Development of a solid self-microemulsifying drug delivery system (SMEDDS) for solubility enhancement of naproxen

Context: Comparative evaluation of liquid and solid self-microemulsifying drug delivery systems (SMEDDS) as promising approaches for solubility enhancement.

Objective: The aim of this work was to develop, characterize, and evaluate a solid SMEDDS prepared via spray-drying of a liquid SMEDDS based on Gelucire® 44/14 to improve the solubility and dissolution rate of naproxen.

Material and methods: Various oils and co-surfactants in combination with Gelucire® 44/14 were evaluated during excipient selection study, solubility testing, and construction of (pseudo)ternary diagrams. The selected system was further evaluated for naproxen solubility, self-microemulsification ability, and in vitro dissolution of naproxen. In addition, its transformation into a solid SMEDDS by spray-drying using maltodextrin as a solid carrier was performed. Scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) were used to evaluate the physical characteristics of the solid SMEDDS obtained.

Results: The selected formulation of SMEDDS was comprised of Miglyol 812®, Peceol?, Gelucire® 44/14, and Solutol® HS 15. The liquid and solid SMEDDS formed a microemulsion after dilution with comparable average droplet size and exhibited uniform droplet size distribution. In the solid SMEDDS, liquid SMEDDS was adsorbed onto the surface of maltodextrin and formed smooth granular particles with the encapsulated drug predominantly in a dissolved state and partially in an amorphous state. Overall, incorporation of naproxen in SMEDDS, either liquid or solid, resulted in improved solubility and dissolution rate compared to pure naproxen.

Conclusion: This study indicates that a liquid and solid SMEDDS is a strategy for solubility enhancement in the future development of orally delivered dosage forms.     

An artificial neural network model for the prediction of critical submergence for intake in a stratified fluid medium

Density differences may occur because of temperature differentials, suspended sediments, dissolved salts or other chemicals. Most of the large surface reservoirs are stably stratified throughout most, or all, of the year. One of the means of assisting the management is to allow a selective withdrawal from the reservoir. And while an intake is used for withdrawal (from the lower layer), a maximum discharge is required not allowing the uptake of the upper layer fluids. The value of the intake's vertical distance from the upper layer elevation (submergence) when the upper layer fluids begin to be drawn into the intake is known as ‘critical submergence’. In this study, the critical submergence for a circular intake pipe in a stratified body (which has different layer thickness) is investigated. Experiments were conducted on a vertically flowing downward intake pipe in a still-water reservoir. Artificial neural network (ANN) models and formulas, which are found by the theoretical analysis of critical spherical sink surface (CSSS), are used for the analysis of experimental results. The CSSS has the same centre and discharge as the intake. The ANN model and CSSS results are compared with the experimental results.     

Adsorption of lead and copper on bentonite and grapeseed activated carbon in single- and binary-ion systems

In this study, bentonite originating from Turkey (Eski?ehir province) and activated carbon obtained from grapeseed were used as adsorbents for the removal of lead (Pb²⁺) and copper (Cu²⁺) ions from aqueous solutions. Experiments were performed in single- and binary-ion systems at constant temperature of 298 K and pH value of 5. In order to describe the adsorption mechanism Langmuir, Freundlich and Temkin isotherms were used. The total adsorption capacity values of adsorbents were compared. It was observed that the total adsorption capacity values were changed depending on the type of adsorbent used, type of metal ion and interaction between metal ions.     

Effect of intracanal medicaments on the push-out bond strength of Biodentine in comparison with Bioaggregate apical plugs

To evaluate the effect of intracanal medicaments on the push-out bond strength of Biodentine in comparison with DiaRoot BioAggregate (BA) when used as apical plugs. Forty single-rooted teeth were prepared using Peeso reamers. The samples were divided into four groups. The intracanal medicaments were applied to the root canals as follows: Group1: a combination of metronidazole–ciprofloxacin–cefaclor, Group2: a combination of metronidazole–ciprofloxacin, Group3: calcium hydroxide, and Group4: no medication. After 21 days, the medicaments were removed. The apical part of each root was horizontally sectioned into 1-mm thick slices. The samples were divided into two subgroups, and the following materials were placed: Biodentine, DiaRoot-BioAggregate. After 48-h incubation, the push-out bond strength was measured. The data were analyzed by a two-way ANOVA. Biodentine showed a significantly higher mean push-out bond strength value than DiaRoot-BioAggregate (P = 0.00). The medications have an effect on the push-out bond strength of both materials (P = 0.002). Biodentine showed better adhesive performance as an apical plug than DiaRoot-BioAggregate.     

