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1.
Pharmaceutics ; 16(4)2024 Apr 17.
Artículo en Inglés | MEDLINE | ID: mdl-38675211

RESUMEN

In recent years, increasing interest has been accorded to polyester-based polymer microstructures, driven by their promising potential as advanced drug delivery systems. This study presents the preparation and characterization of new polymeric microparticles based on poly(ethylene brassylate-co-squaric acid) loaded with norfloxacin, a broad-spectrum antibiotic. Polymacrolactone was synthesised in mild conditions through the emulsion polymerization of bio-based and renewable monomers, ethylene brassylate, and squaric acid. The microparticles were obtained using the precipitation technique and subsequently subjected to comprehensive characterization. The impact of the copolymer/drug ratio on various properties of the new system was systematically evaluated, confirming the structure of the copolymer and the encapsulation of norfloxacin. The microspheres are approximately spherical and predominantly homogeneously distributed. The average hydrodynamic diameter of the microparticles falls between 400 and 2000 nm, a decrease that is observed with the increase in norfloxacin content. All samples showed good encapsulation efficiency and drug loading capacity, with the highest values obtained for microparticles synthesised using an equal ratio of copolymer and drug. In vitro drug release results disclose that norfloxacin molecules are released in a sustained biphasic manner for up to 24 h. Antimicrobial activity was also studied, with samples showing very good activity against E. coli and moderate activity against S. aureus and E. faecalis. In addition, HDFA human fibroblast cell cultures demonstrated the cytocompatibility of the microparticles.

2.
Int J Biol Macromol ; 262(Pt 1): 130034, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38340942

RESUMEN

The multiple uses of cellulose nanofibrils (CNFs) originate from their availability from renewable resources, and are due to their physico-chemical properties, biodegradability and biocompatibility. At the same time, reducing sensitivity to humidity, increasing interfacial adhesion and hydrophobic modification of the CNF surface to diversify applications and improve operation, are current targets pursued. This study focuses on the preparation of a novel gel structure using cellulose nanofibrils (CNFs) and poly(ethylene brassylate-co-squaric acid) (PEBSA50/50), a bio-based copolymacrolactone. The primary goal is to achieve the gel with reduced sensitivity to humidity and enhanced hydrophobic behaviour. The new system was characterized in comparison to its constituent components using various techniques, such as Fourier transform infrared spectroscopy, thermal analysis, X-ray diffraction, and NIR - chemical imaging. Rheological tests demonstrated the formation of the CNF_PEBSA50/50 gel as a result of physical interactions between the two polymeric partners and revealed self-healing abilities for the prepared gels. Determination of the contact angle, surface free energy, as well as dynamic measurements of the vapour sorption of the CNF_PEBSA50/50 system, confirmed the achievement of the study's aim. Furthermore, the CNF_PEBSA50/50 network was utilized to encapsulate citric acid, resulting in the creation of a new bioactive composite with both antioxidant and antimicrobial activity.


Asunto(s)
Celulosa , Nanofibras , Celulosa/química , Antioxidantes/farmacología , Polímeros , Interacciones Hidrofóbicas e Hidrofílicas , Nanofibras/química
3.
Pharmaceutics ; 15(12)2023 Dec 05.
Artículo en Inglés | MEDLINE | ID: mdl-38140071

RESUMEN

In light of the increasing resistance of pathogenic microorganisms to the action of antibiotics, essential oils extracted from plants with therapeutic activity provide a significant alternative to obtaining dressings for the treatment of skin wounds. The encapsulation of essential oils in an amphiphilic gel network allows better dispersion and preservation of hydrophobic bioactive substances while promoting their prolonged release. In this study, we focused on the development of a poly (vinyl alcohol) (PVA)/poly (ethylene brassylate-co-squaric acid) (PEBSA) platform embedded with thymol (Thy), and α-tocopherol (α-Tcp) as a co-drug structure with prospective use for the treatment and healing of skin wounds. The new complex bioactive system was prepared through repeated freeze-thaw processes. The influence of the composition on surface topography, hydrophilic/hydrophobic character, and in vitro interaction with simulated body fluids was evidenced. BALB/3T3 fibroblast cell culture demonstrated the cryogel scaffolds' cytocompatibility. Tests on Wistar rats confirmed their biocompatibility, integration with host tissue, and the absence of inflammatory processes. The bioactive compound significantly enhanced the healing process of full-thickness excision wounds in a rat model. Further investigations on in vivo infection models would assess the potential of the PVA/PEBSA platform with dual bioactive activity for clinical antimicrobial and wound healing therapy.

