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1.
J Esthet Restor Dent ; 31(3): 257-262, 2019 05.
Artículo en Inglés | MEDLINE | ID: mdl-30565846

RESUMEN

OBJECTIVE: To evaluate the shear bond strength of resin cements to zirconia treated with the selective infiltration etching technique (SIE). MATERIALS AND METHODS: Forty-seven zirconia specimens were prepared with a sequence of silicon carbide abrasives, cleaned in an ultrasonic bath. Three samples were separated for atomic force microscope (AFM) analyses (one nontreated for control, one sandblasted, and one selective infiltration etched) and the remaining were randomly distributed in four groups, according to the combination of surface treatment and resin cement: group 1a (sandblasting + Variolink II), group 1b (sandblasting + Panavia SA Plus), group 2a (SIE + Variolink II), group 2b (SIE + Panavia SA Plus). A composite resin cylinder (3 mm × 3 mm) was cemented to the zirconia surface, as per each group's specific protocol. After storing 24 hours in distilled water at 37°C, the specimens were tested for shear bond strength and the results were subjected to statistical analysis. RESULTS: At 24 hours, the highest SBS values were observed in group 2b, where the SIE technique was used in conjunction with Panavia SA Plus. Lowest values were found in group 1a. Increased surface roughness was observed with SIE. CONCLUSIONS: SIE significantly enhanced the resin bond strength to zirconia. However, cement selection was also an important factor, for both surface treatments tested. CLINICAL SIGNIFICANCE: Use of SIE method combined with MDP monomer containing resin cement can provide clinically acceptable bond strength between zirconia and resin cement.


Asunto(s)
Recubrimiento Dental Adhesivo , Cementos de Resina , Cerámica , Cementos Dentales , Grabado Dental , Ensayo de Materiales , Propiedades de Superficie , Circonio
2.
J Prosthodont ; 26(5): 419-423, 2017 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-26845627

RESUMEN

PURPOSE: The purpose of this in vitro study was to evaluate the hot chemical etching method on the shear bond strength between zirconia and two resin cements. MATERIALS AND METHODS: Sixty zirconia specimens (13 × 7.5 × 2.5 mm3 ) were prepared and treated as follows: (1) airborne-particle abrasion with 50 µm Al2 O3 particles; (2) hot chemical etching for 10 minutes; (3) hot chemical etching for 30 minutes. Sixty composite cylinders of 3 mm diameter and height were prepared and bonded to zirconia specimens, which were divided into subgroups A and B. Group A: cemented with conventional resin cement (Variolink II); group B: cemented with 10-metacryloxydecyl dihydrogen phosphate (MDP) monomer containing resin cement (Panavia SA) after the application of surface treatments. Next, the specimens were stored in 37ºC distilled water for 24 hours. Following water storage, shear bond strength test was performed at a 1 mm/min crosshead speed in a universal testing machine. The statistical analyses were performed with one-way ANOVA and post hoc Tukey tests. p < 0.05 was considered statistically significant. RESULTS: The results from all of the tested groups exhibited lower shear bond strength values than group II-B and higher shear bond strength values than group I-A (p < 0.05). CONCLUSION: The use of the hot chemical etching method for 10 minutes increased the shear bond strength of zirconia ceramics to both conventional and resin cements and seems to be an effective method. The MDP monomer-containing resin cement, Panavia SA, improved the resin bonding of zirconia ceramics when combined with airborne-particle abrasion.


Asunto(s)
Cerámica , Recubrimiento Dental Adhesivo/métodos , Grabado Dental/métodos , Metacrilatos/uso terapéutico , Cementos de Resina/uso terapéutico , Itrio , Circonio , Análisis del Estrés Dental , Humanos , Resistencia al Corte
3.
Pharmaceutics ; 15(4)2023 Apr 05.
Artículo en Inglés | MEDLINE | ID: mdl-37111639

RESUMEN

Uterine cancer is the fourth most common cancer in women. Despite various chemotherapy approaches, the desired effect has not yet been achieved. The main reason is each patient responds differently to standard treatment protocols. The production of personalized drugs and/or drug-loaded implants is not possible in today's pharmaceutical industry; 3D printers allow for the rapid and flexible preparation of personalized drug-loaded implants. However, the key point is the preparation of drug-loaded working material such as filament for 3D printers. In this study, two different anticancer (paclitaxel, carboplatin) drug-loaded PCL filaments with a 1.75 mm diameter were prepared with a hot-melt extruder. To optimize the filament for a 3D printer, different PCL Mn, cyclodextrins and different formulation parameters were tried, and a series of characterization studies of filaments were conducted. The encapsulation efficiency, drug release profile and in vitro cell culture studies have shown that 85% of loaded drugs retain their effectiveness, provide a controlled release for 10 days and cause a decrease in cell viability of over 60%. In conclusion, it is possible to prepare optimum dual anticancer drug-loaded filaments for FDM 3D printers. Drug-eluting personalized intra-uterine devices can be designed for the treatment of uterine cancer by using these filaments.

