Soluble Polymers Research Articles

Encapsulating taurine into liposomes: A promising therapeutic for liver fibrosis.

We summarize the mechanism by which taurine (Tau) inhibits autophagy and induces iron apoptosis in hepatic stellate cells. Tau interacts with autophagy regulates multifunctional proteins, microtubule-associated protein 1 light chain 3 Beta, and autophagy-related gene 5 to inhibit autophagy, binds to ferritin heavy chain 1 and nuclear receptor coactivator 4 to trigger ferritin autophagy, and interacts with glutathione peroxidase 4 to promote iron apoptosis. There is a solid rationale for developing Tau-based therapies targeting autophagy and ferroptosis regulation. From a pharmaceutical point of view, there are certain requirements for Tau protein delivery systems, such as loading efficiency, stability, and targeting. Nanomaterials should also contain a hydrophilic motif similar to Tau to optimize loading efficiency. Since Tau is a hydrophilic molecule with high water solubility, liposomes, micelles, and amphiphilic polymer nanoparticles may represent a superior choice. The nanostructure of the liposome includes a water region and a lipid membrane to sequester hydrophilic and hydrophobic drugs, respectively, whereas Tau is expected to be loaded into the water region. In addition, a representative method of actively targeting hematopoietic stem cells is introduced. A Tau-based method for the treatment of liver fibrosis is proposed based on the formulation of common liposomes (lecithin plus cholesterol).

Bis-cationic crosslinked anion exchange membranes based on carbazole-containing polyaromatics with excellent ionic conductivity for alkaline water electrolysis

As the core component in anion exchange membrane water electrolyser (AEMWE), anion exchange membrane (AEM) directly determines the electrolysis performance and long-term durability of AEMWE. Herein, we synthesized novel poly(carbazole-p-terphenylpiperidine) (PCTP-x) copolymers and then prepared a series of bis-cationic cross-linked AEMs (QPCTP-x-bpip) using the Menshutkin reaction between the cross-linker 4,4′-trimethylenebis(1-methylpiperidine) and the alkyl bromide on the polymer side chains. For comparison, non-crosslinked AEMs containing alkylpiperidinium side chains (QPCTP-x-pip) were prepared via a grafting reaction of alkyl bromide with 1-methylpiperidine. The bis-cationic crosslinked membrane exhibited high hydroxide conductivity of 190.0 mS cm−1, and demonstrated outstanding alkaline stability in a 1 M KOH solution at 80 °C, retaining more than 90 % of the initial hydroxide conductivity and tensile strength after 2200 h alkaline treatment. Meanwhile, the flexural carbazole backbone enhanced polymer solubility, enabling the utilization of QPCTP-20-pip as an anion exchange ionomer (AEI) in AEMWE. For the water electrolysis testing, AEMWE employing QPCTP-20-bpip as the AEM and QPCTP-20-pip as the AEI exhibited excellent performance, achieving a current density of 2910 mA cm−2 at 2.0 V using a 1 M KOH feed at 80℃. Moreover, the voltage increase during the in-situ durability test over 200 h was a mere 0.65 mV/h, demonstrating its promising potential for AEMWE applications.

Modification approaches of walnut proteins to improve their structural and functional properties: A review

Walnut protein has a high gluten content and compact structure, which limits its water solubility and affects its applications. Therefore, improving the sustainability of walnut proteins is an urgent issue that must be addressed. Physical modification can directly alter the structure of walnut proteins, leading to enhanced functional properties. Chemical modifications typically involve the introduction of exogenous substances that react with walnut proteins to obtain novel products with improved processing attributes. As a highly specific modification technique, biomodification uses enzymes or microorganisms to break down walnut proteins into small peptide molecules or cross-link them to form soluble polymers, thereby enhancing their functional properties and bioactivity. This review presents various methods for modifying walnut proteins and their effects on the structure and functional properties of walnut proteins. The challenges associated with the application and development of these unique technologies are also discussed.

