Polymer drug conjugates containing memantine, tacrine and cinnamic acid: promising nanotherapeutics for the treatment of Alzheimer's disease.

AIM: To prepare polymer-drug conjugates containing a combination of memantine, tacrine, and E)-N-(3-aminopropyl)cinnamide, promising therapeutics for the treatment of neurodegenerative disorders. METHODS: The conjugates were characterised by 1HNMR, particle size analysis, SEM, LC-MS, TEM/EDX, and XRD, followed by in vitro anti-acetylcholinesterase and drug release studies. RESULTS: 1H NMR analysis revealed successful drug conjugation with drug mass percentages in the range of 1.3-6.0% w/w. The drug release from the conjugates was sustained for 10 h in the range of 20-36%. The conjugates' capability to inhibit acetylcholinesterase (AChE) activity was significant with IC50 values in the range of 13-44.4 µm which was more effective than tacrine (IC50 =1698.8 µm). The docking studies further confirmed that the conjugation of the drugs into the polymer improved their anti-acetylcholinesterase activity. CONCLUSION: The drug release profile, particle sizes, and in vitro studies revealed that the conjugates are promising therapeutics for treating neurodegenerative disorders.

Preparation of Copper-Decorated Activated Carbon Derived from Platamus occidentalis Tree Fiber for Antimicrobial Applications.

This study focuses on a greener approach to synthesizing activated carbon by carbonizing Platamus occidentalis tree fibers (TFSA) with 98% H2SO4 at 100 °C. The resulted TFSA was employed as an effective adsorbent for copper ions in aqueous media, yielding copper decorated TFSA (Cu@TFSA). The successful adsorption of copper onto the TFSA was proven through extensive characterization techniques. Herein, the TEM and XPS showed that copper nanoparticles were formed in situ on the TFSA surface, without the use of additional reducing and stabilizing agents nor thermal treatment. The surface areas of TFSA and Cu@TFSA were 0.0150 m2/g and 0.3109 m2/g, respectively. Applying the Cu@TFSA as an antimicrobial agent against Escherica coli ( E. coli) and Salmonella resulted in the potential mitigation of complex secondary pollutants from water and wastewater. The Cu@TFSA exhibited outstanding antimicrobial activity against E. coli and Salmonella in both synthetic and raw water samples. This demonstrated a complete growth inhibition observed within 120 min of exposure. The bacteria inactivation took place through the destruction of the bacteria cell wall and was confirmed by the AFM analysis technique. Cu@TFSA has the potential to be used in the water and wastewater treatment sector as antimicrobial agents.

Intercalation of Nb2O5 nano-flowers into the walls of few-layer black phosphorus creating a heterostructure of FL-BP@Nb2O5 with the potential for environmental application.

Herein we report the successful exfoliation of few-layer BP (FL-BP) from bulk BP via ultrasonication in N-methylpyrrolidone (NMP). FL-BP exhibited an orthorhombic phase structure similar to that of bulk BP with weak electrostatic out-of-plane interactions and strong ionic in-plane bonds. The weakened out-of-plane bonds allowed the intercalation of Nb2O5 nano-flowers that were hydrothermally synthesized, forming an intimate contact with the exfoliated BP. The successful formation of the heterointerface was confirmed by the co-existence of crystal phases of both compounds as per the XRD results. The formation of the new intrinsic Nb-P bond was confirmed by the presence of Raman shoulders of both compounds, further substantiated by the XPS analysis. The heterointerface enhanced Nb2O5 light-harvesting capacity as per the UV-vis measurements. The FL-BP's properties of higher carrier effective mass and density were successfully incorporated in the composite, implying an increased flow of electrons in the composite's lattice structure. This was displayed by the great suppression of the fast recombination rate of charge carriers in the composites. The 3% BP@Nb2O5 composite exhibited excellent optoelectrical properties, compared to the other composites, as suggested by the microstrain calculations, PL, and the EIS data. Mott-Schottky plots verified the p-n type heterojunction formed in the composites, and further verified the increased electron density/concentration in the composites, with respect to Nb2O5. Noteworthy, the incorporation of FL-BP in the lattice of Nb2O5 increased the surface area and the pore size and volume, which is a character beneficial for photocatalysis as it presents active sites and diffusion pathways.