4.
Transplant Proc ; 55(5): 1252-1256, 2023 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-37100737

RESUMEN

BACKGROUND: Monitoring biochemical parameters to detect early complications after liver transplantation (LT) is important. Thus, we aimed to investigate parameter trends indicating liver function in patients who did not develop complications after cadaveric LT. METHODS: A total of 266 cadaveric LT operations performed by a single center between 2007-2022 were included in the study. Patients with any early complications were excluded from the study. During the first 15 days, the parameters reflecting the patients' liver integrity and synthesis functions were evaluated. All parameters studied were evaluated at the same time of day and by a single laboratory. RESULTS: Regarding synthesis functions, the coagulation parameters (prothrombin time and international normalized ratio) peaked on the first day and then decreased. Regarding tissue hypoxia, there was no significant change in lactate values. Total and direct bilirubin values also decreased after peaking on the first day. No significant change was observed in albumin, another liver synthesis value. CONCLUSIONS: Although an increase in aspartate aminotransferase, alanine aminotransferase, total and direct bilirubin, prothrombin time, and international normalized ratio, which was especially seen on the first day, is considered normal, values that do not decrease after the second day or lactate values that increase gradually should be a warning in terms of possible early complications.


Asunto(s)
Trasplante de Hígado , Humanos , Trasplante de Hígado/efectos adversos , Hígado , Bilirrubina , Tiempo de Protrombina , Cadáver
5.
Carbohydr Polym ; 89(2): 478-85, 2012 Jun 20.
Artículo en Inglés | MEDLINE | ID: mdl-24750747

RESUMEN

The main objective is to develop a new superabsorbent system especially for using in diaper applications. In this study, hydrogels based on Tara gum/acrylic acid (TG/AAc) were prepared by gamma irradiation, in the presence of N,N'-methylenebisacrylamide (MBAAm) as a crosslinking agent. The polymeric networks formed were characterized by FT-IR and evaluated by swelling studies as a function of MBAAm concentration, temperature and nature of the swelling medium. The swelling kinetics of the hydrogels was studied in terms of the diffusion exponent "n". The results showed that the water diffusion into hydrogels is a non-Fickian type. Mechanical measurements (stress-strain) curves of hydrogels were evaluated to calculate the shear modulus values and the average molecular weight between crosslinks (Mc). Moreover, the absorption under load at 37°C of water and urea aqueous solutions (as a major component of urine) by TG/AAc hydrogels was determined.

6.
Int J Pharm ; 623: 121940, 2022 Jul 25.
Artículo en Inglés | MEDLINE | ID: mdl-35724824

RESUMEN

Immune system deficiencies are crucial in the progression of cancer, predominantly because immune cells are not stimulated by cytokines to eradicate cancer cells. Immunochemotherapy is currently considered an innovative approach that creates pathways in cancer treatment, sometimes also aiding in the efficacy of chemotherapeutics. The aim of this study was to prepare a cyclodextrin (CD) nanoplex based on charge interaction to deliver the anticancer drug 5-fluorouracil (5-FU) and Interleukin-2 (IL-2), thereby forming a nanoscale drug delivery system aimed at chemo-immunotherapy for colorectal cancers. The CD:IL-2 nanoplexes were obtained with a particle size below 100 nm and a cationic surface charge based on the extent of charge interaction of the cationic CD polymer with negatively charged IL-2. The loading capacity of CD nanoplexes was 40% for 5-FU and 99.8% for IL-2. Nanoplexes maintained physical stability in terms of particle size and zeta potential in aqueous solution for 1 week at + 4 °C. Moreover, the structural integrity of IL-2 loaded into CD nanoplexes was confirmed by SDS-PAGE analysis. The cumulative release rates of both 5-FU and IL-2 were found to be more than 80% in simulated biological fluids in 12 h. Cell culture studies demonstrate that CD polymers are safe on healthy L929 mouse fibroblast cells. Drug-loaded CD nanoplexes were determined to have a higher anticancer effect than free drug solution against CT26 mouse colon carcinoma cells. In addition, intestinal permeability studies supported the conclusion that CD nanoplexes could be promising candidates for oral chemotherapy as well. In conclusion, effective cancer therapy utilizing the absorptive/cellular uptake effect of CDs, the synergic effect and co-transport of chemotherapeutic drugs and immunotherapeutic molecules is a promising approach. Furthermore, the transport of IL-2 with this nano-sized system can reduce or avoid its toxicity problem in the clinic.


