Browsing by Author "Salamanca, Constain H."
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Item Decrease of Antimicrobial Resistance through Polyelectrolyte-Coated Nanoliposomes Loaded with β-Lactam Drug(Pharmaceuticals, 2019) Arévalo, Lina M.; Yarce, Cristhian J.; Oñate-Garzón, José; Salamanca, Constain H.Currently, one of the greatest health challenges worldwide is the resistance to antibiotic drugs, which has led to the pursuit of new alternatives for the recovery of biological activity, where the use of different types of nano-systems has shown an interesting potential. In this study, we evaluated the antibiotic activity of a model drug (ampicillin) encapsulated within coated-nanoliposomes on strains of Staphylococcus aureus with different antibiotic-resistance degrees. Hence, liposomes were elaborated by the ethanol injection method and were coated with a cationic polymer (Eudragit E-100) through the layer-by-layer process. Liposome characterization, such as size, polydispersity, zeta potential, and encapsulation efficiency were determined using dynamic light scattering and ultrafiltration/centrifugation techniques. Although biological activity was evaluated using three ATCC strains of S. aureus corresponding to ATCC 25923 (sensitive), ATCC 29213 (resistant) and ATCC 43300 (very resistant). The results showed changes in size (from ~150 to 220 nm), polydispersity (from 0.20 to 0.45) and zeta potential (from −37 to +45 mV) for the coating process. In contrast, encapsulation efficiency of approximately 70% and an increase in antibiotic activity of 4 and 18 times more on those S. aureus-resistant strains have been observed.Item Decrease of antimicrobial resistance through polyelectrolyte-coated nanoliposomes loaded with β-lactam drug(MDPI AG, 2019-03-01) Arévalo, Lina M.; Yarce, Cristhian J.; Oñate-Garzón, José Fernando; Salamanca, Constain H.Currently, one of the greatest health challenges worldwide is the resistance to antibiotic drugs, which has led to the pursuit of new alternatives for the recovery of biological activity, where the use of different types of nano-systems has shown an interesting potential. In this study, we evaluated the antibiotic activity of a model drug (ampicillin) encapsulated within coated-nanoliposomes on strains of Staphylococcus aureus with different antibiotic-resistance degrees. Hence, liposomes were elaborated by the ethanol injection method and were coated with a cationic polymer (Eudragit E-100) through the layer-by-layer process. Liposome characterization, such as size, polydispersity, zeta potential, and encapsulation efficiency were determined using dynamic light scattering and ultrafiltration/centrifugation techniques. Although biological activity was evaluated using three ATCC strains of S. aureus corresponding to ATCC 25923 (sensitive), ATCC 29213 (resistant) and ATCC 43300 (very resistant). The results showed changes in size (from ~150 to 220 nm), polydispersity (from 0.20 to 0.45) and zeta potential (from −37 to +45 mV) for the coating process. In contrast, encapsulation efficiency of approximately 70% and an increase in antibiotic activity of 4 and 18 times more on those S. aureus-resistant strains have been observed. © 2018 by the authors. Licensee MDPI, Basel, Switzerland.Item Evaluation of the Antimicrobial Activity of Cationic Peptides Loaded in Surface-Modified Nanoliposomes against Foodborne Bacteria(International Journal Of Molecular Sciences, 2019) Cantor, Stefania; Vargas, Lina; Rojas A., Oscar E.; Yarce, Cristhian J.; Salamanca, Constain H.; Oñate-Garzón, JoseBacteria are a common group of foodborne pathogens presenting public health issues with a large economic burden for the food industry. Our work focused on a solution to this problem by evaluating antibiotic activity against two bacteria (Listeria monocytogenes and Escherichia coli) of relevance in the field of foodstuffs. We used two approaches: (i) structural modification of the antimicrobial peptides and (ii) nano-vehiculisation of the modified peptides into polymer-coated liposomes. To achieve this, two antimicrobial peptides, herein named ‘peptide +2′ and ‘peptide +5′ were synthesised using the solid phase method. The physicochemical characterisation of the peptides was carried out using measurements of surface tension and dynamic light scattering. Additionally, nanoliposomes were elaborated by the ethanol injection method and coated with a cationic polymer (Eudragit E-100) through the layer-by-layer process. Liposome characterisation, in terms of size, polydispersity and zeta potential, was undertaken using dynamic light scattering. The results show that the degree of hydrophilic modification in the peptide leads to different characteristics of amphipathicity and subsequently to different physicochemical behaviour. On the other hand, antibacterial activity against both bacteria was slightly altered after modifying peptide sequence. Nonetheless, after the encapsulation of the peptides into polymer-coated nano-liposomes, the antibacterial activity increased approximately 2000-fold against that of L. monocytogenes.Item Evaluation of the antimicrobial activity of cationic peptides loaded in surface-modified nanoliposomes against foodborne bacteria(MDPI AG, 2019-02-05) Cantor, Stefania; Vargas, Lina; Rojas, Oscar E.A.; Yarce, Cristhian J.; Salamanca, Constain H.; Oñate-Garzón, José FernandoBacteria are a common