RESUMO
BACKGROUND: The need for therapeutically effective anticancer drug delivery systems constantly persuades researchers to explore novel strategies. OBJECTIVE: In this study a novel cubane based antibacterial nanocomposite was tailored as dual chemotherapy drug delivery vesicle in order to increase the therapeutic outcome in cancer therapy. METHOD: The physico-chemical characterization of engineered nanocarrier was assessed by Fourier transforms infrared spectroscopy (FTIR), Hydrogen nuclear magnetic resonance spectroscopy (1H NMR), Thermogravimetric analysis (TGA), and Field emission scanning electron microscopy-energy dispersive using X-ray (FESEMEDX). The antibacterial activity of novel developed nanocomposite was tested by determining minimum inhibitory concentration (MIC) values against Pseudomonas aeruginosa, Escherichia Coli and Candida albicans. RESULTS: In order to investigate the efficacy of novel engineered nanocomposite (with average particle size of 50 nm) as dual anticancer drug delivery, DOX and MTX were bind to nanocarrier with encapsulation efficiency and loading content of around 97.3 ± 2.7% and 20.8 ± 1.6 %, respectively. Dual drugs released simultaneously with distinct tumor targeted, pH responsive sustained release manner. Moreover, the probable antitumoral activity of this engineered nanocomposite system against MCF7 cell lines was evaluated by MTT assay and cell cycle studies. The outcomes showed that novel engineered nanocomposite had no cytotoxic effects, while DOX@MTX-loaded nanocomposite possessed higher growth inhibition property and higher S-phase arrest as compared to cells treated with DOX@MTX alone. CONCLUSION: It was concluded that this novel cubane based drug delivery vehicle could process antibacterial and anticancer therapeutics spontaneously, representing promising tumor targeted system in nanomedicine.
Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Doxorrubicina/farmacologia , Metotrexato/farmacologia , Nanocompostos/química , Antibacterianos/síntese química , Antibacterianos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Candida albicans/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Doxorrubicina/química , Ensaios de Seleção de Medicamentos Antitumorais , Escherichia coli/efeitos dos fármacos , Humanos , Células MCF-7 , Metotrexato/química , Estrutura Molecular , Pseudomonas aeruginosa/efeitos dos fármacos , Relação Estrutura-Atividade , Células Tumorais CultivadasRESUMO
The goal of oral insulin delivery devices is to protect the sensitive drug from proteolytic degradation in the stomach and upper portion of the small intestine. Copolymers of 2-hydroxyethyl methacrylate (HEMA) and methacrylic acid (MAA) based hydrogels containing 2, 4, and 6% of a crosslinking agent (CA) were studied as drug delivery systems. Cubane-1, 4-dicarboxylic acid (CDA) was linked to two HEMA groups as CA. Radical copolymerizations of HEMA and MAA with the various ratios of CA were performed at 70 degrees C. The compositions of the crosslinked three-dimensional polymers were determined using Fourier transform infrared spectroscopy. Glass-transition temperature of the network polymers was determined calorimetrically. The effect of copolymer composition on the swelling behavior and hydrolytic degradation was studied in simulated gastric fluid (pH 1) and simulated intestinal fluid (pH 7.4). The swelling and hydrolytic behavior of the copolymers was dependent on the content of MAA groups and caused a decrease in gel swelling in simulated gastric fluid or an increase in gel swelling in simulated intestinal fluid. The drug-release profiles indicate that the amount of drug release depends on their degree of swelling and crosslinking.