Encapsulation of a drug into electrospun fibers spun from water soluble polymers to control solubility and release

Electrospun fibers prepared from water-soluble polymers (PVP, PVA, and HPMC) were loaded with pregabalin, a BCS I drug, to address its fast release and adverse effects. The drug dissolved partially (1.8–2.8 wt%) in the polymers, with excess pregabalin in crystalline form within the fibers. The solubility of the drug varied with the pH of the dissolution medium. Most of the drug encapsulated into the fibers during electrospinning, but some was lost due to technical reasons. PVP showed no impact on drug release, offering no benefit as a carrier. However, PVA-based fibers exhibited considerably slower release than the dissolution rate of the neat drug and also the release rate from fibers prepared from the other polymers. This indicates the potential of PVA for using it with pregabalin in practical drug formulations with improved release properties. The pH of the dissolution medium influenced solubility and release rate for specific polymers. Overall, the study highlights the importance of polymer selection and pH control in optimizing the release profile of pregabalin in enhanced drug delivery.

Photocatalytic degradation of phenol and polycyclic aromatic hydrocarbons in water by novel acid soluble collagen-polyvinylpyrrolidone polymer embedded in Nitrogen-TiO2

Herein, we have synthesized acid-soluble collagen (ASC), polyvinylpyrrolidone (PVP), and nitrogen-doped titanium dioxide to form a novel hybrid photocatalyst nanocomposite (N-TiO2/ASC-PVP). The results of XRD, SEM and TEM revealed that the as-synthesized photocatalyst was composed of spheroidal particles, which were smaller than undoped TiO2.XPS analysis revealed that N was effectively incorporated into the lattice of TiO2 through substituting oxygen atoms, and N might coexist in the form of substitutional N (O–Ti–N) and interstitial N (TiON). The N-TiO2/ASC-PVP composite calcined at 200 and 400 °C exhibited high photocatalytic degradation rates for phenol, naphthalene (Nap), fluoranthene (Flu), phenanthrene (Phe), pyrene (Pyr), benz[a]anthracene (BaA), and anthracene (Ana), achieving a 98.6 % removal rate within 120 min at a dosage of 10 mg/L. The enhanced visible light photocatalytic activity was mainly attributed to the smaller crystal size, more surface hydroxyl groups, stronger light absorption in visible region and narrower band gap energy. This innovative hybrid photocatalyst holds immense potential for applications in materials science and nanotechnology, promising to revolutionize various industries.

Improving multifunctional properties of the polyvinylidene fluoride (PVDF) membrane with crosslinked dialdehyde-starch (DAS) and polyethyleneimine (PEI) coating

Dialdehyde-soluble starch (DAS) and polyethyleneimine (PEI) were used to coat the polyvinylidene fluoride (PVDF) membrane for improving its antifouling and multifunctional properties through a combination of dip-coating and spray-coating techniques. The resulting membrane demonstrated excellent hydrophilicity and underwater oleophobicity due to hydrophilic DAS and PEI on its surface. The membrane achieved an impressive oil removal rate of 99.8 % and a flux 1420.8 ± 26.5 L·m−2·h−1 when it was used for oil-water emulsion separation. The hydration layer formed by the DAS and PEI greatly enhanced the membrane antifouling property, and its flux recovery rate was up to 96.6 % in BSA filtration experiments. The positive charge PEI and the negative charge DAS contributed to high separation efficiency of 99.1 % for the anion dye MO with the membrane D10P20, and high separation efficiency of 88.3 % for the cation dye RhB with the membrane P5D20. In addition, the coating layer was stable due to the cross-linked DAS and PEI. This research contributes greatly to the preparation of antifouling and multifunctional membrane using environmentally friendly material including polysaccharide derivatives and water soluble polymer.

The effect of fluorinated conjugated side chains on the photovoltaic performance of polymers based on benzodithiophene (BDT) and carbazolobistriazole (CTA)

