RESUMO

In this study, films of chitosan and 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile (6CN), a 2-aminothiophene derivative with great pharmacological potential, were prepared as a system for a topical formulation. 6CN-chitosan films were characterized by physicochemical analyses, such as Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (XRD), and scanning electronic microscopy (SEM). Additionally, the antifungal potential of the films was evaluated in vitro against three species of Candida (C. albicans, C. tropicalis, and C. parapsilosis). The results of the FTIR and thermal analysis showed the incorporation of 6CN in the polymer matrix. In the diffractogram, the 6CN-chitosan films exhibited diffraction halos that were characteristic of amorphous structures, while the micrographs showed that 6CN particles were dispersed in the chitosan matrix, exhibiting pores and cracks on the film surface. In addition, the results of antifungal investigation demonstrated that 6CN-chitosan films were effective against Candida species showing potential for application as a new antifungal drug.

Assuntos

Antifúngicos , Candida , Quitosana , Tiofenos , Administração Tópica , Antifúngicos/administração & dosagem , Antifúngicos/química , Antifúngicos/farmacologia , Candida/efeitos dos fármacos , Quitosana/química , Portadores de Fármacos/química , Tiofenos/química

RESUMO

Industrial application of lycopene is limited due to its chemical instability and low bioavailability. This study proposes the development of fucan-coated acetylated cashew gum nanoparticles (NFGa) and acetylated cashew gum nanoparticles (NGa) for incorporation of the lycopene-rich extract from red guava (LEG). Size, polydispersity, zeta potential, nanoparticles concentration, encapsulation efficiency, transmission electron microscopy (TEM) and atomic force microscopy (AFM) were used to characterize nanoparticles. The antioxidant activity was determinated and cell viability was evaluated in the human breast cancer cells (MCF-7) and human keratinocytes (HaCaT) by MTT assay. The toxic effect was evaluated by hemolysis test and by Galleria mellonella model. NFGa showed higher stability than NGa, having a size of 162.10 ± 3.21 nm, polydispersity of 0.348 ± 0.019, zeta potential -30.70 ± 0.53 mV, concentration of 6.4 × 109 nanoparticles/mL and 60% LEG encapsulation. Microscopic analysis revealed a spherical and smooth shape of NFGa. NFGa showed antioxidant capacity by ABTS method and ORAC assay. The NFGa presented significant cytotoxicity against MCF-7 from the lowest concentration tested (6.25-200 µg/mL) and did not affect the cell viability of the HaCaT. NFGa showed non-toxic effect in the in vitro and in vivo models. Therefore, NFGa may have a promising application in LEG stabilization for antioxidant and antitumor purposes.

Assuntos

Anacardium/química , Antineoplásicos/administração & dosagem , Antioxidantes/administração & dosagem , Licopeno/administração & dosagem , Nanopartículas/química , Gomas Vegetais/química , Animais , Antineoplásicos/química , Antineoplásicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Células HaCaT , Humanos , Licopeno/química , Licopeno/farmacologia , Células MCF-7 , Polissacarídeos/química , Psidium/química , Ovinos

RESUMO

In the present work, we investigated the minimal inhibitory concentration (MIC) against fungal strains (Fonsecaea pedrosoi, Microsporum canis, Candida albicans, Cryptococcus neoformans), and cytotoxicity to normal cell lines for modified red angico gum (AG) with eterifying agent N-chloride (3-chloro-2-hydroxypropyl) trimethylammonium (CHPTAC). Quaternized ammonium groups were linked to AG backbone using N-(3-chloro-2-hydroxypropyl) trimethylammonium chloride. The chemical features of the quaternized gum derivatives (QAG) were analyzed by: FTIR, elemental analysis, Zeta potential and gel permeation chromatography. The angico quaternizated gum presented a degree of substitution (DS) of 0.22 and Zeta potential of +36.43. For the antifungal test, it was observed that unmodified gum did not inhibit fungal growth. While, QAG inhibited the growth of most fungi used in this study. By AFM technique QAG interacted with the fungal surface, altering wall roughness significantly. The probable affinity of fragments of the QAG structure for the fungal enzyme 5I33 (Adenylosuccinate synthetase) has been shown by molecular docking. Low cytotoxicity was observed for polymers (unmodified gum and QAG). The results demonstrate that the quaternized polymer of AG presented in this study is a quite promising biomaterial for biotechnological applications.

Assuntos

Antifúngicos , Citotoxinas , Inibidores Enzimáticos , Fabaceae/química , Proteínas Fúngicas , Fungos/enzimologia , Simulação de Acoplamento Molecular , Polissacarídeos , Animais , Antifúngicos/química , Antifúngicos/farmacologia , Citotoxinas/química , Citotoxinas/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Proteínas Fúngicas/antagonistas & inibidores , Proteínas Fúngicas/química , Células HEK293 , Humanos , Ligases/antagonistas & inibidores , Ligases/química , Camundongos , Polissacarídeos/química , Polissacarídeos/farmacologia

RESUMO

OBJECTIVES: Tuberculosis (TB) remains a major public health problem, particularly in low and middle-income countries. The aim of this study is to consensualise improvement actions for the Tuberculosis Control Programme of the Pernambuco state (SPTC), Brazil. METHODS: Firstly, a preliminary workshop was conducted with experts (n = 8), including key stakeholders and health professionals, to select structure and process indicators pertaining to the tuberculosis control programme. Then, an e-Delphi was carried out with a purposive sample of 11 local TB experts. The first-round questionnaire was comprised of 19 open-ended questions on possible improvement actions, based on programme indicators obtained in the previous stage. In the second-round experts rated each action for relevance and feasibility, using a four-point scale. In the last round the participants rated the actions again, in the light of group's answers. We used published criteria to define consensus at the outset of the study. KEY FINDINGS: Eighty-nine improvement actions achieved a high degree of consensus in both feasibility and relevance in round three. Eighty-six actions were grouped under 19 structure and process indicators, while three were consideredcross-sectional in scope (i.e. related to more than one indicator). Ten out of the 86 actions obtained at least 70% of ratings on the highest score of the scale both for relevance and feasibility. These included: "Request and availability of sputum pots can be made by any health professional in the health unit". CONCLUSIONS: The wide array of actions obtained in this Delphi represent a resource from which local SPTC services can select the actions most suitable for each context. The ten most relevant and feasible actions represent a particularly useful starting point to streamline change and potentially improve programme indicators.