[Fabrication and coating of microgranules of acetylsalicylic acid: use of eudragit L30D].
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Acrylic Resins↗
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Results for “Polymethacrylic Acids”
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Bioerodible polyanhydrides for antibiotic drug delivery: in vivo osteomyelitis treatment in a rat model system.
Acute and chronic osteomyelitis can be difficult to treat by conventional means. Current methods of treatment involve the use of systemic antibiotics, the local implantation of non-degradable drug carriers, and surgical débridement. Each method has specific drawbacks. We report on the use of a new controlled release system utilizing gentamicin and bioerodible, biocompatible polymers (polyanhydrides) designed for drug delivery applications for the treatment of clinical osteomyelitis. We compared this system's ability to reduce bacterial levels in infected bone with that of conventional non-degradable delivery systems based on polymethylmethacrylate (PMMA) and gentamicin. Polyanhydride copolymers of bis-carboxyphenoxypropane and sebacic acid P loaded with gentamicin sulfate and PMMA/gentamicin matrices were implanted in the long bones of Sprague-Dawley rats infected with a strain of Staphylococcus aureus. After 3 weeks of implantation, the polymeric delivery devices were removed and quantitative cultures were used to determine bacterial levels in bone. The polyanhydride/gentamicin matrices demonstrated significant degradation over the 3 week implantation period. Levels of bacteria, measured in colony forming units, were significantly lower in bone implanted with the polyanhydride/gentamicin release system than in long bones of control animals without an implant (p < 0.01), of animals with a polyanhydride polymer implant alone (p < 0.01), and of animals with a PMMA/gentamicin implant (p = 0.03). Bioerodible polyanhydrides show promise as a new treatment modality for infections in bone.
Animals↗
Preparation and evaluation of Eudragit gels. VIII. Rectal absorption of 5-fluorouracil from Eudispert hv gels in rats.
Rectal absorption of the hydrophilic 5-fluorouracil (5-FU) in rats was studied with Eudispert hv gels with or without fatty acids as the rectal bases. In the absence of fatty acids, absolute bioavailabilities of 5-FU for Eudispert hv hydrogel and xerogel preparations increased approximately 2.5 times compared with those of Witepsol H-15 and PEG 2000 suppositories. When n-capric acid or linolenic acid was used as an absorption enhancer, absolute bioavailabilities of 5-FU were, respectively, 25.5 and 30.9% for Witepsol H-15 and 64.4 and 66.1% for PEG 2000. Furthermore, the absolute bioavailabilities of 5-FU for Eudispert hv hydrogel with n-capric acid or linolenic acid were 95.6% and 81.7%. The addition of capric acid or linolenic acid to the hydrogel was a useful method for increasing 5-FU permeability through the rectal membranes. These results are consistent with the observation that the total amounts of 5-FU remaining in the lumenal contents of the rectum and that accumulated in the rectal tissue decreased in relation to the increase in the bioavailabilities. Thus, the Eudispert hv hydrogel containing 5-FU with capric acid may be a useful rectal preparation for increasing the maximum plasma level and improving the absolute bioavailability of 5-FU.
Acrylic Resins↗
Endodontic dowel retention with resinous cements.
This study compared the capability of three composite resin cements to sustain a standard endodontic dowel. All of the systems incorporated some form of smear layer removal on the dentin of the endodontic channel. One system that used a methyl ethyl ketone drying agent provided inadequate clinical resistance to dislodgment of 5.4 DaN. A second cementing system that used only smear layer removal resisted loads at 54.7 DaN. The third cementing regimen that included a surface-initiated dentinal adhesive and smear layer removal recorded retention of 77.4 DaN. This study supported the concept that passively cemented dowels with composite resin can be as effective as actively seated dowels.
Acrylic Resins↗
The effect of substrate molecular mobility on surface induced immune complement activation and blood plasma coagulation.
