Understanding the Protective Effect of Phytate in Bone Decalcification Related-Diseases

Myo-inositol hexaphosphate (phytate; IP6) is a natural compound that is abundant in cereals, legumes, and nuts, and it can bind to crystal surfaces and disturb crystal development, acting as crystallization inhibitor. The adsorption of such inhibitors to crystal faces can also inhibit crystal dissolution. The binding of phytate to metal cofactors suggests that it could be used for treatment of osteoporosis. Our in-vitro study showed that phytate inhibits dissolution of hydroxyapatite (HAP). The effect of phytate was similar to that of alendronate and greater than that of etidronate. This led us to perform a cross-sectional study to investigate the impact of consumption of IP6 on bone mineral density (BMD) in post-menopausal women. Our data indicate that BMD and t-score of lumbar spine increased with increasing phytate consumption, and a phytate consumption higher than 307 mg/day was associated with a normal BMD (t-score > −1). These data suggest that phytate may have a protective effect in bone decalcification by adsorbing on the surfaces of HAP, and a daily consumption of phytate-rich foods (at least one serving/day of legumes or nuts) may help to prevent or minimize bone-loss disorders, such as osteoporosis. However, further studies are needed to gain a better understanding about the mechanism of inhibition of phytate in bone-related diseases (see graphical abstract).

The Mechanism of Improvement of Film Solubility: Design and Evaluation of Film Forming System with Terbinafine as a Model Drug

Purpose: Film forming system (FFS) combines the advantages of patch and gel, it is expected to replace small doses of topical administration in the future. This work targets the design and evaluation of HPC-acrylic FFS with different excipients in appearance, rheology and in vitro properties. Also, the reason of improving the solubility of terbinafine film was illustrated by melting enthalpy thermo analysis.Methods: In this work, we prepared 8 HPC-acrylic FFS samples with different excipients, and characterized the film forming solutions and films in appearance, rheological properties, drug crystallization and in vitro performance. Then used melting enthalpy thermo-analysis to explain the mechanism of improvement of film solubility.Results: According to appearance evaluation, the samples which had a small amount of plasticizer could achieve an uniform surface morphology. The XRD and DSC demonstrated HPC could maintain drug amorphous in films. Based on oscillation frequency sweep, short chain plasticizer tributyl citrate (TBC) leading to strong entanglement and hydrogen bonding among the molecules. In vitro release test showed FP1 had favorable release. And the melting enthalpy thermo-analysis explained why FP1 had favorable release. Conclusions: HPC acted as an effective crystallization inhibitor. TBC could lead stronger intermolecular hydrogen bonds. The poloxamer had favorite miscibility with HPC-acrylic FFS. The combination of MCT and poloxamer with HPC resulted in a high Terbinafine solubility.

Designing a next generation solar crystallizer for real seawater brine treatment with zero liquid discharge

Proper disposal of industrial brine has been a critical environmental challenge. Zero liquid discharge (ZLD) brine treatment holds great promise to the brine disposal, but its application is limited by the intensive energy consumption of its crystallization process. Here we propose a new strategy that employs an advanced solar crystallizer coupled with a salt crystallization inhibitor to eliminate highly concentrated waste brine. The rationally designed solar crystallizer exhibited a high water evaporation rate of 2.42 kg m−2 h−1 under one sun illumination when treating real concentrated seawater reverse osmosis (SWRO) brine (21.6 wt%). The solar crystallizer array showed an even higher water evaporation rate of 48.0 kg m−2 per day in the outdoor field test, suggesting a great potential for practical application. The solar crystallizer design and the salt crystallization inhibition strategy proposed and confirmed in this work provide a low-cost and sustainable solution for industrial brine disposal with ZLD.

Amorphous solid dispersions of enzalutamide and novel polysaccharide derivatives: investigation of relationships between polymer structure and performance

Amorphous solid dispersion (ASD) is a widely employed formulation technique for drugs with poor aqueous solubility. Polymers are integral components of ASDs, but mechanisms by which polymers lead to the generation and maintenance of supersaturated solutions, which enhance oral absorption in vivo, are poorly understood. Herein, a diverse group of newly synthesized cellulose derivatives was evaluated for their ability to inhibit crystallization of enzalutamide, a poorly soluble compound used to treat prostate cancer. ASDs were prepared from selected polymers, specifically a somewhat hydrophobic polymer that was extremely effective at inhibiting drug crystallization, and a less effective, but more hydrophilic, crystallization inhibitor, that might afford better release. Drug membrane transport rate was evaluated in vitro and compared to in vivo performance, following oral dosing in rats. Good correlation was noted between the in vitro diffusion cell studies and the in vivo data. The ASD formulated with the less effective crystallization inhibitor outperformed the ASD prepared with the highly effective crystallization inhibitor in terms of the amount and rate of drug absorbed in vivo. This study provides valuable insight into key factors impacting oral absorption from enabling ASD formulations, and how best to evaluate such formulations using in vitro approaches.

Low Protein Natural Rubber Latex - Based Polymer Blends for Transdermal Patches of Mefenamic Acid

Transdermal patches are attraction and acceptance for the patient due to avoid first-pass metabolism, easy to administer and removal, allows rapid termination of treatment if required etc. Low protein natural rubber latex (LPNRL) is a natural polymer that removed the allergic protein from fresh NRL prepared by treatment with proteolytic enzyme and centrifuging process. LPNRL is used for medical skin applications with the non-allergenic product. The objective of this research aimed to prepare the mefenamic acid – loaded transdermal patches made from LPNRL blended with either hydroxypropyl methylcellulose (HPMC) or polyvinyl alcohol (PVA), glycerin and polyvinylpyrrolidone were used as plasticizer and crystallization inhibitor, respectively. The moisture uptake and swelling ratio showed the increment value after either HPMC or PVA was blended in LPNRL because of the increment of their hydrophilicity. These patches showed the homogeneous films that observed by the researcher. The in vitro release showed a faster release rate after either HPMC or PVA was blended in LPNRL. It was concluded that mefenamic acid – loaded transdermal patches could be prepared by using LPNRL blended with either HPMC or PVA as matrix film former could provide an increased and controlled release of the drug. Moreover, it was safe to apply on the skin as did not cause irritation.