Asunto(s)
Neoplasias del Colon , Ciclodextrinas , Nanopartículas , Animales , Neoplasias del Colon/tratamiento farmacológico , Neoplasias del Colon/patología , Ciclodextrinas/uso terapéutico , Fluorouracilo , Inmunoterapia , Interleucina-2 , Ratones , Nanopartículas/química
7.
Colloids Surf B Biointerfaces ; 193: 111111, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-32531647

RESUMEN

Calcified cartilage extracellular matrix (ECM) is a critical interface at the osteochondral junction which plays an important role in maintaining the structural continuity between articular cartilage and subchondral bone. This mineralized network is primarily composed of glycosaminoglycans (GAGs) and collagen type II (col II) and hosts hypertrophic chondrocytes. This work aimed to investigate the effect of gel composition and collagen II content on the behavior and hypertrophic differentiation of ATDC5 cells for regeneration of calcified cartilage tissue. For this purpose, chitosan/collagen type II/nanohydroxyapatite (chi/col II/nHA) composite hydrogels were prepared to mimic the calcified cartilage ECM. ATDC5 cells were encapsulated within the composite gels and the viability, ECM production and hypertrophic gene expression were assessed during culture. All composites were favorable for ATDC5 viability and proliferation, whereas specific ECM production and hypertrophic differentiation were dependent on gel composition. Chitosan: collagen II ratio had an impact on ATDC5 cell fate. Hypertrophic differentiation was best pronounced in chi/col II/nHA 70:30 composition. The results obtained from this study offers a scaffold-based approach for calcified cartilage regeneration and provide an insight for biomimetic design and preparation of more complicated gradient osteochondral units.


Asunto(s)
Cartílago Articular/metabolismo , Condrocitos/metabolismo , Matriz Extracelular/metabolismo , Hipertrofia/metabolismo , Animales , Cartílago Articular/química , Células Cultivadas , Matriz Extracelular/química , Ratones , Tamaño de la Partícula , Propiedades de Superficie
8.
Int J Biol Macromol ; 156: 681-690, 2020 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-32320808

RESUMEN

Tissue engineering approach offers alternative strategies to develop multi-layered/multi-component osteochondral mimetic constructs to meet the requirements of the heterogeneous and layered structure of native osteochondral tissue. Herein, an iterative overlaying process to fabricate a multi-layered scaffold with a gradient composition and layer specific structure have been developed by combining the natural extracellular matrix (ECM) components-chitosan, type I collagen, type II collagen, nanohydroxyapatite- of the osteochondral tissue in biomimetic compositions. Subchondral bone layer was prepared by using freeze-drying method to obtain 3D porous scaffolds. The calcified cartilage and cartilage layers were prepared by thermal gelation method in the hydrogel form. Osteochondral scaffolds fabricated by iterative overlaying of each distinct layer exhibited a porous, continuous gradient structure and supported cell proliferation in a co-culture of MC3T3-E1 preosteoblasts and ATDC5 chondrocytes. Histology and biochemical analysis showed enhanced extracellular matrix production and demonstrated collagen and glycosaminoglycan deposition. Expression of genes specific for bone, calcified cartilage and cartilage were improved in the osteochondral scaffold. Overall, these findings suggest that iterative overlaying of freeze-dried scaffolds and hydrogel matrices prepared by using ECM components in biomimetic ratios to fabricate gradient, multi-layered structures can be a promising strategy without the need for growth factors.