group of foodborne pathogens presenting public health issues with a large economic burden for the food industry. Our work focused on a solution to this problem by evaluating antibiotic activity against two bacteria (Listeria monocytogenes and Escherichia coli) of relevance in the field of foodstuffs. We used two approaches: (i) structural modification of the antimicrobial peptides and (ii) nano-vehiculisation of the modified peptides into polymer-coated liposomes. To achieve this, two antimicrobial peptides, herein named ‘peptide +2′ and ‘peptide +5′ were synthesised using the solid phase method. The physicochemical characterisation of the peptides was carried out using measurements of surface tension and dynamic light scattering. Additionally, nanoliposomes were elaborated by the ethanol injection method and coated with a cationic polymer (Eudragit E-100) through the layer-by-layer process. Liposome characterisation, in terms of size, polydispersity and zeta potential, was undertaken using dynamic light scattering. The results show that the degree of hydrophilic modification in the peptide leads to different characteristics of amphipathicity and subsequently to different physicochemical behaviour. On the other hand, antibacterial activity against both bacteria was slightly altered after modifying peptide sequence. Nonetheless, after the encapsulation of the peptides into polymer-coated nano-liposomes, the antibacterial activity increased approximately 2000-fold against that of L. monocytogenes. © 2019 by the authors. Licensee MDPI, Basel, Switzerland.Item Increases in hydrophilicity and charge on the polar face of alyteserin 1c helix change its selectivity towards gram-positive bacteria(MDPI AG, 2019-11-27) Liscano, Yamil; Salamanca, Constain H.; Vargas, Lina; Cantor, Stefania; Laverde Rojas, Valentina; Oñate Garzón, JoséRecently, resistance of pathogens towards conventional antibiotics has increased, representing a threat to public health globally. As part of the fight against this, studies on alternative antibiotics such as antimicrobial peptides have been performed, and it has been shown that their sequence and structure are closely related to their antimicrobial activity. Against this background, we here evaluated the antibacterial activity of two peptides developed by solid-phase synthesis, Alyteserin 1c (WT) and its mutant derivative (ΔM), which shows increased net charge and reduced hydrophobicity. These structural characteristics were modified as a result of amino acid substitutions on the polar face of the WT helix. The minimum inhibitory concentration (MIC) of both peptides was obtained in Gram-positive and Gram-negative bacteria. The results showed that the rational substitutions of the amino acids increased the activity in Gram-positive bacteria, especially against Staphylococcus aureus, for which the MIC was one-third of that for the WT analog. In contrast to the case for Gram-positive bacteria, these substitutions decreased activity against Gram-negative bacteria, especially in Escherichia coli, for which the MIC was eight-fold higher than that exhibited by the WT peptide. To understand this, models of the peptide behavior upon interacting with membranes of E. coli and S. aureus created using molecular dynamics were studied and it was determined that the helical stability of the peptide is indispensable for antimicrobial activity. The hydrogen bonds between the His20 of the peptides and the phospholipids of the membranes should modulate the selectivity associated with structural stability at the carboxy-terminal region of the peptides.Item Synthesis, characterisation and biological evaluation of ampicillin-chitosan-polyanion nanoparticles produced by ionic gelation and polyelectrolyte complexation assisted by high-intensity sonication(MDPI AG, 2019-10-21) Ciro, Yhors; Rojas, John; Oñate Garzon, Jose; Salamanca, Constain H.Recently, one of the promising strategies to fight sensitive and resistant bacteria, and decrease the morbidity and mortality rates due to non-nosocomial infections, is to use antibiotic-loaded nanoparticles. In this study, ampicillin-loaded chitosan–polyanion nanoparticles were produced through the techniques of ionic gelation and polyelectrolyte complexation assisted by high-intensity sonication, using several crosslinking agents, including phytic acid (non-polymeric polyanion), sodium and potassium salts of poly(maleic acid-alt-ethylene) and poly(maleic acid-alt-octadecene) (polymeric polyanions). These nanoparticles were analysed and characterised in terms of particle size, polydispersity index, zeta potential and encapsulation efficiency. The stability of these nanosystems was carried out at temperatures of 4 and 40 °C, and the antimicrobial effect was determined by the broth microdilution method using sensitive and resistant Staphylococcus aureus strains. The results reveal that most of the nanosystems have sizes <220 nm, positive zeta potential values and a monodisperse population, except for the nanoparticles crosslinked with PAM-18 polyanions. The nanometric systems exhibited adequate stability preventing aggregation and revealed a two-fold increase in antimicrobial activity when compared with free ampicillin. This study demonstrates the potential application of synthesised nanoparticles in the field of medicine, especially for treating infections caused by pathogenic S. aureus strains.