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Drug Release (drug + release)
Kinds of Drug Release Terms modified by Drug Release Selected AbstractsA Multifunctional Nanodevice Capable of Imaging, Magnetically Controlling, and In Situ Monitoring Drug ReleaseADVANCED FUNCTIONAL MATERIALS, Issue 21 2009Shang-Hsiu Hu Abstract The multifunctional nanodevice described here integrates nanoscaled imaging, targeting, and controlled drug delivery, as well as the capability to monitor, in situ, the amount of drug released from the nanodevice with single-cell resolution. The nanodevice is composed of a polymer core/single-crystal iron oxide shell nanostructure bonded to a quantum dot. It shows outstanding release and retention characteristics via an external on/off manipulation of a high-frequency magnetic field. Upon magnetic stimulation, the single-crystal iron oxide shell demonstrates formation of nanometer-sized polycrystal domains of varying orientation. This allows a variation between retention and slow release of the drug. Further stimulation causes permanent rupturing of the shell, causing release of the drug in a burst-like manner. The quantum dot bonded to the nanodevice provides optical information for in situ monitoring of the drug release through use of a magnetic field. Remote control drug release from the nanodevice in a cancerous cell line (HeLa) was successfully accomplished using the same induction scenario. When nanodevices equipped with quantum dots are taken into cancerous cells, they are able to provide real-time drug dose information through a corresponding variation in emission spectrum. The nanodevice designed in this study has achieved its potential as a cell-based drug-delivery system for therapeutic applications. [source] Temperature-Sensitive Nanocapsules for Controlled Drug Release Caused by Magnetically Triggered Structural DisruptionADVANCED FUNCTIONAL MATERIALS, Issue 4 2009Ting-Yu Liu Abstract Self-assembled nanocapsules containing a hydrophilic core and a crosslinked yet thermosensitive shell are successfully prepared using poly(ethylene-oxide)-poly(propylene-oxide)-poly(ethylene-oxide) block copolymers, 4-nitrophenyl chloroformate, gelatin, and 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide. The core is further rendered magnetic by incorporating iron oxide nanoparticles via internal precipitation to enable externally controlled actuation under magnetic induction. The spherical nanocapsules exhibit a hydrophilic-to-hydrophobic transition at a characteristic but tunable temperature reaching 40,°C, triggering a size contraction and shrinkage of the core. The core content experiences very little leakage at 25,°C, has a half life about 5,h at 45,°C, but bursts out within a few minutes under magnetic heating due to iron oxide coarsening and core/shell disruption. Such burst-like response may be utilized for controlled drug release as illustrated here using a model drug Vitamin B12. [source] Hydrophobic Functional Group Initiated Helical Mesostructured Silica for Controlled Drug Release,ADVANCED FUNCTIONAL MATERIALS, Issue 23 2008Lei Zhang Abstract In this paper a novel one-step synthetic pathway that controls both functionality and morphology of functionalized periodic helical mesostructured silicas by the co-condensation of tetraethoxysilane and hydrophobic organoalkoxysilane using achiral surfactants as templates is reported. In contrast to previous methods, the hydrophobic interaction between hydrophobic functional groups and the surfactant as well as the intercalation of hydrophobic groups into the micelles are proposed to lead to the formation of helical mesostructures. This study demonstrates that hydrophobic interaction and intercalation can promote the production of long cylindrical micelles, and that the formation of helical rod-like morphology is attributed to the spiral transformation from bundles of hexagonally-arrayed and straight rod-like composite micelles due to the reduction in surface free energy. It is also revealed that small amounts of mercaptopropyltrimethoxysilane, vinyltrimethoxysilane, and phenyltrimethoxysilane can cause the formation of helical mesostructures. Furthermore, the helical mesostructured silicas are employed as drug carriers for the release study of the model drug aspirin, and the results show that the drug release rate can be controlled by the morphology and helicity of the materials. [source] Preparation, Bioactivity, and Drug Release of Hierarchical Nanoporous Bioactive Glass Ultrathin FibersADVANCED MATERIALS, Issue 6 2010Youliang Hong Hierarchical nanoporous bioactive glass ultrathin fibers with different pore diameters from 1.5-nm micropores up to 65-nm macropores are synthesized using P123,PEO co-templates and an electrospinning technique (see image). Experiments demonstrate that the prepared bioactive glass fibers are highly homogenous and bioactive and their nanopores can control drug release well. [source] Polymer Networks Combining Controlled Drug Release, Biodegradation, and Shape Memory CapabilityADVANCED MATERIALS, Issue 32-33 2009Axel T. Neffe A triple functional polymer network system that combines shape-memory capability, biodegradability, and drug release is developed. The