Asunto(s)
Biomimética , Regeneración Ósea , Quitosano/química , Colágeno/química , Ingeniería de Tejidos , Andamios del Tejido/química , Animales , Biomarcadores , Cartílago , Células Cultivadas , Técnicas de Cocultivo , Matriz Extracelular , Inmunohistoquímica , Ratones , Esferoides Celulares
9.
Eur J Pharm Sci ; 130: 114-123, 2019 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-30690187

RESUMEN

As research progresses on personalized medicines, it is clear that personalized and flexible formulations can provide effective treatment with reduced side effects especially for diseases like cancer, characteristic of high patient variability. 2D and 3D printers are frequently reported in the literature for the preparation of pharmaceutical products with adjusted dose and selected drug combinations. However, in-depth characterization studies of these formulations are rather limited. In this paper, ex vivo and mechanical characterization studies of antiviral and anticancer drug printed film formulations designed for personalized application were performed. Effects of the printing process with pharmaceutical formulations such as paclitaxel (PCX):cyclodextrin (CD) complex or cidofovir (CDV) encapsulated into poly(ethylene glycol)-polycaprolactone (PEG-PCL) nanoparticles on the films were evaluated through a series of mechanical characterization studies. Inkjet printing process was found to cause no significant change in the thicknesses of the film formulations, while mechanical strength and surface free energy increased and nano-sized voids in the film structure decreased. According to the mechanical characterization data, the unprinted film had maximum force (Fmax) value of 15.6 MPa whereas Fmax increased to 43.8 MPa for PCX:CD complex printed film and to 37.7 MPa for the antiviral CDV-PEG-PCL nanoparticle printed film. In the light of ex vivo findings of sheep cervix-uterine tissue, bioadhesive properties of film formulations significantly improved after inkjet printing with different drug formulations. It has also been shown that the anticancer formulation printed on the film was maintained at the cervix tissue surface for >12 h. This study has shown for the first time that inkjet printing process does not adversely affect the mechanical properties of the bioadhesive film formulations. It has also been shown that durable bioadhesive film formulations for personalized dosing can be prepared by combining nanotechnology and inkjet printing.


Asunto(s)
Adhesivos/administración & dosificación , Antineoplásicos/administración & dosificación , Antivirales/administración & dosificación , Nanopartículas/administración & dosificación , Impresión Tridimensional , Neoplasias del Cuello Uterino/tratamiento farmacológico , Adhesivos/síntesis química , Adhesivos/farmacocinética , Animales , Antineoplásicos/síntesis química , Antineoplásicos/farmacocinética , Antivirales/síntesis química , Antivirales/farmacocinética , Evaluación Preclínica de Medicamentos/métodos , Femenino , Nanopartículas/química , Nanopartículas/metabolismo , Ovinos , Resultado del Tratamiento , Neoplasias del Cuello Uterino/metabolismo
10.
J Pharm Sci ; 97(4): 1519-29, 2008 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-17705171

RESUMEN

In the current formulation of clinical use paclitaxel (PCX) is associated with solubilizers that may produce severe side effects. In this study, PCX was complexed to an amphiphilic cyclodextrin (CD), 6-O-CAPRO-beta-CD, capable of forming nanoparticles spontaneously in order to mask its physicochemical properties via the formation of inclusion complexes of the drug with amphiphilic CD before the nanoparticle is formed. Complexes have been characterized with various techniques such as (1)H NMR, Fourier Transform Infrared (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) confirming the formation of inclusion complex between PCX and 6-O-CAPRO-beta-CD. Nanospheres and nanocapsules were prepared directly from the preformed PCX/6-O-CAPRO-beta-CD inclusion complex by the nanoprecipitation technique, showing a size from 150 to 250 nm for nanospheres and from 500 to 500 nm for nanocapsules. Zeta potentials of the nanospheres and nanocapsules indicate stable colloidal dispersions within the range of -18 to -39 mV. A 12-month physical stability was demonstrated for blank nanoparticles. PCX encapsulation was high with three-fold increase in loading when nanoparticles are prepared directly from preformed inclusion complexes of the drug with 6-O-CAPRO-beta-CD. In vitro liberation profiles of PCX from CD nanoparticles show a prolonged release profile for this drug up to 12 h for nanospheres and 24 h for nanocapsules.