4.
Pharmaceutics ; 15(11)2023 Nov 09.
Artículo en Inglés | MEDLINE | ID: mdl-38004586

RESUMEN

Owing to its antibacterial, anti-inflammatory, and antioxidant activities, in the last few years, lavender essential oil (LVO) has been used in medical applications as a promising approach for treating infected wounds. However, the practical applicability of LVO is limited by its high volatility and storage stability. This study aimed to develop a novel hybrid hydrogel by combining phytic acid (PA)-crosslinked sodium alginate (SA) and poly(itaconic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro[5.5] undecane (PITAU) and evaluate its potential effectiveness as an antibacterial wound dressing after incorporating LVO. The influence of the mass ratio between SA and PITAU on the properties and stability of hydrogels was investigated. After LVO loading, the effect of oil addition to hydrogels on their functional properties and associated structural changes was studied. FTIR analysis revealed that hydrogen bonding is the primary interaction mechanism between components in the hybrid hydrogels. The morphology was analyzed using SEM, evidencing a porosity dependent on the ratio between SA and PITAU, while LVO droplets were well dispersed in the polymer blend. The release of LVO from the hydrogels was determined using UV-VIS spectroscopy, indicating a sustained release over time, independent of the LVO concentration. In addition, the hybrid hydrogels were tested for their antioxidant properties and antimicrobial activity against Gram-positive and Gram-negative bacteria. Very good antimicrobial activity was obtained in the case of sample SA_PITAU3+LVO10% against S. aureus and C. albicans. Moreover, in vivo tests showed an increased antioxidant effect of the SA_PITAU3+LVO10% hydrogel compared to the oil-free scaffold that may aid in accelerating the healing process of wounds.

5.
Gels ; 9(3)2023 Feb 22.
Artículo en Inglés | MEDLINE | ID: mdl-36975622

RESUMEN

The inability to meet and ensure as many requirements as possible is fully justified by the continuous interest in obtaining new multifunctional materials. A new cryogel system based on poly(vinyl alcohol) (PVA) and poly(ethylene brassylate-co-squaric acid) (PEBSA) obtained by repeated freeze-thaw processes was previously reported and used for the incorporation of an antibacterial essential oil-namely, thymol (Thy). Furthermore, the present study aims to confer antioxidant properties to the PVA/PEBSA_Thy system by encapsulating α-tocopherol (α-Tcp), targeting a double therapeutic effect due to the presence of both bioactive compounds. The amphiphilic nature of the PEBSA copolymer allowed for the encapsulation of both Thy and α-Tcp, via an in situ entrapment method. The new PVA/PEBSA_Thy_α-Tcp systems were characterized in terms of their influence on the composition, network morphology and release profiles, as well as their antimicrobial and antioxidant properties. The study underlined the cumulative antioxidant efficiency of Thy and α-Tcp, which in combination with the PEBSA copolymer have a synergistic effect (97.1%). We believe that the convenient and simple strategy offered in this study increases applicability for these new PVA/PEBSA_Thy_α-Tcp cryogel systems.

