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1.
Langmuir ; 38(18): 5915-5923, 2022 05 10.
Artículo en Inglés | MEDLINE | ID: mdl-35439019

RESUMEN

Cationic polymers are known to attach on an anionic cell surface and favor gene transportation/transfection into the cells. However, when the positive charges accumulate, they tend to cause cell damage and delivery failure. Chitosan (CS) is a potential cationic bio-derived polymer whose chemical structures can be modified to fine-tune the charges as well as the add-on functions. The present work demonstrates (i) the decoration of a nucleic acid sequence-like brush structure on CS to allow the specific interaction with DNA and (ii) delivery into the cell. By simply applying mercaptoacetic acid as the chain transfer agent, the grafting of poly(hydroxyethyl methacrylate) (PHEMA) containing Thy (P(HEMA-Thy)) on CS is possible. The brush-like P(HEMA-Thy) leads Thy moieties to be in sequences. The Thy sequences perform as poly[T] for the specific interaction with ssDNA. The synergistic effect of CS and Thy sequences, i.e., electrostatic and base pairing interactions, results in an effective and efficient binding with ssDNA as well as significant delivery, especially in cellular uptake and cell viability. The use of CS in combination with Thy sequences in brush-like structures on CS is a model for other polysaccharides to be conjugated with the as-designed nucleic acid sequences for potential gene delivery.


Asunto(s)
Quitosano , Cationes , Quitosano/química , ADN de Cadena Simple , Técnicas de Transferencia de Gen , Polihidroxietil Metacrilato/química , Timina
2.
Biomacromolecules ; 23(12): 5361-5372, 2022 Dec 12.
Artículo en Inglés | MEDLINE | ID: mdl-36456928

RESUMEN

Multistimuli-responsive polymers are important for controlled release. Owing to the fact that these polymers are derived from vinyl-based monomers, their decoration with other molecules is limited. Polysaccharides, especially chitosan (CS) and hyaluronic acid (HA), are pH-responsive biopolymers, whose chemical structures contain reactive functional groups for feasible chemical modifications to obtain add-on functions. The present work demonstrates the introduction of polymers with upper critical solution temperature (UCST) and lower critical solution temperature (LCST) performances onto CS and HA, respectively. By simply varying the mole ratio between the CS-containing UCST polymer and the HA-containing LCST polymer along with adjusting the pH, a polymer system with a UCST-LCST-pH multiresponsive window can be obtained. This multiresponsive window enables us to control the encapsulation and release with repeatability as evidenced from a model study on lysozyme. The present work, for the first time, shows a simple approach to obtain multiresponsive biodegradable polymers through the formation of a single polymer complex to tailor a specific multiresponsive window.


Asunto(s)
Quitosano , Polímeros , Polímeros/química , Ácido Hialurónico , Temperatura , Concentración de Iones de Hidrógeno
3.
J Liposome Res ; 26(1): 69-79, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-25945393

RESUMEN

CONTEXT: Oral delivery of peptide and protein drugs still remains the area of challenges due to their low stability and permeability across GI tract. Among numerous attempts, the receptor-mediated drug targeting is a promising approach to enhance GI permeability. OBJECTIVE: The aim of this study was to prepare mannosylated buserelin acetate (MANS-BA) proliposome powders grafted with N-octadecyl-d-mannopyranosylamine (SAMAN) as targeting moiety and evaluate their permeability across Caco-2 cell monolayers. MATERIALS AND METHODS: The MANS-BA proliposome powders were prepared by coprecipitation method. The targeting moiety SAMAN was synthesized in-house and confirmed by characterization using Fourier transform infrared (FTIR) and differential scanning calorimeter (DSC). RESULTS: The MANS-BA liposomes reconstituted from proliposome powders exhibited the oligolamellar vesicular structure of phospholipid bilayer. Their size, zeta potential and entrapment efficiency were in the ranges of 93.11-218.95 nm, -24.03 to -37.15 mV and 21.12-33.80%, respectively. The permeability of reconstituted MANS-BA liposomes across Caco-2 cell monolayers was significantly enhanced to about 1.2- and 2.2-fold over those of conventional BA liposomes and solution, respectively. DISCUSSION: Increase in dicetylphosphate, cholesterol and SAMAN contents resulted in significant increase in size and zeta potential of reconstituted MAN-BA liposomes. The entrapment efficiency was increased with increasing dicetylphosphate and mannitol contents in liposomes containing cholesterol. CONCLUSIONS: The significantly enhanced permeability across Caco-2 cell monolayers of MANS-BA liposomes might be due to the role of mannose receptor on intestinal enterocytes.


