RESUMEN
Chitosan/chondroitin sulfate (CHT/CS) curcumin-charged hydrogels were prepared through polyelectrolytic complexation (PEC) following two methodologies (PEC-CUR and PEC-T-CUR) and were applied on apoptosis of HeLa, HT29 and PC3 cancer cells. PEC-T-CUR (ionic liquid (IL) mixed using ultraturrax homogenizer) results show to be far better than for PEC-CUR (IL mixed using magnetic stirring), with IC50 being improved 5.13 times to HeLa cancer cells (from 1675.2 to 326.7 µg mL-1). PECs produced by this methodology presented favorable characteristics, such as particle size, hydrophobicity, pH swelling. Beyond this, the IL was quantitatively recovered in both cases. CUR entrapment levels were hugely loaded into PEC at around 100%. Swelling, dissolution/degradation, and pHpzc assays showed that PECs may positively act in several environments, releasing the CUR, the CHT and CS as well. Characterization through FTIR, SEM, TEM, TGA, DSC, and WAXS confirmed CUR presence in both types of PECs, and cytotoxic studies showed the significant anticancer effects of CUR-containing PECs.
Asunto(s)
Antineoplásicos/química , Materiales Biocompatibles/química , Materiales Biocompatibles/farmacología , Quitosano/química , Curcumina/química , Portadores de Fármacos/química , Hidrogeles/química , Líquidos Iónicos/química , Nanopartículas/química , Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Sulfatos de Condroitina/química , Células HT29 , Células HeLa , Humanos , Hidrogeles/farmacología , Concentración de Iones de Hidrógeno , Interacciones Hidrofóbicas e Hidrofílicas , Células PC-3 , Tamaño de la Partícula , Polielectrolitos/químicaRESUMEN
Strategies for incorporating water-insoluble photosensitisers (PS) in drug delivery systems have been extensively studied. In this work, we evaluate the formation, characterisation, drug sorption studies, and cytotoxicity of chitosan (CHT)/chondroitin sulphate (CS) polyelectrolyte complexes (PECs) coated with polystyrene-block-poly(acrylic acid) (PS-b-PAA) nanoparticles (NPs) loaded with chloroaluminum phthalocyanine (AlClPc). The PECs were characterised by infrared spectroscopy (FTIR), differential scanning calorimetric (DSC), X-ray diffraction (XRD), and scanning electron microscopy (SEM). The PS-b-PAA NPs on the PEC surface was confirmed by scanning electron microscopy (SEM). Additionally, optical images distinguished the PEC structures containing PS-b-PAA or PS-b-PAA/AlClPc from the unloaded PEC. Kinetic and equilibrium studies investigate the sorption capacity of the PEC/PS-b-PAA toward AlClPc. The encapsulation efficiency reached 95% at 190 µg mL-1 AlClPc after only 15 min. The Brunauer-Emmett-Teller (BET) isotherm and pseudo-second-order kinetic fitted well to the experimental data. The PS-b-PAA NPs on the PEC surfaces increase the AlClPc bioavailability and the PEC structure stabilizes the PS-b-PAA/AlClPc nanostructures. The materials were cytocompatible upon healthy VERO (kidney epithelial cells), and cytotoxic against colorectal cancerous cells (HT-29 cells). For the first time, we associate PS-b-PAA/AlClPc with a hydrophilic and cytocompatible polysaccharide matrix. We suggest the use of these materials in strategies to treat cancer by using photodynamic therapy.
Asunto(s)
Antineoplásicos/farmacología , Materiales Biocompatibles/farmacología , Neoplasias Colorrectales/tratamiento farmacológico , Polielectrolitos/farmacología , Polisacáridos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Materiales Biocompatibles/síntesis química , Materiales Biocompatibles/química , Conformación de Carbohidratos , Línea Celular , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Neoplasias Colorrectales/patología , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Tamaño de la Partícula , Polielectrolitos/síntesis química , Polielectrolitos/química , Polisacáridos/síntesis química , Polisacáridos/químicaRESUMEN
Pectin and chitosan films containing glycerol (Gly) at 5, 10, 15, 20, 30, and 40 wt % were prepared in an aqueous HCl solution (0.10 M) by the solvent evaporation method. The unwashed film (UF) containing 40 wt % Gly (UF40) had elongation at break (ε, %) of 19%. Washed films (WFs) had high tensile strength (σ > 46 MPa) and low elongation at break (ε, <5.0%), enabling their use in food packaging applications. The polymers' self-assembling occurred during the washing, increasing the stiffness. The XPS analysis suggests that some HCl is lost during the drying process, resulting in a low acid content on the UF surfaces. The UF40 (at 5.0 mg/mL) exhibits cytocompatibility toward mammalian cells and antimicrobial and anti-adhesive properties against Escherichia coli. The remaining HCl in the UF40 can be a disadvantage for food packaging applications; the UF40 (∅ = 8.5 mm; 55 µm thickness) releases H3O+/HCl, reducing the pH to approximately 3.0 when kept in 200 mL distilled water for approximately 30 min. Therefore, we propose the use of UF40 to coat commercial food packaging. The UF40 has low permeability to water vapor and oxygen and works as a barrier against ultraviolet light. The UF40 is also colorless and completely transparent. The UF40 maintained tomatoes' structural integrity for 18 days at room temperature with no oxidation or microorganism contamination. This paper presents a critical viewpoint concerning chitosan-based films with antimicrobial activities.