Asunto(s)
Antineoplásicos Fitogénicos/química , Nanopartículas/química , Paclitaxel/química , beta-Ciclodextrinas/química , Química Farmacéutica , Espectroscopía de Resonancia Magnética , Paclitaxel/administración & dosificación , Solubilidad , beta-Ciclodextrinas/administración & dosificación
11.
J Clin Neurosci ; 15(10): 1102-4, 2008 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-18653341

RESUMEN

Post-dural puncture headache (PDPH) is a common complication of lumbar puncture. As invasive treatments for PDPH have known complications, pharmacologic management may be preferable. The aim of this study was to evaluate and to compare the efficacy of intravenous theophylline treatment for PDPH, in comparison with a placebo. We found that intravenous theophylline infusion was effective for decreasing the painfulness of PDPH compared with the control group. The mean visual analogue scale (VAS) value was 7.05+/-1.47 before the theophylline infusion and 2.88+/-2.31 after infusion. An average of 59.1% relief of pain was obtained in the group treated with theophylline infusion. The improvement in VAS in the study group was significant (p < 0.001), whereas that in the control group was not (p = 0.15). The mean VAS decrease after theophylline infusion was 4.17+/-2.03 in the study group and 0.41+/-0.71 in the control group; the difference in improvement between the groups was significant (p < 0.001). Intravenous theophylline infusion is an easy, rapid, minimally invasive, an effective treatment for PDPH. It may be attempted in PDPH patients before invasive techniques are used. To the best of our knowledge, this is the first report on the effect of intravenous infusion of theophylline compared with a placebo in the treatment of PDPH.


Asunto(s)
Cefalea Pospunción de la Duramadre/prevención & control , Punción Espinal/efectos adversos , Teofilina/administración & dosificación , Vasodilatadores/administración & dosificación , Adulto , Distribución de Chi-Cuadrado , Femenino , Humanos , Infusiones Intravenosas , Vértebras Lumbares , Masculino , Persona de Mediana Edad , Dimensión del Dolor , Cefalea Pospunción de la Duramadre/etiología , Estadísticas no Paramétricas , Resultado del Tratamiento
12.
J Adv Prosthodont ; 10(1): 43-49, 2018 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-29503713

RESUMEN

PURPOSE: The purpose of this in vitro study is to examine the effects of a nano-structured alumina coating on the adhesion between resin cements and zirconia ceramics using a four-point bending test. MATERIALS AND METHODS: 100 pairs of zirconium bar specimens were prepared with dimensions of 25 mm × 2 mm × 5 mm and cementation surfaces of 5 mm × 2 mm. The samples were divided into 5 groups of 20 pairs each. The groups are as follows: Group I (C) - Control with no surface modification, Group II (APA) - airborne-particle-abrasion with 110 µm high-purity aluminum oxide (Al2O3) particles, Group III (ROC) - airborne-particle-abrasion with 110 µm silica modified aluminum oxide (Al2O3 + SiO2) particles, Group IV (TCS) - tribochemical silica coated with Al2O3 particles, and Group V (AlC) - nano alumina coating. The surface modifications were assessed on two samples selected from each group by atomic force microscopy and scanning electron microscopy. The samples were cemented with two different self-adhesive resin cements. The bending bond strength was evaluated by mechanical testing. RESULTS: According to the ANOVA results, surface treatments, different cement types, and their interactions were statistically significant (P<.05). The highest flexural bond strengths were obtained in nanostructured alumina coated zirconia surfaces (50.4 MPa) and the lowest values were obtained in the control group (12.00 MPa), both of which were cemented using a self-adhesive resin cement. CONCLUSION: The surface modifications tested in the current study affected the surface roughness and flexural bond strength of zirconia. The nano alumina coating method significantly increased the flexural bond strength of zirconia ceramics.

13.
J Adv Prosthodont ; 10(3): 205-210, 2018 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-29930790

RESUMEN

PURPOSE: The purpose of this study was to evaluate the efficiency of a gas-phase fluorination method under different fluorination periods through using two resin cements. MATERIALS AND METHODS: 84 zirconia specimens in dimensions of 5 mm × 5 mm × 2 mm were prepared and surface treated with 50 µm aluminum oxide particles or gas phase fluorination for 2 min, 5 min, or 10 min. One specimen in each group was surface analyzed under scanning electron microscope. The remaining specimens were bonded to composite cylinders in dimensions of 2 mm diameter and 3 mm high with Panavia SA Plus or Variolink N. Then, the specimens were stored in 37℃ distilled water for 24 hours and shear bond strength test was applied at a speed of 1 mm/min. RESULTS: The highest shear bond strength values were observed in the samples fluorinated for 5 minutes and cemented with Panavia SA Plus. Variolink N did not elicit any statistical differences between surface treatments. Panavia SA Plus resin cement and Variolink N resin cements featured statistically significant difference in shear bond strength values only in the case of 5 minutes of fluorination treatment. CONCLUSION: According to the results of this study, application of 5 minutes of fluorination with 10-methacryloyloxydecyl dihydrogen phosphate monomer (MDP) containing Panavia SA Plus resin cement increased the resin bond strength of zirconia. Fluorination of the zirconia surface using conventional resin cement, Variolink N, did not lead to an increase in bond strength.