Asunto(s)
Amino Azúcares/química , Buserelina/química , Liposomas/química , Amino Azúcares/síntesis química , Buserelina/síntesis química , Células CACO-2 , Humanos , Ligandos , Liposomas/síntesis química , Permeabilidad
4.
Biosci Biotechnol Biochem ; 77(5): 1068-74, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-23649275

RESUMEN

The antioxidant activities of Salak plum (Salacca edulis) peel extracts were assessed by 1, 1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothaiazoline)-6-sulfonic acid (ABTS), and ferric reducing ability of plasma (FRAP) assays. The ethyl acetate (EtOAc) fraction was the most potent (DPPHIC50=2.932 ± 0.030 µg/mL, ABTSIC50=7.933 ± 0.049 µg/mL, FRAPEC=7,844.44 ± 40.734). Chlorogenic acid was detected as the marker (1.400 ± 0.102 g/kg). The EtOAc fraction was non-cytotoxic in vero and normal human fibroblast (NHF) cells. It exhibited cellular oxidative prevention and damage treatment at 5-40 µg/mL in NHF cells. Salak plum peel loaded liposome consisting of lecithin and hydrophobically modified hydroxyethylcellulose (HMHEC) was developed and found stable with adequate entrapment efficacy. Thus Salak plum peel was highlighted as a potential ecological antioxidant for health promotion aspects, and for cosmetics.


Asunto(s)
Antioxidantes/aislamiento & purificación , Arecaceae/química , Cosméticos/aislamiento & purificación , Epidermis de la Planta/química , Extractos Vegetales/aislamiento & purificación , Seguridad , Acetatos/química , Animales , Antioxidantes/química , Antioxidantes/toxicidad , Chlorocebus aethiops , Cosméticos/química , Cosméticos/toxicidad , Estabilidad de Medicamentos , Humanos , Liposomas , Nanopartículas/química , Extractos Vegetales/química , Extractos Vegetales/toxicidad , Estándares de Referencia , Células Vero
5.
Anal Biochem ; 429(2): 142-7, 2012 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-22809874

RESUMEN

The use of microarray-based immunoassay is often limited by its sensitivity. To increase the sensitivities of such an immunoassay, liposome encapsulation was explored. Two different liposome formations and several preparation methods were examined to optimize encapsulation and signal-enhancing efficacy for enzyme-linked immunosorbent assay (ELISA) and antibody array. The signal amplification by liposome encapsulation was demonstrated through a detection for foodborne pathogenic Listeria. In plate-trapped antigen (PTA) ELISA, horseradish peroxidase (HRP)-loaded liposome increased signal 9-fold more than the control. Limits of detection (LODs) of HRP-encapsulated liposome were 6.4 × 10(5) and 5.5 × 10(6)CFU/ml in sandwich ELISA and antibody array, respectively. Furthermore, when chromogenic 4-chloro-1-naphthol (4-CN) substrate was used for signal development in the antibody array, the signal could be detected with the naked eye. These results suggest that the liposome encapsulation technique can have great potential for signal amplification and, therefore, for increasing assay sensitivity for various formats of immunoassay, especially microarray-based format.


Asunto(s)
Inmunoensayo , Liposomas/química , Anticuerpos/química , Anticuerpos/inmunología , Antígenos/análisis , Química Farmacéutica , Colorimetría , Peroxidasa de Rábano Silvestre/química , Peroxidasa de Rábano Silvestre/metabolismo , Listeria/metabolismo , Nanotecnología , Naftoles/química , Análisis por Matrices de Proteínas
6.
Carbohydr Res ; 504: 108336, 2021 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-33964507

RESUMEN

The development of hybrid polysaccharide-protein complexes as Pickering emulsion stabilizers has attracted increasing research interest in recent years. This work presents an eco-friendly surface modification strategy to functionalize hydrophilic cellulose nanocrystals (CNC) using hydrophobic soy protein isolate (SPI) via mussel adhesive-inspired poly (l-dopa) (PLD) to develop improved nanoconjugates as stabilizers for oil-in-water Pickering emulsion. The physicochemical properties of the CNC-PLD-SPI nanoconjugate were evaluated by solid-state 13C NMR, FT-IR, TGA, XRD, contact angle analysis, and TEM. The modified CNC (conjugation content of 38.22 ± 1.21%) had lowered crystallinity index, higher thermal stability, and more hydrophobic than unmodified CNC, with an average particle size of 309.9 ± 8.0 nm. Use of amphiphilic CNC-PLD-SPI nanoconjugate with greater conformational flexibility as Pickering stabilizer produced oil-in-water emulsions with greater physical stability.