Changing the length of the alkyl ester side chain in poly(alkyl methacrylates) provides a unique opportunity to systematically vary the mobility of the polymer chains, or in other words vary the glass transition temperature (T(g)), without greatly affect the solid surface energy (gamma(s)) of the polymer. A series of poly(alkyl methacrylate) coatings was therefore analysed with regard to the human immune complement (IC) activation and the surface associated blood plasma coagulation cascade (CC) properties. For the IC and CC measurements we used a quartz crystal microbalance (QCM) where we modified the chemistry of the sensor surface by applying 10-30 nm thick poly(alkyl methacrylate) coatings. The surface energy was calculated from water contact angles and small differences between the coatings were observed. The surface chemistry of the coatings, as determined with X-ray photoelectron spectroscopy (XPS), showed no deviation from expected compositions. Tapping mode atomic force microscopy (TM-AFM) measurements revealed that all coatings displayed similar morphology and the roughness was in the range of 0.7-0.9 nm. Increased polymer mobility correlated with a decrease in IC activation, measured as a decreased C3c deposition at the surface. The surface induced CC, measured as fibrin clot formation at the surface, was different between the different coatings but no correlation with molecular mobility was observed. Thus, the molecular mobility of the polymer chains had a major effect on both the IC and the CC and it seems that different aspects of the chemistry of the solid surface regulate activation of the IC and the CC.
Biocompatible Materials↗
Thermosensitive and biodegradable polymeric micelles for paclitaxel delivery.
The preparation, release and in vitro cytotoxicity of a novel polymeric micellar formulation of paclitaxel (PTX) were investigated. The micelles consisted of an AB block copolymer of poly(N-(2-hydroxypropyl) methacrylamide lactate) and poly(ethylene glycol) (pHPMAmDL-b-PEG). Taking advantage of the thermosensitivity of pHPMAmDL-b-PEG, the loading was done by simply mixing of a small volume of a concentrated PTX solution in ethanol and an aqueous polymer solution and subsequent heating of the resulting solution above the critical micelle temperature of the polymer. PTX could be almost quantitatively loaded in the micelles up to 2 mg/mL. By dynamic light scattering and cryo-transmission electron microscopy, it was shown that PTX-loaded micelles have a mean size around 60 nm with narrow size distribution. At pH 8.8 and 37 degrees C, PTX-loaded micelles destabilized within 10 h due to the hydrolysis of the lactic acid side group of the pHPMAmDL. Because the hydrolysis of the lactic acid side groups is first order in hydroxyl ion concentration, the micelles were stable for about 200 h at physiological conditions. The presence of serum proteins did not have an adverse effect on the stability of the micelles during at least 15 h. Interestingly, the dissolution kinetics of pHPMAmDL-b-PEG micelles was retarded by incorporation of PTX, indicating a strong interaction between PTX and the pHPMAmDL block. The PTX-loaded micelles showed a release of the incorporated 70% of PTX during 20 h at 37 degrees C and at pH 7.4. PTX-loaded pHPMAmDL-b-PEG micelles showed comparable in vitro cytotoxicity against B16F10 cells compared to the Taxol standard formulation containing Cremophor EL, while pHPMAmDL-b-PEG micelles without PTX were far less toxic than the Cremophor EL vehicle. Confocal laser-scanning microscopy (CLSM) and fluorescence activated cell sorting (FACS) analysis of fluorescently labelled micelles showed that pHPMAmDL-b-PEG micelles were internalized by the B16F10 cells. The present results suggest that pHPMAmDL-b-PEG block copolymer micelles are a promising delivery system for the parenteral administration of PTX.
Animals↗
Alterations of energy metabolism and glutathione levels of HL-60 cells induced by methacrylates present in composite resins.