Synthesis and characterization of alginate beads encapsulated zinc oxide nanoparticles for bacteria disinfection in water.

The use of polymer nanocomposites as novel materials for water remediation has emerged as a promising alternative for disinfection of bacteria contaminated water. Sodium alginate, a natural biopolymer has been investigated in this study by encapsulating antimicrobial zinc oxide nanoparticles supported bentonite. The confirmation of the alginate nanocomposites was done by use of TEM, SEM-EDS and XRD. The antimicrobial activity of the alginate nanocomposites was investigated by batch studies using surface water and synthetic bacteria contaminated water containing Staphylococcus aureus. The effect of nanocomposite amount and initial bacteria concentration has been studied. The inactivation results indicated that the nanocomposite effectively inactivated bacteria in both the synthetic and surface water. With an amount of 0.5 g of the nanocomposites, no bacteria was observed in the water after 70 min of contact time with initial bacteria concentration of 200 cfu/ml for synthetic water and within a min, no bacteria was observed in the water for surface water. It is worth noting that 200 cfu/ml is the bacteria concentration range in which environmental water is likely to contain. Therefore, the results of this study have indicated that the alginate nanocomposites can be deemed as a potential antimicrobial agent for water disinfection.

Polylactide-based Magnetic Spheres as Efficient Carriers for Anticancer Drug Delivery.

To improve traditional cancer therapies, we synthesized polylactide (PLA) spheres coencapsulating magnetic nanoparticles (MNPs, Fe3O4) and an anticancer drug (doxorubicin, DOX). The synthesis process involves the preparation of Fe3O4 NPs by a coprecipitation method and then PLA/DOX/Fe3O4 spheres using the solvent evaporation (oil-in-water) technique. The Fe3O4 NPs were coated with oleic acid to improve their hydrophobicity and biocompatibility for medical applications. The structure, morphology and properties of the MNPs and PLA/DOX/Fe3O4 spheres were studied using various techniques, such as FTIR, SEM, TEM, TGA, VSM, UV-vis spectroscopy, and zeta potential measurements. The in vitro DOX release from the spheres was prolonged, sustained, and pH-dependent and fit a zero-order kinetics model and an anomalous mechanism. Interestingly, the spheres did not show a DOX burst effect, ensuring the minimal exposure of the healthy cells and an increased drug payload at the tumor site. The pronounced biocompatibility of the PLA/DOX/Fe3O4 spheres with HeLa cells was proven by a WST assay. In summary, the synthesized PLA/DOX/Fe3O4 spheres have the potential for magnetic targeting of tumor cells to transform conventional methods.

The adsorption of Pb2+ and Cu2+ onto gum ghatti-grafted poly(acrylamide-co-acrylonitrile) biodegradable hydrogel: isotherms and kinetic models.