Asunto(s)
Celulosa , Emulsiones , Nanoconjugados , Proteínas de Soja
7.
J Microencapsul ; 27(5): 436-46, 2010.
Artículo en Inglés | MEDLINE | ID: mdl-20001503

RESUMEN

The objective of this work has been the microencapsulation of Asiatic Pennywort (AP) extract with lecithin from soybean. The effect of various quantities of non-ionic surfactant (Montanov82) on liposomes upon physicochemical characteristics as well as their in vitro bio-activities was investigated. An addition of surfactant resulted in a decrease in particle size and an increase in percentage AP entrapment efficiency of liposomes. The surfactant-loaded liposomes demonstrated higher stability than surfactant-free liposomes where higher percentage AP remaining of liposomes can be achieved depending on surfactant concentration. No significant difference was found on AP release profiles among varied surfactant concentrations, although a presence of surfactant resulted in prolonged AP release rate. Liposomal AP with 20% w/w surfactant or higher demonstrated low cytotoxicity, a stronger anti-oxidation effect and collagen production on dermal fibroblast cells when compared with free AP and surfactant-free liposomes, possibly due to better cell internalization and less AP degradation in cells.


Asunto(s)
Antioxidantes/administración & dosificación , Antioxidantes/farmacología , Centella/química , Fibroblastos/efectos de los fármacos , Liposomas/química , Extractos Vegetales/administración & dosificación , Extractos Vegetales/farmacología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Colágeno/metabolismo , Composición de Medicamentos , Fibroblastos/metabolismo , Humanos , Lecitinas/química , Tamaño de la Partícula , Glycine max/química , Tensoactivos
8.
AAPS PharmSciTech ; 11(1): 64-72, 2010 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-20058108

RESUMEN

The aim of this study was to investigate chitosan/siRNA complexes formulated with various chitosan salts (CS) including chitosan aspartate (CS-Asp), chitosan glutamate (CS-Glu), chitosan acetate (CS-Ac), and chitosan hydrochloride (CS-HCl) for in vitro siRNA delivery into stable and constitutive enhanced green fluorescent protein (EGFP)-expressing HeLa cells. The CS/siRNA complexes were characterized by 2% agarose gel electrophoresis and investigated for their transfection efficiency in stable and constitutive EGFP-expressing HeLa cells. The cytotoxicity of the complexes was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. The formation of complexes CS/siRNA is mainly dependent on the weight ratio, whereas salt form and molecular weight has less effect. The particle sizes of the complete complexes were in the range of 270-373 nm except the complete complex of CS-Ac, with a slightly positive charge of less than 2 mV. The ability of CS to transfer functionally active siRNA into cell culture is mainly dependent on the weight ratio and molecular weight of CS whereas salt form of CS has less effect. The high gene-silencing efficiency was observed with low MW of CS (20 kDa) and high weight ratio of 32. Over 80% average cell viabilities were observed for CS/siRNA complexes in all weight ratios comparison to untreated cells. This study suggests CS salts have the potential to be used as safe siRNA delivery vectors.


Asunto(s)
Quitosano/metabolismo , Quitosano/farmacología , ARN Interferente Pequeño/genética , Sales (Química)/farmacología , Animales , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/genética , Cricetinae , Electroforesis en Gel de Agar , Silenciador del Gen , Vectores Genéticos , Glutamatos/genética , Glutamatos/metabolismo , Glutamatos/farmacología , Proteínas Fluorescentes Verdes , Células HeLa , Humanos , Peso Molecular , Tamaño de la Partícula , Polímeros/metabolismo , Polímeros/farmacología , ARN Interferente Pequeño/farmacología , Sales (Química)/metabolismo , Cloruro de Sodio/metabolismo , Cloruro de Sodio/farmacología , Sales de Tetrazolio , Tiazoles , Transfección
9.
Colloids Surf B Biointerfaces ; 196: 111270, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32777659