Reasonable regulation of the structure-performance relationship is extremely crucial to enhancing the device performance of organic solar cells (OSCs). As a novel fused-benzotriazole (BTA) electron-accepting (A) unit, carbazolobistriazole (CTA) has excellent luminescent properties, and the alkyl chains on the three N atoms allow flexible modulation of polymer solubility. However, higher molecular energy levels and weak crystallinity restrict the enhancement of device performance. Herein, a new donor polymer PE97 with CTA as A unit and 4,8-bis(4-(2-ethylhexyl)-3,5-difluorophenyl)benzo[1,2-b:4,5-b’]dithiophene (BDT-P2F) as electron-donating (D) unit was designed and synthesized. In comparison with the first CTA-based polymer PE93 with 4,8-bis(5-(2-ethylhexyl)-4-fluorothiophen-2-yl)benzo[1,2-b:4,5-b’]dithiophene (BDT-TF) as D unit, PE97 realizes stronger molecular stacking conducive to modulation of the active layer morphology and a deeper highest occupied molecular orbital (HOMO) level, which are favorable to increase short-circuit current density (JSC) and open-circuit voltage (VOC) of OSCs. When paired with Y-series non-fullerene acceptor eC9-2F, PE97-based OSC devices have achieved a higher power conversion efficiency (PCE) of 15.5 %, with a VOC of 0.81 V, a JSC of 25.3 mA cm−2, and a fill factor (FF) of 75.7 %, which figures significantly surpass efficiency (13.6 %) of PE93-based devices. These results indicate that the BDT-P2F unit can excellently modulate the optoelectronic properties of CTA-based polymers. This highlights the potential of the BDT-P2F as a promising D unit for polymers with weak crystallinity and limited electron-withdrawing properties.

Assessment of Solubility Behavior of a Copolymer in Supercritical CO2 and Organic Solvents: Neural Network Prediction and Statistical Analysis.

In the industrial sector, understanding the behavior of block copolymers in supercritical solvents is crucial. While qualitative agreement with polymer solubility curves has been evaluated using complex theoretical models in many cases, quantitative predictions remain challenging. This study aimed to create a rapid and accurate artificial neural network (ANN) model to predict the lower critical solubility and upper critical solubility space of an atypical block copolymer, poly(styrene-co-octafluoropentyl methacrylate) (PSOM), in different supercritical solvent systems over a wide range of temperatures (51.75-182.05 °C) and high pressure (3.28-200.86 MPa). The experimental data set used in this study included one copolymer, five supercritical solvents, one cosolvent, and one initiator. It consisted of seven unique copolymer-solvent combinations (252 cloud point pressures) used to predict the model quantitatively and qualitatively. To predict the PSOM-solvent interactions, the study considered two different input systems: a six-variable system, a five-variable system, and one target output. Initially, we used a three-layer feed-forward neural network to select the best learning algorithm (Levenberg-Marquardt) from 14 different algorithms, considering one sample PSOM-solvent system. Then, the network topology was optimized by varying hidden neuron numbers from 2 to 80 for all seven PSOM-solvent combination systems. The predicted cloud point pressures were in excellent agreement with the experimental cloud point pressures, confirming the model's accuracy. It is clear from the results of a minimum mean square error (≤1.90 × 10-27) and maximum linear regression R 2 (≥0.99) during training, validation, and testing of all the data sets. Further, the ANN model accuracy was tested by statistical analysis, confirming the model's ability to accurately capture the miscibility regions of polymers, enabling efficient processing of various polymer materials. This data-driven approach facilitates the prediction of coexistence curves for other polymers and complex macromolecular systems.

Integrating Multiple Strategies Using Biotechnology to Design High‐Performance Electrocatalysts for Hydrogen and Oxygen Evolution

AbstractCombining multiple design strategies often enhances catalyst performance but usually comes with high costs and low reproducibility. A technique that enhances catalyst performance in multiple strategies is urgently needed. Herein, a novel bioregulation technique is introduced, allowing simultaneous control over morphology, particle size, doping, interface engineering, and electronic properties. Bioregulation technique utilizes the soluble extracellular polymer from Aspergillus niger as a templating agent to construct high‐performance catalysts for hydrogen and oxygen evolution reaction (HER and OER). This technique controls catalyst morphology, introduces biological N and S doping, and regulates the electronic structure of the catalyst surface. Biomolecule modification enhances surface hydrophilicity, and the nanostructure increases surface roughness and gas‐release efficiency. Theoretical calculations show that the bioregulation technique shortens the d/p‐band center, optimizing reaction intermediate adsorption and desorption. The Bio‐Pt/Co3O4 catalyst with trace Pt on the surface, designed with these strategies, achieves HER (η10 of 42 mV), OER (η10 of 221 mV), and overall water‐splitting performance (1.51 V at 10 mA cm−2), maintaining stability for over 50 h, outperforming most Pt‐based catalysts. Notably, using spent lithium‐ion battery cathodes leachate, rich in Co2⁺, successfully replicates the experiment. This approach holds promise as a mainstream method for synthesizing high‐performance materials in the future.