6.
Polymers (Basel) ; 15(3)2023 Jan 26.
Artículo en Inglés | MEDLINE | ID: mdl-36771937

RESUMEN

Double network (DN) hydrogels composed of self-assembling low-molecular-weight gelators and a hybrid polymer network are of particular interest for many emerging biomedical applications, such as tissue regeneration and drug delivery. The major benefits of these structures are their distinct mechanical properties as well as their ability to mimic the hierarchical features of the extracellular matrix. Herein, we describe a hybrid synthetic/natural polymer gel that acts as the initial network based on sodium alginate and a copolymer, namely poly(itaconic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro (5,5) undecane). The addition of amino acids and peptide-derived hydrogelators, such as Fmoc-Lys-Fmoc-OH and Fmoc-Gly-Gly-Gly-OH, to the already-made network gives rise to DNs crosslinked via non-covalent interactions. Fourier transform infrared spectroscopy (FTIR) and thermal analysis confirmed the formation of the DN and highlighted the interactions between the two component networks. Swelling studies revealed that the materials have an excellent water absorption capacity and can be classified as superabsorbent gels. The rheological properties were systematically investigated in response to different variables and showed that the prepared materials present injectability and a self-healing ability. SEM analysis revealed a morphology consisting of a highly porous and interconnected fibrous network. Finally, the biocompatibility was evaluated using the MTT assay on dermal fibroblasts, and the results indicated that the new structures are non-toxic and potentially useful for biomedical applications.

7.
Polymers (Basel) ; 15(3)2023 Feb 03.
Artículo en Inglés | MEDLINE | ID: mdl-36772082

RESUMEN

Development of natural protein-based hydrogels with self-healing performance and tunable physical properties has attracted increased attention owing to their wide potential not only in the pharmaceutical field, but also in wounds management. This work reports the development of a versatile hydrogel based on enzymatically-crosslinked gelatin and nanogels loaded with amoxicillin (Amox), an antibiotic used in wound infections. The transglutaminase (TGase)-crosslinked hydrogels and encapsulating nanogels were formed rapidly through enzymatic crosslinking and self-assembly interactions in mild conditions. The nanogels formed through the self-assemble of maleoyl-chitosan (MAC5) and polyaspartic acid (PAS) may have positive influence on the self-healing capacity and drug distribution within the hydrogel network through the interactions established between gelatin and gel-like nanocarriers. The physicochemical properties of the enzymatically-crosslinked hydrogels, such as internal structure, swelling and degradation behavior, were studied. In addition, the Amox release studies indicated a rapid release when the pH of the medium decreased, which represents a favorable characteristic for use in the healing of infected wounds. It was further observed through the in vitro and in vivo biocompatibility assays that the optimized scaffolds have great potential to be used as wound dressings.

8.
Antioxidants (Basel) ; 11(12)2022 Dec 15.
Artículo en Inglés | MEDLINE | ID: mdl-36552679

RESUMEN

The study presents the achievement of a new assembly with antioxidant behaviour based on a copolymacrolactone structure that encapsulates erythritol (Eryt). Poly(ethylene brassylate-co-squaric acid) (PEBSA) was synthesised in environmentally friendly conditions, respectively, through a process in suspension in water by opening the cycle of ethylene brassylate macrolactone, followed by condensation with squaric acid. The compound synthesised in suspension was characterised by comparison with the polymer obtained by polymerisation in solution. The investigations revealed that, with the exception of the molecular masses, the compounds generated by the two synthetic procedures present similar properties, including good thermal stability, with a Tpeak of 456 °C, and the capacity for network formation. In addition, the investigation by dynamic light scattering techniques evidenced a mean diameter for PEBSA particles of around 596 nm and a zeta potential of -25 mV, which attests to their stability. The bio-based copolymacrolactone was used as a matrix for erythritol encapsulation. The new PEBSA-Eryt compound presented an increased sorption/desorption process, compared with the PEBSA matrix, and a crystalline morphology confirmed by X-ray diffraction analysis. The bioactive compound was also characterised in terms of its biocompatibility and antioxidant behaviour.

9.
Gels ; 8(10)2022 Oct 12.
Artículo en Inglés | MEDLINE | ID: mdl-36286150

RESUMEN

Hydrogels based on natural, biodegradable materials have gained considerable interest in the medical field due to their improved drug delivery profiles and tissue-mimicking architecture. In this regard, this study was devoted to the preparation and characterization of new physically crosslinked hydrogels based on carboxymethyl cellulose and an unconventional crosslinking agent, phytic acid. Phytic acid, in addition to its antioxidant and antibacterial effects, can improve the biological properties and stability of gels, without adding toxicity. Fourier transform infrared (FTIR) spectroscopy, rheological studies and thermal analysis confirmed the hydrogel formation. The influence of the ratio between the cellulose derivative and the crosslinker upon the morphological structure and water uptake was evidenced by scanning electron microscopy (SEM) and swelling measurements in simulated body fluids. Furthermore, procaine was entrapped within the hydrogels and used as a model drug for in vitro studies, which highlighted the dependence of the drug release on the phytic acid content of the matrix. The materials demonstrated antibacterial effects against Escherichia coli and Staphylococcus aureus bacteria. The biocompatibility was assessed on fibroblast cells, and according to our results, hydrogels can improve cell viability highlighting the potential of these systems as therapeutic scaffolds for skin tissue engineering.