RESUMEN

Cisplatin (Cis) is a widely used chemotherapeutic drug for cancer treatment. However, toxicities and drug resistance limit the use of cisplatin. This study was aimed to improve cisplatin delivery using a targeting strategy to reduce the toxicity. In the present study, combinations of poly lactic-co-glycolic acids (PLGA) and liposomes were used as carriers for cisplatin delivery. In addition, to target the nanoparticle towards tumor cells, the liposome was conjugated with Avastin®, an anti-VEGF antibody. Cisplatin was loaded into PLGA using the double emulsion solvent evaporation method and further encapsulated in an Avastin® conjugated liposome (define herein as L-PLGA-Cis-Avastin®). Their physicochemical properties, including particle size, ζ-potential, encapsulation efficiency and drug release profiles were characterized. In addition, a study of the efficiency of tumor targeted drug delivery was conducted with cervical tumor bearing mice via intravenous injection. The therapeutic effect was examined in a 3D spheroid of SiHa cell line and SiHa cells bearing mice. The L-PLGA-Cis-Avastin® prompted a significant effect on cell viability and triggered cytotoxicity of SiHa cells. A cell internalization study confirmed that the L-PLGA-Cis-Avastin® had greater binding specificity to SiHa cells than those of L-PLGA-Cis or free drug, resulting in enhanced cellular uptake. Tumor targeting specificity was finally confirmed in xenograft tumors. Taken together, this nanoparticle could serve as a promising specific targeted drug for cervical cancer treatment.


Asunto(s)
Nanopartículas , Neoplasias del Cuello Uterino , Animales , Línea Celular Tumoral , Cisplatino , Portadores de Fármacos , Femenino , Glicoles , Humanos , Liposomas , Ratones , Tamaño de la Partícula , Neoplasias del Cuello Uterino/tratamiento farmacológico
10.
Nanomedicine ; 5(2): 240-9, 2009 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-19223243

RESUMEN

An antibacterial activity of apatite-coated titanium dioxide (TiO2) against four types of bacteria (Staphylococcus aureus, Escherichia coli, methicillin-resistant Staphylococcus aureus (MRSA), and Micrococcus luteus) was investigated. Its antibacterial performance was observed under black light, visible light, and dark conditions. The number of viable bacteria decreased with irradiation time and became most prominent at 24 hours. Distortion of bacterial cells by the nanoparticles was demonstrated by scanning electron microscopy. Apatite-coated TiO2 was fixed on cotton textiles by dip-coat technique, and the antimicrobial properties of corresponding fabrics were then investigated. The effect of irradiation source on antimicrobial activity of coated cotton fabrics was examined, wherein black-light irradiation demonstrated higher antibacterial activity than either visible-light irradiation or dark conditions. Microbial populations of coated cotton fabrics decreased with increasing irradiation intensity. Coated cotton fabrics have been shown to be nontoxic to human dermal fibroblasts. Our findings suggest that the presence of apatite-coated TiO2 shows antibacterial activity in the presence of black light or visible light, suggesting its potential use in reducing the risk of microorganism transmission for textile applications.


Asunto(s)
Antibacterianos/química , Apatitas/química , Materiales Biocompatibles Revestidos/química , Materiales Biocompatibles Revestidos/farmacología , Textiles , Titanio/química , Titanio/farmacología , Apatitas/farmacología , Recuento de Colonia Microbiana , Escherichia coli/efectos de los fármacos , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Micrococcus luteus/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos
11.
Pharm Dev Technol ; 14(6): 665-71, 2009.
Artículo en Inglés | MEDLINE | ID: mdl-19883256

RESUMEN

The objective of this study is to prepare the gamma-oryzanol-loaded liposomes and investigate their physicochemical properties and antioxidant activity intended for cosmetic applications. Liposomes, Composing phosphatidylCholine (PC) and Cholesterol (Chol), CHAPS or sodium taurocholate (NaTC) were prepared by sonication method. Gamma-oryzanol-loaded liposomes were prepared by using 3, 5 and 10% gamma-oryzanol as an initial concentration. The formulation factors in a particular type and composition of lipid and initial drug loading on the physicochemical properties (i.e., particle size, zeta potential, entrapment efficiency, drug release) and antioxidant activity were studied. The particle sizes of bare liposomes were in nanometer range. The gamma-oryzanol-loaded liposomes in formulations of PC/CHAPS and PC/NaTC liposomes were smaller than PC/Chol liposomes. The incorporation efficiency of 10% gamma-oryzanol-loaded PC/Chol liposomes was less than gamma-oryzanol-loaded PC/CHAPS liposomes and PC/NaTC liposomes allowing higher in vitro release rate due to higher free gamma-oryzanol in buffer solution. The antioxidant activity of gamma-oryzanol-loaded liposomes was not different from pure gamma-oryzanol. Both gamma-oryzanol-loaded PC/CHAPS liposomes and PC/NaTC liposomes were showed to enhance the antioxidant activity in NHF cells. gamma-oryzanol-loaded PC/Chol liposomes demonstrated the lowest cytotoxicity in NHF cells. It was conceivably concluded that liposomes prepared in this study are suitable for gamma-oryzanol incorporation without loss of antioxidant activity.