choice of network structure and switching segment prevent that drug incorporation substantially changes the thermal and mechanical properties as well as the shape-memory functionality (see recovery curves). A diffusion-controlled release that is independent from biodegradation is enabled. [source] AB-polymer Networks with Cooligoester and Poly(n -butyl acrylate) Segments as a Multifunctional Matrix for Controlled Drug ReleaseMACROMOLECULAR BIOSCIENCE, Issue 9 2010Christian Wischke Abstract Semi-crystalline AB-copolymer networks from oligo[(, -caprolactone)- co -glycolide]dimethacrylates and n -butylacrylate have recently been shown to exhibit a shape-memory functionality, which may be used for self-deploying and anchoring of implants. In this study, a family of such materials differing in their molar glycolide contents ,G was investigated to determine structure,property functional relationships of unloaded and drug loaded specimens. Drug loading and release were evaluated, as well as their degradation behavior in vitro and in vivo. Higher ,G resulted in higher loading levels by swelling and a faster release of ethacridine lactate, lower melting temperature of polymer crystallites, and a decrease in shape fixity ratio of the programmed temporary shape. For unloaded networks, the material behavior in vivo was independent of the mechanical load associated with different implantation sites and agreed well with data from in vitro degradation studies. Thus, AB networks could be used as novel matrices for biofunctional implants, e.g., for urogenital applications, which can self-anchor in vivo and provide mechanical support, release drugs, and finally degrade in the body to excretable fragments. [source] Chitosan-Pectin Composite Gel Spheres: Effect of Some Formulation Variables on Drug ReleaseMACROMOLECULAR SYMPOSIA, Issue 1 2004Pornsak Sriamornsak Abstract Chitosan-pectin composite gel spheres were prepared by ionotropic gelation method. Pectin solution containing indomethacin, a model drug, was extruded into a mixture of chitosan and calcium chloride. The release behavior of indomethacin from composite gel spheres was investigated in-vitro. The influence of factors affecting release behavior, such as type of pectin, molecular weight of chitosan, cross-linking time and release medium, were discussed in this study. Adding chitosan into gelation medium could retard the release of indomethacin from gel spheres. The different type of pectin used demonstrated slightly different drug release profiles. The higher molecular weight of chitosan showed less indomethacin release than the lower one. The increased cross-linking time slowed the drug release from composite gel spheres. The release of indomethacin from composite gel spheres was also dependent on the release medium. The drug release was slower in tris buffer where no phosphate ions which can induce the precipitation of calcium phosphate. The results suggested that the composite gel spheres of pectin and chitosan could be used as a controlled release drug delivery carrier. [source] Characterization of Oestrous Induction Response, Oestrous Duration, Fecundity and Fertility in Awassi Ewes During the Non-breeding Season Utilizing both CIDR and Intravaginal Sponge TreatmentsREPRODUCTION IN DOMESTIC ANIMALS, Issue 3 2010N Ozyurtlu Contents The aim of this study was to investigate characterization of oestrous response, onset of induced oestrus, oestrous duration, fecundity and fertility in Awassi ewes treatment with intravaginal sponges and Controlled Intravaginal Drug Release (CIDR) devices in combination with pregnant mare serum gonadotropin (PMSG) under local environmental conditions during the non-breeding season. A total of 62 ewes were divided into three groups. Group CIDR (n = 20) was treated with CIDR devices for 12 days and 400 IU PMSG was injected upon removal of the CIDR. For ewes in Group Sponge (SP) (n = 24), 30 mg fluorogestone acetate was administered to the sheep for 12 days and 400 IU PMSG was injected upon withdrawal of the sponge. Group Control (CON) (n = 18) served as a control group and received no treatment. Adult, intact and sexually experienced Awassi rams were introduced to all groups at the time when the intravaginal devices were removed. There were no significant differences in terms of oestrous response (CIDR: 90%, SP: 87.5%), time to onset of oestrus and duration of induced oestrus between the CIDR and SP groups. The oestrous response of treatment groups was significantly greater (p < 0.05) than in the control ewes. There were no significant differences in pregnancy (CIDR: 70%, SP: 70.8%), lambing (CIDR: 85%, SP: 79.2%) and fecundity rates between ewes treated with CIDR and those treated with sponges. However, pregnancy and lambing rates were significantly (p < 0.05) higher in ewes treated with CIDR or sponges when compared with those in the control group. It was concluded that it is possible to induce fertile oestrus, successful pregnancy and lambing with the treatment of either CIDR or intravaginal sponge in combination with PMSG in Awassi ewes during the non-breeding season. [source] A Point Estimator for the Time Course of Drug ReleaseBIOMETRICAL JOURNAL, Issue 1 2009Stephan Koehne-Voss