Synergistic Effects of Radical Distributions of Soluble and Insoluble Polymers within Electrospun Nanofibers for an Extending Release of Ferulic Acid.

Polymeric composites for manipulating the sustained release of an encapsulated active ingredient are highly sought after for many practical applications; particularly, water-insoluble polymers and core-shell structures are frequently explored to manipulate the release behaviors of drug molecules over an extended time period. In this study, electrospun core-shell nanostructures were utilized to develop a brand-new strategy to tailor the spatial distributions of both an insoluble polymer (ethylcellulose, EC) and soluble polymer (polyvinylpyrrolidone, PVP) within the nanofibers, thereby manipulating the extended-release behaviors of the loaded active ingredient, ferulic acid (FA). Scanning electron microscopy and transmission electron microscopy assessments revealed that all the prepared nanofibers had a linear morphology without beads or spindles, and those from the coaxial processes had an obvious core-shell structure. X-ray diffraction and attenuated total reflectance Fourier transform infrared spectroscopic tests confirmed that FA had fine compatibility with EC and PVP, and presented in all the nanofibers in an amorphous state. In vitro dissolution tests indicated that the radical distributions of EC (decreasing from shell to core) and PVP (increasing from shell to core) were able to play their important role in manipulating the release behaviors of FA elaborately. On one hand, the core-shell nanofibers F3 had the advantages of homogeneous composite nanofibers F1 with a higher content of EC prepared from the shell solutions to inhibit the initial burst release and provide a longer time period of sustained release. On the other hand, F3 had the advantages of nanofibers F2 with a higher content of PVP prepared from the core solutions to inhibit the negative tailing-off release. The key element was the water permeation rates, controlled by the ratios of soluble and insoluble polymers. The new strategy based on core-shell structure paves a way for developing a wide variety of polymeric composites with heterogeneous distributions for realizing the desired functional performances.

Liquid-liquid equilibrium of binary ethanol–polyisobutene and ternary ethanol–water–polyisobutene systems under low- and high-pressure conditions: An assessment using the PC-SAFT equation of state

Sugarcane bioethanol in either anhydrous or hydrous forms stands out as an economically viable bioproduct that can be used as a fuel or feedstock in various innovative applications, reducing human-generated greenhouse gas emissions. Low-molar-mass polyisobutene (PiB) is used as a lubricant in sugarcane-processing plants and is a possible contaminant of sugarcane bioethanol. Understanding the liquid–liquid equilibrium (LLE) of ethanol–PiB binary systems and ethanol–water–PiB ternary systems is essential to avoid undesired phase separation at high-pressure engine conditions and other potential innovative applications. However, the experimental investigation of these systems is significantly hampered by very low polymer solubilities in aqueous ethanol. The LLE of ethanol-PiB and ethanol–water–PiB mixtures was qualitatively investigated using the PC-SAFT equation of state through the development and implementation of extrapolation strategies allowing to estimate ethanol–PiB and water–PiB binary parameters using experimental data obtained for other systems containing lighter alkanes. Phase diagrams were calculated considering temperatures ranging from 298.15 K to 350 K and pressures ranging from 1 bar to 200 bar. It was shown that lower pressures, higher temperatures, lower PiB molar masses, and lower water contents increase the polymer solubility in the solvents. Thus, the risk of liquid–liquid separation can be mitigated by correctly managing such operational parameters. The obtained phase diagrams may present significant quantitative deviations from reality because of the model’s sensitivity to the estimated binary parameters. Thus, they should be interpreted as general qualitative guidelines to avoid and manage undesired phase separation in industrial processes and engines rather than phase equilibrium predictions.