14.
J Ocul Pharmacol Ther ; 33(7): 525-529, 2017 09.
Artículo en Inglés | MEDLINE | ID: mdl-28590790

RESUMEN

PURPOSE: To evaluate the effects of ascorbic acid (vitamin C), the main antioxidant agent in the cornea on transepithelial corneal cross-linking (CXL) where the main mechanism is oxidation. METHODS: Twenty eyes of 20 rabbits were divided into 3 groups: Group 1 (7 eyes) had transepithelial corneal CXL after being fed with normal diet; Group 2 (7 eyes) had corneal CXL after once-daily subcutaneous injections of 200 mg of ascorbic acid in addition to normal diet; and the control group (6 eyes) was fed with normal diet but did not have corneal CXL performed. Ascorbic acid levels were measured in aqueous humor and plasma, and biomechanical measurements were applied to the cornea. RESULTS: There was a significant difference in ascorbic acid levels of plasma (P = 0.008) and aqueous humor (P = 0.006) between group 1 and 2. The Young's modulus values of group 1 and 2 were similar (P = 0.741) and were significantly higher than the control group (P = 0.02 and P = 0.01). The increase rate in Young's modulus values was 37.3% in group 1 and 43.9% in group 2 compared to control group. The ultimate strain values in group 1 and 2 were similar (P = 0.632) and were significantly higher than control group (P = 0.04, P = 0.03). The ultimate stress values in group 1 and 2 were similar (P = 0.836) and were significantly lower than control group (P = 0.001, P = 0.001). CONCLUSIONS: Systemic vitamin C does not appear to decrease effectiveness of transepithelial corneal CXL. Therefore, there is no reason to stop or reduce vitamin C supplementation before corneal CXL therapy.


Asunto(s)
Antioxidantes/farmacología , Ácido Ascórbico/farmacología , Sustancia Propia/efectos de los fármacos , Reactivos de Enlaces Cruzados , Epitelio Corneal/efectos de los fármacos , Fármacos Fotosensibilizantes/uso terapéutico , Riboflavina/uso terapéutico , Animales , Humor Acuoso/metabolismo , Ácido Ascórbico/sangre , Fenómenos Biomecánicos , Colágeno/metabolismo , Sustancia Propia/metabolismo , Elasticidad , Conejos , Rayos Ultravioleta
15.
AAPS PharmSciTech ; 7(2): E38, 2006 Apr 14.
Artículo en Inglés | MEDLINE | ID: mdl-16796356

RESUMEN

The purpose of this study was to achieve a better therapeutic efficacy and patient compliance in the treatment for vaginitis. Clotrimazole (1%) has been formulated in a vaginal gel using the thermosensitive polymer Pluronic F127 (20%) together with mucoadhesive polymers such as Carbopol 934 and hydroxypropylmethylcellulose (0.2% for both). To increase its aqueous solubility, clotrimazole was incorporated as its inclusion complex with 1:1 molar ratio with beta-cyclodextrin. The inclusion complex was thoroughly characterized using various techniques, including 1H NMR spectroscopy, FT IR spectrophotometry, differential scanning calorimetry, scanning electron microscopy, phase solubility studies, and determination of stability constant (k(1:1)). The gelation temperature and rheological behavior of different formulations at varying temperatures were measured. In vitro release profiles of the gels were determined in pH 5.5 citrate buffer. It was observed that complexation with cyclodextrin slowed down the release of clotrimazole considerably. Carbopol 934, on the other hand, was found to interact with beta-cyclodextrin, inducing precipitation. As far as rheological properties are concerned, thermosensitive in situ gelling was obtained with formulations containing drug:cyclodextrin complex rather than with free drug. Thus, the optimum formulation for a controlled-release thermosensitive and mucoadhesive vaginal gel was determined to be clotrimazole:beta-cyclodextrin 1% with 0.2% hydroxypropylmethylcellulose in Pluronic F127 gel (20%) providing continuous and prolonged release of active material above MIC values.