Abstract Procedures for deconvolution of pharmacokinetic data are routinely used in the pharmaceutical industry to determine drug release and absorption which is essential in designing optimized drug formulations. Although these procedures are described extensively in the pharmacokinetic literature, they have been studied less from a statistical point of view and variance estimation has not been addressed. We discuss the statistical properties of a numerical procedure for deconvolution. Based on a point-area deconvolution method we define an estimator for the function that describes the time course of drug release from a drug formulation. Asymptotic distributions are derived and several methods of variance and interval estimation are compared (© 2009 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim) [source] Control of Drug Release through the In Situ Assembly of Stimuli-Responsive Ordered Mesoporous Silica with Magnetic ParticlesCHEMPHYSCHEM, Issue 17 2007Shenmin Zhu Dr. Abstract A site-selective controlled delivery system for controlled drug release is fabricated through the in situ assembly of stimuli-responsive ordered SBA-15 and magnetic particles. This approach is based on the formation of ordered mesoporous silica with magnetic particles formed from Fe(CO)5 via the surfactant-template sol-gel method and control of transport through polymerization of N-isopropyl acrylamide inside the pores. Hydrophobic Fe(CO)5 acts as a swelling agent as well as being the source of the magnetic particles. The obtained system demonstrates a high pore diameter (7.1 nm) and pore volume (0.41 cm3,g,1), which improves drug storage for relatively large molecules. Controlled drug release through the porous network is demonstrated by measuring the uptake and release of ibuprofen (IBU). The delivery system displays a high IBU storage capacity of 71.5 wt,%, which is almost twice as large as the highest value based on SBA-15 ever reported. In vitro testing of IBU loading and release exhibits a pronounced transition at around 32,°C, indicating a typical thermosensitive controlled release. [source] Drug release into external absorber: Concentration-dependent diffusivityAICHE JOURNAL, Issue 2 2009Sung-Hwa Lin First page of article [source] Increasing process understanding by analyzing complex interactions in experimental dataJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 5 2009Kaisa Naelapää Abstract There is a recognized need for new approaches to understand unit operations with pharmaceutical relevance. A method for analyzing complex interactions in experimental data is introduced. Higher-order interactions do exist between process parameters, which complicate the interpretation of experimental results. In this study, experiments based on mixed factorial design of coating process were performed. Drug release was analyzed by traditional analysis of variance (ANOVA) and generalized multiplicative ANOVA (GEMANOVA). GEMANOVA modeling is introduced in this study as a new tool for increased understanding of a coating process. It was possible to model the response, that is, the amount of drug released, using both mentioned techniques. However, the ANOVA model was difficult to interpret as several interactions between process parameters existed. In contrast to ANOVA, GEMANOVA is especially suited for modeling complex interactions and making easily understandable models of these. GEMANOVA modeling allowed a simple visualization of the entire experimental space. Furthermore, information was obtained on how relative changes in the settings of process parameters influence the film quality and thereby drug release. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:1852,1861, 2009 [source] PLGA nanospheres for the ocular delivery of flurbiprofen: Drug release and interactionsJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 12 2008E. Vega Abstract Poly(D,L -lactide- co -glycolide) nanospheres incorporating flurbiprofen were prepared by the solvent displacement technique for purposes of assessing (i) drug,polymer physicochemical interactions, (ii) flurbiprofen release from the polymer matrix and (iii) eye permeation of the drug formulated in the colloidal system. The resulting nanospheres were on average 200,300 nm in size and bore a negative charge (,-potential around ,25 mV). They were shown by atomic force microscopy and transmission electron microscopy to be spherical and regular in shape. Thermal methods, infrared spectroscopy and X-ray diffraction showed that the drug was dispersed inside the particles. These tests evidenced an eutectic mixture meaning more widespread dispersion of the drug in the polymer system. Entrapped flurbiprofen was released in vitro from the polymer system by dissolution and diffusion in high drug loaded nanospheres, whereas those with a lesser load showed only diffusion. The ex vivo corneal permeation study showed that flurbiprofen-loaded nanospheres enhanced drug penetration by about twofold over commercial eye drops containing poly(vinyl alcohol) and by about fourfold over flurbiprofen in pH 7.4 phosphate buffer. The corneal hydration level of each cornea was determined to evaluate potential corneal damage. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:5306,5317, 2008 [source] Characterization of crosslinking effects on the physicochemical and drug diffusional properties of cationic hydrogels designed as bioactive urological biomaterialsJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 10 2005David S. Jones This study examined the effects of concentration and type of crosslinker (tetraethyleneglycol diacrylate, TEGDA; diethyleneglycol dimethacrylate, DEGDMA; and polyethyleneglycol dimethacrylate, PEGDMA) on the mechanical and drug diffusional properties of hydrogels that had been selected as candidate coatings for bioactive medical devices. Hydrogels (dimethylaminoethylmethacrylate-covinylpyrrolidone; 1:1) were prepared by free radical polymerization and characterized using tensile analysis, dynamic contact angle analysis and analysis of swelling at pH 6.0. The release of fusidic acid and chlorhexidine was evaluated using buffered medium at pH 6.0 and, in addition, using dissolution medium that had been buffered to pH 9 in the presence and absence of elevated concentrations of calcium, representative of urinary encrustation. Crosslinker concentration, but not type, affected the advancing and receding contact angles. Conversely, both crosslinker type and concentration affected the mechanical and swelling properties of the hydrogels. Maximum swelling and elongation at break were associated with the PEGDMA-crosslinked hydrogels whereas TEGDA-crosslinked hydrogels exhibited the maximum ultimate tensile strength and Young's modulus. Drug release from all systems occurred by diffusion. The mass of chlorhexidine and fusidic acid released was dependent on crosslinker type and concentration, with hydrogels crosslinked with PEGDMA offering the greatest mass of drug released at each sampling period. The mass of fusidic acid but not chlorhexidine released at pH 9.0 in a calcium augmented medium was lower than that released in the same medium devoid of elevated calcium, due to the formation of the poorly soluble calcium salt. In conclusion, this study has uniquely examined the effects of crosslinker type and concentration on physicochemical and drug release properties essential to the clinical and non-clinical performance of bioactive hydrogels for medical device application. [source] Sustained Release of 5-Fluorouracil from Polymeric NanoparticlesJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 12 2000PAUL A. McCARRON The use of biodegradable nanoparticles loaded with 5-fluorouracil was investigated as a potential means to sustain the release of this drug. Nanoparticles prepared from four biodegradable polymers were loaded with 5-fluorouracil using three loading concentrations of drug and three different concentrations of added polymer. Washing particles using a centrifugation/re-suspension with ultrasound protocol was found to dislodge the majority of drug, resulting in an over-estimation of incorporation efficiency and low levels of strongly entrapped drug. Increasing the initial 5-fluorouracil concentration before polymer/monomer addition increased the drug loading in both washed and unwashed particles. Increasing the amount of polymer used to make nanoparticles did not increase loadings, but did produce increased amounts of unusable polymer waste. Drug release from nanoparticles was evaluated using a Franz cell diffusion apparatus, which showed an initial burst effect followed by a slower release phase over 24 h. Indeed, nanoparticles prepared from poly(lactide-co-glycolide) released 66% of their 5-fluorouracil payload over this period. It was concluded that 5-fluorouracil-loaded nanoparticles could be readily included into a hydrogel-based delivery system to provide sustained drug release for trans-epithelial drug-delivery applications. [source] Controlled Transdermal Delivery of Propranolol Using HPMC Matrices: Design and In-vitro and In-vivo EvaluationJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 2 2000P. R. P. VERMA To improve bioavailability and achieve a smoother plasma-concentration profile as compared with oral administration, a matrix-dispersion-type transdermal delivery system was designed and developed for propranolol using different ratios of hydroxypropyl-methylcellulose (HPMC) K4M, K15M and K100M. Formulations were evaluated for in-vitro dissolution characteristics using a Cygnus' sandwich-patch holder. Drug release followed Higuchi rather than zero-order or first-order kinetics. In-vivo evaluation was carried out on healthy volunteers (21 ± 1.41 years; 60.89 ± 5.35 kg) following the balanced incomplete block design. The dissolution rate constant (k) and data generated from plasma and urine (Cmax, maximum plasma concentration; tmax, time to reach peak plasma concentration; AUC, area under the curve; ke, elimination rate constant; t½e, elimination half-life; ka, absorption rate constant; t½a, absorption half-life) were evaluated statistically by two-way analysis of variance. Statistically excellent correlation was found between the percentage of drug absorbed and Cmax, AUC0,24 and AUC0-,. A highly significant difference (P < 0.001) was observed when Cmax and AUC0-, generated from plasma and urine were compared, but ke, t½e, ka and t½a did not differ significantly (P > 0.1). We conclude that urinary excretion data may be used as a simpler alternative to blood level data in studying the kinetics of absorption and deriving the absorption parameters. [source] Liquid chromatography-tandem mass spectrometry method for determination of Sirolimus coated drug eluting nano porous carbon stentsBIOMEDICAL CHROMATOGRAPHY, Issue 3 2010G. Rajender Abstract Liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has proved to powerful research tool due to its sensitivity, high selectivity, and high throughput efficiency..Sirolimus was extracted from plasma by two-step extraction procedure using chloroform as extracting solvent. Signal intensity was high using ESI+ source provided for the quantitation of samples. Chromatographic separation was performed on phenomenax C-18 column (250 × 4.60,mm 5microns).Mobile phase contains acetonitrile, water (80; 20 v/v) + 0.1% acetic acid, flow rate 1,mL/min. The retention time of Sirolimus 8.4,min, the total run time10,min. Linearity correlation coefficients (r2) curve was 0.997183.calibraction range 10,1000,ng/mL. The UV detection of Sirolimus was at 278(277.78) nm. Sirolimus coated drug eluting stents, MRM (Multiple reaction monitoring) transition of Sirolimus m/z 936.83,208.84 was selected to obtain maximum sensitivity. LC/MS/MS results exhibited consistency in drug content on the stent surface. In-vitro release kinetic indicated the release of Sirolimus in 41 days from the date of implanted. Drug release was found at the first day, burst release was observed at 7th day of implantation. This study involved pharmacological coating of stents, based on the notion that sustained systemic local delivery of anti-proliferative agents. LC-MS/MS method has been successfully used in the pharmacokinetic analysis of Sirolimus coated drug eluting stents. Copyright © 2009 John Wiley & Sons, Ltd. [source] Sustained ophthalmic in situ gel of ketorolac tromethamine: rheology and in vivo studiesDRUG DEVELOPMENT RESEARCH, Issue 6 2009A.S. Manjappa Abstract Most ocular diseases are treated with topical eye drops. The poor bioavailability and therapeutic response exhibited by these conventional eye drops due to rapid precorneal elimination of the drug may be overcome by the use of in situ gelling systems that are instilled as drops into the eye and undergo a sol-to-gel transition in the cul-de-sac. The present work describes the formulation and evaluation of an ophthalmic delivery system of the nonsteroidal anti-inflammatory drug (NSAID), ketorolac tromethamine, based on the concept of pH-triggered in situ gelation. Polyacrylic acid (Carbopol® 934) was used as the gelling agent in combination with hydroxypropylmethylcellulose (Methocel E15LV), which acted as a viscosity enhancer. The prepared formulations were characterized for clarity, pH, drug content, rheology, and in vivo drug release. Clarity, pH, and drug content of the developed formulations were found to be satisfactory. The developed formulation showed pseudo-plastic rheology. The formulation with benzalkonium chloride and edetate disodium improved the rate of corneal absorption but not the extent. The developed formulation is a viable alternative to conventional eye drops by virtue of its ability to enhance bioavailability through its longer precorneal residence time and ability to sustain drug release. Also importantly is the ease of instillation afforded and decreased frequency of instillation resulting in better patient acceptance. Drug Dev Res, 2009. © 2009 Wiley-Liss, Inc. [source] Development of a Controlled Release System for Risperidone Using Polypyrrole: Mechanistic StudiesELECTROANALYSIS, Issue 4 2010Darren Svirskis Abstract Polypyrrole (PPY) film has been selected as a platform material for drug delivery due to its inherent conductivity, ease of preparation and apparent biocompatibility. PPY films were prepared containing the antipsychotic drug risperidone as a model compound. Drug release profiles could be altered by applying different electrical stimulation to these films. Atomic force microscopy was used to investigate changes in PPY film thickness when different stimuli were applied. The highest levels of drug release were observed when PPY was reduced; this was accompanied by expansion of the film. Technology such as this could be utilized for implantable drug delivery devices, where the dose could be adjusted by external signaling. [source] CE-ESI-MS/MS as a rapid screening tool for the comparison of protein,ligand interactionsELECTROPHORESIS, Issue 7 2010Thomas Hoffmann Abstract In drug development, the combinatorial synthesis of drug libraries is common use, therefore efficient tools for the characterization of drug candidates and the extent of interaction between a drug and its target protein is a central question of analytical interest. While biological activity is tested today by enzyme assays, MS techniques attract more and more attention as an alternative for a rapid comparison of drug,target interactions. CE enables the separation of proteins and drug,enzyme complexes preserving their physiological activity in aqueous media. By hyphenating CE with ESI-MS/MS, the binding strength of enzyme inhibitors can be deduced from MS/MS