CHEMICAL MODIFICATION AND BIOLOGICAL ACTIVITY OF ALGINATE-BASED HYDROGELS

In recent years, the problem of wound infection has risen dramatically. Infectious complications of surgical wounds have increased significantly, often leading to severe sepsis. Gram-negative bacteria and microorganisms, which are immune to virtually all currently available antimicrobials, are the main culprits. In this regard, the development and implementation of innovative drugs and wound dressings, purulent and chronic wound treatment methods is an urgent problem of many domestic and foreign researchers. Brown algae are extracted using an alkaline solution to produce the ionic polysaccharide sodium alginate. It still holds one of the top positions among water-soluble polymers of natural origin as a result of various highly useful practical characteristics. Based on alginate hydrogels, it is possible to create new materials for biotechnological, pharmaceutical and medical purposes, as they have high moisture retention capacity, non-toxicity and self-decomposing ability. After reviewing the literature, we concluded that cefepime is a new antibiotic researched for wound dressing using IV generation cephalosporins as an antibacterial agent. It is highly resistant to hydrolysis by most beta-lactamases and quickly penetrates the cells of gram-negative bacteria. Inside the bacterial cell, it targets penicillin-binding proteins. To obtain new derivatives of sodium alginate with special properties, a chemical method, in particular, thiolene reactions, was used. It should be noted that click chemistry refers to a set of chemical reactions for the rapid and reliable synthesis of compounds by the uniform addition of individual components. Thiolene reactions offer significant advantages, includingversatile reaction conditions (including radical reactions and catalytic processes) and the ability to use a wide range of substrates with different unsaturated bonds such as acrylates, methacrylates and ethers. To monitor the rate and efficiency of UV activation, we used a sol-gel assay technique that allowed us to quantify insoluble (spatially cross-linked) and soluble polymers. After UV activation, samples with different ratios of thiol derivative (S-H bond) showed low viscosity, indicating the predominant degradation of polymer molecules in these systems. Since alginate-polymer derivatives primarily exhibit deconstructive behavior, the dominant process in alginate molecules is the breaking of bonds rather than their formation. The size of the gel fraction reflects the efficiency of polymer cross-linking, which in turn affects the efficiency of immobilization of the drug in the hydrogel matrix and its release rate. This study presents an experimental characterization of photocrosslinked hydrogels aimed at evaluating and elucidating the physicochemical and biological properties of the antibiotic cefepime in an alginate polymer. The obtained kinetic parameters of the swelling-dissolving process show that the synthesized alginate hydrogel is capable of providing a diffused and prolonged release of drugs. In addition, the synthesized hydrogel effectively delivers cefepime to the tested bacterial strains, showing high antibacterial activity without toxicity. However, further in vivo studies are needed to evaluate the fate and toxicity of the alginate-based hydrogel before definitive conclusions can be drawn regarding the usefulness of the synthesized drugs. These preliminary results can be the basis for the development of medical products.

Correction to “Regenerating Spent Lithium-Ion Battery Cathodes as Dual-Functional Biocatalysts for Highly-Efficient Oxygen and Hydrogen Evolution Using Aspergillus niger Soluble Extracellular Polymers”

Correction to “Regenerating Spent Lithium-Ion Battery Cathodes as Dual-Functional Biocatalysts for Highly-Efficient Oxygen and Hydrogen Evolution Using <i>Aspergillus niger</i> Soluble Extracellular Polymers”

Formulation and evaluation of melatonin as fast dissolving oral strips using combined polymers

Background and objective: Fast-dissolving oral thin film (FDOF) is a novel and most advanced form of solid dosage form that dissolves or disintegrates in 1 minute when put in the mouth without water or chewing. Pre-gastric absorption of FODFs from the mouth, pharynx, and esophagus as saliva flows down into the stomach would improve the therapeutic benefit of the drug as oral films disintegrated in the mouth. The study is designed and purposed to use most water soluble, best type and concentration of polymers to be selected for use in combination to formulate melatonin oral thin films. Different types of synthetic water soluble polymers were utilized the preparation of films (hydroxypropyl methyl cellulose HPMC15M, sodium carboxy methyl cellulose NACMC). Methods: Solvent casting method was performed for preparation of twelve placebo films at the beginning, to obtain and select suitable polymer type and concentration for use in combination to be formulated for drug loading. The films were evaluated for their characteristics like mechanical properties (thickness and folding endurance), surface pH and disintegration time. Percentage of release and assay of melatonin was taken. Comparison studies were performed on melatonin films from this study with melatonin oral disintegrating tablets release profiles. Best batch could be selected. Drug-excipient compatibility carried out as pre formulation study to see whether there is interaction between the drug and excipients used. Results: Results from FT-IR showed no interaction between melatonin and polymers used, the prepared formulations were clear, transparent, non-sticky and easily removed from the plate surface with the thickness ranging from (0.04-0.07) mm depending on the polymer concentration. The times required for the films to disintegrate was ranging from 21-26 seconds, and the majority of melatonin was released within first 2 minutes within the dosage form. Conclusion: Melatonin can be formulated as fast dissolving oral films using combination of water-soluble polymers by solvent casting method to obtain ease of administration without using water during administration, fast onset of action resulted from rapid disintegration.

