RESUMO
Targeted nanocarriers could reach new levels of drug delivery, bringing new tools for personalized medicine. It is known that cancer cells overexpress folate receptors on the cell surface compared to healthy cells, which could be used to create new nanocarriers with specific targeting moiety. In addition, magnetic nanoparticles can be guided under the influence of an external magnetic field in different areas of the body, allowing their precise localization. The main purpose of this paper was to decorate the surface of magnetic nanoparticles with poly(2-hydroxyethyl methacrylate) (PHEMA) by surface-initiated atomic transfer radical polymerization (SI-ATRP) followed by covalent bonding of folic acid to side groups of the polymer to create a high specificity magnetic nanocarrier with increased internalization capacity in tumor cells. The biocompatibility of the nanocarriers was demonstrated by testing them on the NHDF cell line and folate-dependent internalization capacity was tested on three tumor cell lines: MCF-7, HeLa and HepG2. It has also been shown that a higher concentration of folic acid covalently bound to the polymer leads to a higher internalization in tumor cells compared to healthy cells. Last but not least, magnetic resonance imaging was used to highlight the magnetic properties of the functionalized nanoparticles obtained.
Assuntos
Ácido Fólico/química , Nanopartículas de Magnetita/química , Poli-Hidroxietil Metacrilato/química , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Células HeLa , Células Hep G2 , Humanos , Células MCF-7 , Tamanho da Partícula , PolimerizaçãoRESUMO
An important and well-designed solution to overcome some of the problems associated with new drugs is provided by the molecular encapsulation of the drugs in the cyclodextrins (CDs) cavity, yielding corresponding inclusion complexes (ICs). These types of non-covalent complexes are of current interest to the pharmaceutical industry, as they improve the solubility, stability and bioavailability of the guest molecules. This review highlights several methods for cyclodextrin ICs preparation and characterization, focusing mostly on the mass spectrometry (MS) studies that have been used for the detection of noncovalent interactions of CDs inclusion complexes and binding selectivity of guest molecules with CDs. Furthermore, the MS investigations of several ICs of the CD with antifungal, antioxidants or fluorescent dyes are presented in greater details, pointing out the difficulties overcome in the analysis of this type of compounds.
Assuntos
Química Farmacêutica/métodos , Ciclodextrinas/análise , Espectrometria de Massas , SolubilidadeRESUMO
This study aimed to develop polysaccharide-based emulsions incorporated with lavender essential oil and their application on cellulosic support for patches obtaining. The lavender essential oil has been added to emulsions as an active compound mainly due to its antimicrobial properties. In this study, emulsions were used to deliver active ingredients (lavender essential oil). The chemical composition of essential oil was analyzed using gas chromatography-mass spectrometry (GC/MS). A total of seven emulsions (RiACL) were evaluated by determining rheological parameters and microbiological analysis. One of the emulsions (R7ACL) was applied to cellulosic support to obtain non-irritating textiles with controlled release of the active compound and moisturizing effects. Obtained cellulosic support was analyzed in terms of active compound controlled release, toxicity and antimicrobial testing, and skin analysis in healthy volunteers. It was found that the cellulosic supports treated with O/W emulsions are non-irritating, have softness and moisturizing effects, and can be used safely in topical applications for patches obtaining.
Assuntos
Celulose/química , Lavandula/química , Óleos Voláteis/química , Pele/efeitos dos fármacos , Adolescente , Adulto , Idoso , Anti-Infecciosos/efeitos adversos , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Candida albicans/efeitos dos fármacos , Emulsões/efeitos adversos , Emulsões/química , Emulsões/farmacologia , Humanos , Pessoa de Meia-Idade , Staphylococcus aureus/efeitos dos fármacos , Têxteis/normasRESUMO
BACKGROUND: Alopecia areata (AA) is a T-cell-mediated autoimmune disease and affects up to 2% of the population. There is a need for a more profound and rigorous understanding of the structure and composition of human hair affected by AA in order to manage this disease. The aim of this article is to understand the effects of AA on the structure and composition of human hair. METHODS: Several physico-chemical investigation methods, such as Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM), Energy-Dispersive X-ray Spectroscopy (EDX), and microbeam Small Angle X-ray Scattering (SAXS), were used to analyze human hair samples obtained from healthy donors and patients with AA. RESULTS: SEM revealed more severe hair surface defects for the white regrown hair (W-AA) samples. TEM showed the presence of air-like vesicles located in the endocuticle of regrown hair. Analysis of ultrathin sections of W-AA showed the existence of empty vesicles and smaller melanin granules compared to control samples. SAXS demonstrated that unaffected hair of patients with AA (B-AA) and W-AA melanin aggregates are different in their sizes and shapes compared to the control samples. EDX data showed that W-AA elemental composition was significantly different from the other sample groups. Our study showcases promising non-invasive techniques for a better and more accurate understanding of changes in the internal structure and composition of hair affected by AA.