10.
Biomed Pharmacother ; 149: 112919, 2022 May.
Artículo en Inglés | MEDLINE | ID: mdl-36068778

RESUMEN

The study presents the development of a new copolymacrolactone structure based on ethylene brassylate (EB) and squaric acid (SA) with different ratios between comonomers. The new system was tested as a network for essential oils encapsulation. The structure of the copolymers was confirmed by spectroscopic investigations and correlated in interdependence with the comonomers content. The interfacial characteristics of the poly(ethylene brassylate-co-squaric acid) copolymers were determined, and the transition from a moderate hydrophilic surface towards a hydrophobic region by increasing the molar content of SA comonomer was highlighted. The affinity for hydrophobic substances of the synthesised macromolecular compounds was used in a process of encapsulation of thymol (Thy) and carvacrol (CC). The newly prepared bioactive compounds were characterised by in vivo biocompatibility tests, and antimicrobial activity, Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC).


Asunto(s)
Aceites Volátiles , Antibacterianos/farmacología , Pruebas de Sensibilidad Microbiana , Monoterpenos/farmacología , Aceites Volátiles/farmacología , Polímeros , Timol/farmacología
11.
Polymers (Basel) ; 14(16)2022 Aug 17.
Artículo en Inglés | MEDLINE | ID: mdl-36015611

RESUMEN

One of the methods of obtaining supramolecular gels consists of the possibility of self-assembly of low molecular weight gelators (LMWGs). However, LMWG-based gels are often difficult to handle, easy to destroy and have poor rheological performance. In order to improve the gels' properties, the LMWGs molecules are co-assembled, which induces more cross-links with more stable structures. Starting from these aspects, the present study refers to the preparation of a bionic hydrogel stabilized with a physiologically occurring, bifunctional biomolecule, L-lysine, co-assembled with other amino acids or peptides (such as a modified amino acid (Fmoc-serine or Fmoc-glutamic acid) or a tripeptide (Fmoc-Gly-Gly-Gly)) with the potential to support the repair of injuries or the age-related impaired structures or functions of living tissues. The introduction of a copartner aims to improve hydrogel characteristics from a morphological, rheological and structural point of view. On the other hand, the process will allow the understanding of the phenomenon of specific self-association and molecular recognition. Various characterization techniques were used to assess the ability to co-assemble: DLS, FT-IR, SEM and fluorescence microscopy, rheology and thermal analysis. Studies have confirmed that the supramolecular structure occurs through the formation of inter- and intramolecular physical bonds that ensure the formation of fibrils organized into 3D networks. The rheological data, namely the G' > G″ and tan δ approximately 0.1−0.2 gel-like behavior observed for all studied samples, demonstrate and sustain the appearance of the co-assembly processes and the ability of the samples to act as LMWG. From the studied systems, the Fmoc−Lys−Fmoc_ Fmoc−Glu sample presented the best rheological characteristics that are consistent with the observations that resulted from the dichroism, fluorescence and SEM investigations.

12.
Nanomaterials (Basel) ; 12(14)2022 Jul 14.
Artículo en Inglés | MEDLINE | ID: mdl-35889641

RESUMEN

Physical cryogels were obtained using the successive freeze-thaw technique of poly(vinyl alcohol) (PVA)/poly(ethylene brassylate-co-squaric acid) (PEBSA) solutions. The cryogel systems were prepared by using two different molecular weights of PVA and PEBSA with three different ratios between the ethylene brassylate (EB) and squaric acid (SA) comonomers. The presence of interactions, the thermal properties and the morphology were investigated using Fourier Transform Infrared Spectroscopy (FT-IR), thermogravimetry (TGA and DTG) and scanning electron microscopy (SEM), respectively. The influence of the composition on the degree of swelling in a physiological environment was demonstrated. The study highlighted improvements in terms of new network flexibility due to the intermolecular chains interactions brought by the introduction of PEBSA in the cryogel structure. We also concluded that the presence of PEBSA in the PVA/PEBSA cryogel network improved the loading capacity of the new system with specific hydrophobic agents, for example essential oils, which (due to their antimicrobial character) can lead to the use of new systems obtained for various applications.