experiments, which selectively release the inhibitor from the drug,target complex after CID. In this study, ,-chymotrypsin (CT), a serine protease, was chosen as a model compound. Chymostatin is a naturally occurring peptide aldehyde binding to CT through a hemiacetal bond and electrostatic interaction. First, a CE separation was developed, which allows the analysis of ,-CT and a chymotrypsin,chymostatin complex under MS-compatible conditions. The use of neutral-coated CE capillaries was mandatory to reduce analyte,wall interactions. ESI-quadrupole ion trap-MS was worked out to demonstrate the selective drug release after CID. Fragmentation of the drug,enzyme complex was monitored in dependence from the excitation energy in the ion trap, leading to the V50 voltage that enables 50% complex fragmentation as a reference value for chymotrypsin,chymostatin complex. A stable CE-ESI-MS/MS setup was established, which preserves the drug,enzyme complexes during ionization,desolvation processes. With this optimized setup, different CT inhibitors could be investigated and compared. [source] Surface Activation of a Ferrimagnetic Glass,Ceramic for Antineoplastic Drugs GraftingADVANCED ENGINEERING MATERIALS, Issue 7 2010Enrica Vernè A ferrimagnetic glass,ceramic, belonging to the system SiO2,Na2O,CaO,P2O5,FeO,Fe2O3, has been studied as potential carrier for antineoplastic agents, in order to exploit the combination of hyperthermia and chemotherapy. Different material pre-treatments, such as ultrasonic washing, water, or simulated body fluid dipping, were evaluated to promote the surface activation of the glass,ceramic, i.e., the hydroxyl groups formation on it. X-ray photoelectron spectroscopy, scanning electron microscopy, energy dispersion spectrometry, and wettability measurements were performed to observe the samples surface modification. The best results in terms of free hydroxyl groups exposition were obtained by dipping the samples in distilled water for 7 days at 37,°C. Two different anticancer drugs were selected in order to test the reactivity of the activated surface: cisplatinum and doxorubicin. The uptake and release of doxorubicin and cisplatinum were evaluated on glass,ceramic powders, by using UV,Visible spectrometry and graphite furnace atomic absorption spectroscopy, respectively. After 1 day of uptake at 37,°C, the quantity of doxorubicin incorporated into the glass,ceramic is 77,±,7 wt%, while only 42,±,9.6 wt% of cisplatinum is grafted onto the material surface. For both antitumoral agents, the maximum drug release after soaking in aqueous solutions at 37,°C was obtained in few hours, with a randomly distributed kinetics trend. [source] Biphasic Resorbable Calcium Phosphate Ceramic for Bone Implants and Local Alendronate Delivery,ADVANCED ENGINEERING MATERIALS, Issue 5 2010Shashwat S. Banerjee A novel biphasic calcium phosphate ceramic composed of tricalcium phosphate (TCP) and calcium pyrophosphate (CP) is synthesized in order to tailor the biodegradation behavior of the ceramic. The results show that biphasic TCP/CP ceramic has a strength of 62.2,±,2.1 MPa, which is superior to single-phase TCP and CP ceramics, which show strengths of 44.3,±,3.0 and 53.0,±,4.8 MPa, respectively. In addition, biphasic TCP/CP ceramic displays a controlled strength degradation from 62.2,±,2.1 to 40.5,±,1.0 MPa in stimulated body fluid over a period of 28 d. An in vitro cell materials interaction study using human fetal osteoblast cells indicates that TCP/CP ceramic is cytocompatible. TCP/CP ceramic also show a good loading capacity for alendronate. Adsorption of alendronate (AD) on the TCP/CP surface is found to proceed via ligand exchange mechanism and the in vitro release profile of AD from TCP/CP surface is characterized by an initial fast release followed by a slow and sustained release. Strong electrostatic interactions between AD groups and surface Ca2+ ions enable the slow and sustained release of AD. These results demonstrate that the newly developed biphasic ceramic, with its controlled strength degradation and drug release, shows promise for use in orthopedic and tissue engineering applications. [source] The effect of topically applied salicylic compounds on serotonin-induced scratching behaviour in hairless ratsEXPERIMENTAL DERMATOLOGY, Issue 4 2002J. S. Thomsen Abstract: There is a strong need for antipruritic substances for treating itch in clinical dermatology. In one recent human study, topically applied acetylsalicylic acid has been described to rapidly decrease histamine-induced itch. We have established a model for periferally elicited pruritus by injecting serotonin into the rostral back area (neck) in rats. Using this model, we aimed to investigate the antipruritic potential of four different salicylic compounds, which all possess different skin penetration characteristics. Eighteen rats were studied for 6 weeks. Prior to serotonin injections (2 mg/ml, 50 µl), 10 µl of test substances was applied to a circular area 18 mm in diameter. The four substances were salicylic acid, butyl salicylate, diethylamine salicylate and salicylamide, all solubilized in dimethyl isosorbide to a concentration of 5% w/w. Diethylamine salicylate and salicylamide were previously