RESUMO
Oral drug administration, especially when composed of mucoadhesive delivery systems, has been a research trend due to increased residence time and contact with the mucosa, potentially increasing drug bioavailability and stability. In this context, this study aimed to develop self-assembly mucoadhesive beads composed of blends of κ-carrageenan and sericin (κ-Car/Ser) loaded with the anti-inflammatory drug indomethacin (IND). We investigated the swelling, adhesion behaviour, and mechanical/physical properties of the beads, assessing their effects on cell viability, safety and permeation characteristics in both 2D and triple-culture model. The swelling ratio of the beads indicated pH-responsiveness, with maximum water absorption at pH 6.8, and strong mucoadhesion, increasing primarily with higher polymer concentrations. The beads exhibited thermal stability and no chemical interaction with IND, showing improved mechanical properties. Furthermore, the beads remained stable during accelerated and long-term storage studies. The beads were found to be biocompatible, and IND encapsulation improved cell viability (>70 % in both models, 79 % in VN) and modified IND permeation through the models (6.3 % for F5 formulation (κ-Car 0.90 % w/v | Ser 1.2 % w/v| IND 3.0 g); 10.9 % for free IND, p < 0.05). Accordingly, κ-Car/Ser/IND beads were demonstrated to be a promising IND drug carrier to improve oral administration while mitigating the side effects of non-steroidal anti-inflammatories.
Assuntos
Carragenina , Preparações de Ação Retardada , Indometacina , Sericinas , Indometacina/química , Indometacina/administração & dosagem , Indometacina/farmacocinética , Carragenina/química , Administração Oral , Humanos , Sericinas/química , Preparações de Ação Retardada/química , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Sobrevivência Celular/efeitos dos fármacos , Microesferas , Animais , Células CACO-2 , Concentração de Íons de HidrogênioRESUMO
The crosslinking of the polymer matrix with compatible macromolecules results in a three-dimensional network structure that offers an enhancement in the controlled release properties of the material. In this sense, this work aimed to improve the release profile of mefenamic acid (MAC) through crosslinking strategies. κ-Carrageenan/sericin crosslinked blend was obtained by covalent and thermal crosslinking and the different formulations were characterized. The gastroresistant potential and release profile were evaluated in the dissolution assay. The effect and characterization of the particles were investigated. Multiple units presented high entrapment efficiency (94.11-104.25), high drug loading (36.50-47.50 %) and adequate particle size (1.34-1.57 mm) with rough surface and visually spherical shape. The Weibull model showed that drug release occurred by relaxation, erosion and Fickian diffusion. Material stability and absence of MAC -polymer interactions were demonstrated by FTIR and thermogravimetric analysis. DSC showed a stable character of MAC in the drug-loaded beads. Moreover, the application studies of κ-Car/Ser/carboxymethylcellulose in the in vitro intestine mode showed that the crosslinked blend increased cell viability (>85 %), while free MAC exhibited a cytotoxic effect. Finally, the crosslinked k-Car/Ser blend MAC -loaded showed promising properties of a sustained release form of anti-inflammatory drug.
Assuntos
Sericinas , Sericinas/química , Ácido Mefenâmico/farmacologia , Polímeros , Carragenina/química , Liberação Controlada de Fármacos , Preparações de Ação Retardada/químicaRESUMO
Silk sericin is a globular protein whose resistance against fouling is important for applications in biomaterials and water-purification membranes. Here it is shown how sericin generates a water-exclusion zone that may facilitate antifouling behavior. Negatively charged microspheres were used to mimic the surface charge and hydrophobic domains in bacteria. Immersed in water, regenerated silk sericin formed a 100-µm-sized exclusion zone (for micron-size foulants), along with a proton gradient with a decrease of >2 pH-units. Thus, when in contact with sericin, water molecules near the surface restructure to form a physical exclusionary barrier that might prevent biofouling. The decreased pH turns the aqueous medium unviable for neutrophilic bacteria. Therefore, resistance to biofouling seems explainable, among other factors, on the basis of water-exclusionary phenomena. Furthermore, sericin may play a role in triggering the fibroin assembly process by lowering the pH to the required value.