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A novel DPyDB-C[double bond, length as m-dash]N-18C6 compound was synthesised by linking a pyrene moiety to each phenyl group of dibenzo-18-crown-6-ether, the crown ether, through -HC[double bond, length as m-dash]N- bonds and characterized by FTIR, 1H-NMR, 13C-NMR, TGA, and DSC techniques. The quantitative 13C-NMR analysis revealed the presence of two position isomers. The electronic structure of the DPyDB-C[double bond, length as m-dash]N-18C6 molecule was characterized by UV-vis and fluorescence spectroscopies in four solvents with different polarities to observe particular behavior of isomers, as well as to demonstrate a possible non-bonding chemical association (such as ground- and excited-state associations, namely, to probe if there were forming dimers/excimers). The interpretation of the electronic structure was realized through QM calculations. The TD-CAM-B3LYP functional, at the 6-311+G(d,p) basis set, indicated the presence of predominant π â π* and mixed π â π* + n â π* transitions, in line with the UV-vis experimental data. Even though DPyDB-C[double bond, length as m-dash]N-18C6 computational studies revealed a π-extended conjugation effect with predominantly π â π* transitions, thorough fluorescence analysis was observed a weak emission, as an effect of PET and ACQ. In particular, the WAXD analysis of powder and thin films obtained from n-hexane, 1,2-dichloroethane, and ethanol indicated an amorphous organization, whereas from toluene a smectic ordering was obtained. These results were correlated with MD simulation, and it was observed that the molecular geometry of DPyDB-C[double bond, length as m-dash]N-18C6 molecule played a defining role in the pyrene stacking arrangement.
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In the present study, the antitumoral potential of three gel formulations loaded with carbon dots prepared from N-hydroxyphthalimide (CD-NHF) was examined and the influence of the gels on two types of skin melanoma cell lines and two types of breast cancer cell lines in 2D (cultured cells in normal plastic plates) and 3D (Matrigel) models was investigated. Antitumoral gels based on sodium alginate (AS), carboxymethyl cellulose (CMC), and the carbomer Ultrez 10 (CARB) loaded with CD-NHF were developed according to an adapted method reported by Hellerbach. Viscoelastic properties of CD-NHF-loaded gels were analyzed by rheological analysis. Also, for both CD-NHF and CD-NHF-loaded gels, the fluorescence properties were analyzed. Cell proliferation, apoptosis, and mitochondrial activity were analyzed according to basic methods used to evaluate modulatory activities of putative anticancer agents, which include reference cancer cell line culture assays in both classic 2D and 3D cultures. Using the rheological measurements, the mechanical properties of gel formulations were analyzed; all samples presented gel-like rheological characteristics. The presence of CD-NHF within the gels induces a slight decrease of the dynamic moduli, indicating a flexible gel structure. The fluorescence investigations showed that for the gel-loaded CD-NHF, the most intense emission peak was located at 370 nm (upon excitation at 330 nm). 3D cell cultures displayed visibly larger structure of tumor cells with less active phenotype appearance. The in vitro results for tested CD-NHF-loaded gel formulations revealed that the new composites are able to affect the number, size, and cellular organization of spheroids and impact individual tumor cell ability to proliferate and aggregate in spheroids.
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Thin polymer films that prevent the adhesion of bacteria are of interest as coatings for the development of infection-resistant biomaterials. This study investigates the influence of grafting density and film thickness on the adhesion of Staphylococcus epidermidis to poly(poly(ethylene glycol)methacrylate) (PPEGMA) and poly(2-hydroxyethyl methacrylate) (PHEMA) brushes prepared via surface-initiated atom transfer radical polymerization (SI-ATRP). These brushes are compared with poly(ethylene glycol) (PEG) brushes, which are obtained by grafting PEG onto an epoxide-modified substrate. Except for very low grafting densities (ρ = 1%), crystal violet staining experiments show that the PHEMA and PPEGMA brushes are equally effective as the PEG-modified surfaces in preventing S. epidermis adhesion and do not reveal any significant variations as a function of film thickness or grafting density. These results indicate that brushes generated by SI-ATRP are an attractive alternative to grafted-onto PEG films for the preparation of surface coatings that resist bacterial adhesion.