13.
Nanomaterials (Basel) ; 12(14)2022 Jul 17.
Artículo en Inglés | MEDLINE | ID: mdl-35889669

RESUMEN

Squaric acid (SA) is a compound with potential to crosslink biomacromolecules. Although SA has become over the last years a well-known crosslinking agent as a result of its good biocompatibility, glutaraldehyde (GA), a compound with proven cytotoxicity is still one of the most used crosslinkers to develop nanomaterials. In this regard, the novelty of the present study consists in determining whether it may be possible to substitute GA with a new bifunctional and biocompatible compound, such as SA, in the process of enzyme immobilization on the surface of magnetic nanoparticles (MNPs). Thus, a direct comparison between SA- and GA-functionalized magnetic nanoparticles was realized in terms of physico-chemical properties and ability to immobilize catalytic enzymes. The optimal conditions of the synthesis of the two types of GOx-immobilized MNPs were described, thus emphasizing the difference between the two reagents. Scanning Electron Microscopy and Dynamic Light Scattering were used for size, shape and colloidal stability characterization of the pristine MNPs and of those coupled with GOx. Binding of GOx to MNPs by using GA or SA was confirmed by FT-IR spectroscopy. The stability of the immobilized and free enzyme was investigated by measuring the enzymatic activity. The study confirmed that the resulting activity of the immobilized enzyme and the optimization of enzyme immobilization depended on the type of reagent used and duration of the process. The catalytic performance of immobilized enzyme was tested, revealing that the long-term colloidal stability of SA-functionalized MNPs was superior to those prepared with GA. In conclusion, the SA-functionalized bioconjugates have a better potential as compared to the GA-modified nanosystems to be regarded as catalytic nanodevices for biomedical purposes such as biosensors.

14.
Gels ; 7(4)2021 Nov 27.
Artículo en Inglés | MEDLINE | ID: mdl-34940301

RESUMEN

This study reports a strategy for developing a biohybrid complex based on a natural/synthetic polymer conjugate as a gel-type structure. Coupling synthetic polymers with natural compounds represents an important approach to generating gels with superior properties and with potential for biomedical applications. The study presents the preparation of hybrid gels with tunable characteristics by using a spiroacetal polymer and alginate as co-partners in different ratios. The new network formation was tested, and the structure was confirmed by FTIR and SEM techniques. The physical properties of the new gels, namely their thermal stability and swelling behavior, were investigated. The study showed that the increase in alginate content caused a smooth increase in thermal stability due to the additional crosslinking bridges that appeared. Moreover, increasing the content of the synthetic polymer in the structure of the gel network ensures a slower release of carvacrol, the encapsulated bioactive compound.

15.
Int J Biol Macromol ; 189: 335-345, 2021 Oct 31.
Artículo en Inglés | MEDLINE | ID: mdl-34425119

RESUMEN

In the last decade, numerous innovative strategies have been used to obtain highly efficient synthetic or semi-synthetic biomaterials. Between these innovative biomaterials, hydrogels occupy a distinct place due to their superior biological and physico-chemical characteristics. Alginate is a natural linear polysaccharide with important physico-chemical and biological properties. Recently, we obtained a new hydrogel based on alginate and phytic acid with improved physico-chemical properties. In the present study, the hydrogels previously obtained were tested in terms of their biological properties and possibilities of use in the biomedical field. For this purpose, the hydrogels were loaded with norfloxacin (NRF), an antibacterial compound utilised in the treatment against Gram-negative and Gram-positive organisms. Unfortunately, NRF has low solubility and permeability. In order to provide protection against loss, but also for enhanced bioavailability, and controlled-release of norfloxacin, a drug inclusion complex with cyclodextrin was realized. The effect of complexation on the release profile was highlighted. The addition of NRF to the hydrogel matrices greatly improved the antibacterial activity of the tested compounds. The presence of CD did not affect the homogeneity of the drug distribution. Changes in the polymeric matrix structure were registered after the incorporation of the drug, which were attributed to the relaxation of the network subsequently to the penetration and diffusion of the drug solution simultaneously with the swelling process. The release of NRF from Alg_PA polymeric network has been successfully modulated by the use of CD as a host molecule.