Asunto(s)
Antibacterianos/química , Quitosano/química , Materiales Biocompatibles Revestidos/química , Escherichia coli/crecimiento & desarrollo , Embalaje de Alimentos , Glicerol/química , Membranas Artificiales , Pectinas/químicaRESUMEN
To obtain pectin-based films is challenging due to the aqueous instability of polyelectrolyte mixtures. We overcome this issue by blending chitosan to pectin of high O-methoxylation degree (56%), followed by solvent evaporation. A durable film containing 74 wt% pectin content was produced and used as an adsorbent material toward Cu(II) ions. Kinetic and adsorption equilibrium studies showed that the pseudo-second-order and Sips isotherm models adjusted well to the experimental data, respectively. Langmuir isotherm indicated a maximum adsorption capacity (qm) for Cu(II) removal of 29.20 mg g-1. Differential scanning calorimetry, contact angle measurements, and X-ray photoelectron spectroscopy confirm the adsorption. The chemisorption plays an essential role in the process; thereby, the film reusability is low. After adsorption, the cytocompatible film/Cu(II) pair prevents the proliferation of Escherichia coli.
Asunto(s)
Antiinfecciosos/química , Antiinfecciosos/farmacología , Cobre/química , Cobre/aislamiento & purificación , Pectinas/química , Pectinas/farmacología , Agua/química , Adsorción , Quitosano/química , Escherichia coli/efectos de los fármacos , Cinética , Ensayo de Materiales , Metilación , SolucionesRESUMEN
[Hmim][HSO4] ionic liquid (IL) and bio-renewable sources as chitosan (CHT) and chondroitin sulfate (CS) were used to yield hydrogel-based materials (CHT/CS). The use of IL to solubilize both polysaccharides was considered an innovative way based on "green chemistry" principle, aiming the production of CHT/CS blended systems. CHT/CS hydrogels were carried out in homogeneous medium from short dissolution times. The hydrogels were characterized and achieved with excellent stabilities (in the 1.2-10pH range), larger swelling capacities, as well as devoid of cytotoxicity towards the normal VERO and diseased HT29 cells. The CHT/CS hydrogels carried out in [Hmim][HSO4] could be applied in many technological purposes, like medical, pharmaceutical, and environmental fields.
Asunto(s)
Quitosano/química , Sulfatos de Condroitina/química , Hidrogeles/síntesis química , Líquidos Iónicos/química , Supervivencia Celular/efectos de los fármacos , Células HT29 , Humanos , Hidrogeles/toxicidadRESUMEN
Nanoparticles (NPs) based on N,N-dimethyl chitosan (DMC) and N,N,N-trimethyl chitosan (TMC), physical crosslinked with sodium tripolyphosphate (TPP) were successful obtained, using water/benzyl alcohol emulsion system. NPs morphologies were evaluated by Scanning Electron Microscopy and Transmission Electron Microscopy. NPs were characterized by Infrared Spectroscopy (FTIR), Thermogravimetric Analysis, Zeta Potential, Differential Scanning Calorimetry and Wide-angle X-ray Scattering. Curcumin (CUR) was loaded onto NPs and controlled release studies were evaluated in simulated intestinal fluid and in simulated gastric fluid. Cytotoxicity assays showed only loaded TMC/TPP particles containing CUR were slightly cytotoxic on human cervical tumor cells (SiHa cells), concerning unloaded TMC/TPP particles. Conversely, loaded NPs (TMC/TPP/CUR and DMC/TPP/CUR), especially TMC/TPP/CUR sample presented greater biocompatibility toward healthy VERO cells than unloaded NPs (TMC/TPP and DMC/TPP).