Synthesis and characterization of cellulose acetate from cellophane industry residues. Application as acetaminophen controlled-release membranes

Journal of Thermal Analysis and Calorimetry - Cellophane film production generates cellulosic residues from scraps, edges, and low-quality films. In this work, cellophane was used as a raw material...     

Multiple-frequency EPR spectra of two aqueous Gd3+ polyamino polypyridine carboxylate complexes: a study of high field effects

In the search for highly efficient magnetic resonance imaging contrast agents, polyamino polypyridine carboxylate complexes of Gd3+ have shown unusual properties with both very rapid and very slow electron spin relaxation in solution observed by electron paramagnetic resonance. Since the relationship between the molecular structure and the electron spin properties remains quite obscure at this point, detailed studies of such complexes may offer useful clues for the design of Gd3+ compounds with tailored electronic features. Furthermore, the availability of very high-frequency EPR spectrometers based on quasi-optical components provides us with an opportunity to test the existing relaxation theories at increasingly high magnetic fields and observation frequencies. We present a detailed EPR study of two gadolinium polyamino polypyridine carboxylate complexes, [Gd(tpaen)]- and [Gd(bpatcn)(H2O)], in liquid aqueous solutions at multiple temperatures and frequencies between 9.5 and 325 GHz. We analyze the results using the model of random zero-field splitting modulations through Brownian rotation and molecular deformations. We consider the effect of concentration on the line width, as well as the possible existence of an additional g-tensor modulation relaxation mechanism and its possible impact on future experiments. We use (17)O NMR to characterize the water exchange rate on [Gd(bpatcn)(H2O)] and find it to be slow (approximately 0.6 x 10(6) s-1).     

Efficient <Emphasis Type="Italic">Candida rugosa</Emphasis> lipase immobilization on Maghnite clay and application for the production of (<Emphasis Type="Italic">1R</Emphasis>)-(−)-Menthyl acetate

This work focused on the identification of natural, economical, and efficient supports for immobilization of Candida rugosa lipase (CRL) to catalyze the resolution of (±)-menthol. To this purpose, CRL has been immobilized on natural montmorillonite from Algeria (Maghnite-H), ion-exchange resins (Amberjet^®1200-H and Amberjet^®4200-Cl), and diatomaceous earth (Celite^®545). After a preliminary screening of supports, the immobilization of CRL led to a markedly improved enantioselectivity. Excellent enantioselectivity (E ≥ 134) was achieved by the four supported lipases (E = 68 for free enzyme). Compared to the three other supports tested, higher enantioselectivity was observed with Maghnite-H used as immobilization matrix. In this work, the effects of solvent, reaction time, and temperature, on the conversion as well as on enantioselectivity were investigated. The maximum of conversion (% C = 43%) with high enantiomeric excess of products (eep > 99) was obtained when the reaction is catalyzed by CRL immobilized on Maghnite-H at 30 °C for 24 h, and using toluene as selected solvent. Immobilized CRL on Maghnite-H exhibited good thermostability over a wide temperature range (30–90 °C) compared to the free one. These results suggest that CRL immobilized on Maghnite-H has good potential as biocatalyst for the production of (1R)-(?)-menthyl acetate.     

Cationic,Methylene‐Bridged,Intramolecular Donor‐Acceptor Systems Based on Zirconium and Hafnium and Phosphino‐methanides

A new access to cationic zirconium and hafnium compounds [L₂MCH₂PR₂][MeB(C₆F₅)₃] (L = Cp, Ind; R = iso‐Pr, tert‐Bu; M = Zr, Hf) exhibiting an intramolecular donor‐acceptor system was established by treating the precursors L₂M(Me)CH₂PR₂ with B(C₆F₅)₃ (BCF). Precursors 1 – 6 [L₂M(Me)CH₂PR₂ with L = Cp, Ind; R = iso‐Pr, tert‐Bu; M = Zr, Hf] were fully characterized. The crystal structures of these compounds revealed large M–CH₂–P bond angles with values of about 134° indicating the absence of interactions between the Lewis‐acid and Lewis‐base. The cationic compounds [L₂MCH₂PR₂][MeB(C₆F₅)₃] ( 7 – 12 ) were obtained by treatment of 1 – 6 with BCF. They were characterized by NMR spectroscopy, mass spectrometry, and elemental analyses; in H/D‐scrambling experiments with H₂/D₂ mixtures 7 – 12 disclosed their reactivity towards cleavage of hydrogen.     

Improved Dermal and Transdermal Delivery of Curcumin with SmartFilms and Nanocrystals

Poor aqueous solubility of active compounds is a major issue in today’s drug delivery. In this study the smartFilm-technology was exploited to improve the dermal penetration efficacy of a poorly soluble active compound (curcumin). Results were compared to the dermal penetration efficacy of curcumin from curcumin bulk suspensions and nanocrystals, respectively. The smartFilms enabled an effective dermal and transdermal penetration of curcumin, whereas curcumin bulk- and nanosuspensions were less efficient when the curcumin content was similar to the curcumin content in the smartFilms. Interestingly, it was found that increasing numbers of curcumin particles within the suspensions increased the passive dermal penetration of curcumin. The effect is caused by an aqueous meniscus that is created between particle and skin if the dispersion medium evaporates. The connecting liquid meniscus causes a local swelling of the stratum corneum and maintains a high local concentration gradient between drug particles and skin. Thus, leading to a high local passive dermal penetration of curcumin. The findings suggest a new dermal penetration mechanism for active compounds from nano-particulate drug delivery systems, which can be the base for the development of topical drug products with improved penetration efficacy in the future.     

