Antimicrobial Silver-Polyethyleneimine-Polylactic Acid Polymer Composite Film for Coating Methacrylate-Based Denture Surfaces

To prepare an antimicrobial polymer composite composed of silver- (Ag-) polyethyleneimine- (PEI-) polylactic acid (PLA) in chloroform, for coating the mucosal surfaces of methacrylate-based dentures as a prospective therapy for denture stomatitis. The water-insoluble, tightly bound, hard, micrometre-thin, and colourless film exerts its effects by direct contact with the pathogens and via the active constituents (Ag, PEI, and Ag-PEI) released slowly into the mucosa’s salivary layer. Silver and PEI were blended at 140°C, then bound to PLA. The Ag-PEI complex was characterised by dynamic light scattering and transmission electron microscopy, and the Ag-PEI-PLA composite was examined by atomic force microscopy and micro-computed tomography. The characteristic was measured by atomic force microscopy (AFM) and micro-computed tomography (micro-CT). The quantity of water-soluble Ag-PEI complex released from the composite film was measured with gravimetry. The cellular physiological effects were analysed by impedimetry and computer-based morphometry using human gingival epithelial cells. A real-time cell proliferation assay revealed moderate toxic effects of Ag-PEI on the epithelium. The viscous Ag-PEI-PLA solution produced could be applied as a thin film on methacrylate surfaces. Active antimicrobial components (Ag, PEI, and Ag-PEI) were released from the hard, tightly bound Ag-PEI-PLA coating. This study’s findings verified the applicability of the antimicrobial Ag-PEI-PLA composite for coating the inner surfaces of acrylate dentures. Owing to the well-known antimicrobial effects of silver and PEI and the supplementary effects of chloroform, this composite provides a new therapeutic method for denture stomatitis that can be easily performed by dentists

The use of Trojan-horse drug delivery system in managing periodontitis

ABSTRACT: The aim of this review is to evaluate the possibility of delivering a silver-acid complex via a Trojan-horse mechanism for managing periodontits. We theroised that the complex could be an effective treatment option for bacterial inflammatory processes in the oral cavity. Searches were conducted using MEDLINE, Embase, Web of Science Core Collection, and Google Scholar search engines. We also reviewed several reference lists of the included studies or relevant reviews identified by the search. By using Medical Subject Headings (MeSH) terminology, a comprehensive search was performed for the following keywords: silver, folic acid, periodontitis, macrophages, Trojan-horse mechanism, toxicity, and targeting. Using the keywords mentioned earlier, we selected 110 articles and after appropriate elimination the review was written based on 37 papers. Accordingly the we noted that silver isons were an effective approach to kill oral pathogens. Secondly the Trojan-horse mechanism. could be used by macrophages (as the Trojan horse) to deliver silver ions in large quantities to the inflammatory focus to kill the periodontopathogens. The Trojan-horse mechanism has never been described in the field of dentistry before. The proposed novel approach using the principle of Trojan Horse delivery of drugs/chemicals could be used to manage oral inflammatory conditions. This method can be used to supplement regular treatments

Suivi et évaluation de la Qualité de l'Air.

Additional file 2: Table S1. Holographic morphometry (simple parameters: area, thickness, volume) of A2058 melanoma cells treated with alizarin and purpurin. Table S2. Holographic morphometry (complex derived parameters: roughness, eccentricity, Hull convexity, irregularity) of A2058 melanoma cells treated with alizarin and purpurin. Table S3. Holographic morphometry (simple parameters: area, thickness, volume) of HT168-M1 melanoma cells treated with alizarin and purpurin. Table S4. Holographic morphometry (complex derived parameters: roughness, eccentricity, Hull convexity, irregularity) of HT168-M1 melanoma cells treated with alizarin and purpurin

Investigation of the Antitumor Effects of Tamoxifen and Its Ferrocene-Linked Derivatives on Pancreatic and Breast Cancer Cell Lines