OBJECTIVES: Methacrylic compounds such as 2-hydroxyethyl methacrylate (HEMA), triethylene glycol dimethacrylate (TEGDMA) and bisphenol A glycerolate (1 glycerol/phenol) dimethacrylate (Bis-GMA) are largely present in auto- or photopolymerizable composite resins. Since the polymerization reaction is never complete, these molecules are released into the oral cavity tissues and biological fluids where they could cause local adverse effects. The aim of this work was to verify the hypothesis that the biological effects of HEMA, TEGDMA and Bis-GMA - at a non-cytotoxic concentration - depend on the interaction with mitochondria and exert consequent alterations of energy metabolism, GSH levels and the related pathways in human promyelocytic cell line (HL-60). METHODS: The biological effects of methacrylic monomers were determined by analyzing the following parameters: GSH concentration, glucose-6-phosphate dehydrogenase (G6PDH) and glutathione reductase (GR) activity, oxygen and glucose consumption and lactate production along with cell differentiation and proliferation. RESULTS: All monomers induced both cellular differentiation and decrease in oxygen consumption. Cells treated with TEGDMA and Bis-GMA showed a significant enhancement of glucose consumption and lactate production. TEGDMA and HEMA induced GSH depletion stimulating G6PDH and GR activity. CONCLUSIONS: All the monomers under study affect the metabolism of HL-60 cells and show differentiating activity. Since alterations in cellular metabolism occurred at compound concentrations well below cytotoxic levels, the changes in energy metabolism and glutathione redox balance could be considered as potential mechanisms for inducing clinical and sub-clinical adverse effects and thus providing useful parameters when testing biocompatibility of dental materials.
Bisphenol A-Glycidyl Methacrylate↗
Influence of time and adhesive system on the extrusion shear strength between feldspathic porcelain and bovine dentin.
OBJECTIVES: The behavior of dual-cure cements over time remains unclear. This study evaluated the extrusion shear strength of the bond between feldsphatic porcelain and bovine dentin at different time intervals, using three adhesive systems based on dual-cure cements and one based on a self-cure cement. METHODS: The adhesive systems evaluated included: C&B/One-Step, Enforce/Prime&Bond NT Dual-Cure, RelyX ARC/Single Bond and Variolink II/Syntac SC. Discs of bovine root dentin, 2.5 mm thick, had the root canal prepared with a standardized taper. Porcelain truncated cones etched with 4% hydrofluoric acid and silanized were bonded into the perforations. The extrusion shear test was performed after 15 min, 4 h, 12 h, 24 h, and 7 days. Data were analyzed using the Weibull distribution. The failure mode was accessed by stereomicroscope and SEM. RESULTS: Statistical differences were found between 15 min and 7 days for Variolink II/Syntac SC and RelyX ARC/Single Bond, and between 15 min and 24 h for Enforce/Prime&Bond NT Dual-Cure. For C&B/One-Step, difference was found between 15 min and 4 h. Between 24 h and 7 days, only the system RelyX ARC/Single Bond showed a significant increase in the characteristic strength. SEM analysis revealed that the failure involved the hybrid layer/dentin or the hybrid layer/adhesive interfaces, regardless of the time interval and adhesive system. SIGNIFICANCE: High characteristic strengths were observed after 15 min when dual-cure cements were used. In general, the values found at 24 h or 7 days were higher than at 15 min. However, there was always a considerable probability of bonding failure at low stress levels for all the systems tested.
Acid Etching, Dental↗
In vitro inhibition of enamel demineralization by a polymerizable amphiphilic film.
An amphiphilic coating is configured as a substantive film that has a tendency for an in-plane two-dimensional polymerization. This coating is hypothesized to protect enamel from in vitro acid decalcification, assessed through the following artificial caries model. Three regions on labial enamel of eight bovine incisors were treated with an acid resistant varnish (A), the amphiphilic coating (B), or left undisturbed (C), and the teeth were immersed for 3 wk in lactic acid gel. Mineral loss (deltaZ-value) was determined by a cross-sectional microhardness technique. deltaZ-values (mean +/- SD; volume percent mineral-microm) were: -4 +/- 24 (A), 29 +/- 69 (B), and 7,372 +/- 1,766 (C). deltaZ-value of the uncoated enamel (C) was significantly different from the other groups. Scanning electron microscopy showed enamel etched pattern from citric acid, and the coating firmly attached on enamel surface. This amphiphilic coating can inhibit enamel decalcification under the present experimental condition.