shown to be slowly absorbed through rat skin in contrast to salicylic acid and butyl salicylate. After serotonin injections, scratching was monitored by video recording for 1.5 h. Compared with the vehicle, a lower number of scratch sequences were seen when diethylamine salicylate (P < 0.001) and salicylamide (P = 0.005) had been applied. The numbers of scratch sequences were lower with diethylamine salicylate and salicylamide than with the vehicle throughout the 1.5-h study period. We conclude that topical application of diethylamine salicylate and salicylamide could suppress serotonin-induced scratching in rats. The antipruritic effect seems to be related to the slow drug release of the two substances. The results may be clinically relevant as serotonin induces itch in humans. [source] Fabrication and Drug Delivery of Ultrathin Mesoporous Bioactive Glass Hollow FibersADVANCED FUNCTIONAL MATERIALS, Issue 9 2010Youliang Hong Abstract Ultrathin mesoporous bioactive glass hollow fibers (MBGHFs) fabricated using an electrospinning technique and combined with a phase-separation-induced agent, poly(ethylene oxide) (PEO), are described. The rapid solvent evaporation during electrospinning and the PEO-induced phase separation process demonstrated play vital roles in the formation of ultrathin bioactive glass fibers with hollow cores and mesoporous walls. Immersing the MBGHFs in simulated body fluid rapidly results in the development of a layer of enamel-like apatite mesocrystals at the fiber surfaces and apatite nanocrystals inside the hollow cores. Drug loading and release experiments indicate that the drug loading capacity and drug release behavior of the MBGHFs strongly depends on the fiber length. MBGHFs with fiber length >50,µm can become excellent carriers for drug delivery. The shortening of the fiber length reduces drug loading amounts and accelerates drug release. The MBGHFs reported here with sophisticated structure, high bioactivity, and good drug delivery capability can be a promising scaffold for hard tissue repair and wound healing when organized into 3D macroporous membranes. [source] Synthesis of Magnetic, Up-Conversion Luminescent, and Mesoporous Core,Shell-Structured Nanocomposites as Drug CarriersADVANCED FUNCTIONAL MATERIALS, Issue 7 2010Shili Gai Abstract The synthesis (by a facile two-step sol,gel process), characterization, and application in controlled drug release is reported for monodisperse core,shell-structured Fe3O4@nSiO2@mSiO2@NaYF4: Yb3+, Er3+/Tm3+ nanocomposites with mesoporous, up-conversion luminescent, and magnetic properties. The nanocomposites show typical ordered mesoporous characteristics and a monodisperse spherical morphology with narrow size distribution (around 80,nm). In addition, they exhibit high magnetization (38.0,emu g,1, thus it is possible for drug targeting under a foreign magnetic field) and unique up-conversion emission (green for Yb3+/Er3+ and blue for Yb3+/Tm3+) under 980,nm laser excitation even after loading with drug molecules. Drug release tests suggest that the multifunctional nanocomposites have a controlled drug release property. Interestingly, the up-conversion emission intensity of the multifunctional carrier increases with the released amount of model drug, thus allowing the release process to be monitored and tracked by the change of photoluminescence intensity. This composite can act as a multifunctional drug carrier system, which can realize the targeting and monitoring of drugs simultaneously. [source] Smart Hydrogels Co-switched by Hydrogen Bonds and ,,, Stacking for Continuously Regulated Controlled-Release SystemADVANCED FUNCTIONAL MATERIALS, Issue 4 2010Fang Li Abstract A series of hydrogels with continuously regulatable release behavior can be achieved by incorporating hydrogen bonding and ,,, stacking co-switches in polymers. A poly(nitrophenyl methacrylate- co -methacrylic acid) hydrogel (NPMAAHG) for control over drug release is fabricated by copolymerizing 4-nitrophenyl methacrylate and methacrylic acid using ethylene glycol dimethacrylate as a crosslinker. The carboxylic acid groups and nitrylphenyl groups form hydrogen bonds and ,,, stacking interactions, respectively, which act as switches to control the release of guest molecules from the polymers. As revealed by the simulated gastrointestinal tract drug release experiments, the as-synthesized NPMAAHG hydrogels can be regulated to release only 4.7% of drugs after 3,h in a simulated stomach and nearly 92.6% within 43,h in the whole digestive tract. The relation between the release kinetics and structures and the mechanism of the smart release control are analyzed in terms of diffusion exponent, swelling interface number, drug diffusion coefficient, and velocity of the swelling interface in detail. The results reveal that the release of guest molecules from the hydrogels can be continuously regulated for systemic administration by controlling the ratio of the hydrophilic hydrogen bonds and the hydrophobic ,,, stacking switches. [source] Integrated Multifunctional Nanosystems for Medical Diagnosis and TreatmentADVANCED FUNCTIONAL MATERIALS, Issue 21 2009*Article first published online: 9 OCT 200, Donglu Shi Abstract This article provides an