Asunto(s)
Antioxidantes/administración & dosificación , Portadores de Fármacos/química , Fenilpropionatos/administración & dosificación , Liposomas Unilamelares/química , Administración Tópica , Antioxidantes/química , Antioxidantes/farmacocinética , Antioxidantes/farmacología , Disponibilidad Biológica , Compuestos de Bifenilo/química , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Colesterol/química , Ácidos Cólicos/química , Portadores de Fármacos/farmacología , Fibroblastos/citología , Fibroblastos/efectos de los fármacos , Depuradores de Radicales Libres/administración & dosificación , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/farmacocinética , Depuradores de Radicales Libres/farmacología , Humanos , Peróxido de Hidrógeno/farmacología , Tamaño de la Partícula , Fenilpropionatos/química , Fenilpropionatos/farmacocinética , Fenilpropionatos/farmacología , Fosfatidilcolinas/química , Picratos/química , Ácido Taurocólico/química , Liposomas Unilamelares/farmacología
12.
Pharm Dev Technol ; 14(1): 70-9, 2009.
Artículo en Inglés | MEDLINE | ID: mdl-18800295

RESUMEN

This study reports on the use of electrospun polyvinyl alcohol (PVA) nanofiber mats loaded with meloxicam (MX) as a transdermal drug delivery system. The amounts of MX loaded in the base PVA solution (10% w/v solution) were 2.5, 5, 10 and 20% weight, based on the dry weight of PVA (% wt). The average diameters of these fibers ranged from 121-185 nm. In all concentrations of MX loaded in spun PVA fiber mats, an amorphous nanodispersion of MX with PVA was obtained. Both the degree of swelling and the weight loss of the electrospun PVA mats were greater than those of the as-cast PVA films. The tensile strength of the as-spun fiber mats was lower than that of the as-cast PVA films, but the strain at the maximum of the as-spun fiber mats was about six times higher than that of the as-cast PVA films. The skin permeation flux of the MX permeated from MX-loaded as-spun PVA were significantly higher than from MX-loaded as-cast PVA films, and increased when the MX content in both MX-loaded as-spun PVA and MX-loaded as-cast PVA films was increased. Our research suggests a potential use for MX-loaded electrospun PVA mats as a transdermal drug delivery system.


Asunto(s)
Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/uso terapéutico , Técnicas Electroquímicas/métodos , Alcohol Polivinílico/química , Tecnología Farmacéutica/métodos , Tiazinas/química , Tiazinas/uso terapéutico , Tiazoles/química , Tiazoles/uso terapéutico , Administración Cutánea , Relación Dosis-Respuesta a Droga , Conductividad Eléctrica , Meloxicam , Estructura Molecular , Permeabilidad , Piel/efectos de los fármacos , Piel/metabolismo , Soluciones/química , Temperatura , Resistencia a la Tracción , Viscosidad
13.
J Cosmet Sci ; 59(3): 233-42, 2008.
Artículo en Inglés | MEDLINE | ID: mdl-18528591

RESUMEN

Electrospinning is a process used to produce ultrafine fibers with diameters in the nanometer range. Electrospun fiber mats have high potentials for biomedical uses, due to their high surface area and ease of drug incorporation into the fibers. They can be used as carriers for drug delivery and can enhance drug release and skin permeability. The aim of this study was to prepare electrospun fiber mats and to incorporate extracts from the fruit hull of mangosteen. Antioxidant activity and extract release were determined and compared between the extract incorporated in the electrospun fiber mats and in the cast films. Poly(vinyl alcohol) (PVA) was selected as the polymer matrix. Extracts in the amount of 2.5%, 5%, and 10% w/w, based on the weight of PVA, were incorporated with 10% w/w PVA to finally obtain electrospun fiber mats and cast films. The extract content was evaluated by antioxidative activity using the 2,2-diphenyl-1-picryhydrazyl (DPPH) method. The morphology of the electrospun fiber mats was analyzed using a scanning electron microscope (SEM). The results showed that the diameters of the fibers were in nanoscales and that no crystal of the extract was found at any concentration of the extract. The extract contents in the electrospun fiber mats prepared at 2.5%, 5%, and 10% w/w of the extract were 9.6%, 9.7%, and 10.8% of the initial loading concentration, respectively, whereas, those in the cast films were 23.9%, 14.5%, and 21.0%, respectively. The release of the extract from the electrospun fiber mats prepared at 2.5%, 5%, and 10% w/w of the extract at 120 min were 73.2%, 83.6%, and 81.3% w/w, respectively. However, much slower release from the cast films was observed (i.e., 4.3%, 29.1%, and 40.8% w/w, respectively).