Acrylates↗
The effects of chewing gum on gastric content prior to induction of general anesthesia.
To study the effects on gastric content and subjective well being of chewing gum in the immediate preoperative period, 60 female nonsmokers were randomized to use regular, sugar-free chewing gum preoperatively or to continue the overnight fast. In a similar fashion 44 habitual smokers were randomized to use nicotine gum 2 mg or not. Nonsmokers using chewing gum had significantly larger gastric fluid volumes than controls (mean 30 +/- 19 mL vs 20 +/- 15 mL; 95% confidence interval (CI) for difference 1-19 mL; P = 0.03), with no difference in gastric fluid acidity. In smokers, neither gastric fluid volume nor acidity differed significantly between those who were or were not chewing gum. Although the use of nicotine gum in smokers was associated with a reduction in dryness of the mouth, thirst, and irritability, nonsmokers chewing regular gum did not report significant improvements in patient well being. In habitual smokers unable to abstain from nicotine, the use of nicotine gum on the morning of surgery may be beneficial. Although it is difficult to prove a direct influence on the incidence of pulmonary aspiration of increased gastric contents, the fact that regular, sugar-free chewing gum increased gastric fluid volumes probably means that it should not be used on the morning of surgery.
Adult↗
Experience with Eudragit-S-coated mesalamine (Asacol) in inflammatory bowel disease. An open study.
We reviewed the courses of 63 patients with inflammatory bowel disease (IBD) treated in a private gastroenterology practice. All were allergic, unresponsive, or in some way intolerant of sulfasalazine and therefore were treated with Eudragit-S-coated mesalamine (Asacol). Thirty-eight patients had ulcerative colitis (UC) and 25 had Crohn's disease. In 22 and 14, respectively, mesalamine was used to treat active disease; in 16 and 11, respectively, it was introduced to maintain remission. In some patients, mesalamine was used along with other medications. Symptomatic and endoscopic response was seen in seven of nine (77%) with active UC treated with measalamine alone; remission was maintained in seven of eight (94%) when mesalamine was used alone. Therapeutic success was noted in eight of 10 (80%) with active Crohn's disease, and remission was maintained in seven of nine (78%) when mesalamine was used alone. Adverse reactions of varying severity occurred in 21 of 63 (33%), but the drug had to be terminated in only 9 of 63 (14%). Eudragit-S-coated mesalamine appears to be effective in the treatment and maintenance of remission of UC in 82% of those patients allergic or intolerant to the parent drug, sulfasalazine. Furthermore, contrary to what was expected, we found it effective in a much larger percentage of patients with Crohn's disease (79%) than the parent drug.
Acrylic Resins↗
Dentin-polymer bond mediated by glutaraldehyde/HEMA.
A restorative resin was bonded to EDTA-treated dentin by means of a mixture of glutaraldehyde and HEMA. The bond exhibited a tensile strength of 17.5 +/- 1.0 MPa (mean +/- SEM) and was unaffected by water storage at 37 degrees C for up to 6 months. The glutaraldehyde/HEMA mixture was found to be most effective when the pH was between 2 and 5; an application time of 10 s was found to be sufficient for the glutaraldehyde/HEMA mixture as well as for the EDTA-solution.
Acrylates↗
Adhesion to dentin mediated by Gluma: effect of pretreatment with various amino acids.
Dentin surfaces were treated with various amino acids. The treatment caused an alteration of the dentin surface that influenced the tensile bond strength to a restorative resin obtained with the Gluma system. The bond strengths varied between 5.6 and 14.2 MPa. Among the amino acids tested, N-phenylglycine produced the strongest bonds.