Asunto(s)
Clotrimazol/administración & dosificación , Clotrimazol/química , Preparaciones de Acción Retardada/química , Adhesivos Tisulares/química , Cremas, Espumas y Geles Vaginales/química , beta-Ciclodextrinas/administración & dosificación , beta-Ciclodextrinas/química , Antifúngicos/administración & dosificación , Antifúngicos/química , Preparaciones de Acción Retardada/administración & dosificación , Preparaciones de Acción Retardada/análisis , Difusión , Combinación de Medicamentos , Evaluación Preclínica de Medicamentos , Femenino , Humanos , Ensayo de Materiales , Membrana Mucosa/química , Temperatura , Adhesivos Tisulares/administración & dosificación , Adhesivos Tisulares/análisis , Vagina/química , Cremas, Espumas y Geles Vaginales/administración & dosificación , Vaginitis/tratamiento farmacológico
16.
Int J Pharm ; 509(1-2): 375-390, 2016 Jul 25.
Artículo en Inglés | MEDLINE | ID: mdl-27282534

RESUMEN

As nanomedicines are gaining momentum in the therapy of cancer, new biomaterials emerge as alternative platforms for the delivery of anticancer drugs with bioavailability problems. In this study, two novel amphiphilic cyclodextrins (FCD-1 and FCD-2) conjugated with folate group to enable active targeting to folate positive breast tumors were introduced. The objective of this study was to develop and characterize new folated-CD nanoparticles via 3(2) factorial design for optimal final parameters. Full physicochemical characterization studies were performed. Blank and paclitaxel loaded FCD-1 and FCD-2 nanoparticles remained within the range of 70-275nm and 125-185nm, respectively. Zeta potential values were neutral and -20mV for FCD-1 and FCD-2 nanoparticles, respectively. Drug release studies showed initial burst release followed by a longer sustained release. Blank nanoparticles had no cytotoxicity against L929 cells. T-47D and ZR-75-1 human breast cancer cells with different levels of folate receptor expression were used to assess anti-cancer efficacy. Through targeting the folate receptor, these nanoparticles were efficiently engulfed by the breast cancer cells. Additionally, breast cancer cells became more sensitive to cytotoxic and/or cytostatic effects of PCX delivered by FCD-1 and FCD-2. In conclusion, these novel folate-conjugated cyclodextrin nanoparticles can therefore be considered as promising alternative systems for safe and effective delivery of paclitaxel with a folate-dependent mechanism.


Asunto(s)
Ciclodextrinas/química , Ácido Fólico/química , Nanopartículas/química , Paclitaxel/química , Animales , Antineoplásicos/química , Antineoplásicos/farmacología , Línea Celular , Línea Celular Tumoral , Ciclodextrinas/farmacología , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Liberación de Fármacos , Humanos , Ratones , Nanomedicina/métodos , Tamaño de la Partícula
17.
J Biomed Mater Res A ; 74(2): 187-96, 2005 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-15962270

RESUMEN

Poly(N-vinyl-2-pyrrolidone)-kappa-carrageenan hydrogels (PVP-KC) were prepared by irradiating the mixtures of aqueous solutions of PVP, KC, potassium chloride, and poly(ethylene glycol) by gamma-rays at different doses. Their preliminary laboratory tests were evaluated to identify their usability in wound dressing applications. For investigation of the effect of components on the gelation of PVP, sol-gel analyses were made and gel fractions of the hydrogels were determined. Mechanical experiments were conducted for both unirradiated and irradiated samples. For investigation of the fluid uptake capacity of the hydrogels, swelling experiments were performed in pseudo-extracellular fluid solution at various temperatures. Acidity/alkalinity (pH) and electrical conductivity tests were achieved from aqueous extracts of hydrogels, and bioadhesion strength of the hydrogels was investigated on human skin.


Asunto(s)
Vendajes , Carragenina , Rayos gamma , Hidrogeles , Povidona , Carragenina/síntesis química , Conductividad Eléctrica , Humanos , Concentración de Iones de Hidrógeno , Ensayo de Materiales , Povidona/síntesis química , Piel
18.
J Pharm Sci ; 91(5): 1214-24, 2002 May.
Artículo en Inglés | MEDLINE | ID: mdl-11977097