Novel colloidal nanofiber electrolytes from PVA‐organoclay/poly(MA‐alt‐MVE), and their NaOH and Ag‐carrying polymer complexes

Novel multifunctional polymer nanofiber electrolytes with covalence crosslinked structures from various solution blends of reactive intercalated poly(vinyl alcohol)/octadecylamine montmorillonite (as a matrix polymer), poly(maleic anhydride‐alt‐methyl vinyl ether) (as a partner polymer) and their NaOH‐absorbing and Ag‐carrying polymer complexes were fabricated via electrospinning. Chemical, physical, morphological, and electrical properties of nanofiber structures were investigated by FTIR, XRD, SEM, and electrical analysis methods. Ag precursors in fiber composites significantly improved phase separation processing, fiber morphologies, diameter distributions, and electrical properties of the fibers. In situ generation of Ag nanoparticles and their distribution on nanofiber surfaces during fiber formation occurred via complex formation between silver cations and electronegative functional groups from both matrix and partner polymers as stabilizing/reducing agents. Electrical resistance and conductivity strongly depended on matrix/partner polymer ratios and absorption time of NaOH solution on nanofibers. Addition of NaOH changed the electrical properties of fiber structures from almost dielectric state to excellent conductivity form. The fabricated unique nanofiber electrolytes are promising candidates for applications in power and fuel cell nanotechnology, electrochemical, and bioengineering processes as reactive semiconductive platforms. POLYM. ENG. SCI., 56:204–213, 2016. © 2015 Society of Plastics Engineers     

Stabilized electrospinning of heat stimuli/in situ crosslinkable nanofibers and their self‐same nanocomposites

We present a strategy for stabilizing the morphological integrity of electrospun polymeric nanofibers by heat stimuli in situ crosslinking. Amorphous polymer nanofibers, such as polystyrene (PS) and its co‐polymers tend to lose their fiber morphology during processing at temperatures above their glass transition temperature (T_g) typically bound to happen in nanocomposite/structural composite applications. As an answer to this problem, incorporation of the crosslinking agents, phthalic anhydride (PA) and tributylamine (TBA), into the electrospinning polymer solution functionalized by glycidylmethacrylate (GMA) copolymerization, namely P(St‐co‐GMA), is demonstrated. Despite the presence of the crosslinker molecules, the electrospinning polymer solution is stable and its viscosity remains unaffected below 60 °C. Crosslinking reaction stands‐by and can be thermally stimulated during post‐processing of the electrospun P(St‐co‐GMA)/PA‐TBA fiber mat at intermediate temperatures (below the T_g). This strategy enables the preservation of the nanofiber morphology during subsequent high temperature processing. The crosslinking event leads to an increase in T_g of the base polymer by 30 °C depending on degree of crosslinking. Crosslinked nanofibers are able to maintain their nanofibrous morphology above the T_g and upon exposure to organic solvents. In situ crosslinking in epoxy matrix is also reported as an example of high temperature demanding application/processing. Finally, a self‐same fibrous nanocomposite is demonstrated by dual electrospinning of P(St‐co‐GMA) and stabilized P(St‐co‐GMA)/PA‐TBA, forming an intermingled nanofibrous mat, followed by a heating cycle. The product is a composite of crosslinked P(St‐co‐GMA)/PA‐TBA fibers fused by P(St‐co‐GMA) matrix. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 44090.     

Photocrosslinked biobased phase change material for thermal energy storage

A series of novel photocrosslinked biobased shape‐stabilized phase change materials (PCMs) based on octadecanol, eicosanol and docosanol have been prepared by UV technique for the purpose of thermal energy storage applications. Epoxidized soybean oil was reacted with acrylic acid to form acrylated soybean oil (ASO). The structure and composition, cross‐section morphology, thermal stability performances and phase change behaviors of ASO and UV‐cured PCMs were examined by using Attenuated total reflection fourier transform infrared spectroscopy, thermogravimetric analysis system (TGA), scanning electron microscopy, and differential scanning calorimetry. The results indicate that the UV‐cured biobased PCMs possess perfect phase change properties and a suitable working temperature range. The heating process phase change enthalpy is measured between 30 and 68 J/g, and the freezing process phase change enthalpy is found between 18 and 70 J/g. The decomposition of UV‐cured PCMs started at 260 °C and reached a maximum of 430 °C. All the biobased UV‐cured PCMs improved latent heat storage capacity in comparison with the pristine ASO sample. With the obtained results we conclude that, these materials promise a great potential in thermal energy storage applications. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 43757.     

Synthesis,characterization and polymerization of novel sugars based on methacrylate

The present study describes the synthesis and characterizations of polymerizable vinyl sugars. Glucose, mannose, galactose and fructose are abundant and sustainable natural compounds. As it is not possible to make many derivatives of sugars without using protective groups, first of all, diacetone derivatives [diacetone-d-glucose (1), diacetone-d-mannose (2), diacetone-d-galactose (3) and diacetone-d-fructose (4)] were synthesized according to the literature as starting compounds. The remaining free hydroxyl groups on C-3 (diacetone glucose), C-6 (diacetone galactose), C-1 (diacetone fructose) and C-1 (diacetone mannose), were reacted with epichlorohydrin (1-chloro-2,3-epoxypropane) to produce then “-O-(2′,3′-epoxypropane-1′-yl)” ether derivatives (5, 6, 7, and 8) which are epoxy sugars in the basic medium. Next, the epoxy rings of the ethers (5, 6, 7, and 8) were opened with methacrylic acid in DMF to produce new sugar based methacrylates (9, 10, 11, and 12). Finally, free radical polymerization of these sugar based methacrylate monomers was performed, producing related polymers (13, 14, 15 and 16). The polymerizations were carried out using AIBN as an initiator at 70 °C in DMF. All the products were characterized by FTIR, ¹HNMR and ¹³CNMR techniques. Thermal properties of all polymers were investigated by TG, DTG and DSC. The data obtained has suggested that thermal stability of the synthesized polymers has changed with the structure of the sugar and increase in molecular weight.