Adhesiveness↗
In vivo effects of prostaglandin E2 and arachidonic acid on phagocytosis of fluorescent methacrylate microbeads by rat peritoneal macrophages.
Several studies have suggested that prostaglandin E2 (PGE2) might influence the phagocytic activity of macrophage cells. The present study was designed to examine the in vivo effects of PGE2, the prostaglandin synthesis inhibitor meclofenamate, the prostaglandin precursor arachidonic acid, and the biologically inactive fatty acid 11,14,17-eicosatrienoic acid on phagocytosis by peritoneal macrophage cells in the rat. Following 3 days of treatment with either agent, fluorescent methacrylate microbeads were injected intraperitoneally into all rats. Peritoneal exudates were harvested after administration of the microbeads and the percent phagocytosis determined in macrophage cells using a fluorescence-activated cell sorter (FACS II). The administration of PGE2 was associated with a significant decrease in the percentage of peritoneal macrophages ingesting the fluorescent methacrylate microbeads. In contrast, treatment with arachidonic acid or 11,14,17-eicosatrienoic acid significantly enhanced the percentage of phagocytic macrophage cells. A significant increase in the number of macrophages undergoing phagocytosis of the methacrylate microbeads was also observed in rats treated with meclofenamate. This later observation, taken together with the inhibitory effect induced by PGE2 on macrophage phagocytosis, points to a potential modulator role of PGE2 on the phagocytic activity of macrophages. These data also suggest that arachidonic acid might influence macrophage phagocytosis by a mechanism independent of PGE2.
Animals↗
Shear bond strength of five porcelain repair systems on cerec porcelain.
The purpose of this in vitro investigation was to evaluate the shear bond strength of composite resin bonded to Cerec Vitablocs Mark II porcelain with four different porcelain repair systems. The systems evaluated in this study were Scotchbond/ RelyX Primer (S/ 3M), Ultradent Porcelain Repair Kit (U, Ultradent), Vivadent Ceramic Repair Kit (V, Vivadent) and Prime & Bond NT/ Calibra Silane Coupling Agent (P, Dentsply). Seventy five Cerec Vitablocks Mark II porcelain were embedded in metal rings, leaving 7 mm of porcelain exposed above the ring surface. Samples were ground wet on 400 grit SiC paper to roughen the surface and then screened for surface defects. The five porcelain repair agents were applied according to manufacturers' instructions and matching composite stubbs, then bonded onto 15 treated porcelain surfaces, using an Ultradent mould with a diameter of 2,38 mm. All samples were stored in distilled water for 24 hours at 37 degrees C before the bonds were stressed to failure, using a shear load in a Texture Analyser (TAXT2i) (Stable Micro Systems) Data was analyzed statistically (ANOVA). The effects of the pretreatments on the porcelain surfaces after treatment with the different systems were examined in a Scanning Electron Microscope (SEM), and the modes of fracture were assessed under a light microscope. The mean SBS (MPa) for the products in descending order were: U = 26.6 1.7; V = 20.9 3.4; C = 19.4 5.3; S = 18.0 2.0 and P = 15.9 2.1. The Student-t Test revealed a statistical significant difference (p < 0.05) between the mean shear bond strengths of P and U. There was also a statistical significant difference (p < 0.05) between the mean shear bond strengths of P and V. Most debonded specimens showed cohesive fractures in the porcelain. Significant shear bond strength differences were observed for the different repair systems. All the systems tested can probably be used to repair Cerec Vitablocs Mark II porcelain, with some systems providing higher bond strengths.
Acrylic Resins↗
Pharmacokinetics of a novel HIV-1 protease inhibitor incorporated into biodegradable or enteric nanoparticles following intravenous and oral administration to mice.