Asunto(s)
Ácido Fítico/química , Alginatos/química , Animales , Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Materiales Biocompatibles/química , Creatinina/sangre , Reactivos de Enlaces Cruzados/química , Ciclodextrinas/química , Liberación de Fármacos , Hidrogeles/química , Cinética , Masculino , Ratones , Pruebas de Sensibilidad Microbiana , Norfloxacino/farmacología , Tamaño de la Partícula , Análisis de Componente Principal , Espectroscopía Infrarroja por Transformada de Fourier , Espectroscopía Infrarroja Corta , Urea/sangre
16.
Molecules ; 26(11)2021 Jun 07.
Artículo en Inglés | MEDLINE | ID: mdl-34200350

RESUMEN

A considerable interest in cancer research is represented by the development of magnetic nanoparticles based on biofunctionalized polymers for controlled-release systems of hydrophobic chemotherapeutic drugs targeted only to the tumor sites, without affecting normal cells. The objective of the paper is to present the synthesis and in vitro evaluation of the nanocomposites that include a magnetic core able to direct the systems to the target, a polymeric surface shell that provides stabilization and multi-functionality, a chemotherapeutic agent, Paclitaxel (PTX), and a biotin tumor recognition layer. To our best knowledge, there are no studies concerning development of magnetic nanoparticles obtained by partial oxidation, based on biotinylated N-palmitoyl chitosan loaded with PTX. The structure, external morphology, size distribution, colloidal and magnetic properties analyses confirmed the formation of well-defined crystalline magnetite conjugates, with broad distribution, relatively high saturation magnetization and irregular shape. Even if the ability of the nanoparticles to release the drug in 72 h was demonstrated, further complex in vitro and in vivo studies will be performed in order to validate the magnetic nanoparticles as PTX delivery system.


Asunto(s)
Antineoplásicos Fitogénicos/química , Biotina/química , Quitosano/análogos & derivados , Nanopartículas de Magnetita/química , Paclitaxel/química , Línea Celular Tumoral , Quitosano/química , Coloides/química , Preparaciones de Acción Retardada/química , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Humanos , Interacciones Hidrofóbicas e Hidrofílicas/efectos de los fármacos , Células MCF-7 , Polímeros/química
17.
Int J Biol Macromol ; 181: 561-571, 2021 Jun 30.
Artículo en Inglés | MEDLINE | ID: mdl-33798571

RESUMEN

Alginate hydrogels are extremely versatile and flexible biomaterials, with an enormous potential for bio-applications use. Their similarity with extracellular matrix is a key factor in their performance for cell and tissue regeneration. In this study superabsorbent high porous hydrogels based on sodium alginate physical crosslinked with a natural crosslinker compound namely phytic acid were prepared and evaluated from the viewpoint of their specific properties. The resulting hydrogels obtained with different ratios between alginate and phytic acid were characterized by Fourier transform infrared spectroscopy technique, scanning electron microscopy, XRD measurements, swelling tests in physiological environment, and thermal analysis by using a simultaneous TG/FT-IR/MS system. There are put into evidence the differences in physico-chemical properties of the hydrogels in relation with their composition, which endows them tunable properties and versatility.