Unravelling the Phytochemical Composition and the Pharmacological Properties of an Optimized Extract from the Fruit from Prunus mahaleb L.: From Traditional Liqueur Market to the Pharmacy Shelf

Prunus mahaleb L. fruit has long been used in the production of traditional liqueurs. The fruit also displayed scavenging and reducing activity, in vitro. The present study focused on unravelling peripheral and central protective effects, antimicrobial but also anti-COVID-19 properties exerted by the water extract of P. mahaleb. Anti-inflammatory effects were studied in isolated mouse colons exposed to lipopolysaccharide. Neuroprotection, measured as a blunting effect on hydrogen-peroxide-induced dopamine turnover, was investigated in hypothalamic HypoE22 cells. Antimicrobial effects were tested against different Gram+ and Gram- bacterial strains. Whereas anti-COVID-19 activity was studied in lung adenocarcinoma H1299 cells, where the gene expression of ACE2 and TMPRSS2 was measured after extract treatment. The bacteriostatic effects induced on Gram+ and Gram- strains, together with the inhibition of COX-2, TNFα, HIF1α, and VEGFA in the colon, suggest the potential of P. mahaleb water extract in contrasting the clinical symptoms related to ulcerative colitis. The inhibition of the hydrogen peroxide-induced DOPAC/DA ratio indicates promising neuroprotective effects. Finally, the downregulation of the gene expression of ACE2 and TMPRSS2 in H1299 cells, suggests the potential to inhibit SARS-CoV-2 virus entry in the human host. Overall, the results support the valorization of the local cultivation of P. mahaleb.     

Yield,Characterization, and Possible Exploitation of Cannabis Sativa L. Roots Grown under Aeroponics Cultivation

Cannabis sativa L. has been used for a long time to obtain food, fiber, and as a medicinal and psychoactive plant. Today, the nutraceutical potential of C. sativa is being increasingly reappraised; however, C. sativa roots remain poorly studied, despite citations in the scientific literature. In this direction, we identified and quantified the presence of valuable bioactives (namely, β-sitosterol, stigmasterol, campesterol, friedelin, and epi-friedelanol) in the root extracts of C. sativa, a finding which might pave the way to the exploitation of the therapeutic potential of all parts of the C. sativa plant. To facilitate root harvesting and processing, aeroponic (AP) and aeroponic-elicited cultures (AEP) were established and compared to soil-cultivated plants (SP). Interestingly, considerably increased plant growth—particularly of the roots—and a significant increase (up to 20-fold in the case of β-sitosterol) in the total content of the aforementioned roots’ bioactive molecules were observed in AP and AEP. In conclusion, aeroponics, an easy, standardized, contaminant-free cultivation technique, facilitates the harvesting/processing of roots along with a greater production of their secondary bioactive metabolites, which could be utilized in the formulation of health-promoting and health-care products.     

A Practical Approach for the In Vitro Safety and Efficacy Assessment of an Anti-Ageing Cosmetic Cream Enriched with Functional Compounds

(1) Background: Cosmeceuticals are topical products applied to human skin to prevent skin ageing and maintain a healthy skin appearance. Their effectiveness is closely linked to the compounds present in a final formulation. In this article, we propose a panel of in vitro tests to support the efficacy assessment of an anti-ageing cream enriched with functional compounds. (2) Methods: biocompatibility and the irritant effect were evaluated on reconstructed human epidermis (RHE) and corneal epithelium (HCE) 3D models. After a preliminary MTT assay, normal human dermal fibroblasts (NHDF) and keratinocytes (HaCaT) were used to evaluate the extracellular matrix (ECM) protein synthesis, and interleukin-6 (IL-6) and metalloproteinase-1 (MMP-1) production. (3) Results: data collected showed good biocompatibility and demonstrated the absence of the irritant effect in both 3D models. Therefore, we demonstrated a statistical increase in collagen and elastin productions in NHDF cells. In HaCaT cells, we highlighted an anti-inflammatory effect through a reduction in IL-6 levels in inflammatory stimulated conditions. Moreover, the reduction of MMP-1 production after UV-B radiation was demonstrated, showing significant photo-protection. (4) Conclusion: a multiple in vitro assays approach is proposed for the valid and practical assessment of the anti-ageing protection, anti-inflammatory and biocompatible claims that can be assigned to a cosmetic product containing functional compounds.     

Modification of Branched Poly(ethylene imine) with d-Fructose for Selective Delivery of siRNA into Human Breast Cancer Cells

Branched poly(ethylene imine) (bPEI) is frequently used in RNA interference (RNAi) experiments as a cationic polymer for the delivery of small interfering RNA (siRNA) because of its ability to form stable polyplexes that facilitate siRNA uptake. However, the use of bPEI in gene delivery is limited by its cytotoxicity and a need for target specificity. In this work, bPEI is modified with d- fructose to improve biocompatibility and target breast cancer cells through the overexpressed GLUT5 transporter. Fructose-substituted bPEI (Fru−bPEI) is accessible in three steps starting from commercially available protected fructopyranosides and bPEI. Several polymers with varying molecular weights, degrees of substitution, and linker positions on d- fructose (C1 and C3) are synthesized and characterized with NMR spectroscopy, size exclusion chromatography, and elemental analysis. In vitro biological screenings show significantly reduced cytotoxicity of 10 kDa bPEI after fructose functionalization, specific uptake of siRNA polyplexes, and targeted knockdown of green fluorescent protein (GFP) in triple-negative breast cancer cells (MDA-MB-231) compared to noncancer cells (HEK293T).