A biodegradable hydrogel polymer of gum ghatti (Gg) with a copolymer mixture of acrylamide (AAm) and acrylonitrile (AN) was synthesized using the free-radical graft copolymerization technique. The effect of graft copolymerization on the surface area of Gg was studied using BET analyses. The graft copolymerization of Gg with poly(AAm-co-AN) was characterized using Fourier transform infrared spectroscopy, CHN analysis, thermogravimetric analysis, atomic force microscopy, and scanning electron microscopy. The adsorption of Pb(2+) and Cu(2+) from aqueous solution using the Gg-cl-P(AAm-co-AN) hydrogel polymer was studied in batch mode. The adsorption process was found to be highly pH dependent, and the maximum adsorption efficiency was observed at pH 5.0 for both metal ions. The adsorption isotherm data were analyzed by applying five different isotherm models, namely, the Langmuir, Freundlich, Temkin, Flory-Huggins, and Dubinin-Kaganer-Radushkevich isothermal models. The Langmuir model was found to fit well with the experimental isotherm data, with a maximum adsorption capacity of 384.6 and 203.7 mg/g for Pb(2+) and Cu(2+), respectively. The metal ion-adsorption process was found to be controlled by the pseudo-second-order rate model. The Gg-cl-P(AAm-co-AN) hydrogel polymer retained its original adsorption capacity for three successive cycles of adsorption-desorption. In summary, the potential for remediating industrial wastewater polluted by metal ions using the biodegradable Gg-cl-P(AAm-co-AN) hydrogel polymer has been demonstrated.

Structure and properties of highly toughened biodegradable polylactide/ZnO biocomposite films.

Zinc oxide (ZnO) powder was investigated in terms of its use as filler in order to improve the inherent properties of PLA. Biocomposite films of PLA with different loadings of ZnO were prepared by solution casting method. Morphological analyses using SEM and POM showed that the ZnO particles were well dispersed at low ZnO loading, with starfish-like morphology. However, ZnO agglomeration was found at higher ZnO loadings. Tensile testing showed improvements in strength and a moderate improvement in toughness at 2 wt% ZnO loading. This is consistent with the homogeneous dispersion of ZnO particles in the PLA matrix. ZnO particles incorporation improved the thermal stability of PLA. In summary, ZnO particles were shown to have the potential as a toughener in the preparation of biocomposites with better integrity, although other approaches, such as the use of compatibilizer in the surface modification of ZnO will be needed for the concurrent improvement of PLA properties.

Role of specific interfacial area in controlling properties of immiscible blends of biodegradable polylactide and poly[(butylene succinate)-co-adipate].

Binary blends of two biodegradable polymers: polylactide (PLA), which has high modulus and strength but is brittle, and poly[(butylene succinate)-co-adipate] (PBSA), which is flexible and tough, were prepared through batch melt mixing. The PLA/PBSA compositions were 100/0, 90/10, 70/30, 60/40, 50/50, 40/60, 30/70, 10/90, and 0/100. Fourier-transform infrared measurements revealed the absence of any chemical interaction between the two polymers, resulting in a phase-separated morphology as shown by scanning electron microscopy (SEM). SEM micrographs showed that PLA-rich blends had smaller droplet sizes when compared to the PBSA-rich blends, which got smaller with the reduction in PBSA content due to the differences in their melt viscosities. The interfacial area of PBSA droplets per unit volume of the blend reached a maximum in the 70PLA/30PBSA blend. Thermal stability and mechanical properties were not only affected by the composition of the blend, but also by the interfacial area between the two polymers. Through differential scanning calorimetry, it was shown that molten PBSA enhanced crystallization of PLA while the stiff PLA hindered cold crystallization of PBSA. Optimal synergies of properties between the two polymers were found in the 70PLA/30PBSA blend because of the maximum specific interfacial area of the PBSA droplets.

Polylactide-based bionanocomposites: a promising class of hybrid materials.