CGP 57813 is a peptidomimetic inhibitor of human immunodeficiency virus type 1 (HIV-1) protease. This lipophilic compound was successfully entrapped into poly(D,L-lactic acid) (PLA) and pH sensitive methacrylic acid copolymers nanoparticle. The intravenous administration to mice of PLA nanoparticles loaded with CGP 57813 resulted in a 2-fold increase of the area under the plasma concentration-time curve, compared to a control solution. An increase in the elimination half-life (from 13 to 61 min) and in the apparent volume of distribution (1.7-3.6 L/kg) was observed for the nanoparticle incorporated compound vs control solution. Following oral administration, only nanoparticles made of the methacrylic acid copolymer soluble at low pH provided sufficient plasma levels of CGP 57813. In vitro, these nanoparticles dissolved completely within 5 min at pH 5.8. PLA nanoparticles, which are insoluble in the gastrointestinal tract, did not provide significant plasma concentrations of CGP 57813. From these observations, one can conclude that the passage of intact PLA nanoparticles across the gastrointestinal mucosa appears to be very low.
Acrylic Resins↗
Application of sucrose fatty acid esters in transdermal therapeutic systems.
Transdermal therapeutic systems (TTSs) were studied applying different sucrose fatty acid esters (SEs) as drug delivery agents. Matrix and membrane controlled TTSs were prepared and compared. Membrane was made from a methacrylic polymer (Eudragit NE) of pH independent permeability which can achieve diffusion controlled drug liberation. Model drug was a water soluble beta-blocker, metoprolol, which has short biological half-life, so applying it in a TTS, the duration of its action could be prolonged. Sucrose fatty acid esters of different fatty acid chain lengths and consequently different hydrophilic-lipophilic balance (HLB) values were studied considering their effect on the metoprolol release from TTSs. Different mathematical models were applied for the evaluation of the release process. The results of the in vitro studies indicated that SEs of shorter fatty acid chain length and higher HLB value increased the amount of released drug about 10 times. SEs could be promising agents in transdermal therapeutic systems to control the drug release and cutaneous absorption.
Administration, Cutaneous↗
Influence of the morphology of poly(EGDMA-co-HEMA) on the chemical modifications and retention of O-phosphothreonine.
The influence of the morphology of ethylene glycol dimethacrylate-hydroxyethyl methacrylate copolymer [poly(EGDMA-co-HEMA)] base support to obtain different Fe(3+)-containing sorbents and their properties in retention of O-phosphothreonine [Thre(P)] is examined in this paper. Three base supports poly(EGDMA-co-HEMA) (I-III) were obtained using different quantities of initiator in suspension polymerization reactions. These products were submitted to chemical modifications using 1,4-butanediol diglycidyl ether (BDGE) in activation reactions and different chelating agents (iminodiacetic acid, IDA; disodium ethylenediamine tetraacetate, EDTA; and hexamethylenediamine tetrapropanoic acid, HMDTP) in coupling reactions to attain Fe(3+)-containing sorbents. Properties such as specific surface area (S(s)), specific pore volume (V(p)), scanning electron microscopy (SEM), IR spectroscopy, quantity of functional groups (oxirane and carboxyl), amount of chelated metal ion, ligand occupation (L), swelling studies as well as quantity of O-phosphoamino acid retained were used as comparative parameters for matrices. In general, the derivatization reactions proved to be more efficient when higher S(s) of macropores (50-400,000 nm) were available in the matrix. In our case, it was observed when highest percentage of initiator was used. On the other hand, the effect of accessibility of surface area on the yield of coupling reactions was noticed when comparing the different chelating agents since the number of carboxyl groups present in products was higher when the molecular size of the chelating agent was lower. Although all Fe(3+)-containing sorbents resulted efficient to retain Thre(P), the values of retention of the amino acid were slightly higher when IDA-containing matrices were used irrespective of the quantity of metal chelated. This could be probably due to the fact that the IDA ligand could be bounded to the matrix in sites that though accessible for the center of adsorption were hard for Thre(P) to access.
Biophysics↗