A mixed-ligand approach for building a N-rich porous metal-organic framework for drug release and anticancer activity against oral squamous cell carcinoma

Abstract

A new Zn(II) metal-organic framework (MOFs), [Zn(BTC)(HME)]·(DMAc)(H₂O) (1, H₃BTC =1,3,5-benzenetricarboxylic acid, HME?=?protonated melamine, DMAc?=?N,N-dimethylacetamide), has been synthesized under solvothermal conditions. In the structure of 1, the four-coordinate Zn(II) ions are connected by BTC^3? ligands into a 3-D framework with (3)-connected utg-type topology. This MOF shows permanent porosity after lattice solvent removal with a calculated pore size distribution around 0.72?nm. With abundant N-donor sites and suitable pore size, the desolvated 1 (1a) was used as a drug carrier for the loading of anticancer drug 5-fluorouracil (5-Fu) molecules. Moderate 5-Fu loading capacity and long drug release time were observed for 1a. The computational simulation results reveal that strong H-bond interactions between the 5-Fu molecules and the nitrogen sites allow slow release of the drug 1a. In addition, the in vitro cytotoxicity of 1 and 5-Fu loaded 1a were also evaluated using MTT assays against human oral squamous cell carcinoma (SCC-251 and HSC-4).     

Thermal and acid labile polyurethanes as a new class of responsive materials in polymeric nanoparticles and nanocapsules

A new class of polyurethanes has been designed, containing tertiary carbamate groups in the main chain of the polymer, which enable the resulting polymer to degrade completely under acid and thermal treatment. The decomposition temperatures of the polymers were determined by measuring the evolution of carbon dioxide and other decomposition products using TGA‐MS. Until decomposition of the polymer, no glass transition was found. The polymers exhibit excellent solubility in common organic solvents like chloroform and tetrahydrofuran, making them to suitable materials for film formation. From the obtained polymers, nanoparticles were synthesized by the solvent evaporation method combined with the miniemulsion technique. The resulting nanoparticles can be used as intelligent fillers in films and sensors, since they degrade at temperatures of above 180 °C, which can be detected by a color change reaction with ninhydrin. Polymeric nanocapsules were prepared by an interfacial polyaddition reaction from 2,4‐toluene diisocyanate and tertiary diols performed at the droplet's interface in inverse (water‐in‐oil) miniemulsions. These nanocapsules with an encapsulated photoacid generator can act as a release system, whereby an acidic release through irradiation with ultraviolet light can be triggered. © 2011 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2012     

Synthesis of Depo‐Medrol–chitosan hydrogel as new drug slow‐release appliance and investigation of release kinetics by high‐performance liquid chromatography

The present study deals with preparation and optimization of a novel chitosan hydrogel‐based matrix by suspension cross‐linking method for controlled release of Depo‐Medrol. The controlled release of Depo‐Medrol for effective Rheumatoid arthritis disease has become an imperative field in the drug delivery system. In this context, it was intended to optimize loading circumstances by experimental design and also study the release kinetics of Depo‐Medrol entrapped in the chitosan matrix in order to obtain maximal efficiency for drug loading. The optimum concentrations of chitosan (2.5 g), glutaraldehyde (3.05 μL) and Depo‐Medrol (0.1 mg) were set up to achieve the highest value of drug loaded and the most sustained release from the chitosan matrix. In vitro monitoring of drug release kinetic using high‐performance liquid chromatography showed that 73% of the Depo‐Medrol was released within 120 min, whereas remained drug was released during the next 67 h. High correlation between first‐order and Higuchi's kinetic models indicates a controlled diffusion of Depo‐Medrol through the surrounding media. Moreover, recovery capacity >82% and entrapment efficiency of 58–88% were achieved under optimal conditions. Therefore, the new synthesized Depo Medrol–chitosan is an applicable appliance for arthritis therapy by slow release mechanism. Copyright © 2016 John Wiley & Sons, Ltd.     

On the Effects of UV Radiation on the Release Ability of Glucose Embedded in Hydroxypropyl Cellulose Films

New drug delivery systems based on hydroxypropyl cellulose (HPC) and different percents of glucose were prepared and characterized to check their suitability as UV resistant patches. The spectral absorption properties of the HPC and HPC-glucose blends before and after UV irradiation were analyzed. The surface polarity and hydrophilicity were correlated with the morphology of the films and analyzed with respect to the UV exposure time and the embedded amount of glucose. The effects of UV radiation on in vitro evaluation of glucose release from the HPC films are reported. The mechanism involved in the drug release process, evaluated using the Korsmeyer-Peppas equation, was dependent on the introduced amount of glucose and less on the UV exposure time. A more polar, smoother, and less dense surface releases the glucose over larger periods of time, making the system with lower percents of glucose more adequate for the pursued purpose.     

Dynamics of pulsatile flows through microtubes from nonlocality

In this paper we introduce a new notion of complexified nonlocal-in-time-space material derivative operator and we discuss its implications in fluid mechanics. After deriving the complexified fluid equations, we investigate the problem of laminar flow of a particle fluid in a microtube. We demonstrate the occurrence of pulsatile flows through microtubes in agreement with recent findings.     

Effect of polymer and ion concentration on mechanical and drug release behavior of gellan hydrogels using factorial design

Developing optimized hydrogel products requires an in-depth understanding of the mechanisms that drive hydrogel tunability. Here, we performed a full 4 × 4 factorial design study investigating the impact of gellan, a naturally derived polysaccharide (1%, 2%, 3%, or 4% w/v) and CaCl₂ concentration (1, 3, 7, or 10 mM) on the viscoelastic, swelling, and drug release behavior of gellan hydrogels containing a model drug, vancomycin. These concentrations were chosen to specifically provide insight into gellan hydrogel behavior for formulations utilizing polymer and salt concentrations expanding beyond those commonly reported by previous studies exploring gellan. With increasing gellan and CaCl₂ concentration, the hydrogel storage moduli (0.1–100 kPa) followed a power-law relationship and on average these hydrogels had higher liquid absorption capability and greater total drug release over 6 days. We suggest that the effects of gellan and CaCl₂ concentration and their interactions on hydrogel properties can be explained by various phenomena that lead to increased swelling and increased resistance to network expansion.