Modulation of acid-induced pea protein gels by gellan gum and glucono-δ-lactone: Rheological and microstructural insights

This study investigated the effect of gellan gum (GG) and glucono-δ-lactone (GDL) on the acid-induced gel properties of pea protein isolate (PPI) pretreated with media milling. The inclusion of GG substantially enhanced the gel hardness of PPI gel from 18.69 g to 792.47 g though slightly reduced its water holding capacity (WHC). Rheological analysis showed that GG increased storage modulus (G’) and decreased damping factor of gels in the small amplitude oscillatory shear region and transformed its strain thinning behavior into weak strain overshoot behavior in the large amplitude oscillatory shear region. SEM revealed that GG transformed the microstructure of gel from a uniform particle aggregate structure to a chain-like architecture composed of filaments with small protein particles attached. Turbidity and zeta potential analysis showed that GG promoted the transformation of PPI from a soluble polymer system to an insoluble coagulant during acidification. When GG content was relatively high (0.2 %-0.3 %), high GDL content increased the electrostatic interaction between PPI and GG molecules, causing their rapid aggregation into a dense irregular aggregate structure, further enhancing gel strength and WHC. Overall, GG and GDL can offer the opportunity to modulate the microstructure and gel properties of acid-induced PPI gels, presenting potential for diversifying food gel design strategies through PPI-GG hybrid systems.

Impact of the alkyl side-chain length on solubility, interchain packing, and charge-transport properties of amorphous π-conjugated polymers

Increasing the length of alkyl side chains is a typical way to improve the solubility of π-conjugated polymers designed for use in solution-processed devices. However, these modifications have also been reported to alter the film morphology. Given that the mechanism leading to improved solubility is not well documented yet and the nanoscale (local) morphologies of amorphous π-conjugated polymer films are difficult to characterize experimentally, here, we combine molecular dynamics simulations and long-range corrected density functional theory calculations to examine at the molecular scale the impact that the alkyl side-chain length has on polymer solubility and film morphologies. As a representative example, we consider poly(thieno[3,4-c]pyrrole-4,6-dione-alt-3,4-difluorothiophene) (PTPD[2F]T) with two different lengths of the alkyl side chains on the thieno[3,4-c]pyrrole-4,6-dione (TPD) moieties, i.e., 2-hexyldecyl (2HD) and 2-decyltetradecyl (2DT). A detailed analysis of polymer–solvent and polymer–polymer interactions provides a picture that describes the underlying mechanism for improved solubility in going from 2HD to 2DT. We then underline an intrinsic characteristic that decreasing the side-chain length brings a greater extent of backbone planarity and lesser side chain-TPD interactions, which leads to higher interchain π-π packing density and order, while the interchain π-π packing patterns remain similar in the two films. These morphologies are discussed in terms of the charge-transport properties between neighboring PTPD[2F]T chains, which point to a higher electron mobility in the PTPD[2F]T films with shorter alkyl side chains. Overall, our findings offer guidance in the field of solution-processed electronic devices by pointing out that the polymer alkyl side-chain length could be minimized to improve carrier mobility while ensuring polymer solubility.

Proximal Photocleavage: Controlling Polymer Solubility through Pathway Dependent Wavelength‐Orthogonal Photoreactions

AbstractCurrent families of reversible photochemical reactions present challenges for light‐controlled polymers of either photostationary states, which are common in photoinduced cycloaddition/cycloreversion reactions, or exclusively intramolecular bond changes, which characterize most photochromic units. In response to these challenges, here the concept of “proximal photocleavage” is presented, which combines photochemical crosslinking with a photocleavable linker, enabling a one‐time bond formation/cleavage sequence. Proximal photocleavage methacrylate monomers comprising, in series along the pendant of the methacrylate, a coumarin unit for crosslinking and either a phenacyl or ortho‐nitrobenzyl photocleavable group for decrosslinking are reported. The photophysical properties of these monomers and their statistical copolymers with methyl methacrylate are described, and wavelength selective crosslinking and de‐crosslinking of thin polymer films are demonstrated.