Asunto(s)
Garcinia mangostana/química , Alcohol Polivinílico/química , Microscopía Electrónica de Rastreo
14.
Int J Pharm ; 538(1-2): 21-29, 2018 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-29225100

RESUMEN

In this study, the inclusion complex formation between α-mangostin and water-soluble quaternized ß-CD grafted-chitosan (QCD-g-CS) was investigated. Inclusion complex formation with encapsulation efficiency (%EE) of 5, 15 and 75% can be varied using high speed homogenizer. Tuning %EE plays a role on physicochemical and biological properties of α-mangostin/QCD-g-CS complex. Molecular dynamics simulations indicate that α-mangostin is included within the hydrophobic ß-CD cavity and being absorbed on the QCD-g-CS surface, with these results being confirmed by Fourier transform infrared (FTIR) spectroscopy. Probing the release characteristics of the inclusion complex at various %EE (5%, 15% and 75%) in simulated saliva (pH 6.8) demonstrated that α-mangostin release rates were dependent on % EE (order 5% > 15% > 75%). Additionally, higher antimicrobial and anti-inflammation activities were observed for the inclusion complex than those of free α-mangostin due to enhance the solubility of α-mangostin through the inclusion complex with QCD-g-CS.


Asunto(s)
Química Farmacéutica/métodos , Quitosano/química , Xantonas/administración & dosificación , beta-Ciclodextrinas/química , Antiinfecciosos/administración & dosificación , Antiinfecciosos/química , Antiinfecciosos/farmacología , Antiinflamatorios/administración & dosificación , Antiinflamatorios/química , Antiinflamatorios/farmacología , Línea Celular , Portadores de Fármacos/química , Liberación de Fármacos , Humanos , Interacciones Hidrofóbicas e Hidrofílicas , Simulación de Dinámica Molecular , Saliva/metabolismo , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Agua/química , Xantonas/química , Xantonas/farmacología
15.
Colloids Surf B Biointerfaces ; 161: 497-507, 2018 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-29128836

RESUMEN

Despite advances in neuroscience cancer research during the past decades, the survival of cancer patients has only marginally improved and the cure remains unlikely. The blood-brain barrier (BBB) is a major obstacle protecting the entry of therapeutic agents to central nervous system, especially for primary central nervous system lymphoma (PCNSL). Thus, the use of small nanoparticle as a drug carrier may be new strategies to overcome this problem. In this study, we fabricated liposome consisting of superparamagnetic iron oxide nanoparticles (SPIONs) functionalized with anti-CD20 (Rituximab; RTX). The designed nanoparticles have a theranostic property which is not only to improve drug delivery, but also to offer diagnostic and monitoring capabilities. TEM images revealed the spherical shape of liposome with the approximately average diameters about 140-190nm with slightly negatively charge surfaces. Superparamagnetic property of SPIONs-loaded liposomes was confirmed by VSM. Liposome colloidal could be prolonged at 4°C and 25°C storages. RTX conjugated liposome induced cell internalization and apoptosis effect in B-lymphoma cells. Drug targeting and therapeutic effect was investigated in BBB model. The result confirmed that liposome nanocarrier is required as a drug carrier for effectively RTX across the BBB.


Asunto(s)
Neoplasias del Sistema Nervioso Central/tratamiento farmacológico , Compuestos Férricos/química , Linfoma/tratamiento farmacológico , Nanopartículas de Magnetita/química , Rituximab/administración & dosificación , Ensayos Antitumor por Modelo de Xenoinjerto , Animales , Antineoplásicos Inmunológicos/administración & dosificación , Antineoplásicos Inmunológicos/química , Antineoplásicos Inmunológicos/farmacocinética , Barrera Hematoencefálica/metabolismo , Línea Celular Tumoral , Neoplasias del Sistema Nervioso Central/metabolismo , Neoplasias del Sistema Nervioso Central/patología , Portadores de Fármacos/química , Humanos , Liposomas/química , Liposomas/ultraestructura , Linfoma/metabolismo , Linfoma/patología , Fenómenos Magnéticos , Nanopartículas de Magnetita/ultraestructura , Ratones Desnudos , Rituximab/química , Rituximab/farmacocinética , Nanomedicina Teranóstica/métodos
16.
PDA J Pharm Sci Technol ; 61(6): 461-71, 2007.
Artículo en Inglés | MEDLINE | ID: mdl-18410047