Assuntos
Incrustação Biológica , Sericinas/química , Animais , Bombyx , Água/químicaRESUMO
In this study, two novel low water-soluble sericin and alginate-based biosorbents were successfully developed for precious metal removal from wastewater: sericin and alginate particles chemically crosslinked by proantocyanidins (SAPAs) and sericin, alginate and polyvinyl alcohol particles (SAPVA). The proportions of proantocynidins (PAs) or polyvinyl alcohol (PVA) added to sericin (2.5% w/v) and alginate (2.0% w/v) blend were 0.5, 1.5, 2.5 and 3.5% w/v. Among these concentrations, particles produced with 0.5% w/v of PVA or 2.5% w/v of PAs presented the lowest water solubility percentages (3.74 ± 0.05 and 3.56 ± 0.21%, respectively) and the following metallic affinity order: AuCl4- > PdCl42- > PtCl62- > Ag+. Then, gold biosorption kinetics by SAPAs was evaluated at three gold initial concentrations (72.88, 187.12, and 273.79 mg/L), and its performance was compared to activated carbon adsorbent uptake. The data modeling revealed that the process follows pseudo-first-order kinetics and is mainly controlled by external diffusion. SAPAs before and after gold biosorption (SAPAs-gold) were characterized by scanning electron microscopy coupled with energy dispersive X-ray spectroscopy, optical microscopy, helium pycnometry, mercury porosimetry, N2 physisorption, and Fourier-transform infrared spectroscopy.
Assuntos
Alginatos/química , Álcool de Polivinil/química , Sericinas/análise , Ouro , Cinética , Microscopia Eletrônica de Varredura , Sericinas/química , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Águas ResiduáriasRESUMO
In this study, particles produced from sericin-alginate blend were used as non-conventional bioadsorbent for removing Cr(III) and Cr(VI) from aqueous solutions. Besides chromium mitigation, the use of sericin-alginate particles as bioadsorbent aims to offer an environmental solution of added value for sericin, which is a by-product from silk industry. Sericin-alginate particles in natura and loaded with Cr(III) and Cr(VI) were characterized using N2 physical adsorption analysis, optical microcopy, mercury porosimetry, helium pycnometry, scanning electron microscope coupled with energy dispersive X-ray spectrometer, Fourier transform infrared spectrometer, and X-ray diffraction. Kinetic studies on the removal of Cr(III) (at pH = 3.5) and Cr(VI) (at pH = 2) indicate the ion exchange mechanism with Ca(II) and the predominance of external mass transfer resistance. Cr(VI) uptake occurs through an adsorption-coupled reduction process, and bioadsorption equilibrium is reached after ~ 1000 min. Cr(III) bioadsorption occurs faster (~ 210 min). The Cr(VI) bioadsorption is endothermic, as bioadsorption capacity increases with temperature: 0.0783 mmol/g (20 °C), 0.1960 mmol/g (30 °C), 0.4570 mmol/g (40 °C), and 0.7577 mmol/g (55 °C). The three-parameter isotherm model of Tóth best represents the equilibrium data of total chromium. From Langmuir isotherm model, the maximum bioadsorption capacity is higher for total chromium, 0.25 mmol/g (30 °C), than for trivalent chromium, 0.023 mmol/g (30 °C). The comparison of bioadsorption capacities with different biomaterials confirms sericin-alginate particles as potential bioadsorbent of chromium.
