivery system of the drug combination. Thus, the formulation of the floating bilayer tablets successfully resulted in a biphasic drug release. Moreover, the formulation (F7) offered the combination of two drugs in a single-tablet formulation containing various polymers (sodium alginate, chitosan, and HPMC polymers) as the best treatment option for local infections such as gastric ulcers.
1 October 2017 in Russian Journal of General Chemistry
Metal complexes display functional interfaces for association with and stimulation of certain enzymes, that are liable to transfer genetic information in DNA for synthesis of specific proteins....
The treatment adherence of narcotics-addicted individuals with reduced incidences of relapse can be enhanced by a sustained drug release formulation of antinarcotics. So far, different drug formulations have been reported with sustained drug release periods of 28 and 35 days. To further enhance this duration, different formulations of injectable hydrogels (IHs) have been developed by combining low molecular weight (LMW) and high molecular weight (HMW) chitosan (CS) with guar gum (GG) and crosslinking them by sodium bi phosphate dibasic. The structural, morphological, and physicochemical properties of LMW-CS IH, and HMW-CS IH were evaluated using Fourier transform infrared spectroscopy (FT-IR), thermo-gravimetric analysis (TGA), scanning electron microscopy (SEM), and rheological, swelling, and biodegradation analysis. The HMW-CS IH showed high crosslinking, increased thermal stability, high mechanical strength, elevated swelling, and low biodegradation. The antinarcotic drugs naltrexone (NTX) and disulfiram (DSF) were loaded separately into the HMW-CS IH and LMW-CS IH. The release of NTX and DSF was investigated in phosphate buffer saline (PBS) and ethanol (0.3%, 0.4%, and 0.5%) over a 56-day period using an UV spectrophotometer. The drug release data were tested in zero-order, first-order, and Korsemeyer–Peppas mathematical models. In PBS, all prepared formulations followed non-Fickian drug release, while in ethanol, only NTX HMW-CS IH followed non-Fickian release in all three different concentrations of ethanol.
Background: Candida auris is a significant global health concern, due to its rapid transmission, high mortality rate, and resistance to commonly available antifungal drugs. Methodology: During the current study, a cationic polymeric hydrogel was developed using chitosan (CS), polyethylene glycol (PEG), and methacrylic acid (MAA). The respective solutions were mixed in a volumetric ratio of 2:1:1. After characterization, the hydrogel was assessed using antifungal, antibiofilm, and hemocompatibility assays. Results: The hydrodynamic radius of 554.7 ± 90.1 nm and zeta potential of 15.6 ± 1.09 mV indicate the ideal size and charge for topical applications and in vivo studies, respectively. The formulation exhibited improved thermal stability, enhanced swelling, and a drug release profile for non-Fickian diffusion. The hydrogel effectively inhibited fungal growth in agar plates (42 ± 7.31 mm zone of inhibition), with a mean IC50 of 15.17 ± 4.01 μg/mL and MIC of 29.30 ± 11.72 μg/mL. Calcofluor white (CFW) staining showed diffuse irregular yeast cells, suggesting increased membrane permeability, eventually leading to cell death. The hemocompatibility assay revealed no visible agglutination or hemolysis at the MIC value. The formulation exhibited significantly reduced biofilm formation compared to the growth control (p < 0.05). Additionally, in silico analysis revealed that MAA showed superior oral bioavailability, no inhibitory activity on cytochrome P450 enzymes, and low potential for toxicity through nuclear receptor signaling pathways. Conclusions: Cationic hydrogels show promise as potential antifungal treatments. The development of cost-effective and improved therapeutic methods is crucial to combat this deadly pathogen and to improve patient outcomes.
Aromatic polyamides are well-known as high-performance materials due to their outstanding properties making them useful in a wide range of applications. However, their limited solubility in common organic solvents restricts their processability and becomes a hurdle in their applicability. This study is focused on the synthesis of processable ferrocene-based terpolyamides and their polydimethylsiloxane (PDMS)-containing block copolymers, using low-temperature solution polycondensation methodology. All the synthesized materials were structurally characterized using FTIR and 1H NMR spectroscopic techniques. The ferrocene-based terpolymers and block copolymers were soluble in common organic solvents, while the organic analogs were found only soluble in sulfuric acid. WXRD analysis showed the amorphous nature of the materials, while the SEM analysis exposed the modified surface of the ferrocene-based block copolymers. The structure–property relationship of the materials was further elucidated by their water absorption and thermal behavior. These materials showed low to no water absorption along with their high limiting oxygen index (LOI) values depicting their good flame-retardant behavior. DFT studies also supported the role of various monomers in the polycondensation reaction where the electron pair donation from HOMO of diamine monomer to the LUMO of acyl chloride was predicted, along with the calculation of various other parameters of the representative terpolymers and block copolymers.
The limited shelf life of carbon prepreg waste (CPW) from component manufacturing restricts its use as a composite reinforcement fibre on its own. However, CPW can be recycled with glass fibre (GF) reinforcement to develop a unique remediate material. Therefore, this study fabricated (1) a glass fibre-carbon prepreg waste reinforced polymer hybrid composite (GF-CPW-PP), (2) a polypropylene composite (PP), (3) a carbon prepreg waste reinforced composite (CPW-PP), and (4) a glass fibre reinforced composite (GF-PP) and reported their degradation and residual tension properties after immersion in water. The polymer hybrid composites were fabricated via extrusion technique with minimum reinforce glass-carbon prepreg waste content of 10 wt%. The immersion test was conducted at room temperature using distilled water. Moisture content and diffusion coefficient (DC) were determined based on water adsorption values recorded at 24-h intervals over a one-week period. The results indicated that GF-PP reinforced composites retained the most moisture post-168 h of immersion. However, hardness and tensile strength were found to decrease with increased water adsorption. Tensile strength was found to be compromised since pores produced during hydrolysis reduced interfacial bonding between glass fibre and prepreg carbon reinforcements and the PP matrix.