RESUMEN

The objective of this study was to formulate high loading with good stability of all-trans retinoic acid (ATRA) lipid emulsion. Lipid emulsions loaded with ATRA were composed of lecithin, medium chain triglyceride and poloxamer-188 or polysorbate-80. The formulation factors in a particular type and amount of oil, emulsifier, and co-emulsifier on the physicochemical properties (i.e., particle size, size distribution, droplets surface charge, pH, percentage yield, drug release, and stability of lipid emulsions) were studied. The particle size of ATRA-loaded lipid emulsions was in the nano-size range of 124.4-378.2 nm with the narrow polydispersity index of 0.04-0.09, which decreased as the amount of co-emulsifiers was increased. The amount of ATRA released from lipid emulsions was operated using a dialysis bag. The receptor medium was ethanol:polysorbate-80:water (10:15:75), adjusted to pH 8.5. ATRA release kinetics in this study were found to follow zero-order kinetics. As the concentration of co-emulsifiers increased, the flux of ATRA released from the lipid emulsions increased. In stability studies, the higher the amount of co-emulsifiers added, the lower the crystallization of ATRA was found. The percentage yield of ATRA was retained at about 70-90% and 60-72% after storage for 60 days at 4 degrees C and 25 degrees C, respectively. These results show a successful incorporation of ATRA into lipid emulsions with high loading capacity and good stability.


Asunto(s)
Emulsiones Grasas Intravenosas/química , Tretinoina/química , Fenómenos Químicos , Química Farmacéutica , Química Física , Cromatografía Líquida de Alta Presión , Excipientes , Tamaño de la Partícula , Fosfolípidos/química , Poloxámero/química , Polisorbatos/química , Solubilidad
17.
Carbohydr Polym ; 144: 419-27, 2016 Jun 25.
Artículo en Inglés | MEDLINE | ID: mdl-27083834

RESUMEN

Biomimetic nanofibrous scaffolds derived from natural biopolymers for bone tissue engineering applications require good mechanical and biological performances including biomineralization. The present work proposes the utility of chitin whisker (CTWK) to enhance mechanical properties of chitosan/poly(vinyl alcohol) (CS/PVA) nanofibers and to offer osteoblast cell growth with hydroxyapatite (HA) mineralization. By using diacid as a solvent, electrospun CS/PVA nanofibrous membranes containing CTWK can be easily obtained. The dimension stability of nanofibrous CS/PVA/CTWK bionanocomposite is further controlled by exposing to glutaraldehyde vapor. The nanofibrous membranes obtained allow mineralization of HA in concentrated simulated body fluid resulting in an improvement of Young's modulus and tensile strength. The CTWK combined with HA in bionanocomposite is a key to promote osteoblast cell adhesion and proliferation. The present work, for the first time, demonstrates the use of CTWKs for bionanocomposite fibers of chitosan and its hydroxyapatite biomineralization with the function in osteoblast cell culture. These hydroxyapatite-hybridized CS/PVA/CTWK bionanocomposite fibers (CS/PVA/CTWK-HA) offer a great potential for bone tissue engineering applications.


Asunto(s)
Huesos/citología , Quitina/química , Quitosano/química , Durapatita/química , Nanocompuestos/química , Nanofibras/química , Ingeniería de Tejidos/métodos , Células 3T3 , Animales , Materiales Biocompatibles/química , Materiales Biocompatibles/farmacología , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Fenómenos Mecánicos , Ratones , Osteoblastos/citología , Osteoblastos/efectos de los fármacos , Alcohol Polivinílico/química
18.
Carbohydr Polym ; 138: 156-65, 2016 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-26794748

RESUMEN

Monocarboxylic acids are common solvents for chitosan to fabricate nanofibers however the unpleasant odor and the additional step of fiber stabilization using crosslinkers, which might cause toxicity, are always the points to be aware of. The present work demonstrates the potential use of multicarboxylic acids as environment-friendly solvents and in situ crosslinking agents for chitosan electrospinning. The use of these solvents leads to the tunable physicochemical properties, cellular compatibility, and cost effective production. By changing di-, to tri-, and tetracarboxylic acids combining with the simple thermal treatment, the stability and mechanical properties of the nanofibrous mats, especially the elastic modulus and elongation at break, can be altered. The resulting nanofibers exhibit biocompatibility favorable for proliferation and adhesion of the osteoblast cells. The multicarboxylic acids allow us lab-scale reproducibility and possibility to semi-production of nanofibrous chitosan using Nanospider™.


