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Development and in vitro evaluation of microparticles of fluoxetine in galactomannan against biofilms of S. aureus methicilin resistant
Carbohydrate Polymers ( IF 10.7 ) Pub Date : 2020-10-05 , DOI: 10.1016/j.carbpol.2020.117184
Maria Aparecida Alexandre Josino , Cecília Rocha da Silva , João Batista de Andrade Neto , Fátima Daiana Dias Barroso , Lisandra Juvêncio da Silva , Bruno Coêlho Cavalcanti , Manoel Odorico de Moraes , Débora Hellen Almeida Brito , Nágila Maria Pontes Silva Ricardo , Hélio Vitoriano Nobre Júnior

The emergence of multidrug-resistant (MDR) bacteria is a global problem, by reducing the effectiveness of traditional antibiotics and decreasing the therapeutic arsenal to treat bacterial infections. This has led to an increase in researches about how to overcome this resistance to antibiotics. One strategy is the repositioning (or repurposing) of existing drugs not previously used to combat microorganisms, rather than the development of new drugs. Fluoxetine (FLX) is a selective serotonin reuptake inhibitor (SSRIs) and is considered one of the first highly selective antidepressants of the monoamine neurotransmitter serotonin (5-HT). The objective of this study is to prepare and physically characterize fluoxetine microparticles with galactomannan and evaluate their efficacy against strains of Staphylococcus aureus sensitive and resistant to methicillin. The microparticles were analyzed by differential scanning calorimetry (DSC), infrared analysis (IR) and X-ray diffraction (XRD). In addition, the percentage of encapsulation efficiency (EE%) and drug release kinetics were determined in vitro, along with the determination of the minimum inhibitory concentration (MIC) and evaluation of the action against biofilms. Physical tests were conducted to characterize galactomannan (GAL), FLX, oxacillin (OXA) and the galactomannan/fluoxetine microparticles (GFM). The EE% value was 98 % and, in regard the release, tests with the microparticles released about 60 % of the drug in 200 min. The isolated MIC results for FLX (255 μg/mL) and OXA MIC (1.97–15.62 μg/mL) showed that the strains were resistant. Furthermore, in the biofilms, microparticles showed statically significant improvement for all concentrations used. The study revealed that fluoxetine encapsulated in microparticles has the potential to act as an effective antimicrobial agent.



中文翻译:

半乳甘露聚糖中氟西汀微粒对金黄色葡萄球菌耐甲氧西林的生物膜的开发和体外评价

通过降低传统抗生素的有效性并减少用于治疗细菌感染的治疗性武器库,多重耐药性(MDR)细菌的出现是一个全球性问题。这导致了关于如何克服这种对抗生素抗性的研究的增加。一种策略是重新定位(或重新定位)以前未用于对抗微生物的现有药物,而不是开发新药物。氟西汀(FLX)是选择性5-羟色胺再摄取抑制剂(SSRIs),被认为是单胺神经递质5-羟色胺(5-HT)的首批高度选择性抗抑郁药之一。这项研究的目的是用半乳甘露聚糖制备氟西汀微粒并对其进行物理表征,并评估其对金黄色葡萄球菌菌株的功效。对甲氧西林敏感和耐药。通过差示扫描量热法(DSC),红外分析(IR)和X射线衍射(XRD)分析微粒。另外,在体外测定包封率(EE%)和药物释放动力学的百分比,以及最小抑菌浓度(MIC)的确定和对生物膜的作用评估。进行了物理测试以表征半乳甘露聚糖(GAL),FLX,奥沙西林(OXA)和半乳甘露聚糖/氟西汀微粒(GFM)。EE%值为98%,就释放而言,用微粒进行的测试在200分钟内释放了约60%的药物。FLX(255μg/ mL)和OXA MIC(1.97–15.62μg/ mL)的分离MIC结果表明,该菌株具有耐药性。此外,在生物膜中,对于所有使用的浓度,微粒都显示出明显的静态改善。该研究表明,包裹在微粒中的氟西汀具有充当有效抗菌剂的潜力。

更新日期:2020-10-16
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