Formulation and investigation of differently charged β-cyclodextrin-based meloxicam potassium containing nasal powders

Nasal systemic drug delivery may provide an easy way to substitute parenteral or oral dosing, however, the excipients have an important role in nasal formulations to increase the permeability of the mucosa and prolong the residence time of the drug. In this work, we aimed to produce meloxicam potassium monohydrate (MXP) containing nasal powders by a nano spray drier with the use of a neutral, an anionic and a cationic β-cyclodextrin as permeation enhancers, and (polyvinyl)alcohol (PVA) as a water soluble polymer. The following examinations were performed in order to study the effect of the applied excipients on the nasal applicability of the formulations: laser scattering, scanning electron microscope measurement, XRPD, DSC and FTIR measurements, adhesivity, in vitro drug release and permeability tests through an artificial membrane and RPMI 2650 cells. Based on our results, spherical particles were prepared with a size of 1.89–2.21 µm in which MXP was present in an amorphous state. Secondary interactions were formed between the excipients and the drug. The charged cyclodextrin-based formulations showed significantly higher adhesive force values regardless of the presence of PVA. The drug release was fast and complete. The passive diffusion of MXP was influenced not only by the charge of the cyclodextrin, but the presence of PVA, too. The permeation of the drug was enhanced in the presence of the anionic cyclodextrin testing it on RPMI 2650 cell model.

Gas permeability, diffusivity, and solubility in polymers: Simulation-experiment data fusion and multi-task machine learning

Machine learning (ML) models for predicting gas permeability through polymers have traditionally relied on experimental data. While these models exhibit robustness within familiar chemical domains, reliability wanes when applied to new spaces. To address this challenge, we present a multi-tiered multi-task learning framework empowered with advanced machine-crafted polymer fingerprinting algorithms and data fusion techniques. This framework combines scarce “high-fidelity” experimental data with abundant diverse “low-fidelity” simulation or synthetic data, resulting in predictive models that display a high level of generalizability across novel chemical spaces. Additionally, this multi-task scheme capitalizes on known physics and interrelated properties, such as gas diffusivity and solubility, both of which are closely tied to permeability. By amalgamating high throughput generated simulation data with available experimental data for gas permeability, diffusivity, and solubility for various gases, we construct multi-task deep learning models. These models can simultaneously predict all three properties for all gases under consideration, with markedly enhanced predictive accuracy, particularly compared to traditional models reliant solely on experimental data for a singular property. This strategy underscores the potential of coupling high-throughput classical simulations with data fusion methodologies to yield state-of-the-art property predictors, especially when experimental data for targeted properties is scarce.

Teneligliptin hydrobromide hydrate mouth dissolving strip: Formulation and evaluation

Oral route is considered as one of the most convenient route for administration of various pharmaceutical dosage form like tablet, capsule, syrup, suspension and emulsion. Fast Dissolving Drug Delivery systems have developed various fast disintegrating preparations like Oral disintegrating film, ODF. Oral disintegrating film is the solid oral drug delivery system, in which water soluble polymer involve to disintegrate film into mouth fastly. Oral disintegrating film is superior as compare to orally disintegrating tablet as the cost of production is low. The present research was undertaken to develop oral disintegrating film of tteneligliptin hydrobromide hydrate to have rapid onset of action. of tteneligliptin hydrobromide hydrate which is an anti-diabetic. The mechanism action of Teneligliptin is to increase incretin levels (GLP-1 and GIP), which inhibit glucagon release, which in turn increases insulin secretion, decreases gastric emptying, and decreases blood glucose levels.The concept of formulating fast disintegrating film Teneligliptin containing offers a suitable and practical approach in serving desired objective of faster disintegration and dissolution characteristics with increased bioavailability. ODF of Teneligliptin were prepared by solvent casting method and evaluated physicochemical parameters like thickness, weight variation, moisture content, folding endurance, drug content, etc. All the formulations of Teneligliptin ODF displayed optimum folding endurance, which indicates the formulation prepared can withstand handling and transportation. From the results obtained, it was concluded that the formulation of oral disintegrating film has better physical chemical properties with good disintegration property.