Polylactide (PLA) is the oldest and potentially one of the most interesting and useful biodegradable man-made polymers because of its renewable origin, controlled synthesis, good mechanical properties, and inherent biocompatibility. The blending of PLA with functional nanoparticles can yield a new class of hybrid materials, commonly known as bionanocomposites, where 1-5% nanoparticles by volume are molecularly dispersed within the PLA matrix. The dispersed nanoparticles with their large surface areas and low percolation thresholds both can improve the properties significantly in comparison with neat PLA and can introduce new value-added properties. Recently, researchers have made extraordinary progress in the practical processing and development of products from PLA bionanocomposites. The variation of the nanofillers with different functionalities can lead to many bionanocomposite applications including environmentally friendly packaging, materials for construction, automobiles, and tissue regeneration, and load-bearing scaffolds for bone reconstruction. This Account focuses on these recent research efforts, processing techniques, and key research challenges in the development of PLA-based bionanocomposites for use in applications from green plastics to biomedical applications. Growing concerns over environmental issues and high demand for advanced polymeric materials with balanced properties have led to the development of bionanocomposites of PLA and natural origin fillers, such as nanoclays. The combination of nanoclays with the PLA matrix allows us to develop green nanocomposites that possess several superior properties. For example, adding ∼5 vol % clay to PLA improved the storage modulus, tensile strength, break elongation, crystallization rate, and other mechanical properties. More importantly, the addition of clay decreases the gas and water vapor permeation, increases the heat distortion temperature and scratch resistance, and controls the biodegradation of the PLA matrix. In biomedicine, researchers have employed the design rules found in nature to fabricate PLA-based bionanocomposites. The incorporation of functional nanoparticles in the PLA matrix has improved the physical properties and changed the surface characteristics of the matrix that are important for tissue engineering and artificial bone reconstruction, such as its thermal and electrical conductivity, surface roughness, and wettability. Finally, of the introduction of bionanocomposite biocompatible surfaces on drugs, such as antibiotics, could produce delivery systems that act locally.

Effect of nanoclay loading on the thermal and mechanical properties of biodegradable polylactide/poly[(butylene succinate)-co-adipate] blend composites.

Polylactide/poly[(butylene succinate)-co-adipate] (PLA/PBSA)-organoclay composites were prepared via melt compounding in a batch mixer. The weight ratio of PLA to PBSA was kept at 70:30, while the weight fraction of the organoclay was varied from 0 to 9%. Small angle X-ray scattering patterns showed slightly better dispersion in PBSA than PLA, and there was a tendency of the silicate layers to delaminate in PBSA at low clay content. Thermal analysis revealed that crystallinity was dependent on the clay content as well its localization within the composite. On the other hand, thermal stability marginally improved for composites with <2 wt % clay content in contrast to the deterioration observed in composites with clay content >2 wt %. Tensile properties showed dependence on clay content and localization. Composite with 2 wt % clay content showed slight improvement in elongation at break. Overall, the optimum property was found for a composite with 2 wt % of the organoclay. This paper therefore has demonstrated the significance of the clay content and localization on the properties of the PLA/PBSA blends.

Dispersion characteristics and properties of poly(methyl methacrylate)/multi-walled carbon nanotubes nanocomposites.

The preparation, characterization, and properties of poly(methyl methacrylate) (PMMA)/multi-walled carbon nanotubes (MWCNTs) nanocomposites are described. Nanocomposites have been prepared by melt-blending in a batch mixer. Both unmodified and surface modified MWCNTs have been used for the nanocomposites preparation. Using both unmodified and modified MWCNTs, the effect of surface modification in nanocomposites is investigated by focusing on three major aspects: dispersion characteristics, mechanical properties, and electrical conductivity measurements. Dispersion of the MWCNTs in the PMMA matrix is examined by scanning and transmission electron microscopy that revealed a homogeneous distribution-dispersion of MWCNTs in the PMMA matrix for both unmodified and modified MWCNTs. Thermomechanical behavior is studied by dynamic mechanical analyzer and results showed a substantial improvement in the mechanical properties of PMMA in conjunction to an increase in the elastic behavior. The tensile properties of neat PMMA moderately improved after nanocomposites preparation with both modified and unmodified MWCNTs, however, electrical conductivity of neat PMMA significantly improved after nanocomposites preparation with 2 wt% unmodified MWCNTs. For example, the through plane conductivity increased from 3.6 x 10(-12) S x cm(-1) for neat PMMA to 3.6 x 10(-9) S x cm(-1) for nanocomposite. The various property measurements have been conducted and results have shown that, in overall, surface modifications have very little or no effect on final properties of neat PMMA.