RESUMEN

The purpose of this study was to synthesize and characterize amphiphilic beta-cyclodextrins modified on the primary face with substituents of varying chain lengths (C6 and C14) and bond types (ester or amide). We also aimed to evaluate the potentiality of the new amphiphilic beta-cyclodextrins as excipients for the preparation and optimization of nanocapsules without using surface-active agents. Amphiphilic beta-cyclodextrin derivatives were characterized by (1)H-nuclear magnetic resonance spectroscopy, Fourier transform infrared spectroscopy, mass spectroscopy, differential scanning calorimetry, and elemental analysis. Nanocapsules prepared by nanoprecipitation were characterized by particle size and zeta potential determination and freeze fracture followed by transmission electron microscopy. The appropriate amphiphilic beta-cyclodextrin and its optimum concentration to be used were determined. Formation and characteristics of the nanocapsules were highly dependent on the structural properties of the modified cyclodextrin, its behavior in the oil-water interface and the viscosity and miscibility of the organic solvent with water. Physical stability after 5-month storage was also evaluated. The results indicated that derivatives with 6C aliphatic chains on the primary face proved to be the most efficient among the amphiphilic beta-CDs in this study. They avoid the use of surfactants in parenteral formulations of nanocapsules.


Asunto(s)
Ciclodextrinas/síntesis química , Excipientes/síntesis química , Tensoactivos/síntesis química , beta-Ciclodextrinas , Cápsulas , Fenómenos Químicos , Química Física , Ciclodextrinas/análisis , Estabilidad de Medicamentos , Excipientes/análisis , Técnica de Fractura por Congelación/métodos , Microscopía Electrónica , Nanotecnología , Tamaño de la Partícula , Tensoactivos/análisis
19.
Int J Pharm ; 251(1-2): 143-53, 2003 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-12527184

RESUMEN

Amphiphilic beta-cyclodextrins were formulated as nanospheres and characterised by particle size, zeta potential and TEM following freeze-fracture. The nanospheres were loaded with progesterone with different loading techniques involving the spontaneous formation of nanospheres from pre-formed inclusion complexes of amphiphilic beta-cyclodextrins modified on the primary or secondary face with progesterone. Inclusion complexes were characterised with various techniques including Differential Scanning Calorimetry (DSC), Fast Atom Bombardment Mass Spectrometry (FAB MS) and 1H NMR spectroscopy; and progesterone was believed to be partially included in the CD cavity. Loading properties of conventionally-loaded nanospheres were compared with those prepared directly from pre-formed inclusion complexes and loading technique was found to enhance associated drug percentage significantly (P<0.05). Although both amphiphilic beta-cyclodextrins (6-N-CAPRO-beta-CD and beta-CDC6) were capable of high progesterone loading, beta-CDC6 displayed slightly higher entrapment efficiency due to the possible higher affinity of progesterone to the 14 alkyl chains surrounding this molecule resulting in higher drug adsorption to particle surface. Progesterone was released within a period of 1 h from all formulations. Progesterone-loaded amphiphilic beta-CD nanospheres were proved to be a promising non-surfactant injectable delivery system providing high-quantity of water-insoluble progesterone rapidly within 1 h.


Asunto(s)
Ciclodextrinas/química , Nanotecnología/métodos , Progesterona/química , Tensoactivos/química , beta-Ciclodextrinas , Ciclodextrinas/farmacocinética , Microesferas , Progesterona/farmacocinética , Tensoactivos/farmacocinética
20.
Carbohydr Polym ; 114: 546-552, 2014 Dec 19.
Artículo en Inglés | MEDLINE | ID: mdl-25263925

RESUMEN

Better understanding of the chemistry of radiation-induced degradation is becoming of increasing importance on account of the utilization of polymeric materials in a variety of radiation environments as well as beneficial uses of degraded polymers. In this report the importance of environmental humidity on the degrading effect of radiation has been considered from the point of view of controlling the molecular weights of kappa- and iota-carrageenans. These two polysaccharides were irradiated in solid form under strictly controlled environmental humidity conditions by incubating and later irradiating the samples over saturated aqueous salt solutions of NaCl, NaNO3 and MgCl2. The degradation was followed in detail by a careful gel permeation chromatographic analysis of their respective molecular weights before and after irradiation. The chain scission yield values G(S) were found to decrease with the water adsorbed from environment at every absorbed dose in the range of 5-100 kGy. On the other hand at very high water uptakes the yield of chain scission again increases especially at low doses. The decrease in degradation yield was attributed to the plastifying effect of water trapped in between the polymer chains facilitating the macroradical recombinations thus reducing the extent of chain scission. This study showed that although carrageenans were irradiated in solid form, the difference in their water uptake from changing environmental humidity has a profound effect in controlling their molecular weights by irradiation with ionizing radiation.


Asunto(s)
Carragenina/química , Cromatografía en Gel , Relación Dosis-Respuesta en la Radiación , Humedad
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