Asunto(s)
Materiales Biocompatibles/química , Ácidos Carboxílicos/química , Quitosano/química , Nanofibras/química , Alcohol Polivinílico/química , Solventes/química , Animales , Materiales Biocompatibles/farmacología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Ratones , Microscopía Electrónica de Rastreo , Nanofibras/toxicidad , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Resistencia a la Tracción
19.
J Colloid Interface Sci ; 480: 240-248, 2016 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-27442151

RESUMEN

This study emphasizes the development of a novel surface modified liposome as an anticancer drug nanocarrier. Quaternized N,O-oleoyl chitosan (QCS) was synthesized and incorporated into liposome vesicles, generating QCS-liposomes (Lip-QCS). The Lip-QCS liposomes were spherical in shape (average size diameter 171.5±0.8nm), with a narrow size distribution (PDI 0.1±0.0) and zeta potential of 11.7±0.7mV. In vitro mucoadhesive tests indicated that Lip-QCS possesses a mucoadhesive property. Moreover, the presence of QCS was able to induce the cationic charge on the surface of liposome. Cellular internalization of Lip-QCS was monitored over time, with the results revealing that the cell entry level of Lip-QCS was elevated at 24h. Following this, Lip-QCS were then employed to load cisplatin, a common platinum-containing anti-cancer drug, with a loading efficiency of 27.45±0.78% being obtained. The therapeutic potency of the loaded Lip-QCS was investigated using a 3D spheroid cervical cancer model (SiHa) which highlighted their cytotoxicity and apoptosis effect, and suitability as a controllable system for sustained drug release. This approach has the potential to assist in development of an effective drug delivery system against cervical cancer.


Asunto(s)
Antineoplásicos/administración & dosificación , Quitosano/química , Cisplatino/administración & dosificación , Sistemas de Liberación de Medicamentos , Nanoestructuras/química , Fosfolípidos/química , Neoplasias del Cuello Uterino/tratamiento farmacológico , Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Cisplatino/farmacología , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Humanos , Liposomas/química , Estructura Molecular , Relación Estructura-Actividad , Neoplasias del Cuello Uterino/patología
20.
Colloids Surf B Biointerfaces ; 130: 229-36, 2015 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-25937384

RESUMEN

Mucoadhesive poly (lactic-co-glycolic acid) (PLGA) nanoparticles having a modified shell-matrix derived from polyvinyl alcohol (PVA) and Carbopol (CP), a biodegradable polymer coating, to improve the adhesion and cell transfection properties were developed. The optimum formulations utilized a CP concentration in the range of 0.05-0.2%w/v, and were formed using modified emulsion-solvent evaporation technique. The resulting CP-PLGA nanoparticles were characterized in terms of their physical and chemical properties. The absorbed CP on the PLGA shell-matrix was found to affect the particle size and surface charge, with 0.05% CP giving rise to smooth spherical particles (0.05CP-PLGA) with the smallest size (285.90 nm), and strong negative surface charge (-25.70 mV). The introduction of CP results in an enhancement of the mucoadhesion between CP-PLGA nanoparticles and mucin particles. In vitro cell internalization studies highlighted the potential of 0.05CP-PLGA nanoparticles for transfection into SiHa cells, with uptake being time dependent. Additionally, cytotoxicity studies of CP-PLGA nanoparticles against SiHa cancer cells indicated that low concentrations of the nanoparticles were non-toxic to cells (cell viability >80%). From the various formulations studied, 0.05CP-PLGA nanoparticles proved to be the optimum model carrier having the required mucoadhesive profile and could be an alternative therapeutic efficacy carrier for targeted mucosal drug delivery systems with biodegradable polymer.


Asunto(s)
Resinas Acrílicas/química , Adhesivos/química , Ácido Láctico/química , Nanopartículas/química , Ácido Poliglicólico/química , Adhesión Celular , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos , Endocitosis , Humanos , Ácido Láctico/farmacología , Espectroscopía de Resonancia Magnética , Microscopía Confocal , Microscopía Electrónica de Transmisión , Mucinas/química , Nanopartículas/administración & dosificación , Nanopartículas/ultraestructura , Tamaño de la Partícula , Ácido Poliglicólico/farmacología , Copolímero de Ácido Poliláctico-Ácido Poliglicólico , Alcohol Polivinílico/química , Espectroscopía Infrarroja por Transformada de Fourier , Propiedades de Superficie
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