Tamoxifen is a long-known anti-tumor drug, which is the gold standard therapy in estrogen receptor (ER) positive breast cancer patients. According to previous studies, the conjugation of the original tamoxifen molecule with different functional groups can significantly improve its antitumor effect. The purpose of this research was to uncover the molecular mechanisms behind the cytotoxicity of different ferrocene-linked tamoxifen derivates. Tamoxifen and its ferrocene-linked derivatives, T5 and T15 were tested in PANC1, MCF7, and MDA-MB-231 cells, where the incorporation of the ferrocene group improved the cytotoxicity on all cell lines. PANC1, MCF7, and MDA-MB-231 express ERα and GPER1 (G-protein coupled ER 1). However, ERβ is only expressed by MCF7 and MDA-MB-231 cells. Tamoxifen is a known agonist of GPER1, a receptor that can promote tumor progression. Analysis of the protein expression profile showed that while being cytotoxic, tamoxifen elevated the levels of different tumor growth-promoting factors (e.g., Bcl-XL, Survivin, EGFR, Cathepsins, chemokines). On the other hand, the ferrocene-linked derivates were able to lower these proteins. Further analysis showed that the ferrocene-linked derivatives significantly elevated the cellular oxidative stress compared to tamoxifen treatment. In conclusion, we were able to find two molecules possessing better cytotoxicity compared to their unmodified parent molecule while also being able to counter the negative effects of the presence of the GPER1 through the ER-independent mechanism of oxidative stress induction

Novel Polycondensed Partly Saturated β-Carbolines Including Ferrocene Derivatives: Synthesis, DFT-Supported Structural Analysis, Mechanism of Some Diastereoselective Transformations and a Preliminary Study of their In Vitro Antiproliferative Effects

Use of a Pictet-Spengler reaction of tryptamine and l-tryptophan methyl ester and subsequent reduction of the nitro group followed by further cyclocondensation with aryl aldehydes and formyl–substituted carboxylic acids, including ferrocene-based components, furnished a series of diastereomeric 6-aryl-substituted 5,6,8,9,14,14b-hexahydroindolo[2′,3′:3,4]pyrido[1-c]-quinazolines and 5,5b,17,18-tetrahydroindolo[2′,3′:3,4]pyrido[1,2-c]isoindolo[2,1-a]quinazolin-11-(15bH)-ones with the elements of central-, planar and conformational chirality. The relative configuration and the conformations of the novel polycyclic indole derivatives were determined by 1H- and 13C-NMR methods supplemented by comparative DFT analysis of the possible diastereomers. The structure of one of the pentacyclic methyl esters with defined absolute configuration “S” was also confirmed by single crystal X-ray diffraction measurement. Accounting for the characteristic substituent-dependent diastereoselective formation of the products multistep mechanisms were proposed on the basis of the results of DFT modeling. Preliminary in vitro cytotoxic assays of the products revealed moderate-to-significant antiproliferative effects against PANC-1-, COLO-205-, A-2058 and EBC-1 cell lines that proved to be highly dependent on the stereostructure and on the substitution pattern of the pending aryl substituent

Long-term shelf-life liposomes for delivery of prednisolone and budesonide

Liposomes are nanoscale drug delivery systems built up from lipid layers and are able to spontaneously self- assemble in an aqueous environment. Both hydrophilic and hydrophobic drugs can be delivered by liposomes and this kind of nanoformulation offers many advantages regarding biodistribution, drug absorption and controlled drug release. Corticosteroids as lipophilic molecules are able to integrate into the lipid bilayer. This novel approach can improve the efficacy of several anti-inflammatory, such as asthma therapy. Our aim was to create liposomes with long shelf-life, which can incorporate and release corticosteroids such as Prednisolone (Pred) and Budesonide (Bud) at the temperature of inflamed tissues. Two kinds of liposome samples were prepared from three different kinds of phospholipids to get unilamellar vesicles with 100 nm in diameter and characterize their physicochemical properties and effect on living cells. Their main phase transition tem- perature in the physiologically relevant temperature range was measured by differential scanning calorimetry. According to the size distributions determined by dynamic light scattering, all drug-containing liposomes were stable for 6 months. All of the liposome types have a slightly negative zeta potential value. The Fourier-transform infrared spectroscopy revealed no chemical interaction between the drug and lipid molecules. The entrapment efficacy was determined by size-exclusion gel chromatography combined with UV–VIS spectrophotometry and it was very high in both cases (between 70 and 87%). The drug leakage was 35–40% for Pred and 6–8% for Bud in the first 30 min. The effect of liposomal drugs on cell viability was measured on the EBC-1 human lung carcinoma cell line. Neither the free corticosteroids nor their liposomal form were toxic to the cells. The cellular inter- nalization of the liposomes was proved by flow cytometry and confocal microscopy. In summary, these liposomes could be useful in the delivery of corticosteroids (Pred or particularly Bud) in more effective asthma therapy, having fewer side effects due to the nanoformulation