Assuntos
Alginatos/química , Bombyx/metabolismo , Cromo/química , Sericinas/química , Poluentes Químicos da Água/química , Purificação da Água , Adsorção , Animais , Cinética , Difração de Raios XRESUMO
Sericin is a silk protein woven from silkworm cocoons (Bombyx mori). In animal model, sericin has been reported to have anti-tumoral action against colon cancer. The mechanisms underlying the activity of sericin against cancer cells are not fully understood. The present study investigated the effects of sericin on human colorectal cancer SW480 cells compared to normal colonic mucosal FHC cells. Since the size of the sericin protein may be important for its activity, two ranges of molecular weight were tested. Sericin was found to decrease SW480 and FHC cell viability. The small sericin had higher anti-proliferative effects than that of the large sericin in both cell types. Increased apoptosis of SW480 cells is associated with increased caspase-3 activity and decreased Bcl-2 expression. The anti-proliferative effect of sericin was accompanied by cell cycle arrest at the S phase. Thus, sericin reduced SW480 cell viability by inducing cell apoptosis via caspase-3 activation and down-regulation of Bcl-2 expression. The present study provides scientific data that support the protective effect of silk sericin against cancer cells of the colon and suggests that this protein may have significant health benefits and could potentially be developed as a dietary supplement for colon cancer prevention.
Assuntos
Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Colo/efeitos dos fármacos , Neoplasias do Colo/patologia , Sericinas/farmacologia , Seda/química , Animais , Bombyx , Bovinos , Linhagem Celular Tumoral , Sobrevivência Celular , Colo/citologia , Neoplasias do Colo/metabolismo , Neoplasias do Colo/prevenção & controle , Humanos , Mucosa Intestinal/citologia , Mucosa Intestinal/efeitos dos fármacos , Peso Molecular , Sericinas/químicaRESUMO
Sericin is a silk protein woven from silkworm cocoons (Bombyx mori). In animal model, sericin has been reported to have anti-tumoral action against colon cancer. The mechanisms underlying the activity of sericin against cancer cells are not fully understood. The present study investigated the effects of sericin on human colorectal cancer SW480 cells compared to normal colonic mucosal FHC cells. Since the size of the sericin protein may be important for its activity, two ranges of molecular weight were tested. Sericin was found to decrease SW480 and FHC cell viability. The small sericin had higher anti-proliferative effects than that of the large sericin in both cell types. Increased apoptosis of SW480 cells is associated with increased caspase-3 activity and decreased Bcl-2 expression. The anti-proliferative effect of sericin was accompanied by cell cycle arrest at the S phase. Thus, sericin reduced SW480 cell viability by inducing cell apoptosis via caspase-3 activation and down-regulation of Bcl-2 expression. The present study provides scientific data that support the protective effect of silk sericin against cancer cells of the colon and suggests that this protein may have significant health benefits and could potentially be developed as a dietary supplement for colon cancer prevention.
Assuntos
Animais , Bovinos , Humanos , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Colo/efeitos dos fármacos , Neoplasias do Colo/patologia , Sericinas/farmacologia , Seda/química , Bombyx , Linhagem Celular Tumoral , Sobrevivência Celular , Colo/citologia , Neoplasias do Colo/metabolismo , Neoplasias do Colo/prevenção & controle , Mucosa Intestinal/citologia , Mucosa Intestinal/efeitos dos fármacos , Peso Molecular , Sericinas/químicaRESUMO
Wild Silkmoth cocoons are difficult or impossible to reel under conditions that work well for cocoons of the Mulberry silkmoth, Bombyx mori . Here we report evidence that this is caused by mineral reinforcement of Wild Silkmoth cocoons and that washing these minerals out allows for the reeling of commercial lengths of good quality fibers with implications for the development of the "Wild Silk" industry. We show that in the Lasiocampid silkmoth Gonometa postica , the mineral is whewellite (calcium oxalate monohydrate). Evidence is presented that its selective removal by ethylenediaminetetraacetic acid (EDTA) leaves the gum substantially intact, preventing collapse and entanglement of the network of fibroin brins, enabling wet reeling. Therefore, this method clearly differs from the standard "degumming" and should be referred to as "demineralizing". Mechanical testing shows that such preparation results in reeled silks with markedly improved breaking load and extension to break by avoiding the damage produced by the rather harsh degumming, carding, or dry reeling methods currently in use, what may be important for the development of the silk industries not only in Asia but also in Africa and South America.