overview on the development of integrated multifunctional nanosystems for medical diagnosis and treatment. In particular, a novel system is developed specifically for achieving simultaneous diagnosis and treatment of cancer. Critical issues are addressed on the architecture and assembly of nanocomponents based on medical requirements: targeted in vivo imaging, controlled drug release, localized hyperthermia, and toxicity. Nanotube-based carriers are summarized with surface functionalized properties. Other types of nanocarriers are also included such as super paramagnetic composite nanospheres and biodegradable hydroxylapatite nanoparticles. In addition, polymeric-based nanosystems are introduced with several novel features: they can be bio-dissolved due to environmental pH and temperature fluctuations. The nanocarriers are surface tailored with key functionalities: surface antibodies for cell targeting, anti-cancer drug loading, and magnetic nanoparticles for both hyperthermia and MRI. Future requirements, aims, and trends in the development of multifunctional nanosystems, particularly with intelligent functionalities for fundamental studies, are also provided. [source] A Multifunctional Nanodevice Capable of Imaging, Magnetically Controlling, and In Situ Monitoring Drug ReleaseADVANCED FUNCTIONAL MATERIALS, Issue 21 2009Shang-Hsiu Hu Abstract The multifunctional nanodevice described here integrates nanoscaled imaging, targeting, and controlled drug delivery, as well as the capability to monitor, in situ, the amount of drug released from the nanodevice with single-cell resolution. The nanodevice is composed of a polymer core/single-crystal iron oxide shell nanostructure bonded to a quantum dot. It shows outstanding release and retention characteristics via an external on/off manipulation of a high-frequency magnetic field. Upon magnetic stimulation, the single-crystal iron oxide shell demonstrates formation of nanometer-sized polycrystal domains of varying orientation. This allows a variation between retention and slow release of the drug. Further stimulation causes permanent rupturing of the shell, causing release of the drug in a burst-like manner. The quantum dot bonded to the nanodevice provides optical information for in situ monitoring of the drug release through use of a magnetic field. Remote control drug release from the nanodevice in a cancerous cell line (HeLa) was successfully accomplished using the same induction scenario. When nanodevices equipped with quantum dots are taken into cancerous cells, they are able to provide real-time drug dose information through a corresponding variation in emission spectrum. The nanodevice designed in this study has achieved its potential as a cell-based drug-delivery system for therapeutic applications. [source] Photoluminescence-Based Sensing With Porous Silicon Films, Microparticles, and NanoparticlesADVANCED FUNCTIONAL MATERIALS, Issue 20 2009Michael J. Sailor Abstract Here, chemical sensors made from porous Si are reviewed, with an emphasis on systems that harness photoluminescence and related energy- and charge-transfer mechanisms available to porous Si-derived nanocrystallites. Quenching of luminescence by molecular adsorbates involves the harvesting of energy from a delocalized nanostructure that can be much larger than the molecule being sensed, providing a means to amplify the sensory event. The interaction of chemical species on the surface of porous Si can exert a pronounced influence on this process, and examples of some of the key chemical reactions that modify either the surface or the bulk properties of porous Si are presented. Sensors based on micron-scale and smaller porous Si particles are also discussed. Miniaturization to this size regime enables new applications, including imaging of cancerous tissues, indirect detection of reactive oxygen species (ROS), and controlled drug release. Examples of environmental and in vivo sensing systems enabled by porous Si are provided. [source] Temperature-Sensitive Nanocapsules for Controlled Drug Release Caused by Magnetically Triggered Structural DisruptionADVANCED FUNCTIONAL MATERIALS, Issue 4 2009Ting-Yu Liu Abstract Self-assembled nanocapsules containing a hydrophilic core and a crosslinked yet thermosensitive shell are successfully prepared using poly(ethylene-oxide)-poly(propylene-oxide)-poly(ethylene-oxide) block copolymers, 4-nitrophenyl chloroformate, gelatin, and 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide. The core is further rendered magnetic by incorporating iron oxide nanoparticles via internal precipitation to enable externally controlled actuation under magnetic induction. The spherical nanocapsules exhibit a hydrophilic-to-hydrophobic transition at a characteristic but tunable temperature reaching 40,°C, triggering a size contraction and shrinkage of the core. The core content experiences very little leakage at 25,°C, has a half life about 5,h at 45,°C, but bursts out within a few minutes under magnetic heating due to iron oxide coarsening and core/shell disruption. Such burst-like response may be utilized for controlled drug release as illustrated here using a model drug Vitamin B12. [source] | |||||||||||||||||||||||||||||||