Asunto(s)
Alginatos/química , Hidrogeles/síntesis química , Ácido Fítico/química , Hidrogeles/química , Espectrometría de Masas , Análisis de Componente Principal , Espectroscopía Infrarroja por Transformada de Fourier , Espectroscopía Infrarroja Corta , Temperatura , Termogravimetría , Difracción de Rayos X
18.
Pharmaceutics ; 13(4)2021 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-33916007

RESUMEN

Bio-based compounds are a leading direction in the context of the increased demand for these materials due to the numerous advantages associated with their use over conventional materials, which hardly degrade in the environment. At the same time, the use of essential oils and their components is generated mainly by finding alternative solutions to antibiotics and synthetic preservatives due to their bioactive characteristics, but also to their synergistic capacity during the manifestation of different biological properties. The present study is devoted to poly(ethylene brassylate-co-squaric acid) (PEBSA), synthesis and its use for thymol encapsulation and antibacterial system formation. The synthesized copolymer, performed through ethylene brassylate macrolactone ring-opening and copolymerization with squaric acid, was physicochemical characterized. Its amphiphilic character allowed the entrapment of thymol (Ty), a natural monoterpenoid phenol found in oil of thyme, a compound with strong antiseptic properties. The copolymer chemical structure was confirmed by spectroscopic analyses. Thermal analysis evidenced a good thermal stability for the copolymer. Additionally, the antimicrobial activity of PEBSA_Ty complex was investigated against eight different reference strains namely: bacterial strains-Staphylococcus aureus ATCC25923, Escherichia coli ATCC25922, Enterococcus faecalis ATCC 29212, Klebsiella pneumonie ATCC 10031 and Salmonella typhimurium ATCC 14028, yeast strains represented by Candida albicans ATCC10231 and Candida glabrata ATCC 2001, and the fungal strain Aspergillus brasiliensis ATCC9642.

19.
Polymers (Basel) ; 12(11)2020 Nov 04.
Artículo en Inglés | MEDLINE | ID: mdl-33158235

RESUMEN

Protein-polysaccharide systems are of increasing interest as their combined attributes allow for fulfilling a broad range of applications in biomedical and pharmaceutical fields. In this study, the preparation of nanogels based on maleic anhydride chitosan derivatives (MAC) and bovine serum albumin (BSA) was achieved through a self-assembly process performed in aqueous phase. A series of experiments performed by varying the concentrations of MAC and BSA were conducted to find an appropriate mixing ratio for the polymer solutions leading to thermodynamically stable nanogels with the ability to encapsulate active compounds. The influence of temperature on the formation of nanogels was also studied. The consequent conformational changes were monitored using ultraviolet-visible (UV-VIS) spectrophotometry. The spectrophotometric investigations combined with diffraction light scattering (DLS) technique and zeta potential measurement results were correlated to determine the interaction mechanism and assess the self-assembling processes during nanogel formation. It was found that the hydrodynamic diameter (Dh) of the nanoparticles increased slightly at acidic pH, and the protonation of ionizable amino groups with the pH was confirmed by the zeta potential measurements. MAC/BSA nanogels also exhibited antimicrobial properties after being loaded with amoxicillin (Amox), which is an antibiotic used for the treatment of various infections. The experimental data resulting from this study provide theoretical guidance for the design and development of attractive nanocarriers for a large variety of biomedical applications.

20.
Biomacromolecules ; 21(10): 4231-4243, 2020 10 12.
Artículo en Inglés | MEDLINE | ID: mdl-32909739

RESUMEN

Maleoyl-chitosan/poly(aspartic acid) nanogels were developed and characterized in order to assess its suitability for biomedical applications. Thus, the physicochemical properties were investigated and correlated with the composition of the new structures. Dynamic light scattering measurements, correlated with transmission electron microscopy images, demonstrated that nanogels size distribution was narrow with average diameter between 186 and 246 nm, and presented positive zeta potential values. The sensitivity of nanogels at pH and temperature was also evaluated. Nanogels loaded with amoxicillin showed a controlled release profile dependent on nanogel content. The formulations loaded with amoxicillin had antibacterial properties, and the cytotoxicity tests indicated good in vivo biocompatibility. In conclusion, the new synthesized polyelectrolyte nanogels, which can provide a stable environment for the encapsulated drugs, can be used as a multifunctional platform for administration of antimicrobial agents from the spectrum of antibiotics that have a very poor biodistribution.


Asunto(s)
Quitosano , Geles , Concentración de Iones de Hidrógeno , Nanogeles , Distribución Tisular
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